Search Result
Results for "
Pathway Inhibitors
" in MedChemExpress (MCE) Product Catalog:
1543
Inhibitors & Agonists
10
Biochemical Assay Reagents
47
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-171115
-
-
-
- HY-164145
-
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TGF-β Receptor
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Others
Cancer
|
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CDD-1653 is a potent and selective BMPR2 inhibitor (IC50=2.8 nM). CDD-1653 reduces the ability of ATP to bind to the kinase domain of BMPR2, thereby affecting the phosphorylation of SMAD1/5/8 transcription factors, which play a key role in the BMP signaling pathway. CDD-1653 can be used to study diseases related to the BMP signaling pathway .
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-
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- HY-150505
-
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Deubiquitinase
Apoptosis
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Cancer
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DC-U4106 is a USP8 targeting inhibitor with the Kdvalue of 4.7 μM and the IC50 value of 1.2 μM. DC-U4106 can target the ubiquitin pathway and facilitate the degradation of Erα. DC-U4106 inhibits tumor growth with minimal toxicity and has the potential for the research of breast cancer .
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-
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- HY-158102
-
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Histone Methyltransferase
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Cancer
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ORIC-944 is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). ORIC-944 is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer.
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-
-
- HY-150761
-
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Microtubule/Tubulin
Apoptosis
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Cancer
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MY-875 is a competitive microtubulin polymerization inhibitor with an IC50 value of 0.92 μM. MY-875 inhibits microtubulin polymerization by targeting colchicine binding sites and activates the Hippo pathway. MY-875 induces apoptosis and has anticancer activity .
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- HY-158102A
-
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Histone Methyltransferase
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Cancer
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ORIC-944 TFA is the TFA salt form of ORIC (HY-158102). ORIC-944 TFA is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). ORIC-944 TFA is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer .
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-
-
- HY-119711
-
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MMP
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Cancer
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NNGH is a stromelysin-1 (MMP-3) inhibitor. MMP-3 is both a direct transcriptional target and a necessary contributor of the Wnt/β-catenin signaling pathway. Matrix metalloproteinases (MMPs) play a well-defined role in later stages of tumor progression .
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-
- HY-B1876
-
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Acetolactate Synthase (ALS)
Photosystem II
Fungal
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Others
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Nicosulfuron is efficient, harmless, antifungal and selective herbicide belonging to the sulfonylurea family. Nicosulfuron is also a photosynthetic system inhibitor and inhibits acetolactate synthase (ALS) enzyme activity. Nicosulfuron degradation by Plectosphaerella cucumerina AR1 is glucose concentration dependent in planktonic lifestyle. Nicosulfuron enhances the glycolysis pathway and tricarboxylic acid cycle to improve the adaptability of sweet maize. Nicosulfuron reduces the synthesis of branched-chain amino acids (BCAAs), which is proming for maize cultivation .
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-
-
- HY-117229
-
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Drug Metabolite
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Cancer
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Sonidegib metabolite M48 is the main circulating metabolite of Sonidegib. Sonidegib is a hedgehog pathway inhibitor. M48 showed a much longer Tmax (60 h) than Sonidegib .
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-
-
- HY-156441
-
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SARS-CoV
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Infection
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SARS-CoV-2-IN-65 (compound 2f (81)) is a potent,orally active and reversible SARS-CoV-2 entry inhibitor. SARS-CoV-2-IN-65 inhibits the pseudovirus entry in a ACE2-dependent pathway, via mainly inhibiting RBD:ACE2 interaction and TMPRSS2 activity in Calu-3 cells .
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-
-
- HY-163507
-
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Anaplastic lymphoma kinase (ALK)
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Cancer
|
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ALK5-IN-79 (compound 57) is an ALK inhibitor with anticancer activity, by blocking TGF-β1/SMAD signaling pathway. ALK5-IN-79 attenuates the production of extracellular matrix (ECM) and deposition of collagen. ALK5-IN-79 exhibits adequate pharmacokinetic (PK) properties and good in vivo tolerance.
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-
-
- HY-138979
-
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Lipoxygenase
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Others
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Lipoxygenin is a non-redox 5-lipoxygenase (5-LO) inhibitor with an IC50 of 5 μM. Lipoxygenin modulates the β-catenin-5-LO complex, inducing a decrease in β-catenin and 5-LO levels in the nucleus .
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- HY-10431
-
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Organoid
TGF-β Receptor
Apoptosis
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Cancer
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SB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitory activity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways .
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- HY-10431R
-
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Apoptosis
TGF-β Receptor
Organoid
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Cancer
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SB-431542 (Standard) is the analytical standard of SB-431542. SB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitory activity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways .
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-
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- HY-139534
-
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ROR
Apoptosis
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Cancer
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ARI-1 is an inhibitor of receptor tyrosine kinase-like orphan receptor 1 (ROR1) inhibitor. ARI-1 effectively inhibits aberrant ROR1 expression, which is associated with the development of non-small cell lung cancer (NSCLC) and EGFR-TKI-induced drug resistance. ARI-1 binds to the extracellular Frizzled domain of ROR1 and regulates PI3K/AKT/mTOR signaling in a ROR1-dependent manner. ARI-1 potently inhibits NSCLC cell proliferation and migration and has antitumor activity in vivo [1] .
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- HY-153750
-
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Wnt
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Cancer
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Wnt pathway inhibitor 3 is a potent wnt inhibitor with an IC50 value of 45 nM. Wnt pathway inhibitor 3 shows antiproliferative activity .
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- HY-169730
-
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Wnt
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Cancer
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Wnt pathway inhibitor 5 (Compound 28) is wnt pathway inhibitor, with an IC50 value of < 0.003 μΜ. Wnt pathway inhibitor 5 inhibits many cancers, including ovarian teratocarcinoma cancer, breast cancer, osteosarcoma, head and neck squamous carcinoma .
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- HY-N10472
-
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STAT
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Cancer
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STAT3-IN-14 (Compound 1) is a STAT3 inhibitor and has STAT3 phosphorylation inhibitory activity. STAT3-IN-14 (Compound 1) can directly bind to the hinge region of STAT3 .
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- HY-160657
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YAP
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Others
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DC-TEADin04 has weak inhibitory activity against TEAD4 palmitoylation .
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- HY-112670
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-
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- HY-129426
-
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Akt
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Cancer
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PDK1/Akt/Flt dual pathway inhibitor is one of a component of KP372-1 (HY-15673 ), and inhibits PDK1/Akt/Flt dual pathway .
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- HY-133558
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VII-31
1 Publications Verification
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E1/E2/E3 Enzyme
Apoptosis
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Cancer
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VII-31 is a potent NEDDylation pathway activator to inhibit the tumor progression in vitro and in vivo. VII-31 induces apoptosis via intrinsic and extrinsic pathways .
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- HY-101275
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-
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- HY-12238
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endo-IWR 1; IWR-1-endo
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Organoid
Wnt
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Cancer
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IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.
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-
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- HY-13324
-
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RTA 402; NSC 713200; CDDO Methyl ester
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Keap1-Nrf2
Autophagy
Apoptosis
Ferroptosis
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Cancer
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Bardoxolone methyl (NSC 713200; RTA 402; CDDO Methyl ester) is a synthetic triterpenoid compound with potential antineoplastic and anti-inflammatory activities, acting as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway.
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- HY-A0293
-
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Pyrvinium embonate
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Wnt
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Cancer
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Pyrvinium pamoate is an FDA-approved antihelmintic agent that inhibits WNT pathway signaling.
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-
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- HY-N1447
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-
-
- HY-13307
-
JK184
2 Publications Verification
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Hedgehog
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Cancer
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JK184 is a potent Hedgehog (Hh) pathway inhibitor with IC50 of 30 nM in mammalian cells.
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-
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- HY-13901
-
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NSC 136476
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Gli
Autophagy
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Cancer
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GANT 61 is an inhibitor of Gli1 and Gli2 targeting the Hedgehog/GLI pathway.
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-
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- HY-112108
-
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COS
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AMPK
Endogenous Metabolite
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Metabolic Disease
Cancer
|
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Chitosan oligosaccharide (COS) is an oligomer of β-(1→4)-linked D-glucosamine. Chitosan oligosaccharide (COS) activates AMPK and inhibits inflammatory signaling pathways including NF-κB and MAPK pathways.
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- HY-149414
-
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Microtubule/Tubulin
Apoptosis
ERK
TGF-beta/Smad
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Cancer
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MY-673 is a colchicine binding site inhibitor (CBSI), that inhibits tubulin polymerization. MY-673 inhibits the ERK signaling pathway, which in turn affects SMAD4 protein expression levels in the TGF-β/SMAD pathway. MY-673 inhibited cell proliferation, migration and induced apoptosis in vivo and in vitro .
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- HY-N15159
-
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Cyclic GMP-AMP Synthase
STING
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Cladophorol A is a cGAS inhibitor that binds to the conserved adenosine nucleobase binding site of cGAS, thereby blocking its activity. At non-cytotoxic concentrations, Cladophorol A effectively inhibits the overactivation of the cGAS-STING pathway with an IC50 of 370 nM. Cladophorol A holds potential for research on inflammatory diseases related to the overactivation of the cGAS-STING pathway .
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- HY-101098
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-
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- HY-16587
-
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IPI-926; Patidegib
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Smo
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Cancer
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Saridegib is a potent and specific inhibitor of Smoothened (Smo), a key signaling transmembrane protein in the Hedgehog (Hh) pathway.
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- HY-W111144
-
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Hedgehog
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Cancer
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T-1330 (Compound 45) is a Hh pathway inhibitor and reduces Gli1 expression .
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-
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- HY-16587A
-
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IPI 926 hydrochloride; Patidegib hydrochloride
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Smo
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Cancer
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Saridegib hydrochloride is a potent and specific inhibitor of Smoothened (Smo), a key signaling transmembrane protein in the Hedgehog (Hh) pathway.
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-
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- HY-N0371
-
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3-O-Acetyltumulosic acid
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Akt
ERK
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Cancer
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Pachymic acid is a lanostrane-type triterpenoid from P. cocos. Pachymic acid inhibits Akt and ERK signaling pathways.
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- HY-N0498
-
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Parasite
Apoptosis
STAT
Topoisomerase
ERK
FAK
p38 MAPK
NF-κB
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Inflammation/Immunology
Cancer
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Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway, also has anti-inflammatory activity. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway .
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- HY-P10469
-
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NF-κB
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Inflammation/Immunology
Cancer
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NBD-2 is an inhibitor of the NEMO-IKKα/β interaction in the NF-κB signaling pathway. NBD-2 specifically inhibits the typical NF-κB signaling pathway in vitro and in vivo, reducing the inflammatory response in lipopolysaccharide (LPS) induced acute lung injury (ALI). NBD-2 exhibits significant anti-inflammatory activity. NBD-2 can be used to study diseases related to NF-κB signaling pathway, including autoimmune diseases, cancer, etc .
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- HY-15735
-
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c-Met/HGFR
|
Cancer
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c-Met inhibitor 1 is an inhibitor of the c-Met receptor signaling pathway useful for the treatment of cancer including gastric, glioblastoma, and pancreatic cancer.
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-
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- HY-153753
-
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Wnt
|
Cancer
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Wnt pathway inhibitor 4 (compound 16D) is an anticancer agent that has anti-proliferative activity .
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- HY-121118
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-
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- HY-129390
-
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ICP-022
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Btk
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Cancer
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Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK .
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- HY-116455
-
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Fluorescent Dye
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Cancer
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BRD-9526 is a potent and selective Sonic Hedgehog (Shh) pathway inhibitor with potential anti-cancer activity. The mechanism of BRD-9526 is similar in some ways to commonly used inhibitors such as cyclopamine, but is significantly different in other ways. The discovery of BRD-9526 may provide a useful probe for studying complex signaling pathways .
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-
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- HY-N11262
-
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p38 MAPK
ERK
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Inflammation/Immunology
|
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Sudachitin, a polymethoxyflavone that can be isolated from Citrus sudachi, suppresses lipopolysaccharide-induced inflammatory responses in mouse macrophage-like RAW264 cells. Sudachitin can activate the p38MAPK pathway and inhibit the ERK1/2 pathway in HaCaT cells .
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-
-
- HY-110247
-
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TNF Receptor
NF-κB
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Cardiovascular Disease
Inflammation/Immunology
|
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TRAF-STOP inhibitor 6877002 is a selective CD40-TRAF6 interaction inhibitor. TRAF-STOP inhibitor 6877002 exerts anti-atherosclerotic activity by blocking the CD40-TRAF6 signaling pathway, inhibiting classical monocyte activation, leukocyte recruitment, and macrophage activation and migration. TRAF-STOP inhibitor 6877002 reduces the phosphorylation levels of signaling intermediates in the canonical NF-κB pathway .
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-
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- HY-N0498R
-
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Parasite
Apoptosis
STAT
Topoisomerase
ERK
FAK
p38 MAPK
NF-κB
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Inflammation/Immunology
Cancer
|
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Nitidine (chloride) (Standard) is the analytical standard of Nitidine (chloride). This product is intended for research and analytical applications. Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway .
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-
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- HY-10590
-
-
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- HY-162970
-
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Wnt
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Cancer
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XD23 is a potent osteosarcoma inhibitor that works by downregulating DKK1 and activating the WNT/β-catenin signaling pathway.
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-
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- HY-143535
-
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Androgen Receptor
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Cancer
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HG122 promotes androgen receptor (AR) degradation through the proteasome pathway inhibiting the castration-resistant prostate cancer.
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-
- HY-17024
-
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11-Deoxojervine
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Hedgehog
Smo
Endogenous Metabolite
|
Cancer
|
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Cyclopamine is a Hedgehog (Hh) pathway antagonist with an IC50 of 46 nM in the Hh cell assay. Cyclopamine is also a selective Smo inhibitor.
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- HY-103180
-
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Adenosine Receptor
|
Neurological Disease
|
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2'-MeCCPA is a potent and selective A1 adenosine receptors (A1AR) agonist. 2'-MeCCPA efficiently inhibits cAMP modulation in both direct pathway medium spiny neurons (dMSNs) and indirect pathway medium spiny neurons (iMSNs) .
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- HY-N6843
-
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Caspase
PI3K
Akt
mTOR
STAT
|
Cancer
|
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Arnicolide D is a sesquiterpene lactone isolated from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K/AKT/mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner .
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- HY-173063
-
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Toll-like Receptor (TLR)
NF-κB
MyD88
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Inflammation/Immunology
|
|
TLR8 antagonist-1 (Compound 10) is a selective TLR8 antagonist. TLR8 antagonist-1 can inhibit TLR8-mediated inflammation and signaling pathways, reduce the recruitment of MyD88, and inhibit the NF-κB and IRF pathways. TLR8 antagonist-1 has anti-inflammatory activity .
|
-
- HY-P10353
-
-
- HY-144903
-
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GDC-1971
|
SHP2
Phosphatase
p38 MAPK
ERK
|
Cancer
|
|
Migoprotafib (GDC-1971) (compound 199) is a SHP2 inhibitor. Migoprotafib inhibits the MAPK/ERK signaling pathway, and exhibits antitumor activity .
|
-
- HY-161259
-
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JAK
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Inflammation/Immunology
|
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JAK-IN-36 (Compound 12e) is a potent and selective inhibitor of Janus Kinase 1 (JAK1) with a IC50 value of 2.2 nM. JAK-IN-36 can be used in the study of autoimmune diseases .
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-
- HY-N12960
-
|
|
Apoptosis
Bcl-2 Family
Caspase
COX
MMP
STAT
|
Cancer
|
|
Artobiloxanthone (Compound AA3) exhibits antitumor activity, particularly against oral squamous cell carcinoma (OSCC). Artobiloxanthone inhibits Akt/mTOR pathway and STAT3 pathway, inhibits proliferation of SAS and T.Tn (with IC50 of 11 and 22 μM), and inhibits the cancer cell migration. Artobiloxanthone arrests cell cycle at S phase, and induces apoptosis in OSCC cells through activation of caspase 3/9 .
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- HY-P10438
-
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Raf
|
Cancer
|
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Tat-braftide is a peptide inhibitor designed to block the dimerization of BRAF, thereby inhibiting its kinase activity. The destruction of BRAF dimer by Tat-braftide makes BRAF protein more susceptible to proteasome degradation, directly inhibits the activity of BRAF kinase, and reduces the activation of MAPK signaling pathway. Tat-braftide can be used for the role of RAF kinase in MAPK signaling pathway and for the study of BRAF mutant cancers .
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-
- HY-107622
-
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ERK
MEK
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Metabolic Disease
|
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(E/Z)-BIX02188 is a MEK5/ERK5 pathway inhibitor. (E/Z)-BIX02188 inhibits the catalytic function of purified MEK5 enzyme.(E/Z)-BIX02188 can be used for the role of MEK5/ERK5 pathway in various biological systems .
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-
- HY-153596
-
|
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CDK
|
Cancer
|
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SNX7 is a Cyclin-Dependent Kinase Inhibitor (CDKI) pathway inhibitor. SNX7 can be used for research of senescence-related and other CDKI-related diseases .
|
-
- HY-135282
-
-
- HY-101130
-
-
- HY-112181
-
KO-947
4 Publications Verification
|
ERK
|
Cancer
|
|
KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential utility in MAPK pathway dysregulated tumors.
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-
- HY-110074
-
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Others
|
Others
|
|
TWS119 TFA is a specific inhibitor of GSK-3β, with an IC50 of 30 nM, and activates the wnt/β-catenin pathway.
|
-
- HY-142967
-
|
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TGF-β Receptor
|
Cancer
|
|
TGFβ-IN-1 is an antitumor growth and metastasis agent through inhibiting the transforming growth factor‑β signaling pathway.
|
-
- HY-153886
-
Wu-5
1 Publications Verification
|
FLT3
AMPK
Apoptosis
|
Cancer
|
|
Wu-5 is a USP10 inhibitor that can inhibit FLT3 and AMPK pathways, induce FLT3-ITD degradation and induce apoptosis .
|
-
- HY-125168
-
EGA
1 Publications Verification
|
EGFR
|
Infection
Inflammation/Immunology
|
|
EGA is an inhibitor that selectively targets the endosomal trafficking pathways. EGA targets the proteins involved in the endosomal trafficking pathways through which multiple toxins and viruses enter cells. EGA exerts its activity by inhibiting the trafficking from early endosomes to late endosomes, blocking the entry of multiple acid-dependent bacterial toxins and viruses into mammalian cells and delaying the lysosomal targeting and degradation of EGFR .
X
|
-
- HY-117930
-
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ACH-4471
|
Complement System
|
Inflammation/Immunology
|
|
Danicopan (ACH-4471), a selective and orally active small-molecule factor D inhibitor, shows high binding affinity to human Factor D with Kd value of 0.54 nM. Danicopan (ACH-4471) inhibits alternative pathway of complement (APC) activity, has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS) .
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- HY-153480
-
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BAX499
|
Factor Xa
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Others
|
|
ARC19499 is an aptamer that inhibits tissue factor pathway inhibitor (TFPI) , thereby enabling clot initiation and propagation via the extrinsic pathway. The core aptamer binds tightly and specifically to TFPI. ARC19499 blocks TFPI inhibition of both factor Xa and the TF/factor VIIa complex. ARC19499 corrects thrombin generation in hemophilia A and B plasma and restores clotting in FVIII-neutralized whole blood.
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-
- HY-153480A
-
|
BAX499 sodium
|
Factor Xa
Factor VIIa
|
Others
|
|
ARC19499 sodium is an aptamer that inhibits tissue factor pathway inhibitor (TFPI) , thereby enabling clot initiation and propagation via the extrinsic pathway. The core aptamer binds tightly and specifically to TFPI. ARC19499 sodium blocks TFPI inhibition of both factor Xa and the TF/factor VIIa complex. ARC19499 sodium corrects thrombin generation in hemophilia A and B plasma and restores clotting in FVIII-neutralized whole blood.
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-
- HY-P10652
-
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Wnt
β-catenin
|
Cancer
|
|
hsBCL9CT-24 is a Wnt/β-catenin (b-cat) pathway inhibitor with potent anti-tumor effect. hsBCL9CT-24 reactivates anti-cancer immune response suppressed by the oncogenic Wnt pathway and can be utilized for cancer research .
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-
- HY-N4231
-
|
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NF-κB
|
Inflammation/Immunology
|
|
Lucyoside B inhibits the production of inflammatory mediators via both NF-κB and activator protein-1 pathways in activated macrophages .
|
-
- HY-119720
-
|
|
NF-κB
NO Synthase
|
Inflammation/Immunology
|
|
Neocryptotanshinone, a fatty diterpenoids from Salvia Miltiorrhiza, inhibits lipopolysaccharide-induced inflammation by suppression of NF-κB and iNOS signaling pathways .
|
-
- HY-137454
-
|
|
Wnt
β-catenin
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Inflammation/Immunology
|
|
Teplinovivint is a potent wnt/β-catenin signaling pathway inhibitor. Teplinovivint has anti-inflammatory activity and has the potential for tendinopathy research .
|
-
- HY-100790
-
|
HPI-4
|
Hedgehog
|
Cancer
|
|
Ciliobrevin A (HPI-4) is a hedgehog (Hh) signaling pathway inhibitor with median inhibitory concentration (IC50) less than 10 μM .
|
-
- HY-157230
-
|
|
IAP
|
Cancer
|
|
XIAP antagonist 1 degrades rather than inhibits XIAP, catalyzing rapid degradation of XIAP through the ubiquitin-proteasome pathway [2].
|
-
- HY-137996
-
|
|
Akt
mTOR
|
Metabolic Disease
|
|
Dehydrovomifoliol is a AKT/mTOR dual inhibitor. Dehydrovomifoliol reduces lipid accumulation and lipogenesis by inhibiting the AKT/mTOR signaling pathway. Dehydrovomifoliol is used in nonalcoholic fatty liver disease research (NAFLD) .
|
-
- HY-50289
-
|
|
Aldose Reductase
|
Metabolic Disease
|
|
Sorbinil is an aldose reductase inhibitor (ARI) that prevents the accumulation of sorbitol in cells or animals. Sorbinil is useful in studying diabetes and diabetic complications, reducing AR activity and inhibiting the polyol pathway .
|
-
- HY-155619
-
|
|
PKC
PKA
|
Cancer
|
|
Protein kinase inhibitor 7 is an inhibitor for protein kinase A and protein kinase C. Protein kinase inhibitor 7 affects autocrine motility factor (AMF) signaling pathway, without affecting the cell motility .
|
-
- HY-164489
-
|
|
EGFR
Akt
ERK
Apoptosis
|
Cancer
|
|
KU004 is a potent dual EGFR/HER2 inhibitor with anticancer effects. KU004 inhibits the proliferation of human breast cancer SKBR3 cells by inducing G1 phase arrest. KU004 blocks the activation of HER2, EGFR and downstream Akt and Erk pathways and induces cell Apoptosis mainly via the extrinsic pathway. KU004 is a quinazoline derivative .
|
-
- HY-158049
-
|
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Apoptosis
Ferroptosis
|
Cancer
|
|
Anticancer agent 199 (Compound G-4) induces apoptosis in triple negative breast cancer (TNBC) cells via the mitochondrial pathway through inhibiting EGFR, AKT and MAPK pathways. Anticancer agent 199 also induces Ferroptosis by down-regulating LCN2. Anticancer agent 199 inhibits TNBC cell viability and migration, and induces S phase cell cycle arrest. Anticancer agent 199 is a derivate of cyclin-dependent kinase inhibitor Rocovitine .
|
-
- HY-158115
-
|
|
Molecular Glues
Raf
MEK
|
Cancer
|
|
NST-628 is a brain-permeable MAPK pathway molecule glue that inhibits RAF phosphorylation and MEK activation. NST-628 also binds RAF and prevents the formation of BRAF-CRAF and BRAF-ARAF heterodimers, effectively inhibiting the RAS-MAPK pathway. NST-628 inhibits RAS- and RAF-driven cancers and demonstrated potent inhibition in mutant KRAS, NRAS, BRAF class II/III, and NF1-mutant tumors .
|
-
- HY-164428
-
|
|
PKC
|
Cancer
|
|
AE 51310 is an OPN4 inhibitor. AE 51310 inhibits the activation of PKC and the downstream BRAF/MEK/ERKs signaling pathway. AE 51310 can be used for cancer research, such as NSCLC .
|
-
- HY-N1447R
-
|
|
Apoptosis
Autophagy
Endogenous Metabolite
|
Cancer
|
|
Ganoderic acid A (Standard) is the analytical standard of Ganoderic acid A. This product is intended for research and analytical applications. Ganoderic acid A can inhibit of the JAK-STAT3 signaling pathway, also inhibit proliferation, viability, ROS.
|
-
- HY-160169
-
-
- HY-120515
-
|
|
PKC
|
Cancer
|
|
7-Oxostaurosporine is a potent protein kinase C (PKC) inhibitor that effectively inhibits tumor growth by inducing apoptosis and inhibiting the nuclear factor (NF)-κB/p-p65 pathway .
|
-
- HY-P99725
-
|
PF-06741086
|
Thrombin
|
Metabolic Disease
|
|
Marstacimab (PF-06741086) is an anti-tissue factor pathway inhibitor (TFPI) monoclonal antibody. Marstacimab can be used for the research of hemophilia .
|
-
- HY-123548
-
|
|
15-PGDH
|
Inflammation/Immunology
|
|
ML148 is a potent and selective 15-PGDH inhibitor with an IC50 of 56 nM. ML148 has the potential for the research of prostaglandin-signaling pathways .
|
-
- HY-N12473
-
|
|
JAK
|
Inflammation/Immunology
|
|
25-Deacetylcucurbitacin A is a Cucurbitane-Type triterpenoid and has the potential to be an anti-cancer agent and JAK/STAT3 signaling pathway inhibitor .
|
-
- HY-15496
-
|
ER-806201
|
MEK
FLT3
|
Cancer
|
|
E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC50 value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC50 value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC50 value of 19 nM. Anti-tumor and anti-psoriasis efficacy .
|
-
- HY-112179
-
GSK180
1 Publications Verification
|
KMO
|
Inflammation/Immunology
|
|
GSK180 is a selective, competitive, and potent inhibitor of kynurenine-3-monooxygenase (KMO), a key enzyme of tryptophan metabolism (IC50, ~6 nM), but shows negligible activity against other enzymes on the tryptophan pathway. GSK180 rapidly changes levels of kynurenine pathway metabolites, and acts as a useful tool to probe the therapeutic potential of KMO inhibition .
|
-
- HY-131592
-
|
|
Apoptosis
Keap1-Nrf2
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Tricetin is a potent competitive inhibitor of the Keap1-Nrf2 Protein Protein Interaction (PPI). Tricetin protects against 6-OHDA-induced neurotoxicity in Parkinson's disease model by activating Nrf2/HO-1 signaling pathway and preventing mitochondria-dependent apoptosis pathway .
|
-
- HY-N12905
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Celastramycin A isomer is an isomer of Celastramycin A (HY-122292), an antibiotic against Gram-negative bacteria and Mycobacterium tuberculosis with an MIC of 0.05-3.1 μg/mL. Celastramycin A exerts immunosuppressive effects in Drosophila ex vivo via the immunodeficiency pathway (IC50 of 8 ng/mL), inhibits human innate immune responses via the TNF-α pathway, and inhibits IL-8 production in HUEVC with an IC50 of 60 ng/mL .
|
-
- HY-144806
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
PI3K/AKT-IN-1 is an effective PI3K/AKT dual inhibitor (IC50 of 6.99, 4.01 and 3.36 μM for PI3Kγ, PI3Kδ and AKT, respectively). PI3K/AKT-IN-1 has anticancer activity and acts by inhibiting PI3K/AKT axis and inducing caspase 3 dependent apoptosis .
|
-
- HY-102067
-
|
|
Wnt
|
Cancer
|
|
3289-8625 is an inhibitor of the PDZ domain of Dishevelled (Dvl) protein (Kd=10.6 μM) and has an inhibitory effect on Wnt signaling. In addition, 3289-8625 can slow the growth of prostate cancer PC-3 cells (IC50=12.5 μM). 3289-8625 can be used in the study of embryonic development and cancer .
|
-
- HY-170496
-
|
|
Wnt
|
Cancer
|
|
Fluc-IN-1 (Compound 3) is an inhibitor for firefly luciferase with an IC50 of 25 nM. Fluc-IN-1 inhibits WNT/β-catenin signaling pathway with an IC50 of 33 nM (measuring by TOPFlash assay) .
|
-
- HY-B1787
-
|
|
mTOR
Drug Metabolite
|
Cancer
|
|
Sulindac sulfone is an mTORC1 pathway inhibitor and a metabolite of Sulindac. Sulindac sulfone inhibits colon cancer cell growth and induces cell cycle arrest. Sulindac sulfone is used in cancer research .
|
-
- HY-15901
-
|
|
mTOR
|
Cancer
|
|
LGB321 is an inhibitor of PIM2-dependent multiple myeloma cell lines, effectively inhibiting proliferation and key signaling pathways such as mTOR-C1 and phosphorylation of BAD .
|
-
- HY-112502C
-
|
Adenosine 5'-(α,β-methylene)diphosphate triammonium
|
CD73
|
Cancer
|
|
MethADP (Adenosine 5'-(α,β-methylene)diphosphate) triammonium is a CD73 inhibitor. MethADP can be used for the research of ATP-adenosine pathway .
|
-
- HY-W775186
-
|
|
Fungal
|
Infection
|
|
Tolprocarb is an oomyces fungicide, which has a strong inhibitory effect on rice blast fungus Magnaporthe grisea by inhibiting polyketide synthase in melanin synthesis pathway .
|
-
- HY-138558
-
-
- HY-120864
-
|
|
Wnt
|
Cancer
|
|
SEN461 is a potent and orally active Wnt pathway inhibitor. SEN461 shows effective anti-tumor activity and can be used for GBM research .
|
-
- HY-108277
-
|
|
Apoptosis
|
Cancer
|
|
Ginsenoside F5, from crude extracts of flower buds of Panax ginseng, remarkably inhibits the growth of HL-60 cells by the apoptosis pathway .
|
-
- HY-163513
-
|
|
Wnt
|
Endocrinology
|
|
AACA is an inhibitor for sclerostin, that binds sclerostin on loop3 region with Kd of 15.4 nM. AACA exhibits anti-osteoporosis activity through Wnt signaling pathway .
|
-
- HY-110218
-
CW 008
1 Publications Verification
|
PKA
Epigenetic Reader Domain
|
Others
|
|
CW 008, a derivative of pyrazole-pyridine, is a CREB or PKA pathway agonist. CW 008 also is a stem cell differentiating agent. CW 008 stimulates osteoblast differentiation of human MSCs and increases bone formation in ovariectomized mice. CW008 promotes osteogenesis by activating cAMP/PKA/CREB signaling pathway and inhibiting leptin secretion .
|
-
- HY-B1014
-
-
- HY-N7695
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
Physalin B, one of the major active steroidal constituents of Cape gooseberry, induces cell cycle arrest and triggers apoptosis in breast cancer cells through modulating p53-dependent apoptotic pathway. Physalin B inhibits the ubiquitin-proteasome pathway and induces incomplete autophagic response in human colon cancer cells in vitro .
|
-
- HY-160169A
-
-
- HY-12808
-
|
|
NAMPT
AMPK
mTOR
|
Cancer
|
|
STF-118804 is a highly specific NAMPT inhibitor. STF-118804 activates AMPK and inhibits mTOR pathways. STF-118804 has antitumor activity against pancreatic cancer .
|
-
- HY-115449
-
|
94G6
|
IGF-1R
Akt
mTOR
|
Cancer
|
|
Chromeceptin (94G6) is an IGF signaling pathway inhibitor. Chromeceptin suppresses IGF2 expression at mRNA and protein levels in hepatocyte and HCC cells. Chromeceptin inhibits the phosphorylation levels of AKT and mTOR .
|
-
- HY-N0247
-
|
|
Smo
|
Cancer
|
|
Saikosaponin B1 is a bioactive constituent of Radix Bupleuri with anticancer activity. Saikosaponin B1 significantly inhibits tumor growth in Medulloblastoma (MB) model by inhibiting the Hedgehog pathway through targeting SMO .
|
-
- HY-N9971
-
-
- HY-112502D
-
|
Adenosine 5'-(α,β-methylene)diphosphate trisodium
|
CD73
|
Cancer
|
|
MethADP (Adenosine 5'-(α,β-methylene)diphosphate) trisodium is a CD73 inhibitor. MethADP trisodium can be used for the research of ATP-adenosine pathway .
|
-
- HY-155646
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 48 is an anti-inflammatory agent based on its role in inhibiting the NF-κB signaling pathway and activating HO-1 expression .
|
-
- HY-153214
-
|
|
Wnt
β-catenin
|
Cancer
|
|
YW2036 (compound 2a) is a potent Wnt/β-Catenin signaling pathway inhibitor with an IC50 value of 637 nM. YW2036 can be used in research of cancer .
|
-
- HY-153730
-
|
|
Hedgehog
|
Inflammation/Immunology
|
|
Hedgehog IN-5 is an orally active small molecule inhibitor of the hedgehog pathway. Hedgehog IN-5 can be used for the research of fibrotic disease .
|
-
- HY-139844
-
|
|
p38 MAPK
NF-κB
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 7 inhibits proinflammatory cytokines by blocking the NF-κB/MAPK signaling pathway in LPS-treated RAW 264.7 cells as well as mice.
|
-
- HY-162966
-
|
|
Cyclic GMP-AMP Synthase
|
Cancer
|
|
MS7829 is a cGAS inhibitor-based deubiquitinase-targeted chimera (DUBTAC), a targeted protein stabilization (TPS) technology. cGAS is a key component in the cGAS-STING pathway. .
|
-
- HY-P99965
-
|
SKY59; RO7112689
|
Complement System
|
Cardiovascular Disease
Metabolic Disease
|
|
Crovalimab (SKY59; RO7112689) is a novel humanized antibody against C5 in a pH-dependent manner with KDs of 15.2 nM and 16.8 μM at pH 7.4 and 5.8, respectively. Crovalimab binds human FcRn with great affinity (KD: 17 μM at pH 6.0). Crovalimab can block cleavage of C5 by the C5 convertase and inhibite the activity of a C5 variant (p.Arg885His). Crovalimab inhibits C5b-9 formation significantly in all three complement pathways, the classical pathway (CP), lectin pathway (LP), and alternative pathway (AP). Crovalimab has the potential for paroxysmal nocturnal hemoglobinuria (PNH) and complement-mediated diseases research .
|
-
- HY-160633
-
|
|
Parasite
|
Infection
|
|
PfFAS-II inhibitor 1 (Compound 3) is a Plasmodium falciparum type II fatty acid biosynthesis pathway (PfFAS-II) inhibitor, with an IC50 of 0.63 μM for PfFabI enzyme. PfFAS-II inhibitor 1 has antimalarial activity .
|
-
- HY-153190A
-
|
|
Ferroptosis
STAT
|
Cancer
|
|
W1131 TFA is a potent STAT3 inhibitor that induces ferroptosis. W1131 inhibits cancer progression in subcutaneous xenograft, organoid, and PDX models of gastric cancer. W1131 effectively alleviates cancer cell chemoresistance to 5-FU (HY-90006). W1131 regulates the cell cycle, DNA damage response, and oxidative phosphorylation, including the IL6-JAK-STAT3 pathway and the ferroptosis pathway .
|
-
- HY-15672
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Neurological Disease
Cancer
|
|
FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC50 of 80 nM in HeLa cells. FM19G11 modulates other signaling pathways, including mTOR and PI3K/Akt/eNOS, when the HIF-1α pathway is inactivated under normoxic conditions .
|
-
- HY-169212
-
|
|
PI3K
Annexin A
ERK
VEGFR
STAT
Raf
FAK
Akt
Ras
|
Cancer
|
|
I194496 is a potent cystathionine γ-lyase (CSE) inhibitor, with an IC50 of 0.79 mM. I194496 can inhibit the growth of human TNBC cells via the dual targeting PI3K/Akt and Ras/Raf/ERK pathway and suppress the metastasis of human TNBC cells via down-regulating Anxa2/STAT3 and VEGF/FAK/Paxillin signaling pathways .
|
-
- HY-N2877
-
|
|
Potassium Channel
Sodium Channel
Na+/K+ ATPase
Calcium Channel
Apoptosis
|
Neurological Disease
Cancer
|
|
Annonacin is an acetylgenin that is toxic by inhibiting the pathway of the mitochondrial complex. Annonacin increases tau phosphorylation in R406W +/+ mice. Annonacin acts as an inhibitor of the sodium/potassium and sarcoplasmic reticulum (SERCA) ATPase pumps. Annonacin has significant killing effect on ovarian cancer cell, cervical cancer cell, breast cancer cell, bladder cancer cell and skin cancer cell. Annonacin induces apoptosis through Bax and Caspase-3-related pathways .
|
-
- HY-107818
-
|
|
NF-κB
|
Cardiovascular Disease
Inflammation/Immunology
|
|
4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity . 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice .
|
-
- HY-126718
-
|
Ketohypoglycin
|
Mitochondrial Metabolism
|
Metabolic Disease
|
|
Methylenecyclopropylpyruvate (Ketohypoglycin) is an inhibitor for gluconeogenesis. Methylenecyclopropylpyruvate inhibits ketogenesis and affects the fatty acids metabolism. Methylenecyclopropylpyruvate may interfere with the mitochondrial β-oxidation pathway, affects the contents and composition of coenzyme A, and affects the glucose homeostasis .
|
-
- HY-126741
-
|
|
Apoptosis
Parasite
NF-κB
Bcl-2 Family
Caspase
|
Infection
Inflammation/Immunology
Cancer
|
|
Azadirachtin is an oral active triterpenoid compound with anticancer, antimalarial, anti-inflammatory, and insecticidal activities. Azadirachtin induces cell apoptosis through the mitochondrial pathway (by inhibiting Bcl-2/Bax ratio or activating Apaf-1 and caspase-3) or through death receptors (by inhibiting TNFR activation). Additionally, Azadirachtin exerts its anti-inflammatory effects by inhibiting NF-кB signaling pathway activation, and it exhibits insecticidal activity by inducing apoptosis in insect cells .
|
-
- HY-P10854
-
|
|
NF-κB
Interleukin Related
STAT
Akt
|
Neurological Disease
Inflammation/Immunology
|
|
TAT-N15 is a p55PIK inhibitor with remarkable anti-inflammatory activity and neuroprotective effects. TAT-N15 can significantly inhibit the activation of IL-6, IL-8, Akt, and NF-κB pathways, as well as suppress the protein expression of phosphorylated STAT3 and NF-κB. By inhibiting the activation of Akt, STAT3, and NF-κB pathways, TAT-N15 is used in research on acute conjunctivitis, allergic rhinitis, chronic obstructive pulmonary disease (COPD), and stroke .
|
-
- HY-N0298
-
-
- HY-127067
-
|
|
Akt
EGFR
mTOR
|
Inflammation/Immunology
Cancer
|
|
Yuanhuadin, extracted from Genkwa Flos Daphne genkwa, has antitumor activity through inhibiting Akt/mTOR and EGFR pathways, induce cell-cycle arrest and abortion .
|
-
- HY-N7507A
-
|
|
Wnt
β-catenin
|
Cancer
|
|
Sempervirine is an alkaloid derived from Gelsemium elegans Benth.. Sempervirine inhibits the proliferation of hepatocellular carcinoma (HCC) cells and induces apoptosis by regulating Wnt/β-catenin pathway .
|
-
- HY-153457
-
|
|
Hedgehog
|
Cancer
|
|
Hedgehog IN-3 (compound 3) is a hedgehog pathway inhibitor (IC50 = 0.01 µM). Hedgehog IN-3 can be used in cancer research .
|
-
- HY-A0293R
-
|
|
Wnt
|
Cancer
|
|
Pyrvinium pamoate (Standard) is the analytical standard of Pyrvinium pamoate. This product is intended for research and analytical applications. Pyrvinium pamoate is an FDA-approved antihelmintic agent that inhibits WNT pathway signaling.
|
-
- HY-N0436
-
|
|
NF-κB
|
Infection
Inflammation/Immunology
|
|
Engeletin is a flavanonol glycoside isolated from Smilax glabra Roxb. , inhibits NF-κB signaling-pathway activation, and possesses anti-inflammatory, analgesic, diuresis, detumescence, and antibiosis effects.
|
-
- HY-N3720
-
|
6-Demethoxycapillarisin
|
PEPCK
|
Metabolic Disease
|
|
Demethoxycapillarisin (6-Demethoxycapillarisin) inhibits PEPCK mRNA levels (IC50: 43 μM) by activation of the PI3K pathway. Demethoxycapillarisin decreases glucose production .
|
-
- HY-121944
-
|
|
Casein Kinase
|
Others
|
|
Ricinine exhibits hepatoprotection in CCl4-induced liver damage. Ricinine is also a CK1α inhibitor, and may activate Wnt pathway .
|
-
- HY-N7674A
-
|
|
STAT
|
Cancer
|
|
Angoline hydrochloride is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline hydrochloride inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation .
|
-
- HY-164478
-
|
|
PARP
|
Cancer
|
|
G-631 is a selective inhibitor for tankyrase. G-631 inhibits tankyrase auto-PARsylation (poly ADP ribosylation) with an IC50 of 7 nM, and inhibits Wnt signaling pathway. G-631 exhibits good pharmacokinetic characteristics in mice .
|
-
- HY-N7674
-
|
|
Interleukin Related
STAT
|
Cancer
|
|
Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation .
|
-
- HY-131542
-
|
|
Aldose Reductase
Apoptosis
|
Metabolic Disease
|
|
APPA is an aldose reductase inhibitor. APPA can effectively prevent apoptosis and the symptoms of Streptozotocin (HY-13753)-induced diabetes by inhibiting the polyol pathway in rats. APPA has the potential for diabetic nephropathy (DN) research .
|
-
- HY-N9647
-
|
|
Wnt
β-catenin
Apoptosis
|
Cancer
|
|
Dalbinol is a rotenoid compound. Dalbinol can inhibit Wnt/β-catenin signaling pathway and promote β-catenin degradation. Dalbinol inhibits tumor cells proliferation and induces apoptosis. Dalbinol has antitumor activity .
|
-
- HY-N3188
-
|
|
Akt
NF-κB
|
Infection
|
|
Niloticin, tetracyclic triterpenoid compound, is a osteoclastogenesis inhibitor. Niloticin shows anti-viral, antioxidative, and mosquitocidal activities. Niloticin inhibits osteoclastogenesis by blocking RANKL-RANK interaction and suppressing the AKT, MAPK, and NF-κB signaling pathways .
|
-
- HY-134919
-
|
|
Cyclic GMP-AMP Synthase
|
Inflammation/Immunology
|
|
CU-76 is an inhibitor for human cyclic GMP-AMP synthase (hcGAS) with an IC50 of 0.24 μM. CU-76 selectively inhibits the DNA pathway in human cells, and can be used in autoimmune research .
|
-
- HY-169671
-
|
|
Wnt
|
Cancer
|
|
21H7 is a selective inhibitor of the Wnt/b-catenin pathway. 21H7 markedly inhibits the growth of HFs. 21H7 potently decreases growth of breast and colon cancer cells .
|
-
- HY-163536
-
|
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
TGF-β1/Smad3-IN-1 (Compound 5aa) is an inhibitor of the TGF-β1/Smad3 signaling pathway(IC50=1.07 μM). TGF-β1/Smad3-IN-1 possesses antifibrotic activity and oral potency .
|
-
- HY-131923
-
|
|
Notch
|
Cancer
|
|
DAPM is a Notch pathway inhibitor with anticancer activity and antiproliferative effects. DAPM effectively inhibits tubular adenoma development by inhibiting cell proliferation and inducing the expression of Krüppel-like factor 4 (KLF4) and p21 in human colon cancer cells .
|
-
- HY-N0738
-
|
|
NF-κB
Endogenous Metabolite
|
Cardiovascular Disease
Cancer
|
|
Stachydrine hydrochloride is the major active constituent of Leonurus artemisia, which is a potential therapy for cardiovascular diseases . Stachydrine can inhibit the NF-κB signal pathway. Anti-hypertrophic activities .
|
-
- HY-141807
-
|
|
PROTACs
Akt
|
Cancer
|
|
MS21, a novel degrader of AKT, selectively inhibits the growth of PI3K/PTEN pathway-mutant cancers with wild-type KRAS and BRAF.
|
-
- HY-N0371R
-
|
|
Akt
ERK
|
Cancer
|
|
Pachymic acid (Standard) is the analytical standard of Pachymic acid. This product is intended for research and analytical applications. Pachymic acid is a lanostrane-type triterpenoid from P. cocos. Pachymic acid inhibits Akt and ERK signaling pathways.
|
-
- HY-145927
-
NXP800
1 Publications Verification
CCT361814
|
HSP
|
Cancer
|
|
NXP800 (CCT361814) is a potent and orally active heat shock factor 1 (HSF1) pathway inhibitor. NXP800 has the potential for cancer research .
|
-
- HY-N1382
-
-
- HY-148052
-
|
|
RIP kinase
|
Cancer
|
|
RIPK3-IN-2 is a RIP3 inhibitor. RIPK3-IN-2 can be used in diseases caused by or associate with activated necrotic pathways research .
|
-
- HY-W874892
-
|
CBDP
|
Reactive Oxygen Species
|
Cancer
|
|
Cannabidiphorol (CBDP) is a phytocannabinoid that increases the production of reactive oxygen species (ROS) and activates cellular pathways related to ROS signaling. Cannabidiphorol inhibits cell viability of breast cancer cells .
|
-
- HY-122019
-
|
|
NF-κB
ERK
Apoptosis
|
Others
|
|
ABD56 is a compound that induces osteoclast apoptosis and has the activity of inhibiting osteoclast formation and inducing apoptosis. ABD56 can inhibit osteoclast formation and induce apoptosis, and its mechanism is related to the inhibition of NFκB and ERK pathways.
|
-
- HY-113054
-
|
|
Acyltransferase
Bacterial
Endogenous Metabolite
|
Infection
Metabolic Disease
|
|
DL-Glyceraldehyde 3-phosphate is an intermediate in several metabolic pathways, including glycolysis and gluconeogenesis. DL-Glyceraldehyde 3-phosphate is a potent inhibitor of the growth of E. coli. DL-Glyceraldehyde 3-phosphate is a competitive inhibitor of the acyltransferase .
|
-
- HY-108441
-
|
|
β-catenin
|
Cancer
|
|
CCT 031374 hydrobromid is a potent inhibitor of β-catenin/transcription factor (TCF) complex signaling. CCT031374 inhibits TCF-dependent transcription of genes of Wnt signaling pathway. CCT 031374 has antitumor activity .
|
-
- HY-149403
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Others
|
|
J-1048 is an activin receptor-like kinase 5 (ALK5) inhibitor. J-1048 can inhibit TAA-induced liver fibrosis in mice by explicitly blocking the TGF-β/Smad signaling pathway .
|
-
- HY-10440
-
|
GDC-0449
|
Hedgehog
Autophagy
|
Cancer
|
|
Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively .
|
-
- HY-N13121
-
|
|
HDAC
Apoptosis
p38 MAPK
|
Cancer
|
|
Daphnegiravone D (compound 70) is an HDAC6 inhibitor with anti-hepatocellular carcinoma activity. Daphnegiravone D can induce apoptosis and selectively inhibit the proliferation of liver cancer cells through the p38 and JNK MAPK pathways .
|
-
- HY-U00460
-
|
|
IRE1
|
Cancer
|
|
3,6-DMAD hydrochloride, an acridine derivative, is a potent IRE1α-XBP1s pathway inhibitor. 3,6-DMAD hydrochloride promotes IL-6 secretion via the IRE1α-XBP1s pathway. 3,6-DMAD hydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD hydrochloride can be used for research of cancer .
|
-
- HY-U00460B
-
|
|
IRE1
|
Cancer
|
|
3,6-DMAD dihydrochloride, an acridine derivative, is a potent IRE1α-XBP1s pathway inhibitor. 3,6-DMAD dihydrochloride promotes IL-6 secretion via the IRE1α-XBP1s pathway. 3,6-DMAD dihydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD dihydrochloride can be used for research of cancer .
|
-
- HY-147082
-
GA-017
2 Publications Verification
|
YAP
|
Cancer
|
|
GA-017 is a potent and selective LATS1 and LATS2 (large tumor suppressor kinase 1/2) inhibitor, with IC50 values of 4.10 and 3.92 nM, respectively. GA-017 is an activator of cell proliferation. GA-017 promotes YAP/TAZ activation and nuclear translocation. GA-017 promotes cell growth under 3D culture conditions. GA-017 enhances the ex vivo formation of mouse intestinal organoids .
|
-
- HY-147670
-
|
|
Hedgehog
Smo
Gli
Apoptosis
|
Cancer
|
|
TPB15 is an orally active and potent Hh (Hedgehog) signaling inhibitor. TPB15 markedly induces cell cycle arrest and apoptosis in MDA-MB-468 cells. TPB15 blocks Smo (Smoothened) translocation into the cilia and reduced Smo protein and mRNA expression. TPB15 inhibits the expression of the downstream regulatory factor glioma-associated oncogene 1 (Gli1). TPB15 shows good anti-tumor activity with low toxicity .
|
-
- HY-156466
-
|
|
JAK
|
Inflammation/Immunology
|
|
QL-1200186 is anorally activeand selective inhibitor ofTYK2. Oral administration of QL-1200186, dose-dependently inhibitsinterferon-γ(IFNγ) production afterinterleukin-12(IL-12) challenge and significantly ameliorates skin lesions in psoriatic mice .
|
-
- HY-N15252
-
|
|
VEGFR
ERK
Akt
|
Cardiovascular Disease
|
|
Eutypenes I (Compound 9) inhibits the secretion of VEGF-A, inhibits the activation of VEGFR and the downstream Erk/Akt signaling pathway. Eutypenes I inhibits the migration of cell HMEC-1, and exhibits anti-angiogenic activity in Sprague-Dawley’s rat models .
|
-
- HY-161239
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
(S)-IB-96212 (compound 4), an oligomycin derivative, inhibits the MurD2 reaction, but not the MurL reaction. (S)-IB-96212 is a specific inhibitor of the alternative pathway of peptidoglycan biosynthesis. (S)-IB-96212 weakly inhibits the MurD reaction .
|
-
- HY-N10458
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Asperbisabolane L, a sesquiterpenoid, exerts the anti-inflammatory activity by inhibiting the NF-κB-activated pathway. Asperbisabolane L inhibits the translocation of NF-κB from cytoplasm to the nucleus. Asperbisabolane L also inhibits NO production in LPS-activated BV-2 microglia cells .
|
-
- HY-W010201
-
|
(±)-Citronellol; (±)-β-Citronellol
|
Reactive Oxygen Species
ERK
PI3K
TNF Receptor
Atg8/LC3
p62
Apoptosis
Necroptosis
Autophagy
Fungal
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Citronellol ((±)-Citronellol) is an orally active inducer of apoptosis. Citronellol can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis .
|
-
- HY-172175
-
|
|
mTOR
Akt
PI3K
Apoptosis
Autophagy
|
Cancer
|
|
HYS-072 is an orally active derivative of chrysin (HY-14589) with antitumor activity. HYS-072 induces apoptosis and autophagy by inhibiting the PI3K/AKT/mTOR signaling pathway and suppresses tumor growth in vivo in xenograft models by modulating autophagy-related pathways. HYS-072 can be used in the research of triple-negative breast cancer .
|
-
- HY-N0231
-
|
Broussochalcone B
|
Bacterial
Antibiotic
NF-κB
PERK
Akt
Autophagy
Apoptosis
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Bavachalcone is a potent inducer of apoptosis. Bavachalcone exerts anticancer activity by promoting autophagy and apoptosis in HepG2 cells. Bavachalcone acts as an anti-neuroinflammatory and antidepressant through the NF-κB pathway. Bavachalcone inhibits osteoclasts by interfering with ERK and Akt signaling pathways and the expression of c-Fos and NFATc1. Bavachalcone exhibits a significant inhibitory effect on baculovirus-expressed BACE-1 in vitro .
|
-
- HY-170585
-
|
|
COX
NF-κB
|
Inflammation/Immunology
|
|
COX-2-IN-51 (E25) is a potent COX-2 inhibitor, with an IC50 of 70.7 nM. COX-2-IN-51 significantly inhibits LPS-induced release of NO and PGE2, expression of COX-2 and iNOS, and activation of NF-κB pathway. COX-2-IN-51 exhibits anti-inflammatory and analgesic effects in diverse murine models through inhibiting NF-κB pathway. COX-2-IN-51 has lower gastrointestinal side effects than Indomethacin (HY-14397) .
|
-
- HY-172088
-
|
|
Microtubule/Tubulin
MMP
NF-κB
Apoptosis
|
Cancer
|
|
Tubulin/MMP-IN-3 (Compound 15j) is the dual inhibitor for tubulin polymerization and MMP, and inhibits MMP-2 and MMP-9 with IC50 of 21.13 μM and 19.24 μM. Tubulin/MMP-IN-3 inhibits NF-κB signaling pathway, causes mitochondrial dysfunction and the apoptosis through a mitochondrial-dependent pathway. Tubulin/MMP-IN-3 exhibits antiproliferative activity in a variety of cancer cells, arrests the cell cycle at G2/M phase, and exhibits antitumor efficacy in mouse models .
|
-
- HY-148877
-
|
|
HSP
HSV
HIF/HIF Prolyl-Hydroxylase
VEGFR
NF-κB
ERK
Akt
FAK
|
Infection
Inflammation/Immunology
Cancer
|
|
AT-533 is a potent Hsp90 and HSV inhibitor. AT-533 suppresses tumor growth and angiogenesis by blocking the HIF-1α/VEGF/VEGFR-2 signaling pathway. AT-533 also inhibits the activation of the downstream pathways, including Akt/mTOR/p70S6K, Erk1/2 and FAK. AT-533 inhibits the tube formation, cell migration, and invasion of human umbilical vein endothelial cells (HUVECs) .
|
-
- HY-N10913
-
-
- HY-119264
-
|
|
HIF/HIF Prolyl-Hydroxylase
Ras
|
Cancer
|
|
PRLX-93936 dihydrochloride (Compound 16) is a HIF-1α inhibitor with anticancer activity. PRLX-93936 can inhibit the activated Ras pathway and can be used in the study of relapsed or refractory multiple myeloma .
|
-
- HY-137443
-
|
|
CDK
Wnt
|
Cancer
|
|
Ipivivint (Compound 38) is an orally active and potent CDC-like kinase (CLK) inhibitor with EC50s of 1 nM, 7 nM for CLK2 and CLK3, respectively. Ipivivint inhibits Wnt pathway (EC50=13 nM) .
|
-
- HY-121280
-
|
|
ERK
|
Cancer
|
|
ERK2-IN-4 (Compound 6o) is an effective and selective ERK2 inhibitor with a Ki of 0.006 μM. ERK2-IN-4 inhibits the ERK signaling pathway and can be used in cancer research .
|
-
- HY-119264A
-
|
|
HIF/HIF Prolyl-Hydroxylase
Ras
|
Cancer
|
|
PRLX-93936 dihydrochloride (Compound 16) is a HIF-1α inhibitor with anticancer activity. PRLX-93936 can inhibit the activated Ras pathway and can be used in the study of relapsed or refractory multiple myeloma .
|
-
- HY-117726
-
-
- HY-14804A
-
|
LY 573636 sodium
|
Apoptosis
|
Cancer
|
|
Tasisulam is a anticancer agent and induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death. Tasisulam inhibits mitotic progression and induces vascular normalization .
|
-
- HY-18770B
-
-
- HY-150169
-
|
|
TGF-β Receptor
|
Cancer
|
|
THRX-144644 is a Lung-restricted ALK5 inhibitor with an IC50 value of 0.14 nM. THRX-144644 avoids systemic toxicities associated with TGFβ pathway inhibition .
|
-
- HY-123752
-
|
|
Hedgehog
Smo
|
Cancer
|
|
MS-0022 is a Smoothened (SMO) antagonist. MS-0022 can inhibit the Hedgehog (Hh) signaling pathway. MS-0022 can be used in anti-tumor research .
|
-
- HY-169508
-
|
|
Wnt
|
Others
|
|
BMD4503-1 is a quinoxaline derivative. BMD4503-1 can inhibit the LRP5/6-Sclerostin interaction and regulate the Wnt signaling pathway .
|
-
- HY-14804
-
|
LY 573636
|
Molecular Glues
Apoptosis
|
Cancer
|
|
Tasisulam is a anticancer agent and induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death. Tasisulam inhibits mitotic progression and induces vascular normalization .
|
-
- HY-N0208
-
|
|
p38 MAPK
NF-κB
|
Inflammation/Immunology
|
|
Kaempferol-3-O-glucorhamnoside, a flavonoid derived from plant Thesium chinense Turcz, inhibits inflammatory responses via MAPK and NF-κB pathways in vitro and in vivo .
|
-
- HY-W001174
-
|
|
ERK
NF-κB
|
Inflammation/Immunology
|
|
2,5-Dihydroxyacetophenone, isolated from Rehmannia glutinosa, inhibits the production of inflammatory mediators in activated macrophages by blocking the ERK1/2 and NF-κB signaling pathways .
|
-
- HY-P99465
-
|
BAY 1093884
|
Thrombin
|
Cardiovascular Disease
|
|
Befovacimab (BAY 1093884) is a fully human monoclonal IgG2 antibody able to bind to tissue factor pathway inhibitor (TFPI). Befovacimab can be used for haemophilia A/B research .
|
-
- HY-145302
-
|
|
Bacterial
|
Infection
|
|
Mycobactin-IN-2 (compound 49) is a mycobactin biosynthesis inhibitor against mycobacteria. Mycobactin-IN-2 binds to salicyl-AMP ligase (MbtA), a key enzyme in the mycobactin biosynthetic pathway .
|
-
- HY-152193
-
|
|
Apoptosis
|
Cancer
|
|
ChoKα inhibitor-4 is a bioisosteric inhibitor of HChoK α1 (IC50=0.66 μM), with inhibitory and antiproliferative effect on cancer cells. ChoKα inhibitor-4 induces apoptosis via mitochondrial pathway, and reduces anti-apoptotic proteins expression .
|
-
- HY-145860
-
|
|
Phosphoglycerate Dehydrogenase (PHGDH)
|
Cancer
|
|
PHGDH-IN-2 is a potent and NAD + competitive PHGDH inhibitor with an IC50 of 5.2 µM. PHGDH-IN-2 inhibits the serine synthetic pathway in MDA-MB-468 cells. PHGDH-IN-2 inhibits the growth of PHGDH-dependent cancer cells .
|
-
- HY-W006230
-
|
|
Cytochrome P450
|
Cancer
|
|
Anthraflavic acid, a flavonoid, is a potent IQ mutagenicity inhibitor by virtue of its ability to inhibit both its microsomal and cytosolic activation pathways. Anthraflavic acid is a potent and specific cytochrome P-448 inhibitor activity an enzyme system closely associated with the activation of many chemical carcinogens .
|
-
- HY-103438A
-
|
|
Apoptosis
Autophagy
Akt
|
Cancer
|
|
BIBU1361 dihydrochloride induces apoptosis and inhibits autophagy. BIBU1361 inhibits pro-survival pathways Akt/mTOR and gp130/JAK/STAT3, and decreased levels of pro-inflammatory cytokine IL-6 .
|
-
- HY-160493
-
|
|
Wnt
β-catenin
|
Cancer
|
|
PTK7/β-catenin-IN-6 (Compound 03653) is an inhibitor for PTK7/β-catenin interaction, which inhibits the Wnt signaling pathway, and exhibits an anticancer activity against colorectal cancer (CRC) .
|
-
- HY-156814
-
|
|
Hedgehog
|
Cancer
|
|
HPP-9 is a Proteolysis-Targeting Chimeras （PROTACs） based on Hedgehog Pathway Inhibitor-1 (HPI-1), with the pIC50 of 6.71, that can degrade BET bromodomains. HPP-9 has antitumor activity [1[.
|
-
- HY-N0883
-
|
Gamabufagin
|
VEGFR
|
Cancer
|
|
Gamabufotalin (Gamabufagin), a main active compound isolated from Chinese medicine Chansu, has been shown to strongly inhibit cancer cell growth and inflammatory response. Gamabufotalin could inhibite angiogenesis by inhibiting the activation of VEGFR-2 signaling pathways.
|
-
- HY-103438
-
|
|
Apoptosis
Akt
Autophagy
|
Cancer
|
|
BIBU1361 induces apoptosis and inhibits autophagy. BIBU1361 inhibits pro-survival pathways Akt/mTOR and gp130/JAK/STAT3, and decreased levels of pro-inflammatory cytokine IL-6 .
|
-
- HY-141891
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
M435-1279 is a UBE2T inhibitor. M435-1279 inhibits the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1 .
|
-
- HY-160040A
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Cobitolimod sodium is a DNA oligonucleotide agonist of TLR-9 with anti-inflammatory activity. Cobitolimod sodium inhibits Th17 cells and induces anti-inflammatory FoxP3 and IL-10 expression, inhibiting the IL-17 signaling pathway .
|
-
- HY-14664DS
-
|
(3S,5R)-XU 62-320-d6 free acid
|
Autophagy
|
Cardiovascular Disease
Cancer
|
|
(3S,5R)-Fluvastatin-d6 is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
|
-
- HY-N3925
-
|
|
Bacterial
|
Infection
Metabolic Disease
Inflammation/Immunology
|
|
Ganoderol A is a terpenoid extracted from Ganoderma lucidum with antimicrobial activities. Ganoderol A inhibits cholesterol synthesis pathway and has significant anti-inflammatory activity and protection against ultraviolet A (UVA) damage .
|
-
- HY-N6017
-
|
|
HDAC
|
Cancer
|
|
Bakkenolide A is a natural product extracted from Petasites tricholobus. Bakkenolide A inhibits leukemia by regulation of HDAC3 and PI3K/Akt-related signaling pathways .
|
-
- HY-17024R
-
|
|
Hedgehog
Smo
Endogenous Metabolite
|
Cancer
|
|
Cyclopamine (Standard) is the analytical standard of Cyclopamine. This product is intended for research and analytical applications. Cyclopamine is a Hedgehog (Hh) pathway antagonist with an IC50 of 46 nM in the Hh cell assay. Cyclopamine is also a selective Smo inhibitor.
|
-
- HY-15398C
-
|
Epicholecalciferol
|
Hedgehog
|
Cancer
|
|
3-epi-Vitamin D3 (Epicholecalciferol) (Compound 4), a Vitamin D3 analogue, is a Hedgehog pathway inhibitor with an IC50 of 39.2 μM measured in U87MG cells .
|
-
- HY-N8311
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Goshonoside F5 can be isolated from the unripe fruits of Rubus chingii. Goshonoside F5 has anti-inflammatory activity, and inhibits NF-κB and MAPK signaling pathway .
|
-
- HY-N7215
-
|
|
β-catenin
Wnt
|
Cancer
|
|
Jatrophone is a diterpenoid with anticancer activity isolated from Jatropha isabelli. Jatrophone interferes with the Wnt/β-catenin pathway to inhibit the proliferation and epithelial-mesenchymal transition (EMT) of triple-negative breast cancer cells.
|
-
- HY-149647
-
-
- HY-N12740
-
|
|
MEK
ERK
|
Others
|
|
Napyradiomycin B4 is a Napyradiomycin derivative, which inhibits the RANKL-induced MEK-ERK signaling pathway. Napyradiomycin B4 attenuates osteoclastogenesis and prevents alveolar bone destruction in experimental periodontitis .
|
-
- HY-119683
-
|
|
Fungal
|
Infection
|
|
Epoxiconazole, a fungicide, is a demethylation inhibitor of the Ergosterol biosynthesis pathway. Epoxiconazole exhibits strong inhibitory effects on both carbendazim-resistant and phenamacril-resistant isolates, and can be used for controlling many crop diseases .
|
-
- HY-W250307
-
|
|
Reactive Oxygen Species
|
Others
|
|
Diphenyliodonium iodide is an inhibitor of reactive oxygen species (ROS). Diphenyliodonium iodide can inhibit the accumulation of bisdemethoxycurcumin in fresh-cut yam by inhibiting the phenylpropanoid pathway and the biosynthesis of bisdemethoxycurcumin, thereby preventing the yellowing of fresh-cut yam. Diphenyliodonium iodide can be used in medicine and fruit preservation .
|
-
- HY-162709
-
|
|
Apoptosis
YAP
|
Cancer
|
|
KHKI-01215 is an inhibitor for NUAK2 with an IC50 of 0.052 μM. KHKI-01215 inhibits the proliferation of cancer cell SW480 with an IC50 of 3.16 μM, induces apoptosis in SW480. KHKI-01215 inhibits the YAP signaling pathway .
|
-
- HY-100830
-
|
|
Wnt
MAP4K
TGF-beta/Smad
|
Cancer
|
|
NCB-0846 is an orally active, selective inhibitor for Wnt, that inhibits Traf2- and Nck-interacting kinase (TNIK) with an IC50 of 21 nM. NCB-0846 blocks TGF-β signaling pathway by inhibiting SMAD2/3 phosphorylation and nuclear translocation .
|
-
- HY-168442
-
|
|
Ras
PERK
|
Cancer
|
|
KRAS inhibitor-40 (Compound 41) is a KRAS inhibitor that interferes with the KRAS G12C-BRAF complex. KRAS inhibitor-40 inhibits the ERK phosphorylation of KRAS downstream signaling pathway. KRAS inhibitor-40 can inhibit the proliferation of tumor cells with different KRAS mutation types and has antitumor activity .
|
-
- HY-163151
-
|
|
PI3K
Akt
p38 MAPK
|
Neurological Disease
Inflammation/Immunology
|
|
JE-133 is an optically active isochromane-2H-chromene conjugate. JE-133 exhibits antioxidant and anti-inflammatory activities. JE-133 is a neuroprotective agent that effectively inhibits neuronal oxidative damage associated with PI3K/Akt and MAPK signaling pathways. JE-133 can also inhibit lipopolysaccharide (LPS) (HY-D1056)-induced neuroinflammation by regulating JAK/STAT and Nrf2 signaling pathways .
|
-
- HY-N0617
-
|
|
Phosphatase
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Sanggenon C, a flavonoid, exerts protective effects against cardiac hypertrophy and fibrosis via suppression of the calcineurin/NFAT2 pathway. Sanggenon C inhibits mitochondrial fission to induce apoptosis by blocking the ERK signaling pathway. Sanggenon C inhibits inducible nitric oxide synthase expression in RAW264.7 cells, and TNF-α-stimulated cell adhesion and VCAM-1 expression, by suppressing NF-κB activity. Sanggenon C possesses antioxidant, anti-inflammatory and antitumor activities .
|
-
- HY-159495
-
|
|
Keap1-Nrf2
|
Metabolic Disease
Cancer
|
|
Keap1-Nrf2-IN-21 (compound 4d) is a glucose metabolism inhibitor with antitumor activity. Keap1-Nrf2-IN-21 inhibits glycolytic activity of cancer cells by targeting the glycolytic pathway, especially by affecting the Keap1-Nrf2 signaling pathway, thereby inhibiting tumor growth. Keap1-Nrf2-IN-21 exhibits cytotoxicity against the HEC1A cell line (IC50=2.60 μM) .
|
-
- HY-163409
-
|
|
β-catenin
|
Inflammation/Immunology
Cancer
|
|
CKG012 is an inhibitor for Wnt/βcatenin signaling pathway. CGK012 inhibits release of HMGB1 and transcription of β-catenin, exhibits attenuating activities against cecal ligation and puncture (CLP)-induced sepsis and multiple myeloma cancer .
|
-
- HY-164528
-
|
|
Wnt
G-quadruplex
|
Cancer
|
|
SJ26 is a Wnt1 inhibitor with anticancer activity. SJ26 inhibits the expression of Wnt1 and Wnt1-mediated downstream signaling pathways in a G-quadruplex structure-dependent manner to suppress the migration activity of cancer cells .
|
-
- HY-W065835
-
|
|
HIV
|
Infection
|
|
2-Bromoaldisine is a pyrrole alkaloid that can be isolated from the Red Sea: marine sponge Stylissa carter. 2-Bromoaldisine inhibits HIV-1 vector infection. 2-Bromoaldisine inhibits Raf/MEK/MAPK pathway .
|
-
- HY-129346
-
|
|
Endogenous Metabolite
|
Cancer
|
|
STF-038533 is a CREB target gene transcription inhibitor with the activity of inhibiting the expression of related genes. STF-038533 plays a regulatory role in cell signaling pathways and has potential application value in exploring the inhibition of CREB-related diseases .
|
-
- HY-108437
-
|
|
Wnt
|
Infection
Cancer
|
|
exo-IWR-1, an inactive stereoisomer of Endo-IWR-1, is a negative control of IWR-1 (HY-12238). IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway .
|
-
- HY-162153
-
|
|
FGFR
|
Cancer
|
|
CYY292 is an FGFR1 inhibitor that specifically targets the FGFR1/AKT/Snail pathway in GBM cells. CYY292 dose-dependently inhibits cancer cell proliferation, epithelial-mesenchymal transition, stemness, invasion, and migration in vitro .
|
-
- HY-115385
-
-
- HY-P10658
-
|
|
Phospholipase
|
Others
|
|
ARF1 (2-17) inhibits both ARF-independent (PLC-β) and ARF-dependent (PLD) pathways. ARF1 (2-17) inhibits GTP-γ-S-stimulated PLD activity, phospholipase C-β (PLC-β), and exocytosis .
|
-
- HY-13675
-
|
NV-143
|
Endogenous Metabolite
|
Cancer
|
|
ME-143 is a second-generation tumor-specific inhibitor of NADH oxidase. ME-143 inhibits the WNT/β-catenin pathway in colorectal cancer cells. ME-143 has broadly active against cancers in vitro and in vivo .
|
-
- HY-P4860
-
|
|
Akt
Gli
JNK
PKA
|
Metabolic Disease
|
|
Adropin (34-76) is a secretory domain of Adropin. Adropin (34-76) can inhibit cAMP level and glucose production in hepatocytes, and has a hypoglycemic effect. Adropin (34-76) plays an antifibrotic role by inhibiting the GLI1 signaling pathway .
|
-
- HY-163743
-
|
|
Salt-inducible Kinase (SIK)
|
Cancer
|
|
SIC-19 is a SIK2 inhibitor and promotes SIK2 protein degradation via the ubiquitination pathway. SIC-19 inhibits cancer cell growth and sensitizes cells to PARP inhibitors (Such as Olaparib (HY-10162)), as well as in ovarian cancer organoids and xenograft models .
|
-
- HY-N0560
-
|
Baicalein 6-methyl ether; 6-Methoxybaicalein
|
HIF/HIF Prolyl-Hydroxylase
Autophagy
Virus Protease
|
Cancer
|
|
Oroxylin A is an active flavonoid compound with strong anti-cancer effects. Oroxylin A inhibits the IL-6/STAT3 pathway and NF-κB signaling, inhibits cell proliferation and induces apoptosis. Oroxylin A inhibits colitis-related carcinogenesis .
|
-
- HY-N1338
-
|
NSC 122417
|
mTOR
Akt
|
Cancer
|
|
Royleanone, a diterpenoid isolated from plants, inhibits the proliferation of cancer cells by inducing cell cycle arrest and mitochondria-mediated apoptosis, also inhibits cell migration potential, inhibits mTOR/PI3/AKT signaling pathway in LNCaP prostate cancer cells .
|
-
- HY-154860
-
|
|
PROTACs
Btk
|
Cancer
|
|
PTD10 is a highly potent PROTAC BTK degrader (DC50: 0.5 nM, KD: 2.28 nM). PTD10 degrades BTK in Ramos and JeKo-1 cells with DC50s of 0.5 and 0.6 nM respectively. PTD10 inhibits cell growth, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 can be used for research of B-cell dysregulation .
|
-
- HY-14664CS
-
|
(3S,5R)-XU 62-320-d6
|
HMG-CoA Reductase (HMGCR)
|
Cardiovascular Disease
Cancer
|
|
(3S,5R)-Fluvastatin-d6 (sodium) is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
|
-
- HY-N8361
-
|
|
HIV
Apoptosis
|
Infection
Cancer
|
|
Glycoborinine, a natural carbazole alkaloid, can be isolated from Glycosmis pentaphylla. Glycoborinine induces HepG2 cell apoptosis through mitochondrial pathway. Glycoborinine also inhibits HIV replication in cells .
|
-
- HY-P2012
-
|
|
Caspase
Bcl-2 Family
|
Others
|
|
TRP-601 is a caspase inhibitor. TRP-601 reversed the increased expression of active caspase-2, the activation of endogenous apoptotic pathway and the up-regulation of key protein triggered by hyperoxia .
|
-
- HY-N2051
-
|
|
Apoptosis
|
Cancer
|
|
Zeylenone, a naturally occurring cyclohexene oxide, inhibits proliferation and induces apoptosis in cervical carcinoma cells via PI3K/AKT/mTOR and MAPK/ERK pathways .
|
-
- HY-117479
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
CL67 is a potent hypoxia-inducible factor (HIF) pathway inhibitor. CL67 interferes G-quadruplex structures within promoter sequences. CL67 can be used in research of renal cancer .
|
-
- HY-N11501
-
|
|
STAT
Apoptosis
|
Cancer
|
|
7-epi-Isogarcinol is a polycyclic polyprenylated acylphloroglucinol (PPAP), with moderate antiproliferative activity. 7-epi-Isogarcinol blocks STAT3 signaling pathway, to induce apoptosis and inhibit cell migration .
|
-
- HY-P2203A
-
|
|
Notch
|
Cancer
|
|
SAHM1 TFA is a Notch pathway inhibitor. SAHM1 TFA stabilizes hydrocarbon-stapled alpha helical peptide. SAHM1 TFA targets the protein-protein interface and prevents Notch complex assembly.
|
-
- HY-P5045
-
-
- HY-B1468
-
|
|
Nucleoside Antimetabolite/Analog
Endogenous Metabolite
|
Cancer
|
|
8-Azaguanine is a purine analogue that shows antineoplastic activity. 8-Azaguanine functions as an antimetabolite and easily incorporates into ribonucleic acids, interfering with normal biosynthetic pathways, thus inhibiting cellular growth .
|
-
- HY-119751
-
|
|
Casein Kinase
Akt
Wnt
Apoptosis
|
Cancer
|
|
Hematein is a oxidation product of hematoxylin acted as a dye . Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells .
|
-
- HY-W400801
-
|
G-749 hydrochloride
|
TAM Receptor
|
Cancer
|
|
Denfivontinib (G-749) hydrochloride is an AXL inhibitor that has synergistic antitumor effects with the PD-1 inhibitor Pembrolizumab (HY-P9902). Denfivontinib can enhance the NOD-like receptor pathway, thereby promoting the formation of the NLRP3 inflammasome .
|
-
- HY-162372
-
|
|
Hedgehog
Smo
|
Cancer
|
|
Hedgehog IN-6 (Compound Q29) is a Hedgehog (Hh) inhibitor that can be used in cancer research. Hedgehog IN-6 inhibits the hedgehog (Hh) pathway by binding to the cysteine-rich domain (CRD) of Smoothened (Smo) and blocking its cholesterization .
|
-
- HY-163888
-
|
|
NO Synthase
NF-κB
COX
|
Inflammation/Immunology
|
|
NO-IN-1 (Compound 7a) inhibits the production of NO (IC50 = 3.13 μΜ). NO-IN-1 has anti-inflammatory effects. NO-IN-1 downregulates the expression of COX-2 and iNOS by inhibiting the NF-κB signaling pathway .
|
-
- HY-P1094
-
|
|
Apoptosis
Caspase
|
Inflammation/Immunology
Cancer
|
|
AZ-10417808 is a selective caspase-3 inhibitor. AZ-10417808 blocks apoptosis signaling pathway by inhibiting caspase-3 activity. AZ-10417808 can be used to study the effect of nicotine on plasmacytoid dendritic cell migration .
|
-
- HY-W010201R
-
|
(±)-Citronellol (Standard); (±)-β-Citronellol (Standard)
|
Reactive Oxygen Species
ERK
PI3K
TNF Receptor
Atg8/LC3
p62
Apoptosis
Necroptosis
Autophagy
Fungal
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Citronellol (Standard) is the analytical standard of Citronellol. Citronellol (Standard) is an orally active inducer of apoptosis. Citronellol (Standard) can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol (Standard) can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol (Standard) can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol (Standard) exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis .
|
-
- HY-N6850
-
|
|
Apoptosis
Pyroptosis
AMPK
Bcl-2 Family
JAK
STAT
Calcium Channel
Interleukin Related
TNF Receptor
SOD
Reactive Oxygen Species
PPAR
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Calenduloside E is a pentacyclic triterpenoid saponin that can be extracted from the bark and roots of Aralia ovata, and has anti-inflammatory and anti-apoptotic activities. Calenduloside E alleviates atherosclerosis by regulating macrophage polarization, improves mitochondrial function by regulating the AMPK-SIRT3 pathway, and alleviates acute liver injury. In addition, Calenduloside E promotes the interaction between L-type calcium channels and Bcl-2 related apoptosis genes, inhibits calcium overload, and alleviates myocardial ischemia/reperfusion injury. Calenduloside E also improves non-alcoholic fatty liver disease by regulating heat shock-dependent pathways, and inhibits ROS mediated JAK1-STAT3 pathways to reduce cellular inflammatory responses .
|
-
- HY-16420
-
|
|
Syk
|
Inflammation/Immunology
|
|
R112 is a fast and reversible inhibitor of spleen tyrosine kinase (Syk) kinase. R112 inhibits Syk kinase activity with an IC50 value of 226 nM and a Ki value of 96 nM. R112 inhibits IgE-FcεRI signaling pathway. R112 can be used for the research of allergic rhinitis .
|
-
- HY-137918
-
|
|
Src
TGF-β Receptor
Anaplastic lymphoma kinase (ALK)
|
Others
|
|
TGF-βRI inhibitor 3 (Compound 9ac) is a selective TGF-β inhibitor. TGF-βRI inhibitor 3 can effectively inhibit the TGF-β signaling pathway. TGF-βRI inhibitor 3 has IC50 values of 13 μM and 0.63 μM for c-Src kinase and ALK5 kinase, respectively .
|
-
- HY-N4202
-
|
|
Mitochondrial Metabolism
Apoptosis
|
Neurological Disease
|
|
Dihydrorotenone, a natural pesticide, is a potent mitochondrial inhibitor. Dihydrorotenone probably induces Parkinsonian syndrome. Dihydrorotenone induces human plasma cell apoptosis by triggering endoplasmic reticulum stress and activating p38 signaling pathway .
|
-
- HY-145301
-
|
|
Bacterial
|
Infection
|
|
Mycobactin-IN-1 (compound 44), a pyrazoline analogue, is a mycobactin biosynthesis inhibitor against mycobacteria. Mycobactin-IN-1 binds to salicyl-AMP ligase (MbtA), a key enzyme in the mycobactin biosynthetic pathway .
|
-
- HY-P3162
-
-
- HY-141432
-
|
Cbl-b-IN-3
|
E1/E2/E3 Enzyme
|
Cancer
|
|
NX-1607 (Compound 23) is an inhibitor of Cbl-b, an E3 enzyme in the ubiquitin-proteasome pathway, with an IC50 value of less than 1 nM. NX-1607 can be used in cancer research .
|
-
- HY-N6684
-
|
Vomitoxin
|
P-glycoprotein
|
Metabolic Disease
|
|
Deoxynivalenol, an orally active mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors .
|
-
- HY-169534
-
|
|
Akt
|
Cancer
|
|
AKT-IN-26 (Compound 453) is an AKT inhibitor that binds to the Pleckstrin homology (PH) domain of AKT. AKT-IN-26 can be used in research related to AKT pathway-associated cell proliferation and cancer .
|
-
- HY-141584
-
|
|
MDM-2/p53
|
Cancer
|
|
ATSP-7041, a selective dual peptide inhibitor of MDM2 and MDMX, effectively reactivates the p53 tumor suppressor pathway in a mechanism-dependent manner in p53-positive cancers .
|
-
- HY-B0444A
-
|
|
Autophagy
Apoptosis
ERK
|
Neurological Disease
Cancer
|
|
Maprotiline is a highly selective noradrenergic reuptake inhibitor that has strong antidepressant, antitumor and neuropathic pain-relieving effects. Maprotiline induces cancer cell apoptosis by targeting the ERK signaling pathway and CRABP1 .
|
-
- HY-N3260
-
-
- HY-104029
-
|
F901318
|
Fungal
Dihydroorotate Dehydrogenase
|
Infection
|
|
Olorofim (F901318) selectively inhibits fungal dihydroorotate dehydrogenase (DHODH), a key enzyme in the pyrimidine biosynthesis pathway. Olorofim (F901318). Olorofim exhibits excellent activity against A. fumigatus and other Aspergillus spp. .
|
-
- HY-100711
-
|
Prodigiosine; NSC47147
|
Bacterial
Apoptosis
Wnt
Fungal
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Prodigiosin (Prodigiosine) is a red pigment produced by bacteria as a bioactive secondary metabolite. Prodigiosin is a potent inhibitor of the Wnt/β-catenin pathway. Prodigiosin has antibacterial, antifungal, antiprotozoal, antimalarial, immunosuppressive, and anticancer properties .
|
-
- HY-N1404
-
|
|
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Sodium aescinate is a triterpene saponin derived from Aesculus hippocastanum seeds, with anti-inflammatory and antioxidant activities . Sodium aescinate inhibits hepatocellular carcinoma growth by targeting CARMA3/NF-κB pathway .
|
-
- HY-N8102
-
|
|
Transmembrane Glycoprotein
Others
|
Cardiovascular Disease
|
|
Echinocystic acid 28-O-β-D-glucoside is a metabolite of Echinocystic acid by microbial oxidation and glucosidation. Echinocystic acid 28-O-β-D-glucoside is a tissue factor pathway inhibitor, with an IC50 of 10.61 nM .
|
-
- HY-P99261
-
|
OMP 21M18; Human Anti-TNFRSF10B Recombinant Antibody
|
Notch
|
Cancer
|
|
Demcizumab (OMP 21M18) is an anti-DLL4 monoclonal antibody. Demcizumab is a potent inhibitor of the Notch pathway. Demcizumab alone or in combination with chemotherapy is effective in various cancer models .
|
-
- HY-N0637
-
-
- HY-N12124
-
|
Monascinol
|
Akt
mTOR
AMPK
Androgen Receptor
Apoptosis
Autophagy
|
Cancer
|
|
Monascuspiloin (Monascinol) exhibits anti-androgenic activity with an IC50 of 7 μM. Monascuspiloin inhibits viability of PC-3 and LNCaP with IC50 of 45 and 47 μM. Monascuspiloin induces apoptosis in LNCaP through inhibition of Akt/mTOR signaling pathway, induces autophagy through activation AMPK signaling pathway and arrest cell cycle at G2/M phase in PC-3. Monascuspiloin exhibits antitumor efficacy in mice .
|
-
- HY-117102
-
|
|
Aryl Hydrocarbon Receptor
Checkpoint Kinase (Chk)
|
Cancer
|
|
ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines .
|
-
- HY-131710
-
|
|
Phosphodiesterase (PDE)
EGFR
Wnt
Apoptosis
|
Cancer
|
|
PDE5-IN-3 (compound 11j) is a potent PDE5 inhibitor with an IC50 of 1.57 nM. PDE5-IN-3 shows moderate EGFR inhibition with IC50 of 5.827 µM. PDE5-IN-3 significantly inhibits the Wnt/β-catenin pathway (IC50=1286.96 ng/mL). PDE5-IN-3 induces the intrinsic apoptotic mitochondrial pathway in HepG2 cells. PDE5-IN-3 has strong antitumor activity .
|
-
- HY-169014
-
|
|
HDAC
Keap1-Nrf2
Ferroptosis
|
Cancer
|
|
HDAC-IN-77 (HL-5s) is an HDAC inhibitor. HDAC-IN-77 can induce ferroptosis and inhibit the Nrf2/HO-1 signaling pathway. HDAC-IN-77 can be used in cancer research .
|
-
- HY-N10175
-
|
|
Fungal
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Berkeleyacetal C, a meroterpenoid compound, shows favorable activity of inhibiting nitrogen oxide (NO) production of macrophages stimulated by lipopolysaccharide (LPS). Berkeleyacetal C exerts anti-inflammatory effects via inhibiting NF-κB, ERK1/2 and IRF3 signaling pathways .
|
-
- HY-107753
-
|
|
Ras
|
Inflammation/Immunology
Cancer
|
|
XRP44X inhibits Ras-induced transcription activation with the IC50 of 10 nM. XRP44X inhibits activation of the Ras-Erk-1/2 pathway by FGF-2 . XRP44X is an inhibitor of Ras/Erk activation of Elk3 that also affects microtubules .
|
-
- HY-122700
-
|
|
Complement System
|
Inflammation/Immunology
|
|
Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases .
|
-
- HY-164524
-
|
|
Eukaryotic Initiation Factor (eIF)
Akt
NF-κB
|
Cancer
|
|
SBI-0640726 is an eIF4G1 inhibitor with antiproliferative activity in melanoma. SBI-0640726 disrupts the eIF4F translation initiation complex by inhibiting AKT and NF-kB signaling pathways. SBI-0640726 inhibits the growth of NRAS and BRAF mutant melanoma in vitro .
|
-
- HY-P2413
-
|
|
Androgen Receptor
Src
|
Others
|
|
Ac-PPPHPHARIK-NH2 (compound S1) is a compound that inhibits the interaction between androgen receptor and Src. It can inhibit the binding of androgen or estrogen-induced receptor and Src in cancer cells, as well as the activation of related signaling pathways, and can also inhibit cell cycle progression and tumor growth.
|
-
- HY-168596
-
|
|
ROCK
Apoptosis
|
Cancer
|
|
RhoA-ROCK-IN-1 (Compound b19) is an inhibitor of RhoA/ROCK. RhoA-ROCK-IN-1 can significantly inhibit cell proliferation, migration, and invasion, while promoting cell apoptosis. RhoA-ROCK-IN-1 demonstrates remarkable anticancer activity by inhibiting the RhoA/ROCK pathway .
|
-
- HY-115734
-
|
S14-95
|
Acyltransferase
|
Inflammation/Immunology
|
|
Phenylpyropene C (S14-95), a JAK/STAT pathway inhibitor, can inhibit IFN-γ mediated expression of the reporter gene (IC50=5.4~10.8 μM). Phenylpyropene C also is an inhibitor of acyl-CoA, with an IC50 of 16.0 μM .
|
-
- HY-160489
-
|
|
β-catenin
|
Cancer
|
|
PTK7/β-catenin-IN-2 (compound 04967) is an inhibitor of PTK7/β-catenin. It inhibits the binding of PTK7 to β-catenin (IC50: 5.6 μM), thereby inhibiting the signaling of the Wnt/β-catenin pathway. PTK7/β-catenin-IN-2 targets cell growth dependent on the Wnt signaling pathway and has anticancer properties. PTK7/β-catenin-IN-2 also showed inhibitory potency against p53 and MDM2 binding with an IC50 of 157.1 μM .
|
-
- HY-164374
-
|
|
PAK
|
Cancer
|
|
AK963/40708899 is a potent PAK1 inhibitor. AK963/40708899 suppresses the proliferation of human gastric cancer cells by downregulation of PAK1-NF-κB-cyclinB1 pathway. AK963/40708899 induces cell cycle arrest at G2 phase and reduces the migration and invasion. AK963/40708899 inhibits the formation of filopodia and promots cell adhesion which in turn inhibits invasive potential of gastric cells by negatively regulating PAK1-LIMKl-cofilin and PAK1-ERK-FAK pathways .
|
-
- HY-W150677
-
|
|
Bacterial
|
Infection
|
|
BioA-IN-1 (Compound 15) is an inhibitor of BioA, a key enzyme in the biotin synthesis pathway of Mycobacterium tuberculosis, with an IC50 value of 0.195 μM. BioA-IN-1 exhibits antibacterial activity but has no cytotoxicity .
|
-
- HY-N2110
-
|
|
Akt
|
Inflammation/Immunology
|
|
Phellopterin is a natural product isolated from Angelica dahurica. Phellopterin reduces TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium .
|
-
- HY-N0020
-
|
|
Wnt
Reactive Oxygen Species
|
Neurological Disease
|
|
Echinacoside, one of the phenylethanoids isolated from the stems of Cistanche deserticola, effectively inhibits Wnt/β-catenin signaling. Echinacoside elicits neuroprotection by activating Trk receptors and their downstream signal pathways. Antiosteoporotic activity .
|
-
- HY-P99895
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
Rulonilimab is a human IgG1 monoclonal antibody against PD-1 that targets, binds and inhibits PD-1 and its downstream signalling pathways with potential immune checkpoint inhibition and anti-tumour activity .
|
-
- HY-15880
-
|
|
Phosphatase
Apoptosis
Autophagy
|
Cancer
|
|
CCT007093 is an effective protein phosphatase 1D (PPM1D Wip1) inhibitor. Wip1 inhibition can activate the mTORC1 pathway and enhance hepatocyte proliferation after hepatectomy .
|
-
- HY-N10312
-
-
- HY-111770
-
|
2-Bromopalmitic acid; 2-Bromopalmitate
|
Pyroptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
2-Bromohexadecanoic acid (2-Bromopalmitate; 2-BP) is a palmitoylation inhibitor targeting DHHC (Asp-His-His-Cys) protein palmitoyltransferase. 2-Bromohexadecanoic acid inhibits palmitoylation of GSDME-C during pyroptosis and inhibits BAK/BAX-Caspase 3-GSDME pathway-mediated pyroptosis .
|
-
- HY-120902
-
|
|
GSK-3
|
Inflammation/Immunology
|
|
GSK-3β inhibitor 8, a thiophenacil derivative, is an effective and selective inhibitor of GSK-3β (IC50=64 nM). GSK-3β inhibitor 8 negatively regulated Wnt signaling pathway and stimulated β cell proliferation .
|
-
- HY-117572
-
|
|
P2Y Receptor
|
Others
|
|
MRS2567 is a P2Y receptor antagonist with the activity of inhibiting contraction of mouse mesenteric arteries. MRS2567 can inhibit the sustained contraction caused by UTP and UDP, and inhibit the Na?, K?, 2Cl? co-transport-dependent signaling pathway, thereby affecting the myogenic tone of mouse mesenteric arteries.
|
-
- HY-N0592A
-
|
|
NF-κB
AMPK
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Demethyleneberberine chloride is a natural mitochondria-targeted antioxidant. Demethyleneberberine chloride alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine chloride could serve as a AMPK activator for researching non-alcoholic fatty liver disease (NAFLD) .
|
-
- HY-P5819
-
|
|
Wnt
PROTACs
β-catenin
|
Cancer
|
|
xStAx-VHLL is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL can inhibit the proliferation of colon cancer cells and has anti-tumor activity .
|
-
- HY-N0177
-
|
|
STAT
MicroRNA
|
Metabolic Disease
|
|
Diosgenin, a steroidal saponin, can inhibit STAT3 signaling pathway . Diosgenin is an exogenous activator of Pdia3/ERp57 . Diosgenin inhibits aortic atherosclerosis progression by suppressing macrophage miR-19b expression .
|
-
- HY-N1193
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Sulfuretin inhibits the inflammatory response by suppressing the NF-κB pathway. Sulfuretin can be used for the research of allergic airway inflammation. Sulfuretin reduces oxidative stress, platelet aggregation, and mutagenesis . Sulfuretin is a competitive and potent inhibitor of monophenolase and diphenolase activities with the IC50 of 13.64 μM .
|
-
- HY-164539
-
|
|
HDAC
Autophagy
|
Cancer
|
|
TMU 35435 is a histone deacetylase (HDAC) inhibitor. TMU-35435 inhibits the NHEJ pathway through ubiquitination of DNA-dependent protein kinase catalytic subunit (DNA-PKcs). In addition, TMU 35435 enhances radiosensitivity by inducing misfolded protein aggregation and autophagy in TNBC .
|
-
- HY-N8307
-
|
|
NO Synthase
NF-κB
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Syringaresinol is a lignan that can be extracted from the dragon's blood of the Dracaena tree. Syringaresinol increases NO production by increasing the phosphorylation and dimerization of endothelial NO synthase, exerting a vasodilatory effect. Syringaresinol also inhibits the NF-κB pathway, exerting anti-inflammatory activity and inhibiting arthritis .
|
-
- HY-151463
-
|
|
CDK
β-catenin
|
Cancer
|
|
CDK8-IN-11 is a potent and selective CDK8 inhibitor with an IC50 value of 46 nM. CDK8-IN-11 inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 can be used in the research of colon cancer .
|
-
- HY-155568
-
|
|
Reactive Oxygen Species
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
|
Flo8 is a potent anti-inflammatory and antioxidant compound. Flo8 inhibits the release of intracellular reactive oxygen species (ROS) and nitric oxide (NO) and suppresses neuronal apoptotic by inhibiting inflammatory and apoptotic signaling pathways. Flo8 can be used for Parkinson's Disease (PD) research .
|
-
- HY-100236
-
|
DDD00107587
|
DNA/RNA Synthesis
|
Cancer
|
|
Madrasin (DDD00107587) is a splicing inhibitor that prevents formation of both splicing intermediates and products in vitro and interferes with one or more early steps in the pathway of spliceosome assembly. Madrasin also can inhibit pre-mRNA splicing in vitro and modify splicing of endogenous pre-mRNA in cells .
|
-
- HY-N0592
-
|
|
NF-κB
AMPK
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Demethyleneberberine is a natural mitochondria-targeted antioxidant. Demethyleneberberine alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine could serve as a AMPK activator for treating non-alcoholic fatty liver disease (NAFLD) .
|
-
- HY-152265
-
|
|
PINK1/Parkin
Mitophagy
|
Neurological Disease
|
|
PARL-IN-1 is a potent PARL inhibitor with an IC50 value of 28 nM. PARL-IN-1 inhibits PARL and leads to a robust activation of the PINK1/Parkin pathway. PARL-IN-1 promotes PINK1/Parkin-dependent mitophagy .
|
-
- HY-N0158
-
|
|
TGF-beta/Smad
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Oxymatrine, an alkaloid from Sophora flavescens Alt. with anti-inflammatory, antifibrosis, and antitumor effects, inhibits the iNOS expression and TGF-β/Smad pathway. Oxymatrine inhibits bocavirus minute virus of canines (MVC) replication, reduces viral gene expression and decreases apoptosis induced by viral infection.
|
-
- HY-151463A
-
|
|
CDK
β-catenin
|
Cancer
|
|
CDK8-IN-11 hydrochloride is a potent and selective CDK8 inhibitor with an IC50 value of 46 nM. CDK8-IN-11 hydrochloride inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 hydrochloride can be used in the research of colon cancer .
|
-
- HY-155052
-
|
|
Protein Arginine Deiminase
|
Cancer
|
|
PAD4-IN-2 (compound 5i) is a PAD4 inhibitor (IC50=1.94 μM). PAD4-IN-2 inhibits tumor growth in mice by specifically inhibiting the PAD4-H3cit-NETs pathway in neutrophils .
|
-
- HY-11006
-
|
NU7441
|
DNA-PK
CRISPR/Cas9
|
Cancer
|
|
KU-57788 (NU7441) is a highly potent and selective DNA-PK inhibitor with an IC50 of 14 nM. KU-57788 is an NHEJ pathway inhibitor. KU-57788 also inhibits PI3K and mTOR with IC50s of 5.0 and 1.7 μM, respectively .
|
-
- HY-Z8643
-
|
|
TGF-β Receptor
Drug Intermediate
|
Others
|
|
HCTZ-CH2-HCTZ is an isomer of HCTZ (HY-B0252). Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway .
|
-
- HY-138154
-
|
|
Lipoxygenase
|
Metabolic Disease
|
|
BLX-3887 is a selective 15-lipoxygenase type 1 (15-LO-1) inhibitor with an IC50 of 32 nM. BLX-3887 can be utilized in research related to the 15-LO pathways .
|
-
- HY-100538
-
DTP3
1 Publications Verification
|
DNA/RNA Synthesis
JAK
|
Cancer
|
|
DTP3 TFA is a potent and selective GADD45β/MKK7 inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway .
|
-
- HY-W100287
-
|
|
NF-κB
p38 MAPK
|
Neurological Disease
Inflammation/Immunology
|
|
Murrayafoline A is a carbazole alkaloid that can be extracted from Murraya tetramera. Murrayafoline A directly targets Specificity protein 1 (Sp1), thereby inhibiting NF-κB and MAPK signaling pathways. Murrayafoline A has anti-neuroinflammatory activity .
|
-
- HY-100711A
-
|
Prodigiosine hydrochloride
|
Bacterial
Apoptosis
Fungal
Wnt
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Prodigiosin (Prodigiosine) hydrochloride is a red pigment produced by bacteria as a bioactive secondary metabolite. Prodigiosin hydrochloride is a potent proapoptotic agent, and inhibits Wnt/β-catenin pathway. Prodigiosin hydrochloride has antibacterial, antifungal, antiprotozoal, antimalarial, immunosuppressive, and anticancer properties .
|
-
- HY-P3162A
-
-
- HY-113680
-
|
|
Apoptosis
Ras
β-catenin
Wnt
|
Cancer
|
|
KY1022 is a small molecule destabilizing Ras via targeting the Wnt/β-catenin pathway. KY1022 can inhibit cellular EMT, metastasis and apoptosis. KY1022 can be used for the research of metastatic colorectal cancer .
|
-
- HY-P99196
-
|
|
c-Met/HGFR
|
Cancer
|
|
Ficlatuzumab is a monoclonal antibody (McAb) targeting human hepatocyte growth factor (HGF). Ficlatuzumab blocks the activation of the HGF/c-Met signaling pathway, and inhibits c-Met receptor-mediated cancer cell proliferation, migration, and invasion .
|
-
- HY-B0444
-
|
|
Autophagy
Apoptosis
ERK
|
Neurological Disease
Cancer
|
|
Maprotiline hydrochloride is a highly selective noradrenergic reuptake inhibitor that has strong antidepressant, antitumor and neuropathic pain-relieving effects with oral activity. Maprotiline hydrochloride induces cancer cell apoptosis by targeting the ERK signaling pathway and CRABP1 .
|
-
- HY-127029A
-
|
|
NO Synthase
Lipoxygenase
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Umbelliprenin, a prenylated coumarin, is an antioxidant with anticancer, anti-inflammatory and immunomodulatory effects. Umbelliprenin inhibits lipoxygenase managing the inflammation pathways. In inflammatory macrophages, Umbelliprenin suppresses nitric oxide production as well as inducible nitric oxide synthase (NO synthase) .
|
-
- HY-135808
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
BIZ 114 (Example 11) is a fatty acid derivative and potent inhibits the TNF-α activated NF-κΒ pathway. BIZ 114 has the potential to prevent and / or treat ophthalmic disorders such as retinal degenerative disorders and ocular inflammatory diseases .
|
-
- HY-P4910
-
|
|
Proteasome
Apoptosis
|
Cancer
|
|
Baceridin is a proteasome inhibitor and a cyclic hexapeptide. Baceridin can be isolated from the culture medium of Epiphytic Bacillus. Baceridin can inhibit cell cycle progression and induce tumor cell apoptosis through a p53-independent pathway. Baceridin can be used in cancer research .
|
-
- HY-147566
-
|
|
ATM/ATR
|
Cancer
|
|
ATR-IN-14 (compound 1) is a potent ATR kinase inhibitor. ATR-IN-14 inhibits ATR signaling pathways downstream CHKI protein phosphorylation, with inhibition of 98.03% at 25 nM. ATR-IN-14 shows good anticancer activity in LoVo cells, with an IC50 of 64 nM .
|
-
- HY-13418
-
|
Compound C dihydrochloride; BML-275 dihydrochloride
|
Organoid
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
|
Dorsomorphin (Compound C) dihydrochloride is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).
|
-
- HY-W716916
-
|
|
Isotope-Labeled Compounds
|
Cancer
|
|
Vismodegib-d7 is deuterium labeled Vismodegib. Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively .
|
-
- HY-132601A
-
|
MRG-106 sodium
|
MicroRNA
|
Cancer
|
|
Cobomarsen sodium is an oligonucleotide inhibitor of miR-155. Cobomarsen sodium inhibits multiple gene pathways associated with cell survival (including JAK/STAT, MAPK/ERK and PI3K/AKT). Cobomarsen sodium can be used for the research of B-cell lymphoma .
|
-
- HY-147515
-
|
|
FGFR
|
Cancer
|
|
FGFR4-IN-11 (Compound 30) is a potent, selective, covalent FGFR4 inhibitor with an IC50 of 2.1 nM. FGFR4-IN-11 significantly inhibits the FGF19/FGFR4 signaling pathway and shows antitumor activity .
|
-
- HY-149816
-
-
- HY-W705354
-
|
|
Isotope-Labeled Compounds
Hedgehog
Autophagy
|
Cancer
|
|
Vismodegib-d4 is deuterium labeled Vismodegib. Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively .
|
-
- HY-P10860
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
cMCoFx1 is a potent and selective FXIIa cyclic peptide inhibitor. cMCoFx1 has high binding affinity (KD: 900 pM) and inhibitory activity (Ki: 370 pM) for FXIIa. cMCoFx1 can effectively inhibit endogenous clotting pathways, and cMCoFx1 is stable in serum and non-cytotoxic .
|
-
- HY-163461
-
|
|
PARP
|
Cancer
|
|
4F-DDC is a novel PARP1 inhibitor with an IC50 value of 82 nM. 4F-DDC induces DNA damage and activates the cGAS–STING pathway. 4F-DDC inhibits the growth of HCC-1937-derived tumor xenografts .
|
-
- HY-111432
-
|
|
Ras
|
Others
|
|
CCG-232601 (compound 8f) is a potent and orally active Rho/MRTF/SRF transcriptional pathway inhibitor. CCG-232601 inhibits the development of Bleomycin-induced dermal fibrosis in mice. CCG-232601 has the potential for the research of antifibrotic for systemic scleroderma .
|
-
- HY-N0330
-
|
|
Apoptosis
Autophagy
PI3K
c-Myc
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Momordin Ic is an orally active triterpenoid saponin that can be isolated from Kochia scoparia. It is also a SUMO specific protease 1 (SENP1) inhibitor, SENP1/c-MYC signaling pathway inhibitor, and apoptosis inducer. Momordin Ic induces autophagy and apoptosis in liver cancer cells through the PI3K/Akt and MAPK signaling pathways mediated by reactive oxygen species. Momordin Ic has the ability to control glucose induced blood glucose elevation, inhibit gastric emptying, resist rheumatoid arthritis, reduce CCl4 (HY-Y0298) induced hepatotoxicity and anti-tumor activity .
|
-
- HY-113509S
-
|
LXA4-d5
|
Interleukin Related
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Lipoxin A4-d5 is the deuterium labeled Lipoxin A4. Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties[1]. Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways[2]. Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC50 value of 25.74 nM[3].
|
-
- HY-153190
-
|
|
Oxidative Phosphorylation
STAT
Ferroptosis
|
Cancer
|
|
W1131 is a potent STAT3 inhibitor, triggering ferroptosis. W1131 suppresses cancer progression in gastric cancer cell subcutaneous xenograft model, organoids model, and PDX model. W1131 effectively alleviates chemical resistance of cancer cells to 5-FU (HY-90006). W1131 regulates cell cycle, DNA damage response, and oxidative phosphorylation, including IL6-JAK-STAT3 pathway and ferroptosis pathway .
|
-
- HY-N0231R
-
|
|
Bacterial
Antibiotic
NF-κB
PERK
Apoptosis
Autophagy
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Bavachalcone (Standard) is the analytical standard of Bavachalcone. This product is intended for research and analytical applications. Bavachalcone is a potent inducer of apoptosis. Bavachalcone exerts anticancer activity by promoting autophagy and apoptosis in HepG2 cells. Bavachalcone acts as an anti-neuroinflammatory and antidepressant through the NF-κB pathway. Bavachalcone inhibits osteoclasts by interfering with ERK and Akt signaling pathways and the expression of c-Fos and NFATc1. Bavachalcone exhibits a significant inhibitory effect on baculovirus-expressed BACE-1 in vitro .
|
-
- HY-135899
-
|
|
Sirtuin
Apoptosis
|
Cancer
|
|
SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway. .
|
-
- HY-I0447A
-
|
4-Aminosalicylic acid sodium salt dihydrate
|
Bacterial
Antibiotic
|
Infection
|
|
Sodium 4-aminosalicylate (Sodium para-Aminosalicylic acid) dihydrate is para-aminosalicylic acid (PAS), a dihydrofolate reductase (DHFR) inhibitor and antituberculous agent. PAS is incorporated into the folate pathway via dihydropteroate synthase (DHPS) and dihydrofolate synthase (DHFS) to generate the hydroxydihydrofolate antimetabolite, which in turn inhibits DHFR enzyme activity .
|
-
- HY-130369
-
|
|
Bacterial
Necroptosis
HSV
|
Infection
Cancer
|
|
NSC10010 hydrochloride inhibits gammaherpesvirus associated B-lymphomas growth through activation of NF-kB and c-Myc-mediated signaling pathways. NSC10010 hydrochloride induces necrotic cell death in gammaherpesvirus infected B-cells. NSC10010 hydrochloride is also an inhibitor of Mtb ClpC1 ATPase .
|
-
- HY-N0781
-
|
|
Apoptosis
|
Cancer
|
|
Linderalactone is an important sesquiterpene lactone isolated from Lindera aggregata. Linderalactone inhibits cancer growth by modulating the expression of apoptosis-related proteins and inhibition of JAK/STAT signalling pathway. Linderalactone also inhibits the proliferation of the lung cancer A-549 cells with an IC50 of 15 μM .
|
-
- HY-162939
-
|
|
Histone Methyltransferase
|
Cancer
|
|
TB22 is a non-nucleoside inhibitor of DOT1LR231Q, possessing anticancer activity. TB22 inhibits the malignant phenotype of lung cancer cells carrying the R231Q mutation through the MAPK/ERK signaling pathway, and can be used for lung cancer research .
|
-
- HY-N1333
-
|
|
NF-κB
|
Cancer
|
|
Rubioncolin C exerts anti-tumor activity by inducing apoptotic and autophagic Cell Death and inhibiting the NF-κB and Akt/mTOR/P70S6K Pathway in Human Cancer Cells .
|
-
- HY-153456
-
|
|
Hedgehog
|
Cancer
|
|
Hedgehog IN-2 (Compound 20) is an inhibitor of Hedgehog pathway with an IC50 value less than 0.003 μM in C3H10T1/2 cells .
|
-
- HY-168609
-
|
|
Apoptosis
c-Met/HGFR
mTOR
PI3K
Akt
|
Cancer
|
|
CRI9 inhibits the c-MET/PI3K/Akt/mTOR pathway, suppressing the growth of liver cancer cells. CRI9 shows strong cytotoxicity against HCC cells, inducing apoptosis .
|
-
- HY-18777
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
KC7F2 is a potent hypoxia inducible factor-1 (HIF-1) pathway inhibitor with an IC50 of 20 μM in LN229-HRE-AP cells, and with potential as a cancer therapy agent .
|
-
- HY-149353
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 145 (compound 1b) is an antibacterial agent depending on bacterial iron uptake pathway. Antibacterial agent 145 disrupts cytoplasmic membrane integrity and inhibits cell metabolism but exhibits low cytotoxic effects to normal cells .
|
-
- HY-49597
-
|
|
Wnt
β-catenin
|
Cancer
|
|
Pin1 modulator 1 (compound IIb-219) is a modulator that specifically targets β-Catenin and inhibits the Wnt pathway. Pin1 modulator 1 can be used in the study of Wnt-mediated related diseases, such as cancer .
|
-
- HY-N12846
-
|
|
Others
|
Metabolic Disease
|
|
Neokadsuranic acid A is a cholesterol biosynthesis inhibitor that reduces the activity of cholesterol. Neokadsuranic acid A is a triterpenoid compound that can be isolated from Kadsura heteroclita, a plant of the Schisandraceae family. Neokadsuranic acid A can be used to study the cholesterol biosynthesis pathway and its role in traditional medicine .
|
-
- HY-163076
-
|
|
Apoptosis
|
Others
|
|
Anticancer agent 174 (BA-3) is an anticancer agent. Anticancer agent 174 induces tumor cell apoptosis through the mitochondrial pathway. Anticancer agent 174 inhibits cancer cell proliferation in melanoma mouse xenograft model .
|
-
- HY-125522
-
|
|
ERK
Apoptosis
|
Inflammation/Immunology
|
|
Methyl helicterate is a triterpenoid, that can be isolated from Helicteres angustifolia (Sterculiaceae). Methyl helicterate inhibits hepatic stellate cell activation and promotes cell apoptosis through downregulating the ERK1/2 signaling pathway .
|
-
- HY-139553
-
|
ATI-450; CDD-450
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
|
|
Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases .
|
-
- HY-122935
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
Nigranoic acid is a triterpenoid separated from Schisandra chinensis. Nigranoic acid inhibits HIV-1 reverse transcriptase. Nigranoic acid exhibits protective effects on brain through PARP/AIF signaling pathway in cerebral ischemia-reperfusion animal model .
|
-
- HY-118312
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
CAY10657 is an inhibitor for NF-κB pathway. CAY10657 downregulates expressions of proinflammatory cytokine (IL-6) and chemokine (MCP-1), and thus exhibits anti-inflammatory efficacy against meningitis induced by Streptococcus suis .
|
-
- HY-18287A
-
|
|
Smo
|
Cancer
|
|
MRT-83 (hydrochloride) is the potent antagonist of Smoothened (Smo) receptor. MRT-83 (hydrochloride) inhibits the Hedgehog (Hh) signaling pathway and BODIPY-cyclopamine binding to human Smo. MRT-83 (hydrochloride) has the potential for researching cancer disease .
|
-
- HY-16724
-
|
1-Methyl-D-tryptophan; NLG-8189
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
Indoximod (1-Methyl-D-tryptophan) is an orally active indoleamine 2,3-dioxygenase (IDO) pathway inhibitor. Indoximod acts as a Trp mimetic in regulating mTOR. Indoximod is an immunometabolic adjuvant used for the research of cancer .
|
-
- HY-B1460B
-
|
(±)-Sulconazole
|
Fungal
|
Cancer
|
|
Sulconazole is a potent antifungal agent in the imidazole class. Sulconazole blocks the NF-κB/IL-8 signaling pathway and CSC (Cancer stem cells) formation. Sulconazole inhibits tumor growth, and can be used for breast cancer research .
|
-
- HY-108516
-
|
|
PARP
|
Cancer
|
|
TC-E 5001 is an inhibitor of Wnt pathway that inhibits tankyrase 1/2 (TNKS1/2) via novel adenosine pocket binding, with Kds of 79 nM and 28 nM, respectively. TC-E 5001 also inhibits Axin2 and STF, with IC50s of 0.709 μM and 0.215 μM, respectively .
|
-
- HY-155052A
-
|
|
Protein Arginine Deiminase
|
Cancer
|
|
PAD4-IN-2 (compound 5i) TFA is a PAD4 inhibitor (IC50=1.94 μM). PAD4-IN-2 TFA inhibits tumor growth in mice by specifically inhibiting the PAD4-H3cit-NETs pathway in neutrophils .
|
-
- HY-124445
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
APC0576 is an inhibitor for the activation of NF-κB signaling pathway, and inhibits the activation of NF-κB depedent gene (IC50 is 1.0 μM for β-gal). APC0576 inhibits IL-1-induced chemokines release, and can be used in research about pathological endothelial cell activation releted diseases .
|
-
- HY-N0410
-
|
Eleutheroside A; β-Sitosterol β-D-glucoside
|
Apoptosis
Reactive Oxygen Species
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Daucosterol is an orally active natural sterol compound, which has anti-inflammatory, anticancer and immunomodulatory activities. Daucosterol inhibits cancer cell proliferation by inducing autophagy through ROS-dependent manner. Daucosterol also inhibits colon cancer growth by inducing apoptosis, inhibiting cell migration and invasion and targeting caspase signalling pathway .
|
-
- HY-150231
-
SU056
2 Publications Verification
|
YB-1
|
Cancer
|
|
SU056 is a YB-1 inhibitor. SU056 induces cell-cycle arrest, apoptosis, and inhibits cell migration in ovarian cancer cells. SU056 interacts with YB-1 and inhibits and its associated downstream proteins and pathways. SU056 can enhance the cytotoxic effects of Paclitaxel (HY-B0015) .
|
-
- HY-168567
-
|
|
RIP kinase
NF-κB
p38 MAPK
|
Inflammation/Immunology
|
|
RIPK2-IN-6 (Compound 15a) is an inhibitor for RIPK, that inhibits the phosphorylation of RIPK2, and thus inhibits the NF-κB and MAPK signaling pathways. RIPK2-IN-6 exhibits anti-inflammatory and anti-fibrotic activities in Dextran sodium sulfate (HY-116282C)-induced mice colitis models .
|
-
- HY-169963
-
|
|
Phosphodiesterase (PDE)
|
Others
|
|
PDE1-IN-8 (Compound 3f) is the inhibitor for PDE1 with an IC50 of 11 nM. PDE1-IN-8 inhibits cAMP and cGMP signaling pathway, inhibits the differentiation and proliferation of cells into myofibroblast, and exhibits anti-fibrotic efficacy in Bleomycin (HY-17565)-induced rat pulmonary fibrosis model .
|
-
- HY-138537
-
|
|
IKK
|
Cancer
|
|
NF-κB-IN-1, a 4-arylidene crucumin analogue, is a potent NF-κB signaling pathway inhibitor. NF-κB-IN-1 directly inhibits IKK to block NF-κB activation. NF-κB-IN-1 effectively inhibits the viability of lung cancer cells and attenuates the clonogenic activity of A549 cells .
|
-
- HY-10594
-
|
TAK-442
|
Factor Xa
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Letaxaban (TAK-442) is an orally active and selective direct FXa inhibitor. Letaxaban is a drug with dual anticoagulant and anti-inflammatory activity that works by directly inhibiting FXa and by intervening in the PAR1 signaling pathway. Letaxaban can be used in the study of thrombotic diseases, cardiovascular diseases and inflammation-related diseases .
|
-
- HY-126390
-
|
NSC 150117
|
Phosphatase
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
(E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway .
|
-
- HY-152265A
-
|
|
PINK1/Parkin
Mitophagy
|
Neurological Disease
|
|
PARL-IN-1 TFA is a potent PARL inhibitor with an IC50 value of 28 nM. PARL-IN-1 TFA inhibits PARL and leads to a robust activation of the PINK1/Parkin pathway. PARL-IN-1 TFA promotes PINK1/Parkin-dependent mitophagy .
|
-
- HY-172097
-
|
|
Drug Derivative
|
Cancer
|
|
HL22 is a harmaline derivative. HL22 significantly inhibits HCT116, MGC803 and MCF7 cancer cell lines, and inhibits MGC803 cell migration and monoclonal formation. The anti-cancer mechanism of HL22 is related to a variety of metabolic pathways and can be used in the study of cancer .
|
-
- HY-P5819A
-
|
|
PROTACs
β-catenin
Wnt
|
Cancer
|
|
xStAx-VHLL TFA is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL TFA inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL TFA can inhibit the proliferation of colon cancer cells and has anti-tumor activity .
|
-
- HY-P10875
-
|
|
Hedgehog
|
Cancer
|
|
HL2-m5 is the inhibitor for the interaction between sonic hedgehog/patched (Shh/PTCH1) with Kd of 170 nM for Shh. HL2-m5 inhibits activation of Hedgehog signaling pathway and transcription of Gli-controlled gene with an IC50 of 230 nM .
|
-
- HY-113628
-
|
VML-530
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
ABT-080 is an orally active inhibitor of leukotriene biosynthesis. ABT-080 simultaneously blocks the leukotriene pathways leading to the synthesis of LTB4 and LTC4, but does not inhibit PGH2 biosynthesis. ABT-080 can block bronchoconstriction and be used in the research of asthma and related inflammations
|
-
- HY-146738
-
|
|
Akt
|
Cancer
|
|
GSD-11 is a potent and selective anti-austerity agent. GSD-11 inhibits the cell migration and colony formation of PANC-1 cells. GSD-11 inhibits the Akt/mTOR signaling pathway. GSD-11 has the potential for the research of pancreatic cancer[1].
|
-
- HY-162143
-
|
|
SphK
Akt
mTOR
|
Cancer
|
|
SKI-349 is a dual-targeted inhibitor of sphingosine kinase 1/2 (SPHK1/2) and microtubule assembly (MDA). SKI-349 has anticancer activity. SKI-349 can inhibit the vitality, invasion, and AKT/mTOR signaling pathway of liver cells .
|
-
- HY-N9971R
-
|
|
NF-κB
Bacterial
|
Infection
Inflammation/Immunology
Cancer
|
|
Hentriacontane (Standard) is the analytical standard of Hentriacontane. This product is intended for research and analytical applications. Hentriacontane is a long-chain alkane. Hentriacontane exerts anti-inflammatory effects by inhibiting the NF-κB pathway. Hentriacontane has anti-inflammatory, antitumor and antibacterial activities .
|
-
- HY-N3974
-
|
(+)-Griffipavixanthone
|
Apoptosis
|
Cancer
|
|
Griffipavixanthone can be extracted from Garcinia schomburgkiana. Griffipavixanthone induces cell apoptosis through mitochondrial apoptotic pathway accompanying with ROS production. Griffipavixanthone is an anti-cancer agent. Griffipavixanthone is a weak sucrase inhibitor (IC50: 4.58 mM) .
|
-
- HY-N6674
-
|
ECO-4601; TLN-4601; BU 4664L
|
Ras
Apoptosis
|
Cancer
|
|
Diazepinomicin (TLN-4601) is a secondary metabolite produced by Micromonospora sp. Diazepinomicin (TLN-4601) inhibits the EGF-induced Ras-ERK MAPK signaling pathway and induces apoptosis. An anti-tumor agent for K-Ras mutant models .
|
-
- HY-N2523
-
|
|
Wnt
|
Cancer
|
|
Gigantol isomer-1 is a bibenzyl compound derived from Dendrobium nobile. Gigantol isomer-1 shows promising therapeutic potential against cancer cells. Gigantol isomer-1 is a novel inhibitor of the Wnt/β-catenin pathway.
|
-
- HY-N6679A
-
|
|
HSP
TGF-beta/Smad
|
Infection
Cancer
|
|
10,11-Dehydrocurvularin is a prevalent fungal phytotoxin and an antibiotic. 10,11-Dehydrocurvularin is a strong activator of the heat shock response. 10,11-Dehydrocurvularin inhibits TGF-β signalling pathway. Anti-tumorous activity .
|
-
- HY-105122
-
|
WIN 49596
|
Androgen Receptor
|
Endocrinology
Cancer
|
|
Zanoterone is an orally active antagonist of the androgen receptor (AR) with a Ki of 2.2 μM. Zanoterone blocks the binding of androgens such as testosterone and dihydrotestosterone (DHT), inhibiting the androgen signaling pathway, thereby reducing androgen-dependent prostate hyperplasia and prostate cancer growth .
|
-
- HY-P99818
-
|
ACE-031
|
TGF-β Receptor
|
Metabolic Disease
|
|
Ramatercept (ACE-031) is a soluble ActRIIB receptor and can be used as a soluble activin receptor 2 (ACVR2) antagonist. Ramatercept inhibits the signal pathway of muscle growth inhibition and has potential application in muscle atrophy .
|
-
- HY-N7128
-
|
|
Cytochrome P450
ERK
p38 MAPK
NF-κB
MMP
PAI-1
|
Cancer
|
|
Flavanone is a naturally occurring flavone. Flavanone has inhibitory activity for human estrogen synthetase (aromatase). Flavanone is the inhibitor for ERK/p38/NF-κB signaling pathway. Flavanone exhibits oral activity and antitumor efficacy .
|
-
- HY-W028127
-
|
|
IKK
|
Inflammation/Immunology
|
|
IKKβ-IN-4 (compound 14) is an IkappaB kinase-β ( IKKβ ) inhibitor with IC50 value of 1.9 μM. IKKβ is a key enzyme in the NF-κB signaling pathway and is involved in the development of many diseases .
|
-
- HY-160040
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Cobitolimod is a DNA oligonucleotide agonist of TLR-9 with anti-inflammatory activity. Cobitolimod suppresses Th17 cells and induces anti-inflammatory FoxP3 and IL-10 expression, inhibiting the IL-17 signaling pathway .
|
-
- HY-162384
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EPIC-0628 is an inhibitor of the HOTAIR-EZH2 interaction and promotes ATF3 expression. The long noncoding RNA HOTAIR has been found to regulate glioblastoma (GBM) progression and mediate DNA damage repair (DDR) by interacting with the catalytic subunit EZH2 of PRC2. EPIC-0628 also inhibits the ATF3-p38-E2F1 DDR pathway to inhibit the HR pathway and upregulates CDKN1A (p21) expression, causing cell cycle arrest. EPIC-0628 also synergizes with Temozolomide (TMZ) (HY-17364) to enhance its in vivo potency .
|
-
- HY-168963
-
|
|
PROTACs
Btk
Itk
p38 MAPK
|
Inflammation/Immunology
Cancer
|
|
PROTAC BTK Degrader-13 (Compound 25) is the PROTAC degrader for BTK with a DC50 of 0.27 μM. PROTAC BTK Degrader-13 inhibits the activity of BTK with an IC50 of 0.44 μM, inhibits IL-2-induced T cell kinase (ITK) with an IC50 of 2.16 μM. PROTAC BTK Degrader-13 inhibits p38 MAPK signaling pathway, block the activation of the BCR (B cell receptor) signaling pathway . (Pink: ligand for target protein BTK ligand 15 (HY-168965); Black: linker (HY-Y0524); Blue: ligand for E3 ligase cereblon (HY-103596))
|
-
- HY-N15267
-
|
|
FAK
Akt
mTOR
|
Cancer
|
|
Ovalitenone is a flavonoid compound that can be isolated from the plant Millettia peguensis. It shows no cytotoxic effects on lung cancer H460 and A549 cells, but it significantly inhibits anchorage-independent growth, CSC-like phenotypes, colony formation, and the migration and invasion capabilities of cancer cells. Ovalitenone can significantly reduce the levels of N-cadherin, snail, and slug, while increasing E-cadherin, thus inhibiting the EMT pathway. Additionally, Ovalitenone suppresses the signaling pathways regulated by focal adhesion kinase (FAK), ATP-dependent tyrosine kinase (AKT), mammalian target of rapamycin (mTOR), and cell division cycle 42 (Cdc42) .
|
-
- HY-172201
-
|
|
NF-κB
Reactive Oxygen Species
Autophagy
Apoptosis
HIF/HIF Prolyl-Hydroxylase
Akt
STAT
PI3K
|
Inflammation/Immunology
Cancer
|
|
NF-κB-IN-19 (Compound 8) is an NF-κB inhibitor. NF-κB-IN-19 effectively induces DNA damage, promotes the generation of ROS, and induces autophagy and apoptosis through the NF-κB signaling pathway in tumor cells. In addition, NF-κB-IN-19 can inhibit the levels of VEGF and HIF-1α, and exert antiproliferative activity in tumor cells through the PI3K/AKT and STAT-3 pathways. NF-κB-IN-19 can effectively overcome cisplatin resistance and has anti-tumor activity .
|
-
- HY-161925
-
|
|
TGF-β Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
sTGFBR3 antagonist 1 (Compound p24) is an antagonist for soluble transforming growth factor beta receptor 3 (sTGFBR3), thus activates TGF-β signaling pathway, and inhibits IκBα/NF-κB signaling pathway. sTGFBR3 antagonist 1 inhibits NO-release in LPS (HY-D1056) -induced BV2 cells with an IC50 of 0.52 μM. sTGFBR3 antagonist 1 exhibits anti-inflammatory and neuroprotective activities with blood brain barrier (BBB) permeability. sTGFBR3 antagonist 1 can be used in Alzheimer’s Disease research .
|
-
- HY-164530
-
|
|
Src
VEGFR
Raf
p38 MAPK
|
Cancer
|
|
SKLB646 is an orally active multi-target kinase inhibitor. SKLB646 shows significant inhibitory effects on SRC and VEGFR2 with IC50 values ??of 0.002 μmol/L and 0.012 μmol/L, respectively. SKLB646 also shows significant inhibitory effects on B-Raf and C-Raf with IC50 values ??of 0.022 μmol/L and 0.019 μmol/L, respectively. SKLB646 inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibiting Raf kinase. In addition, SKLB646 can inhibit the proliferation, migration and invasion of human umbilical vein endothelial cells (HUVEC) to inhibit tumor-induced angiopoietic formation. SKLB646 shows significant anti-proliferative and anti-survival activities against triple-negative breast cancer (TNBC) cell lines .
|
-
- HY-W130965
-
|
|
Influenza Virus
Akt
|
Infection
|
|
1-Formyl-beta-carboline is an alkaloid with inhibitory activity against Newcastle disease virus (NDV). 1-Formyl-beta-carboline can effectively inhibit different genotypes of NDV with IC50 values within 10 μM, and its inhibition rate is more than 90% at a concentration of 20 μM. 1-Formyl-beta-carboline mainly exerts its effects by inhibiting the adsorption and entry processes in the NDV life cycle. 1-Formyl-beta-carboline has been identified as a novel HN inhibitor that can directly interact with the NDV HN protein and affect the adsorption of NDV. 1-Formyl-beta-carboline also inhibits the entry of NDV by inhibiting the PI3K/Akt signaling pathway rather than the ERK pathway .
|
-
- HY-10440R
-
|
|
Hedgehog
Autophagy
|
Cancer
|
|
Vismodegib (Standard) is the analytical standard of Vismodegib. This product is intended for research and analytical applications. Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively .
|
-
- HY-161513
-
|
|
COX
NO Synthase
|
Inflammation/Immunology
|
|
iNOS/COX-2-IN-1 (Compound 12e) is an inhibitor of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS). iNOS/COX-2-IN-1 inhibits the NF-κB and MAPKs signaling pathways and thus exerts anti-inflammatory effects .
|
-
- HY-149992
-
|
|
MyD88
|
Inflammation/Immunology
Cancer
|
|
MyD88-IN-1 (Compound c17) is an orally active MyD88 inhibitor. MyD88-IN-1 inhibits the interaction of TLR4 and MyD88 and suppressed the NF-κB pathway. MyD88-IN-1 can be used in research of cancer and inflammatory .
|
-
- HY-P10072A
-
|
Hsp25 kinase inhibitor acetate; Mk2 pseudosubstrate acetate
|
JNK
HSP
MAPKAPK2 (MK2)
p38 MAPK
ERK
|
Others
|
|
MK2-IN-5 (Hsp25 kinase inhibitor) acetate is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 acetate targets the protein interaction domain in the MAPK pathway. MK2-IN-5 acetate inhibits HSP25 and HSP27 phosphorylation .
|
-
- HY-125276
-
|
|
DNA/RNA Synthesis
|
Inflammation/Immunology
|
|
TH5487 is a potent 8-oxoguanine DNA glycosylase 1 (OGG1) inhibitor with an IC50 of 342 nM. TH5487 stops OGG1 from recognizing its DNA substrate, inhibits DNA repair and modifies OGG1 chromatin dynamics, which results in the inhibition of proinflammatory pathway genes .
|
-
- HY-P10868
-
|
RLS-0071
|
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Pegtarazimod (RLS-0071) is an inhibitor for Complement system via classical and lectin pathways. Pegtarazimod inhibits myeloperoxidase (MPO), reduces ROS generation. Pegtarazimod reduces the formation of neutrophil extracellular traps (NETs). Pegtarazimod exhibits anti-inflammatory activity and can be used in research of acute graft-versus-host disease .
|
-
- HY-159605
-
|
|
Autophagy
JNK
Reactive Oxygen Species
|
Cancer
|
|
Autophagy inducer 5 (compound 21o) is a potent MCF-7 inhibitor (IC50: 2 μM), and a potential breast cancer inhibitor. Autophagy inducer 5 induces cellular autophagy by activating the ROS/JNK signaling pathway, which increases ROS generation and JNK phosphorylation, exerting cytotoxic effects .
|
-
- HY-16125
-
|
L-651582 Orotate; CAI Orotate
|
Calcium Channel
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor. Carboxyamidotriazole Orotate is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory and antiangiogenic effects .
|
-
- HY-132601
-
|
MRG-106
|
MicroRNA
|
Cancer
|
|
Cobomarsen (MRG-106) is an oligonucleotide inhibitor of miR-155. Cobomarsen inhibits multiple gene pathways associated with cell survival (including JAK/STAT, MAPK/ERK and PI3K/AKT). Cobomarsen can be used for the research of B-cell lymphoma .
|
-
- HY-114277A
-
|
AMG-510 racemate
|
Ras
p38 MAPK
|
Cancer
|
|
Sotorasib racemate (Compound A) is an orally active racemate of Sotorasib (HY-114277), a covalent inhibitor of KRAS G12C mutant which induces adaptive feedback activation of MAPK pathway. Sotorasib racemate also exerts inhibitor activity against KRAS G12C induced cancer and can be applied to cancer research .
|
-
- HY-P10323
-
|
Tumstatin (74-98), human
|
Integrin
FAK
mTOR
Apoptosis
|
Cancer
|
|
T7 peptide is an endothelial cell-specific inhibitor. T7 peptide interacts with αVβ3 integrin to inhibit the FAK, PI3-kinase, PKB/Akt, and mTOR signaling pathways in endothelial cells, ultimately suppressing protein synthesis and inducing apoptosis .
|
-
- HY-117885
-
|
|
PDK-1
|
Cancer
|
|
PF-5177624 is a specific and potent inhibitor of PDK1, a key enzyme in the PI3K/AKT signaling pathway that is frequently dysregulated in breast cancer. PDK1 phosphorylates AKT at T308 and other substrates, activating downstream signaling pathways that are important for tumor progression. PF-5177624 blocks IGF-1-stimulated PDK1 activity and downstream AKT and p70S6K phosphorylation, reducing cell proliferation and transformation in breast cancer cells .
|
-
- HY-113439S
-
|
|
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
|
|
12-HETE-d8 is the deuterium labeled 12-HETE. 12-HETE, a major metabolic product of arachidonic acid using 12-LOX catalysis, inhibits cell apoptosis in a dose-dependent manner. 12-HETE promotes the activation and nuclear translocation of NF-κB through the integrin-linked kinase (ILK) pathway[1].12-HETE has both anti-thrombotic and pro-thrombotic effects[2]. 12-HETE is a neuromodulator[3].
|
-
- HY-128634
-
|
|
Apoptosis
PI3K
MEK
|
Cancer
|
|
CML-IN-1 (compound 7) is a potent anticancer agent. CML-IN-1 displays very good induced-apoptosis effect for human chronic myeloid leukemia (CML) cell line K562. CML-IN-1 exerts its effect via a significantly reduced protein phosphorylation of PI3K/Akt signal pathway. CML-IN-1 (compound 4) also inhibits cell proliferation by suppressing the MEK/ERK signaling pathway in colorectal cancer .
|
-
- HY-P10797
-
-
- HY-P10840
-
|
|
JAK
MHC
|
Inflammation/Immunology
|
|
Tkip is a JAK2 specific inhibitor. Tkip can bind the JAK2 autophosphorylation site, inhibit the JAK2 autophosphorylation and the phosphorylation of the IFN-γ receptor subunit IFNGR-1. Tkip inhibits the antiviral activity of IFN-γ and the expression of MHC Class I molecules. Tkip can be used to study the IFN-γ signaling pathway .
|
-
- HY-150567
-
|
|
Smo
Hedgehog
|
Cancer
|
|
SMO-IN-3 (compound 12a) is a potent smoothened (SMO) inhibitor with an IC50 value of 34.09 nM for hedgehog (Hh) signaling pathway. SMO-IN-3 has antiproliferative activity against human medulloblastoma cell line Daoy. Anticancer activity .
|
-
- HY-162404
-
-
- HY-168172
-
|
|
Lactate Dehydrogenase
|
Cancer
|
|
LDH-IN-3 (compound E38) is an inhibitor of LDH, promising protective agent for ischemic nerve damage in the eye and brain. LDH-IN-3 acts its function via HO-1/SIRT1 pathway. .
|
-
- HY-124156A
-
|
|
Wnt
|
Metabolic Disease
|
|
KY-02327 acetate, a metabolically stabilized KY-02061 analog, is a potent Dishevelled (Dvl)-CXXC5 interaction inhibitor. KY-02327 acetate shows an activating effect on the Wnt/β-catenin pathway, resulting in promotion of osteoblast differentiation .
|
-
- HY-N0436R
-
|
|
NF-κB
|
Infection
Inflammation/Immunology
|
|
Engeletin (Standard) is the analytical standard of Engeletin. This product is intended for research and analytical applications. Engeletin is a flavanonol glycoside isolated from Smilax glabra Roxb. , inhibits NF-κB signaling-pathway activation, and possesses anti-inflammatory, analgesic, diuresis, detumescence, and antibiosis effects.
|
-
- HY-14664A
-
-
- HY-N0072
-
|
|
Apoptosis
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Brazilin is a red dye precursor obtained from the heartwood of several species of tropical hardwoods. Brazilin inhibits the cells proliferation, promotes apoptosis, and induces autophagy through the AMPK/mTOR pathway. Brazilin shows chondroprotective and anti-inflammatory activities .
|
-
- HY-N1469R
-
|
|
Potassium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
Kaurenoic acid (Standard) is the analytical standard of Kaurenoic acid. This product is intended for research and analytical applications. Kaurenoic acid is a diterpene from Sphagneticola trilobata, inhibits Inflammatory Pain by the inhibition of cytokine production and activation of the NO–cyclic GMP–PKG–ATP-sensitive potassium channel signaling pathway .
|
-
- HY-146058
-
|
|
NF-κB
Reactive Oxygen Species
|
Cancer
|
|
NF-κB/PON1-IN-1 (Compound 16) is a NF-κB/PON1 pathway inhibitor. NF-κB/PON1-IN-1 has antioxidant (IC50 = 45.76 µM) and hepatoprotective activities .
|
-
- HY-162405
-
-
- HY-150564
-
|
|
Smo
Hedgehog
|
Cancer
|
|
SMO-IN-2 (compound 1) is a potent smoothened (SMO) inhibitor with an IC50 value of 123.4 nM for hedgehog (Hh) signaling pathway. SMO-IN-2 has antiproliferative activity against human medulloblastoma cell line Daoy. Anticancer activity .
|
-
- HY-B0464
-
|
|
Bcl-2 Family
Caspase
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Hydralazine hydrochloride is an antihypertensive agent. Hydralazine hydrochloride can inhibit mitochondrial fission and human peritoneal mesothelial cell proliferation. Hydralazine hydrochloride has immunomodulation and anti-migratory effect. Hydralazine hydrochloride activates the intrinsic pathway of apoptosis and causes DNA damage .
|
-
- HY-N4233
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
Bisabolangelone, a sesquiterpene derivative, is isolated from the roots of Osterici Radix. Bisabolangelone possesses anti-inflammatory properties, which inhibits LPS-stimulated inflammation through the blocking of NF-kappaB and MAPK pathways in macrophages. Bisabolangelone has anti-ulcer activities .
|
-
- HY-121006
-
|
|
Mitochondrial Metabolism
AMPK
|
Metabolic Disease
Cancer
|
|
Biguanide is an orally active antihyperglycemic agent. Biguanide inhibits mitochondrial ATP production, activates the LKB1-AMPK signaling pathway, and damages the energy homeostasis. Biguanide exhibits potential in ameliorating the type 2 diabetes and the insulin-associated cancers .
|
-
- HY-N0697
-
-
- HY-124156
-
|
|
Wnt
|
Metabolic Disease
|
|
KY-02327, a metabolically stabilized KY-02061 analog, is a potent Dishevelled (Dvl)-CXXC5 interaction inhibitor. KY-02327 shows an activating effect on the Wnt/β-catenin pathway, resulting in promotion of osteoblast differentiation .
|
-
- HY-160709
-
|
|
Wnt
β-catenin
|
Cancer
|
|
Wnt/β-catenin-IN-2 (Compound 3235-0367) is a Wnt/β-catenin signaling pathway inhibitor, with IC50 and KD values of 7.1 and 2.5 μM, respectively. Wnt/β-catenin-IN-2 can be used for the research of cancer .
|
-
- HY-157160
-
|
|
Herbicide
|
Others
|
|
PPO-IN-5 (compound 9) is a herbicide based on PPO inhibitors. PPO, protoporphyrinogen oxidase, participates in the biosynthetic pathway of heme and chlorophyll synthesis. PPO-IN-5 is tolerant in cereal crops such as wheat, corn, and rice, and is a potential herbicide in wheat fields .
|
-
- HY-114395
-
|
|
|
Inflammation/Immunology
|
|
NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel agentgable node in the Notch pathway.
|
-
- HY-116050
-
-
- HY-146504
-
|
|
Topoisomerase
PI3K
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Topoisomerase I/II inhibitor 3 (compound 7) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis by inhibiting PI3K/Akt/mTOR signaling pathway. Topoisomerase I/II inhibitor 3 can be used for liver cancer research .
|
-
- HY-161459
-
|
|
Apoptosis
Hedgehog
Gli
|
Cancer
|
|
GLI1-IN-1 (CBC-1) is a GLI-1 inhibitor with excellent water solubility and anticancer activity. GLI1-IN-1 can induce apoptosis and suppress the growth of colorectal cancer by inhibiting the Hedgehog(HH) (IC50=1.3 μM) pathway .
|
-
- HY-121993
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Combretastatin A-1 is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 exhibits anti-tumor and anti-vascular effects .
|
-
- HY-10834
-
|
|
β-catenin
|
Cancer
|
|
β-catenin-IN-6 is a β-catenin inhibitor, targeting to canonical Wingless-related integration site signaling pathway. β-catenin-IN-6 inhibits human colorectal cancer cells proliferation, as well as in a β-catenin/RK3E mouse model .
|
-
- HY-149266
-
THK01
1 Publications Verification
|
ROCK
|
Cancer
|
|
THK01 is a potent ROCK2 inhibitor with IC50 values of 5.7 and 923 nM for ROCK2 and ROCK1, respectively. THK01 inhibits breast cancer metastasis through the ROCK2-STAT3 signaling pathway. THK01 can be used in research of breast cancer .
|
-
- HY-121750
-
|
|
Ras
ROCK
|
Cancer
|
|
CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor . CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis .
|
-
- HY-119378
-
|
CX 295
|
Proteasome
Apoptosis
|
Neurological Disease
|
|
AK 295 (CX 295) is a calpain inhibitor that inhibits apoptosis through a calpain-dependent pathway. AK 295 improves neurological function in a rat model of spinal cord injury (SCI). AK 295 can be used in the study of neurodegenerative diseases, such as bulbar amyotrophy, stroke, Alzheimer's disease, Parkinson's disease, multiple sclerosis .
|
-
- HY-168918
-
|
|
Parasite
Dihydrofolate reductase (DHFR)
|
Infection
|
|
Insecticidal agent 19 (Compound 7b) exhibits antimalarial activity by inhibiting dihydrofolate
reductase-thymidylate synthase (DHFR-TS) and pteridine reductase 1 (PTR1) through the folic acid metabolic pathway. Insecticidal agent 19 inhibits Leishmania major promastigote and amastigote with IC50 of 1.43 μM and 3.78 μM .
|
-
- HY-N0247R
-
|
|
Smo
|
Cancer
|
|
Saikosaponin B1 (Standard) is the analytical standard of Saikosaponin B1. This product is intended for research and analytical applications. Saikosaponin B1 is a bioactive constituent of Radix Bupleuri with anticancer activity. Saikosaponin B1 significantly inhibits tumor growth in Medulloblastoma (MB) model by inhibiting the Hedgehog pathway through targeting SMO .
|
-
- HY-163533
-
|
|
VEGFR
|
Inflammation/Immunology
|
|
CPD-002 is an inhibitor for vascular endothelial growth factor receptor 2 (VEGFR 2), that inhibits angiogenesis through inhibition of VEGFR2/PI3K/AKT signaling pathway. CPD-002 exhibits anti-inflammatory activity and attenuates rheumatoid arthritis .
|
-
- HY-149496
-
-
- HY-P6177
-
|
|
Dipeptidyl Peptidase
|
Inflammation/Immunology
|
|
SGP8 (IAVPGEVA) is an octapeptide produced by hydrolysis of soybean 11S globulin, which has the effects of regulating lipid metabolism, inflammation and fibrosis. SGP8 (IAVPGEVA) exhibits inhibitory activity against DPP4 and inhibits the JNK-c-Jun signaling pathway, and has the ability to inhibit non-alcoholic steatohepatitis (NASH) .
|
-
- HY-101494
-
|
LY3214996
|
ERK
|
Cancer
|
|
Temuterkib (LY3214996) is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. Temuterkib shows potent antitumor activities in cancer models with MAPK pathway alterations.
|
-
- HY-135231
-
NL-1
2 Publications Verification
|
Mitochondrial Metabolism
Autophagy
|
Cancer
|
|
NL-1 is a mitoNEET inhibitor with antileukemic effect. NL-1 inhibits REH and REH/Ara-C cells growth with IC50s of 47.35 μM and 56.26 μM, respectively. NL-1-mediated death in leukemic cells requires the activation of the autophagic pathway .
|
-
- HY-147836
-
|
|
Akt
NF-κB
JNK
TNF Receptor
COX
|
Inflammation/Immunology
|
|
Akt/NF-κB/JNK-IN-1 (Compound 2i) is an inhibitor of Akt, NF-κB and JNK signaling pathways. Akt/NF-κB/JNK-IN-1 inhibits nitric oxide production with an IC50 of 3.15 μM. Akt/NF-κB/JNK-IN-1 shows anti-inflammatory activities .
|
-
- HY-116497
-
|
|
FAK
|
Cancer
|
|
PH11 is a novel focal adhesion kinase (FAK) inhibitor that rapidly induces apoptosis in TRAIL-resistant PANC-1 cells when combined with TRAIL, but has no effect on normal human fibroblasts. The study found that PH11 downregulates c-FLIP through inhibition of FAK and phosphatidylinositol-3-kinase (PI3K)/AKT pathways, thereby restoring the TRAIL apoptotic pathway, suggesting that this combination therapy may provide an attractive therapeutic strategy for the safe and effective treatment of pancreatic cancer. PH11 selectively inhibits c-FLIP expression by modulating upstream signaling pathways and may represent an innovative therapeutic strategy. Although further work is needed to fully elucidate the mechanism of PH11-induced TRAIL sensitization, we believe that our results will provide a new approach to target c-FLIP without the risk of interfering with caspase-8 processing, which could potentially lead to TRAIL resistance. This study also suggests a role for the FAK/AKT signaling pathway in regulating c-FLIP expression in TRAIL-induced apoptosis, and this understanding will provide important clues to control the resistance mechanism to optimize the potential of TRAIL-based pancreatic cancer treatment.
|
-
- HY-N0330R
-
|
|
Apoptosis
Autophagy
PI3K
c-Myc
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Momordin Ic (Standard) is the analytical standard of Momordin Ic. This product is intended for research and analytical applications. Momordin Ic is an orally active triterpenoid saponin that can be isolated from Kochia scoparia. It is also a SUMO specific protease 1 (SENP1) inhibitor, SENP1/c-MYC signaling pathway inhibitor, and apoptosis inducer. Momordin Ic induces autophagy and apoptosis in liver cancer cells through the PI3K/Akt and MAPK signaling pathways mediated by reactive oxygen species. Momordin Ic has the ability to control glucose induced blood glucose elevation, inhibit gastric emptying, resist rheumatoid arthritis, reduce CCl4 (HY-Y0298) induced hepatotoxicity and anti-tumor activity .
|
-
- HY-P10373
-
|
|
JAK
|
Infection
|
|
pJAK2(1001-1013) is a SOCS1/3 antagonist. pJAK2(1001–1013) plays a positive role in antiviral immune response by inhibiting the negative regulatory effect of SOCS proteins and enhancing the JAK/STAT signaling pathway
|
-
- HY-N1382R
-
|
|
NO Synthase
|
Metabolic Disease
Inflammation/Immunology
|
|
Asperuloside (Standard) is the analytical standard of Asperuloside. This product is intended for research and analytical applications. Asperuloside is an iridoid isolated from Hedyotis diffusa, with anti-inflammatory activity. Asperuloside inhibits inducible nitric oxide synthase (iNOS), suppresses NF-κB and MAPK signaling pathways .
|
-
- HY-162257
-
|
|
Btk
|
Cancer
|
|
BTK-IN-34 (compound 9h) is a selective BTK inhibitor. BTK-IN-34 shows antiproliferative activity in RAMOS cells through selective inhibition of pBTK (Tyr223) without affecting Lyn and Syk, upstream proteins in the BCR signaling pathway .
|
-
- HY-N0738R
-
|
|
NF-κB
Endogenous Metabolite
|
Cardiovascular Disease
Cancer
|
|
Stachydrine hydrochloride (Standard) is the analytical standard of Stachydrine hydrochloride. This product is intended for research and analytical applications. Stachydrine hydrochloride is the major active constituent of Leonurus artemisia, which is a potential therapy for cardiovascular diseases . Stachydrine can inhibit the NF-κB signal pathway. Anti-hypertrophic activities .
|
-
- HY-167868
-
|
|
TRP Channel
Apoptosis
|
Neurological Disease
Cancer
|
|
DWP-05195 is a TRPV1 antagonist that can inhibit the pain signal transduction. DWP-05195 induces ER stress-dependent apoptosis through the ROS-p38-CHOP pathway in human ovarian cancer cells .
|
-
- HY-17595
-
|
|
Parasite
Apoptosis
Microtubule/Tubulin
|
Infection
Cancer
|
|
Mebendazole is a highly effective, broad-spectrum antihelmintic against nematode infestations. Mebendazole also exhibits inhibitory effect against glioblastoma multiforme (GBM), inhibits Hedgehog pathway and tubulin polymerization. Mebendazole is orally active and can cross CNS penetration .
|
-
- HY-N12507
-
|
|
STING
NF-κB
|
Others
|
|
Eupenicisirenin C (compound 1) is a sirenin derivative. Eupenicisirenin C has strong NF-κB inhibitory activities. Eupenicisirenin C suppresses effects on cGAS-STING pathway. Eupenicisirenin C inhibits RANKL-induced osteoclast differentiation in bone marrow macrophage cells .
|
-
- HY-162126
-
|
|
Microtubule/Tubulin
YAP
|
Cancer
|
|
Tubulin polymerization-IN-58 (Compound K18) is a tubulin polymerization inhibitor with an IC50 of 0.446 μM. Tubulin polymerization-IN-58 also induces the degradation of oncogenic protein YAP via the UPS pathway, thus can be used for cancer research .
|
-
- HY-142924
-
|
|
ATM/ATR
|
Cancer
|
|
ATR-IN-8 is a potent inhibitor of ATR. ATR is a key enzyme in the homologous recombination repair pathway and belongs to the PIKK family. ATR-IN-8 has the potential for the research of cancer diseases (extracted from patent WO2021143821A1, compound 3) .
|
-
- HY-122961
-
|
1,2-Didehydromiltirone
|
NF-κB
p38 MAPK
|
Inflammation/Immunology
|
|
Dehydromiltirone (1,2-Didehydromiltirone) is a diterpenoid quinone with an anti-inflammatory effect. Dehydromiltirone prevents liver injury by modifying the MAPK and NF-κB signaling pathways, reducing neuroinflammatory responses, and inhibiting platelet aggregation. Dehydromiltirone can be used for osteoporosis research .
|
-
- HY-33298
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
LM10 is a potent inhibitor of tryptophan 2,3-dioxygenase (TDO). Tryptophan 2,3-dioxygenase (TDO) is an unrelated hepatic enzyme that also degrades tryptophan along the kynurenine pathway. LM10 has the potential for the research of cancer diseases .
|
-
- HY-N1472
-
|
|
Apoptosis
Reactive Oxygen Species
PPAR
GSK-3
Tau Protein
Ras
TGF-β Receptor
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Levistolide A is an apoptosis inducer and a PEDV virus inhibitor. Levistolide A can induce apoptosis in colon cancer cells and suppress the replication of porcine epidemic diarrhea virus (PEDV) by promoting ROS generation. Levistolide A activates peroxisome proliferator-activated receptor γ (PPARγ) in N2a/APP695swe cells and reduces excessive phosphorylation of tau through the GSK3α/β pathway, improving symptoms in Alzheimer’s mice. Levistolide A improves kidney damage in 5/6 nephrectomy (Nx) mice by inhibiting the RAS,TGF-β1/Smad, and MAPK pathways .
|
-
- HY-N0560R
-
|
|
HIF/HIF Prolyl-Hydroxylase
Autophagy
Virus Protease
|
Cancer
|
|
Oroxylin A (Standard) is the analytical standard of Oroxylin A. This product is intended for research and analytical applications. Oroxylin A is an active flavonoid compound with strong anti-cancer effects. Oroxylin A inhibits the IL-6/STAT3 pathway and NF-κB signaling, inhibits cell proliferation and induces apoptosis. Oroxylin A inhibits colitis-related carcinogenesis .
|
-
- HY-156109
-
|
|
PDHK
Mitochondrial Metabolism
|
Cancer
|
|
PDK-IN-2 (Compound 1F) is a PDK inhibitor (IC50: 68 nM). PDK-IN-2 inhibits the cellular expression of PDK1 and PDK4. PDK-IN-2 enhances mitochondrial bioenergetics, attenuates glycolytic phenotypes, and induces cell apoptosis in the mitochondrial pathway. PDK-IN-2 inhibits tumor growth in 4T1 syngeneic mice model .
|
-
- HY-118316
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
GSK223 is a quinazolinone NOD1 pathway inhibitor with potential anti-inflammatory activity. GSK223 can selectively inhibit IL-8 release under iE-DAP stimulation without affecting IL-8 secretion caused by TNF receptor, TLR2 or NOD2 agonists. GSK223 does not directly inhibit RIP2 kinase activity.
|
-
- HY-100830A
-
|
|
Wnt
MAP4K
TGF-beta/Smad
|
Inflammation/Immunology
|
|
NCB-0970 is the negative control of NCB-0846 (HY-100830). NCB-0846 is an orally active, selective inhibitor for Wnt, that inhibits Traf2- and Nck-interacting kinase (TNIK) with an IC50 of 21 nM. NCB-0846 blocks TGF-β signaling pathway by inhibiting SMAD2/3 phosphorylation and nuclear translocation .
|
-
- HY-P10436
-
|
|
Raf
|
Cancer
|
|
Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAF G469A with IC50 of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC50 is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence .
|
-
- HY-13755
-
|
|
HDAC
Keap1-Nrf2
Apoptosis
Bcl-2 Family
Caspase
Reactive Oxygen Species
|
Inflammation/Immunology
Cancer
|
|
Sulforaphane is an orally active inducer of the Keap1/Nrf2/ARE pathway. Sulforaphane promotes the transcription of tumor-suppressing proteins and effectively inhibits the activity of HDACs. Through the activation of the Keap1/Nrf2/ARE pathway and further induction of HO-1 expression, Sulforaphane protects the heart. Sulforaphane suppresses high glucose-induced pancreatic cancer through AMPK-dependent signal transmission. Sulforaphane exhibits both anticancer and anti-inflammatory properties .
|
-
- HY-122144
-
|
Teroxirone
|
Endogenous Metabolite
|
Cancer
|
|
α-Triglycidyl isocyanurate (Teroxirone) is an antitumor compound with activity to inhibit DNA replication. α-Triglycidyl isocyanurate exerts its anticancer effect by alkylating and cross-linking DNA. α-Triglycidyl isocyanurate is relatively stable in fresh human plasma and whole blood, showing good biocompatibility. The metabolism of α-Triglycidyl isocyanurate mainly occurs in rat liver and is metabolized through an NADPH-independent pathway. The cytotoxicity of α-Triglycidyl isocyanurate can be partially restored under specific conditions, suggesting the complexity of its metabolic pathway .
|
-
- HY-14664
-
|
XU 62-320 free acid
|
HMG-CoA Reductase (HMGCR)
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
|
-
- HY-W012349
-
|
|
NF-κB
Fungal
Apoptosis
Autophagy
|
Infection
Cancer
|
|
2′-Hydroxychalcone is a hydroxyl derivative of chalcones with anticancer activities. 2'-Hydroxychalcone inhibits NF-κB pathway and induces autophagy and apoptosis in breast cancer cells . 2′-Hydroxychalcone shows a better antifungal activity against the complex Paracoccidioides spp .
|
-
- HY-N7459
-
|
|
AMPK
Autophagy
Fungal
|
Cancer
|
|
Sakurasosaponin is a saponin with potential anticancer activity that can be extracted from the root of Primula sieboldii. Sakurasosaponin can activate the AMPK pathway to induce cell autophagy and exert anti-NSCLC cell proliferation activity. Sakurasosaponin also has antifungal activity and significantly inhibits the growth of anthrax.
|
-
- HY-118375
-
|
ISC-4
|
Apoptosis
|
Cancer
|
|
Phenylbutyl isoselenocyanate (ISC-4) is a selective apoptosis inducer that increases reactive oxygen species levels to inhibit androgen receptor (AR) and activate p53 pathway. Phenylbutyl isoselenocyanate induces apoptosis in LNCaP prostate cancer cells and has anti-prostate cancer properties.
|
-
- HY-B0444R
-
|
|
Autophagy
Apoptosis
ERK
|
Neurological Disease
Cancer
|
|
Maprotiline (hydrochloride) (Standard) is the analytical standard of Maprotiline (hydrochloride). Maprotiline (hydrochloride) (Standard) is a highly selective noradrenergic reuptake inhibitor that has strong antidepressant, antitumor and neuropathic pain-relieving effects. Maprotiline (hydrochloride) (Standard) induces cancer cell apoptosis by targeting the ERK signaling pathway and CRABP1 .
|
-
- HY-19356A
-
|
|
Eukaryotic Initiation Factor (eIF)
Apoptosis
|
Cancer
|
|
Didesmethylrocaglamide, a derivative of Rocaglamide, is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. Didesmethylrocaglamide has potent growth-inhibitory activity with an IC50 of 5 nM. Didesmethylrocaglamide suppresses multiple growth-promoting signaling pathways and induces apoptosis in tumor cells. Antitumor activity .
|
-
- HY-159144
-
|
|
NF-κB
STAT
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 91 (Compound 4o) is an anti-inflammatory agent that can reduce inflammatory cytokines by inhibiting the STAT3 and NF-κB signaling pathways. Anti-inflammatory agent 91 can be used in research to improve skin inflammation associated with psoriasis .
|
-
- HY-138877A
-
|
|
Phosphatase
|
Cancer
|
|
Phosphoglycolic acid (lithium) is a competitive inhibitor of phosphoglycerate mutase (PGAM)-B, an enzyme of the glycolytic pathway. Phosphoglycolic acid increases basal and fMLF-induced levels of G6P in intact neutrophils. Phosphoglycolic acid thereby increases upstream intermediates in neutrophils, thereby amplifying the respiratory oxidative burst .
|
-
- HY-W012980
-
|
|
Endogenous Metabolite
AMPK
PKA
|
Metabolic Disease
|
|
Isovaleric acid is an oral active short-chain fatty acid that inhibits osteoclast differentiation by stimulating AMPK phosphorylation and promotes colonic smooth muscle relaxation by activating the cAMP/PKA pathway. Isovaleric acid can be used in research on skeletal diseases (such as osteoporosis) and intestinal disorders .
|
-
- HY-14828
-
|
SMP-986
|
mAChR
|
Metabolic Disease
|
|
Afacifenacin (SMP-986) is a potent and orally active muscarinic receptor antagonist. Afacifenacin inhibits the bladder afferent pathway through the sodium-channel blockade, increasing volume, and reducing the frequency of urination and incontinence. Afacifenacin has the potential for the research of overactive bladder (OAB) .
|
-
- HY-126771
-
|
Chr-A
|
Antibiotic
Bacterial
Akt
GSK-3
β-catenin
c-Myc
|
Infection
Cancer
|
|
Chrysomycin A (Chr-A), an antibiotic, can be obtained from Streptomyces. Chrysomycin A exhibits antitumor and anti-tuberculous and MRSA activities. As for glioblastoma, Chrysomycin A inhibits the proliferation, migration, and invasion of cancer cells through the Akt/GSK-3β/β-catenin signaling pathway .
|
-
- HY-19528
-
|
SAH (S-Adenosylhomocysteine)
|
Endogenous Metabolite
|
Metabolic Disease
|
|
SAH (S-Adenosylhomocysteine) is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine . SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 µM .
|
-
- HY-146195
-
-
- HY-N0253
-
|
Kalopanaxsaponin B
|
Bacterial
p38 MAPK
NF-κB
Apoptosis
|
Infection
Inflammation/Immunology
|
|
Hederacoside C (Kalopanaxsaponin B) is an ingredient that can be obtained mainly from ivy leaves. Hederacoside C mediates inflammation by inhibiting activation of MAPK/NF-κB and its downstream signaling pathway. Hederacoside C has anti-inflammatory and antibacterial activity .
|
-
- HY-116794
-
|
2,2-Diphenylethyl isothiocyanate
|
Apoptosis
JNK
MDM-2/p53
Caspase
|
Cancer
|
|
SF5 (2,2-Diphenylethyl isothiocyanate) is a sulforaphane analog. SF5 inhibits apoptosis by the JNK-p53-caspase pathway. SF5 can be used as a new renal protective agent for drug-resistant acute renal disease .
|
-
- HY-N2573A
-
|
L-Corydalmine hydrochloride; TLZ-16-CL
|
Fungal
CXCR
|
Infection
Neurological Disease
|
|
Corydalmine hydrochloride inhibits spore germination of some plant pathogenic as well as saprophytic fungi . Corydalmine hydrochloride acts as an oral analgesic agent, exhibiting potent analgesic activity . Corydalmine hydrochloride alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway .
|
-
- HY-N15415
-
|
|
PPAR
Reactive Oxygen Species
NF-κB
|
Inflammation/Immunology
|
|
Zaluzanin C is a sesquiterpene lactone. Zaluzanin C has anti-inflammatory activity and can inhibit the production of mtROS, block the NF-κB signaling pathway, and reduce the production of TNF-α. In addition, Zaluzanin C can inhibit the differentiation of 3T3-L1 preadipocytes into mature adipocytes .
|
-
- HY-19543
-
|
NSC 172924
|
Keap1-Nrf2
Apoptosis
|
Cancer
|
|
Brusatol (NSC?172924) is a unique inhibitor of the Nrf2 pathway that sensitizes a broad spectrum of cancer cells to Cisplatin and other chemotherapeutic agents. Brusatol enhances the efficacy of chemotherapy by inhibiting the Nrf2-mediated defense mechanism. Brusatol can be developed into an adjuvant chemotherapeutic agent . Brusatol increases cellular apoptosis .
|
-
- HY-116364
-
|
3'-Azido-3'-deoxythymidine-5'-triphosphate
|
HIV
DNA/RNA Synthesis
HBV
Reactive Oxygen Species
Apoptosis
|
Infection
|
|
AZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate also inhibits the DNA polymerase of HBV. AZT triphosphate activates the mitochondria-mediated apoptosis pathway .
|
-
- HY-121893
-
|
|
MDM-2/p53
NF-κB
|
Cancer
|
|
p53-MDM2-IN-3 (Compound 5s) is an orally active p53-MDM2 inhibitor with a Ki value of 0.25 μM. p53-MDM2-IN-3 exerts antitumor activity by inhibiting NF-κB pathway .
|
-
- HY-162520
-
|
|
Wnt
|
Cancer
|
|
DJ-1-IN-1 (compound 797780-71-3) is a DJ-1 inhibitor. DJ-1-IN-1 exhibits antiproliferative activity in ACHN cells with an IC50 value of 12.18 μM and can inhibit the Wnt signaling pathway. DJ-1-IN-1 can be used in cancer research .
|
-
- HY-161768
-
|
|
CDK
Apoptosis
|
Cancer
|
|
VCC972839:01 is an inhibitor for cyclin dependent kinase (CDK9), with IC50 of 7 nM. VCC972839:01 inhibits the cell viability of SCLC cells in nanomolar levels. VCC972839:01 induces apoptosis through an intrinsic pathway. VCC972839:01 exhibits antitumor activity in mouse model .
|
-
- HY-N0911
-
|
|
NF-κB
Apoptosis
p38 MAPK
|
Neurological Disease
|
|
Rehmannioside A is a neuroprotective agent that can be isolated from Rehmanniae radix. Rehmannioside A can inhibit the release of proinflammatory mediators from microglia and promote M2 polarization in vitro, thereby protecting co-cultured neurons from apoptosis by inhibiting NF-κB and MAPK signaling pathways. Rehmannioside A can be used in spinal cord injury research .
|
-
- HY-119966
-
|
|
Wnt
β-catenin
|
Cancer
|
|
CCT036477 is a Wnt/β-catenin pathway inhibitor. CCT036477 blocks transcription at β-catenin without altering its levels. CCT036477 inhibits proliferation of various cancer cells, development of embryos, and expression of Wnt target genes (PPARδ, Cyclin D1, TCF4, and ID2) .
|
-
- HY-158818
-
|
|
Parasite
|
Infection
|
|
DXR-IN-2 is a 1-deoxy-D-xylulose-5-phosphate reductoisomerase (DXR) inhibitor and an antimalarial agent (IC50: 0.1062 μM for Plasmodium falciparum DXR and 0.369 μM for Plasmodium falciparum). DXR-IN-2 inhibits Plasmodium falciparum growth by suppressing the methyl erythritol phosphate (MEP) pathway via DXR .
|
-
- HY-154960
-
|
|
Akt
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin/AKT1-IN-1 (Compound D1-1) is an inhibitor of tubulin polymerization and AKT pathway activation. Tubulin/AKT1-IN-1 significantly inhibits the proliferation and metastasis of H1975 cells and slightly induced their apoptosis and can be used for non-small-cell lung cancer (NSCLC) research .
|
-
- HY-116052
-
|
|
MDM-2/p53
NF-κB
|
Cancer
|
|
p53-MDM2-IN-2 (Compound 5q) is an orally active p53-MDM2 inhibitor with a Ki value of 0.25 μM. p53-MDM2-IN-2 exerts antitumor activity by inhibiting NF-κB pathway .
|
-
- HY-123940
-
|
|
AAK1
|
Cancer
|
|
SGC-AAK1-1 is a potent and selective AAK1 (AP2 associated kinase 1) inhibitor with an IC50 of 270 nM and a Ki of 9 nM. SGC-AAK1-1 also potently inhibits BMP2K. SGC-AAK1-1 is used to study Wnt pathway related to AAK1 .
|
-
- HY-143235
-
|
|
Epigenetic Reader Domain
Apoptosis
Bcl-2 Family
Caspase
c-Myc
|
Cancer
|
|
BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research .
|
-
- HY-12875
-
|
|
Ras
|
Cancer
|
|
BQU57 is a selective inhibitor of RalA/RalB small GTPases, with a binding potency (Kb) of 7.7 μM for RalB-GDP. BQU57 can block its interaction with effector proteins (such as SEC5 and EXO84), inhibiting tumor cell migration, invasion and non-adherent growth. BQU57 downregulates the NF-κB signaling pathway, reduces the expression of IL-6, IL-8 and MMP-13, and inhibits apoptosis by regulating the Bcl-2/Bax balance. BQU57 also protects the extracellular matrix by inhibiting the Ral/NF-κB pathway and can be used for the study of degenerative diseases. BQU57 exhibits significant antitumor activity in triple-negative breast cancer (TNBC) models, inhibiting orthotopic tumor growth and lung metastasis and enhancing paclitaxel chemotherapy sensitivity .
|
-
- HY-N8884
-
|
|
PTEN
Akt
NF-κB
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
Coelonin is a dihydrophenanthrene with anti-inflammation activity. Coelonin inhibits LPS-induced PTEN phosphorylation. Coelonin inhibits NF-κB activation and p27Kip1 degradation by regulating the PI3K/AKT pathway negatively. Coelonin can inhibit IκBα phosphorylation and degradation and increases the expression of IκBα protein .
|
-
- HY-B0093
-
|
CGS14824A free base
|
Angiotensin-converting Enzyme (ACE)
Apoptosis
Reactive Oxygen Species
|
Cardiovascular Disease
Cancer
|
|
Benazepril (CGS14824A free base) is an orally active angiotensin-converting enzyme (ACE) inhibitor to reduce angiotensin-II production. Benazepril inhibits oxidative stress and inhibits apoptosis by the PI3K/Akt signaling pathway. Benazepril improves diabetic nephropathy and decreases proteinuria. Benazepril can be used in the study of hypertension, heart failure and diabetic nephropathy .
|
-
- HY-169407
-
|
|
Akt
mTOR
MEK
ERK
Apoptosis
|
Cancer
|
|
KT-IN-24 (Compound M17) is a AKT allosteric inhibitor with anti-tumor activity. KT-IN-24 can target the AKT/mTOR and MEK/ERK signaling pathways and inhibit epithelial-mesenchymal transition, which has a synergistic suppressive effect on TNBC, promoting cell apoptosis while inhibiting proliferation and migration when used in combination with Trametinib (HY-10999) .
|
-
- HY-128033
-
|
|
Fungal
|
Infection
|
|
Fenpropimorph is a fungicide that inhibits the sterol pathway. Fenpropimorph inhibits δ8-δ7-sterol isomerase in yeast at low concentrations, with δ14-sterol reductase being blocked at higher levels, preventing the biosynthesis of ergosterol. Fenpropimorph also inhibits sterol synthesis in certain plants and mammalian cells .
|
-
- HY-144321
-
|
|
Trk Receptor
|
Cancer
|
|
Trk-IN-9 (Compound 12) is a potent inhibitor of TRK. Trk-IN-9 inhibits the proliferation of Km-12 cell lines. Trk-IN-9 induces the apoptosis of Km-12 cells in a concentration-dependent manner. Trk-IN-9 inhibits the phosphorylation of TRK to block downstream pathways. Trk-IN-9 has the potential for the research of NTRK-fusion cancers .
|
-
- HY-17514
-
|
R51211
|
Fungal
Hedgehog
Cytochrome P450
Autophagy
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor .
|
-
- HY-B0093A
-
-
- HY-13645
-
|
|
VEGFR
c-Kit
PDGFR
|
Cancer
|
|
Henatinib is an orally active small-molecule multikinase inhibitor that has demonstrated broad and potent antitumor activities. Henatinib inhibits the activity of VEGFR-2, c-kit, PDGFR with IC50 values of 0.6 nM, 3.3 nM and 41.5 nM, respectively. Henatinib significantly inhibits VEGFR-2 phosphorylation and its downstream signal pathway in human umbilical vein endothelial cells (HUVECs) .
|
-
- HY-N3426
-
|
|
NO Synthase
Akt
AMPK
|
Metabolic Disease
|
|
Kazinol B, a prenylated flavan with a dimethyl pyrane ring, is an inhibitor of nitric oxide (NO) production. Kazinol B improves insulin sensitivity by enhancing glucose uptake via the insulin-Akt signaling pathway and AMPK activation. Kazinol B has the potential for diabetes mellitus research .
|
-
- HY-129529
-
|
|
Others
|
Inflammation/Immunology
|
|
6-Hydroxyluteolin 7-glucoside is a flavonoid from Tanacetum parthenium and T. vulgare. 6-Hydroxyluteolin 7-glucoside inhibits the major pathways of arachidonate metabolism in leukocytes. 6-Hydroxyluteolin 7-glucoside has anti-inflammatory effect .
|
-
- HY-162228
-
|
|
COX
Phospholipase
|
Inflammation/Immunology
|
|
VI-60 is a dual, orally active inhibitor of cPLA2 and COX-2, which reveals an anti-inflammtory efficacy through the inhibition of p38 MAPK/cPLA2/COX-2/PGE2 pathway .
|
-
- HY-145686
-
|
|
Wnt
Nuclear Factor of activated T Cells (NFAT)
|
Inflammation/Immunology
|
|
AV023 is a potent inhibitor of ANKRD22. AV023 promotes the expansion of gastrointestinal mucosal epithelial stem cells and indirectly activates the Wnt classical pathway, which helps the recovery of damaged gastrointestinal mucosal tissues in the body (extracted from patent CN111205231B) .
|
-
- HY-N3354
-
|
8-prenylgenistein
|
Apoptosis
|
Cancer
|
|
Lupiwighteone is an isoflavone present widely in wild-growing plants, with antioxidant, antimicrobial and anticancer effects. Lupiwighteone induces caspase-dependent and -independent apoptosis on human breast cancer cells via inhibiting PI3K/Akt/mTOR pathway .
|
-
- HY-119683R
-
|
|
Fungal
|
Infection
|
|
Epoxiconazole (Standard) is the analytical standard of Epoxiconazole. This product is intended for research and analytical applications. Epoxiconazole, a fungicide, is a demethylation inhibitor of the Ergosterol biosynthesis pathway. Epoxiconazole exhibits strong inhibitory effects on both carbendazim-resistant and phenamacril-resistant isolates, and can be used for controlling many crop diseases .
|
-
- HY-146549
-
|
|
Bacterial
|
Infection
|
|
RmlA-IN-1 (Compound 8a) is a potent inhibitor of glucose-1-phosphate thymidylyltransferase (RmlA) with an IC50 of 0.073 μM. RmlA-IN-1 influences monosaccharide l-Rhamnose biosynthetic pathway. RmlA-IN-1 affects bacterial cell wall permeability .
|
-
- HY-157211
-
|
|
NF-κB
p38 MAPK
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 66 (compound 8) is a pterostilbene derivative with anti-inflammatory activity. Anti-inflammatory agent 66 inhibits pro-inflammatory cytokines by blocking the LPS-induced NF-κB/MAPK signaling pathway and effectively alleviates DSS-induced acute colitis in mice .
|
-
- HY-13991
-
|
|
Ras
Apoptosis
|
Cancer
|
|
CCG-1423 is an inhibitor of Rho/MRTF/SRF pathway. CCG-1423 shows activities in several cancer cells. CCG-1423 is a promising lead compound for the development of novel pharmacologic tools, and it can be used for the research of cancer and diabetes .
|
-
- HY-W762011
-
-
- HY-119683S1
-
|
|
Isotope-Labeled Compounds
Fungal
|
Infection
|
|
Epoxiconazole-d4 is the deuterium labeled Epoxiconazole (HY-119683). Epoxiconazole, a fungicide, is a demethylation inhibitor of the Ergosterol biosynthesis pathway. Epoxiconazole exhibits strong inhibitory effects on both carbendazim-resistant and phenamacril-resistant isolates, and can be used for controlling many crop diseases .
|
-
- HY-135825
-
|
|
Autophagy
|
Neurological Disease
|
|
TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment .
|
-
- HY-169126
-
|
|
β-catenin
Wnt
|
Cancer
|
|
β-catenin modulator IIa-661 is a β-catenin modulator that modulates β-catenin activity and inhibits the activity of the Wnt/wingless (wg) signaling pathway. β-catenin modulator IIa-661 can be utilized in cancer research .
|
-
- HY-163475
-
|
|
CXCR
|
Cancer
|
|
CXCL-CXCR1/2-IN-1 is an orally active ELR +CXCL-CXCR1/2 pathway inhibitor with an EC50 of 42.7 nM for CXCR2 . CXCL-CXCR1/2-IN-1 shows anticancer and antiangiogenic effects .
|
-
- HY-149972
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-96 (Compound D34) is a potent MRE11 inhibitor. Antitumor agent-96 down-regulates the HR pathway by binding with MRE11 and suppressing its endonuclease functions. Antitumor agent-96 induces CM cells apoptosis .
|
-
- HY-N6636
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Valencene is a sesquiterpene isolated from Cyperus rotundus, possesses antiallergic, antimelanogenesis, anti-infammatory, and antioxidant activitivies. Valencene inhibits the exaggerated expression of Th2 chemokines and proinflammatory chemokines through blockade of the NF-κB pathway. Valencene is used to flavor foods and drinks .
|
-
- HY-P10072
-
|
Hsp25 kinase inhibitor; Mk2 pseudosubstrate
|
ERK
JNK
p38 MAPK
HSP
MAPKAPK2 (MK2)
|
Others
|
|
MK2-IN-5 is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 targets the protein interaction domain in the MAPK pathway. MK2-IN-5 inhibits HSP25 and HSP27 phosphorylation .
|
-
- HY-16126R
-
|
|
Calcium Channel
|
Inflammation/Immunology
Cancer
|
|
Carboxyamidotriazole (Standard) is the analytical standard of Carboxyamidotriazole. This product is intended for research and analytical applications. Carboxyamidotriazole (L-651582) is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole shows anti-tumor, anti-inflammatory and antiangiogenic effects .
|
-
- HY-162170
-
|
|
NF-κB
Keap1-Nrf2
p38 MAPK
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 72 (compound 5) is a novel resveratrol derivative hybrid with benzoylhydrazine. Anti-inflammatory agent 72 shows anti-inflammatory and antioxidant activities by activating Nrf2 and inhibiting NF-κB p65/iNOS and MAPKs signaling pathways .
|
-
- HY-P10399
-
|
Mouse KGYY15; KGYY15 peptide
|
TNF Receptor
|
Metabolic Disease
|
|
KGYY15 (Mouse KGYY15) is a CD40 targeting peptide, which weakly inhibits the CD40-CD40L interaction with IC50 of more than 1mM. KGYY15 activates 33% NF-κB pathway at 100 μM .
|
-
- HY-N0822
-
|
C.I. 75535; Isoarnebin 4
|
Chloride Channel
Pyruvate Kinase
NF-κB
TNF Receptor
HIV
AIM2
|
Cancer
|
|
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM . Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway . Shikonin decreases exosome secretion through the inhibition of glycolysis . Shikonin inhibits AIM2 inflammasome activation .
|
-
- HY-B0185A
-
|
Lignocaine hydrochloride
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence . Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor .
|
-
- HY-138281
-
|
|
Complement System
|
Inflammation/Immunology
|
|
Complement factor D-IN-2 is an inhibitor of complement factor D extracted from patent WO2015130838A1, compound 190. Complement factor D-IN-2 targets factor D and inhibits the complement cascade at an early and essential point in the alternative complement pathway. Complement factor D-IN-2 can be used for the research of autoimmune diseases .
|
-
- HY-155122
-
|
|
PARP
|
Cancer
|
|
PARP-1-IN-13 (Compound 19c) is a PARP-1 inhibitor (IC50: 26 nM). PARP-1-IN-13 inhibits DNA single-strand breakage repair and aggravates DNA double-strand breakage. PARP-1-IN-13 promotes the apoptosis of cancer cells through the mitochondrial apoptosis pathway .
|
-
- HY-164372
-
|
17-DR
|
HSP
Apoptosis
|
Cancer
|
|
17-Demethoxy-reblastatin (17-DR) is an inhibitor for heat shock protein 90 (Hsp90), with an IC50 of 1.82 μM for yeast Hsp90 ATPase. 17-Demethoxy-reblastatin inhibits the proliferation of cancer cell HepG2 and SMMC7721, reduces the colony formation, and induces apoptosis through mitochondria and caspase mediated pathway .
|
-
- HY-103381
-
|
|
CDK
GSK-3
|
Cancer
|
|
NSC693868 is a selective inhibitor of CDK1 and CDK5 with IC50s of 600 nM and 400 nM, respectively. NSC693868 less potently inhibits GSK3β with an IC50 of 1 µM) and does not block CDC25 activity. NSC693868 is used to help define the roles of CDK1 and CDK5 in various signaling pathways .
|
-
- HY-N0158R
-
|
|
TGF-beta/Smad
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Oxymatrine (Standard) is the analytical standard of Oxymatrine. This product is intended for research and analytical applications. Oxymatrine, an alkaloid from Sophora flavescens Alt. with anti-inflammatory, antifibrosis, and antitumor effects, inhibits the iNOS expression and TGF-β/Smad pathway. Oxymatrine inhibits bocavirus minute virus of canines (MVC) replication, reduces viral gene expression and decreases apoptosis induced by viral infection.
|
-
- HY-118160
-
|
NSC 73233
|
NO Synthase
|
Inflammation/Immunology
Cancer
|
|
PPM-18 (NSC 73233), a potent anti-inflammatory agent, inhibits nitric oxide synthase expression. PPM-18 is a potent inhibitor of iNOS expression by blocking the binding of NF-κB to promoter . PPM-18, an analog of Vitamin K, induces autophagy and apoptosis in bladder cancer cells through ROS and AMPK signaling pathways .
|
-
- HY-Y0889A
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
1-(2,3-Dichlorphenyl)piperazine hydrochloride is a potent DHCR7 inhibitor with the activity of inhibiting cholesterol biosynthesis. 1-(2,3-Dichlorphenyl)piperazine hydrochloride is often used in biological research to evaluate the function of cholesterol biosynthesis pathway. The application of 1-(2,3-Dichlorphenyl)piperazine hydrochloride is of great significance for understanding diseases related to cholesterol biosynthesis .
|
-
- HY-157570
-
|
|
PROTACs
STING
|
Infection
|
|
Anti-inflammatory agent 70 (N-Me-SP23) is a STING protein PROTAC degrader and inhibits the STING signaling pathway. Anti-inflammatory agent 70 has anti-inflammatory activity. (Pink: STING inhibitor (HY-47709); Black: linker (HY-W008296); Blue: CRBN Ligand (HY-W460193)) .
|
-
- HY-N15380
-
|
|
PARP
Reactive Oxygen Species
Caspase
Apoptosis
Pyroptosis
|
Cancer
|
|
4,4′-Secalonic acid D (Compound 12) is a PARP1 inhibitor. 4,4′-Secalonic acid D induces the accumulation of ROS and DNA damage, activates the caspase-3/GSDME pathway, and triggers apoptosis and pyroptosis of tumor cells by inhibiting PARP1. 4,4′-Secalonic acid D has anti-tumor activity .
|
-
- HY-170936
-
|
|
FAK
Hippo (MST)
YAP
|
Cancer
|
|
MY-1576 is a FAK inhibitor with an IC50 of 8 nM. MY-1576 can activate the Hippo pathway, thereby blocking the regulation of YAP/TAZ. MY-1576 also effectively inhibits tumor growth in the KYSE30 xenograft mouse model, demonstrating good safety, and effectively downregulates the autophosphorylation of FAK and the levels of YAP/TAZ in vivo .
|
-
- HY-B0004
-
|
|
Adenosine Receptor
Phosphodiesterase (PDE)
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Doxofylline is an orally active PDE IV inhibitor and A1AR antagonist. Doxofylline reduces inflammation in epithelial cells via inhibiting mitochondrial ROS production and amelioration of multiple cellular pathways (NLRP3-TXNIP inflammasome activation). Doxophylline can be used in studies of asthma, chronic obstructive pulmonary disease, and bronchospasm .
|
-
- HY-N4107
-
|
|
TGF-beta/Smad
|
Infection
Inflammation/Immunology
Cancer
|
|
Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .
|
-
- HY-Y0889
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
1-(2,3-Dichlorphenyl)piperazine is a potent DHCR7 inhibitor with the activity of inhibiting cholesterol biosynthesis. 1-(2,3-Dichlorphenyl)piperazine is often used in biological research to evaluate the function of cholesterol biosynthesis pathway. The application of 1-(2,3-Dichlorphenyl)piperazine is of great significance for understanding diseases related to cholesterol biosynthesis .
|
-
- HY-142026
-
|
(+)-Vitisin A
|
NF-κB
ERK
|
Inflammation/Immunology
|
|
Vitisin A has antioxidative, anticancer, antiapoptotic, neuroprotective and anti-inflammatory effects. Vitisin A inhibits LPS-induced NO and iNOS production via down-regulation of ERK1/2 and p38 and the NF-κB signal pathway. Vitisin A also inhibits adipocyte differentiation. Vitisin A is a resveratrol tetramer that can be isolated from Vitis vinifera roots .
|
-
- HY-125817
-
|
|
Ras
p38 MAPK
|
Cancer
|
|
BI-3406 (compound I-6) is an orally active, highly potent and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with an IC50 of 6 nM. BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 has anticancer activity .
|
-
- HY-N2573
-
|
L-Corydalmine; TLZ-16
|
Fungal
CXCR
|
Infection
Neurological Disease
|
|
Corydalmine (L-Corydalmine) inhibits spore germination of some plant pathogenic as well as saprophytic fungi . Corydalmine acts as an oral analgesic agent, exhibiting potent analgesic activity . Corydalmine alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway .
|
-
- HY-N0177R
-
|
|
STAT
MicroRNA
|
Metabolic Disease
|
|
Diosgenin (Standard) is the analytical standard of Diosgenin. This product is intended for research and analytical applications. Diosgenin, a steroidal saponin, can inhibit STAT3 signaling pathway . Diosgenin is an exogenous activator of Pdia3/ERp57 . Diosgenin inhibits aortic atherosclerosis progression by suppressing macrophage miR-19b expression .
|
-
- HY-164462
-
|
|
PKC
NF-κB
Apoptosis
|
Cancer
|
|
BHA536 is an orally active selective inhibitor for PKCα/β and NF-kB signaling pathway. BHA536 inhibits the proliferation of CD79-mutated ABC DLBCL cell, arrests cell cycle at G1 phase, and induces apoptosis in TMD8 cell. BHA536 exhibits antitumor efficacy in mice .
|
-
- HY-171242
-
|
|
JAK
STAT
|
Others
|
|
LNK01004 is a JAK inhibitor with strong inhibitory effects on JAK1 (IC50: 10 nM), JAK2 (IC50:＜0.51 nM) and TYK2 (IC50: 1.0 nM) . LNK01004 can simultaneously inhibit multiple cytokine-induced p-STAT signaling pathways. LNK01004 can be used in the research of diseases such as atopic dermatitis .
|
-
- HY-108361
-
|
|
Ras
|
Inflammation/Immunology
Cancer
|
|
CCG-203971 is a second-generation Rho/MRTF/SRF pathway inhibitor. CCG-203971 potently targets RhoA/C-activated SRE-luciferase (IC50 =6.4 μM). CCG-203971 inhibits PC-3 cell migration with an IC50 of 4.2 μM. Potential anti-metastasis Agent .
|
-
- HY-P10719
-
|
|
MyD88
|
Infection
Inflammation/Immunology
|
|
Pepinh-MYD is a MyD88 inhibitor that contains a domain sequence from MyD88 TIR and a protein transduction sequence, enabling it to penetrate the cell membrane. Pepinh-MYD interferes with MyD88-mediated TLR signaling pathways, thereby inhibiting related immune responses. It holds potential for studying the role of MyD88 in viral infections .
|
-
- HY-15959
-
|
Volitinib; HMPL-504; AZD-6094
|
c-Met/HGFR
|
Cancer
|
|
Savolitinib (AZD-6094) is a potent, highly selective, and orally bioavailable c-Met inhibitor with IC50 s of 5 nM and 3 nM for c-Met and p-Met, respectively. Savolitinib (AZD-6094) selectively binds to and inhibits the activation of c-Met in an ATP-competitive manner, and disrupts c-Met signal transduction pathways. Antineoplastic activity .
|
-
- HY-149513
-
|
|
c-Myc
Apoptosis
|
Cancer
|
|
EP12 is a c-Myc inhibitor. EP12 is a c-Myc G4 stabilizer. EP12 induces apoptosis and DNA damage in multiple myeloma cells. EP12 disrupts the nuclear translocation of P65/P50 by interfering with the NF-κB signaling pathway. EP12 inhibits multiple myeloma growth .
|
-
- HY-P1111
-
|
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders .
|
-
- HY-P1111A
-
|
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor TFA can be used for study of asthma, allergic, and other eosinophilic disorders .
|
-
- HY-16343
-
|
|
COX
|
Metabolic Disease
|
|
NB-598 is a potent and competitive inhibitor of squalene epoxidase (SE), and suppresses triglyceride biosynthesis through the farnesol pathway. NB-598 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-158126
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
G-quadruplex ligand 2 (compound A3) is a triphenylamine-based ligand that targets mitochondrial DNA G4s. G-quadruplex ligand 2 activates the cGAS-STING pathway. G-quadruplex ligand 2 inhibits tumor growth and metastasis via regulation of TME .
|
-
- HY-136541
-
YB-0158
2 Publications Verification
Wnt Pathway inhibitor 2
|
Wnt
Apoptosis
|
Cancer
|
|
YB-0158 (Wnt pathway inhibitor 2) is a reverse-turn peptidomimetic and a potent colorectal cancer stem cell (CSC) targeting agent. YB-0158 disrupts Sam68-Src interactions and induces apoptosis in CRC cells. Anti-cancer activities .
|
-
- HY-161351
-
|
|
Akt
STAT
Apoptosis
|
Cancer
|
|
STAT3/AKT-IN-1 is a dual inhibitor for the signal transducer and activator of transcription 3 (STAT3) and protein kinase B (AKT) signalling pathway, exhibits antitumor activity against gastric cancer and induces cell apoptosis in SGC-7901 cells .
|
-
- HY-161180
-
|
|
NAMPT
|
Cancer
|
|
Antitumor Agent-136 (Compound 17) is a potent broad-spectrum antitumor agent and a NAMPT inhibitor with an IC50 of 9.5 nM. Antitumor Agent-136 can reduce the levels of intracellular and extracellular NAMPT protein through the ubiquitin proteasome pathway, thus achieving tumor inhibition .
|
-
- HY-126066
-
|
|
Drug Isomer
NO Synthase
NF-κB
|
Cancer
|
|
(-)-Syringaresinol, is the isoform of Syringaresinol (HY-N8307), which can be found in stems of Annona Montana, possesses anti-cancer activity. Syringaresinol is an activator of NO synthase phosphorylation and induces vasodilation. Syringaresinol also inhibits the NF-κB pathway and exerts anti-inflammatory activity .
|
-
- HY-123422
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
|
|
GSK360A is a potent and orally active HIF-PHD inhibitor with IC50 values of 10, 100, and 126 nM for PHD1, PHD2, and PHD3, respectively. GSK360A activates the HIF-1 alpha pathway and protect the failing heart after myocardial infarction (MI) .
|
-
- HY-P10718
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
IMG-2005 is a TLR signaling pathway inhibitor. IMG-2005 mimics the Toll/interleukin-1 receptor (TIR) domain of MyD88, thereby preventing its homodimerization, which causes damage to tracheal epithelial cells and triggers pulmonary immune diseases .
|
-
- HY-16343C
-
|
|
COX
|
Metabolic Disease
|
|
NB-598 Maleate is a potent and competitive inhibitor of squalene epoxidase (SE), and suppresses triglyceride biosynthesis through the farnesol pathway. NB-598 (Maleate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-15415
-
|
|
Na+/Ca2+ Exchanger
Autophagy
|
Cancer
|
|
KB-R7943 mesylate is a widely used inhibitor of the reverse Na +/Ca 2+ exchanger (NCXrev) with IC50 of 5.7±2.1 μM. KB-R7943 mesylate induces cancer cell death via activating the JNK pathway and blocking autophagic flux.
|
-
- HY-16343A
-
|
|
Others
|
Metabolic Disease
|
|
NB-598 hydrochloride is a potent and competitive inhibitor of squalene epoxidase (SE), and suppresses triglyceride biosynthesis through the farnesol pathway. NB-598 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-B1029
-
Danazol
4 Publications Verification
|
PKC
Apoptosis
Tyrosinase
|
Endocrinology
Cancer
|
|
Danazol inhibits the proliferation of cancer cell MDA-MB-231 and MCF-7 with IC50 of 65 µg/mL and 31 µg/mL. Danazol arrests the cell cycle at G1 phase, induces apoptosis in MDA-MB-231 through PKCα signaling pathway .
|
-
- HY-W015883
-
-
- HY-119767
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
Jolkinolide A is a diterpenoid, can be extracted from the roots of Euphorbia fischeriana Steud. Jolkinolide A exhibits anti-tumor activity, by affecting on angiogenesis of tumor tissues. Jolkinolide A significantly inhibits the Akt-STAT3-mTOR signaling pathway and reduces the expression of VEGF in A549 cells .
|
-
- HY-161146
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-100 (compound 3f) is a EGFR inhibitor with IC50 range of 0.137-0.507 μM. EGFR-IN-100 has antiproliferative activity and induces the apoptosis pathway. EGFR-IN-100 arrests the MCF-7 cell cycle at the S phase .
|
-
- HY-146551
-
|
|
Bacterial
|
Infection
|
|
RmlA-IN-2 (Compound 1d) is a potent inhibitor of glucose-1-phosphate thymidylyltransferase (RmlA) with an IC50 of 0.303 μM. RmlA-IN-2 influences monosaccharide l-Rhamnose biosynthetic pathway. RmlA-IN-2 affects bacterial cell wall permeability .
|
-
- HY-N0145
-
-
- HY-157990
-
|
|
Wnt
β-catenin
|
Cancer
|
|
Wnt/β-catenin-in-1 (compounds 17) is a Wnt/β-catenin signaling pathway inhibitor. Wnt/β-catenin-IN-1 can induce apoptosis of colon cancer cells, has broad-spectrum anticancer activity, and can be used for the reseach of a variety of solid tumors .
|
-
- HY-N0479
-
|
(-)-Licarin B
|
PPAR
GLUT
|
Metabolic Disease
|
|
Licarin B, a nitric oxide production inhibitor extracted from the component of the seeds of Myristica fragrans, improves insulin sensitivity via PPARγ and activation of GLUT4 in the IRS-1/PI3K/AKT pathway .
|
-
- HY-N1913A
-
|
Dan shen suan A sodium; Salvianic acid A sodium
|
Keap1-Nrf2
NF-κB
Reactive Oxygen Species
SARS-CoV
Apoptosis
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Danshensu (Dan shen suan A) sodium, an orally active phenolic compound, can induce Nrf2/HO-1 activation and inhibition of NF-κB pathway. Danshensu sodium reduces reactive oxygen species (ROS) production, upregulates antioxidant defense mechanism and inhibits intrinsic apoptotic pathway. Danshensu sodium displays a potent antiviral activity against SARS-CoV-2 with EC50 of 0.97 μM. Danshensu sodium has anti-oxidation, anti-apoptosis, anti-lung inflammatory and has the potential for COVID-19, cardiovascular and cerebrovascular diseases research .
|
-
- HY-N1913
-
|
Dan shen suan A; Salvianic acid A
|
Keap1-Nrf2
NF-κB
Reactive Oxygen Species
SARS-CoV
Apoptosis
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Danshensu (Dan shen suan A), an orally active phenolic compound, can induce Nrf2/HO-1 activation and inhibition of NF-κB pathway. Danshensu reduces reactive oxygen species (ROS) production, upregulates antioxidant defense mechanism and inhibits intrinsic apoptotic pathway. Danshensu displays a potent antiviral activity against SARS-CoV-2 with EC50 of 0.97 μM. Danshensu has anti-oxidation, anti-apoptosis, anti-lung inflammatory and has the potential for COVID-19, cardiovascular and cerebrovascular diseases research .
|
-
- HY-125542
-
|
|
Apoptosis
PI3K
Akt
|
Cancer
|
|
DCZ3301 is a potent aryl-guanidino inhibitor. DCZ3301 inhibits cell proliferation, induces G2/M cell cycle arrest and apoptosis. DCZ3301 inhibits the activation of the PI3K/AKT pathway by downregulating the protein expression of PI3K and phosphorylation of AKT. DCZ3301 can be used in research of cancer .
|
-
- HY-162382
-
|
|
PI3K
Akt
mTOR
|
Cancer
|
|
KTC1101 is an orally active pan-PI3K inhibitor. KTC1101 can inhibit the PI3K signaling pathway, reduce downstream AKT and mTOR phosphorylation, and reduces the expression of Ki67. The anti-tumor effect of KTC1101 has a dual mechanism of action: directly inhibiting tumor cell growth and dynamically enhancing immune response .
|
-
- HY-170540
-
-
- HY-114454
-
INH14
3 Publications Verification
|
IKK
|
Inflammation/Immunology
Cancer
|
|
INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity .
|
-
- HY-170484
-
|
|
MAP3K
p38 MAPK
|
Neurological Disease
|
|
KAI-11101 is the inhibitor for dual leucine zipper kinase (DLK, MAP3K12) with a Ki of 0.7 nM. KAI-11101 inhibits Paclitaxel (HY-B0015)-induced cJun phosphorylation (IC50=95 nM) and thus inhibits the activation of MAPK pathway. KAI-11101 is blood brain barrier penetrable and can be further investigated for its neuroprotective property .
|
-
- HY-111158
-
|
|
c-Met/HGFR
|
Cancer
|
|
BMS-748730 is an oral tyrosine kinase inhibitor. BMS-748730 inhibits tyrosine kinase activity by competing with the ATP binding site of the tyrosine kinase, which prevents the kinase from phosphorylating the substrate protein, thereby inhibiting signaling pathways associated with cell proliferation and tumor growth. BMS-748730 can be used in the study of certain types of cancer, including chronic myeloid leukemia (CML) .
|
-
- HY-163548
-
|
|
Sialyltransferase
|
Cancer
|
|
SPP-002 is a sulfate analogue that acts as a potential Sialyltransferase (ST) inhibitor. SPP-002 selectively inhibits n-glycosialylation with inhibition at least an order of magnitude greater than that of unmodified parental cholic acid (LCA). SPP-002 reduces tumor cell migration and invasion by inhibiting the integrin /FAK/Paxillin signaling pathway. SPP-002 can be used in the study of tumor metastasis .
|
-
- HY-P1259
-
|
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
|
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
|
-
- HY-107572
-
|
CI 976
|
Acyltransferase
|
Metabolic Disease
|
|
PD 128042 (CI 976) is a potent, orally active, and selective inhibitor of ACAT (acyl coenzyme A:cholesterol acyltransferase) with an IC50s of 73 nM. PD 128042 is also a potent LPAT (lysophospholipid acyltransferase) inhibitor. PD 128042 inhibits Golgi-associated LPAT activity (IC50=15 μM). PD 128042 inhibits multiple membrane trafficking steps, including ones found in the endocytic and secretory pathway .
|
-
- HY-116184
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
PF-05387252 is a potent and selective IRAK4 inhibitor with the activity of inhibiting endogenous TLR signaling pathways. PF-05387252 has shown anti-inflammatory activity in experimental models and may have potential clinical application value in inhibiting psoriasis. Although PF-05387252 and its related compounds have shown anti-inflammatory effects in animal models, their efficacy in inhibiting psoriasis has not yet been verified .
|
-
- HY-128749A
-
|
Calcium D-glucarate tetrahydrate
|
Endogenous Metabolite
|
Cancer
|
|
D-Glucaric acid tetrahydrate is the end-products of the D-glucuronic acid pathway in mammals. D-Glucaric acid tetrahydrate is also found in fruits and vegetables. D-Glucaric acid tetrahydrate can be used to reduce cholesterol and inhibits tumor development. D-Glucaric acid tetrahydrate also enhances human immunity and reduce cancer risks .
|
-
- HY-123037
-
|
|
Fungal
|
Infection
|
|
Triadimefon is a triazole fungicide used to control powdery mildew, rusts, and other fungal pests on grains, fruit and vegetable crops, turf, shrubs, and trees. Triadimefon inhibits lanosterol 14α-demethylase, interfering with oxidative demethylation reactions in the ergosterol biosynthesis pathway of fungi, and also blocks gibberellin biosynthesis.
|
-
- HY-N6684R
-
|
|
P-glycoprotein
|
Metabolic Disease
|
|
Deoxynivalenol (Standard) is the analytical standard of Deoxynivalenol. This product is intended for research and analytical applications. Deoxynivalenol, an orally active mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors .
|
-
- HY-P2249
-
|
|
Arrestin
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
ELA-21 (human) is an apelin receptor agonist with a pKi of 8.52. ELA-21 (human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment with subnanomolar potencies. ELA-21 (human) is an agonist in G-protein-dependent and -independent pathways .
|
-
- HY-161144
-
|
|
Akt
Apoptosis
|
Cancer
|
|
AKT-IN-21 (compound C36) is a potent AKT inhibitor with broad-spectrum cytotoxicity and anticancer activity. AKT-IN-21 also blocks the cell cycle and induces apoptosis of cancer cells by down-regulating the PI3K/AKT pathway .
|
-
- HY-N3542
-
|
|
Glycosidase
|
Cancer
|
|
Carpachromene is a potent α-glucosidase enzyme inhibitor. Carpachromene ameliorates insulin resistance in HepG2 cells via modulating IR/IRS1/PI3k/Akt/GSK3/FoxO1 pathway .
|
-
- HY-N0404
-
|
|
p38 MAPK
AMPK
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Sinigrin is a major glucosinolate present in plants of the Brassicaceae family. Sinigrin inhibits early-stage adipogenesis of 3T3-L1 adipocytes through the AMPK and MAPK signaling pathways. Sinigrin has potent anti-oxidant, anti-tumor and anti-inflammatory effects .
|
-
- HY-113071
-
-
- HY-119917
-
|
|
p38 MAPK
MEK
Bacterial
|
Infection
Cancer
|
|
Gossypetin is a hexahydroxylated flavonoid and is a potent mitogen-activated protein kinase kinase (MKK)3 and MKK6 inhibitor with strongly attenuates the MKK3/6-p38 signaling pathway, has various pharmacological activities, including antioxidant, antibacterial and anticancer activities .
|
-
- HY-B1029R
-
|
|
Tyrosinase
PKC
Apoptosis
|
Endocrinology
Cancer
|
|
Danazol standard inhibits the proliferation of cancer cell MDA-MB-231 and MCF-7 with IC50 of 65 µg/mL and 31 µg/mL. Danazol arrests the cell cycle at G1 phase, induces apoptosis in MDA-MB-231 through PKCα signaling pathway .
|
-
- HY-N0637R
-
|
|
Keap1-Nrf2
Influenza Virus
DNA/RNA Synthesis
Endogenous Metabolite
|
Infection
Inflammation/Immunology
|
|
Eriodictyol (Standard) is the analytical standard of Eriodictyol. This product is intended for research and analytical applications. Eriodictyol is a flavonoid isolated from the Chinese herb, with antioxidant and anti-inflammatory activity. Eriodictyol induces Nrf2 signaling pathway. Eriodictyol is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 18 nM.
|
-
- HY-100507
-
-
- HY-16274
-
|
TAK-475
|
Farnesyl Transferase
|
Metabolic Disease
|
|
Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor, blocking the conversion of farnesyl diphosphate (FPP) to squalene in the cholesterol biosynthesis pathway . Lapaquistat acetate is effective at lowering low-density lipoprotein cholesterol, but it might cause liver damage. Lapaquistat acetate is used for hypercholesterolemia and mevalonate kinase deficiency (MKD) research .
|
-
- HY-N11422R
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Deoxynivalenol (Standard) is the analytical standard of Deoxynivalenol. This product is intended for research and analytical applications. Deoxynivalenol, an orally active mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors .
|
-
- HY-158156
-
|
|
NF-κB
Apoptosis
|
Cancer
|
|
NF-κB-IN-16 (compound 9) is a complex (Pt(IV) complex) of NF-κB inhibitor and Cisplatin (HY-17394), which has high efficacy and low toxicity in anti-tumor activity. active. NF-κB-IN-16 can cause DNA damage, induce mitochondrial dysfunction, produce reactive oxygen species, and induce apoptosis through the mitochondrial pathway and endoplasmic reticulum stress. NF-κB-IN-16 potently inhibits the NF-κB/MAPK signaling pathway and disrupts PI3K/AKT signaling. NF-κB-IN-16 also exhibits excellent in vivo antitumor efficiency and low toxicity in A549 or A549/CDDP xenograft models .
|
-
- HY-P3434
-
|
|
Pyroptosis
|
Inflammation/Immunology
|
|
Ac-FEID-CMK is a potent zebrafish-specific GSDMEb-derived peptide inhibitor.
Ac-FEID-CMK can attenuate the mortality and kidney injury during septic shock. Ac-FEID-CMK inhibits pyroptosis and attenuates septic AKI (acute kidney injury) in vivo. Ac-FEID-CMK can suppress the caspy2-mediated noncanonical inflammasome pathway .
|
-
- HY-N0781R
-
|
|
Apoptosis
|
Cancer
|
|
Linderalactone (Standard) is the analytical standard of Linderalactone. This product is intended for research and analytical applications. Linderalactone is an important sesquiterpene lactone isolated from Lindera aggregata. Linderalactone inhibits cancer growth by modulating the expression of apoptosis-related proteins and inhibition of JAK/STAT signalling pathway. Linderalactone also inhibits the proliferation of the lung cancer A-549 cells with an IC50 of 15 μM .
|
-
- HY-149724
-
|
|
STING
NO Synthase
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 65 (compound 29) is a Hederagonic acid derivative with potent anti-inflammatory activity. Anti-inflammatory agent 65 inhibits nitric oxide (NO) release. Anti-inflammatory agent 65 inhibits the nuclear translocation of IRF3 and p65, and disrupts the STING/IRF3/NF-κB signaling pathway, thereby attenuating the inflammatory response .
|
-
- HY-113756A
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor . Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes .
|
-
- HY-100036
-
|
|
Smo
Apoptosis
Hedgehog
|
Cancer
|
|
MK-4101 is a Smoothened (SMO) antagonist (IC50 of 1.1 μM for 293 cells ) and also a potent inhibitor of the hedgehog pathway (IC50 of 1.5 μM for mouse cells; IC50 of 1 μM for KYSE180 oesophageal cancer cells). MK-4101 has robust antitumor activity that inhibits tumor cell proliferation and induces extensive apoptosis .
|
-
- HY-116364A
-
|
3'-Azido-3'-deoxythymidine-5'-triphosphate TEA
|
HIV
DNA/RNA Synthesis
HBV
Reactive Oxygen Species
Apoptosis
|
Infection
|
|
AZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) TEA is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TEA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TEA also inhibits the DNA polymerase of HBV. AZT triphosphate TEA activates the mitochondria-mediated apoptosis pathway .
|
-
- HY-B0736
-
-
- HY-137135
-
|
|
Phosphatase
Apoptosis
ERK
p38 MAPK
JNK
|
Cancer
|
|
Cantharidic acid is a selective inhibitor for protein phosphatase 2 (PP2A) and protein phosphatase 1 (PP1). Cantharidic acid inhibits cell viability and arrest cell cycle at sub G1 phase, induces apoptosis in cells NPC-39 and HONE-1 through the upregulation of ERK1/2, p38, and JNK1/2 pathway .
|
-
- HY-13691
-
|
Ro-31-7453
|
Akt
mTOR
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
MKC-1 (Ro-31-7453) is an orally active and potent cell cycle inhibitor with broad antitumor activity. MKC-1 inhibits the Akt/mTOR pathway. MKC-1 arrests cellular mitosis and induces cell apoptosis by binding to a number of different cellular proteins including tubulin and members of the importin β family .
|
-
- HY-164460
-
|
|
Pim
|
Cancer
|
|
AZD1897 is a PIM1, PIM2, and PIM3 inhibitor with IC50 values of less than 3 nM for these three PIM kinases. AZD1897 exhibits anticancer activity and synergistically inhibits the activity of acute myeloid leukemia (AML) cells in combination with Capivasertib (HY-15431). This synergistic inhibitory effect is achieved through the inhibition of the mTOR and MCL1 pathways .
|
-
- HY-142125
-
|
|
Xanthine Oxidase
Reactive Oxygen Species
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Broussochalcone A is an antioxidant and an inhibitor of Xanthine Oxidase (IC50=2.21 μM), with free radical scavenging activity. Broussochalcone A inhibits iron-induced lipid peroxidation and nitric oxide synthesis in lipopolysaccharide (LPS) -activated macrophages. Broussochalcone A also induces Apoptosis of human renal carcinoma cells by increasing ROS levels and activating FOXO3 signaling pathways .
|
-
- HY-157809
-
|
|
Interleukin Related
TNF Receptor
NF-κB
p38 MAPK
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 74 (B5) is an anti-inflammatory agent that can inhibit NO, IL-6, and TNF-α, with IC50 values of 10.88 μM and 4.93 μM for NO and IL-6, respectively. Anti-inflammatory agent 74 alleviates acute lung injury (ALI) by regulating inflammatory mediators and inhibiting the MAPK and NF-κB signaling pathways .
|
-
- HY-B0736A
-
|
FI7056
|
Fungal
Autophagy
Apoptosis
p38 MAPK
Microtubule/Tubulin
|
Infection
Cancer
|
|
Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole nitrate is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells .
|
-
- HY-116364B
-
|
3'-Azido-3'-deoxythymidine-5'-triphosphate tetraammonium
|
HIV
DNA/RNA Synthesis
HBV
Reactive Oxygen Species
Apoptosis
|
Infection
|
|
AZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) tetraammonium is an active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate tetraammonium exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate tetraammonium also inhibits the DNA polymerase of HBV. AZT triphosphate tetraammonium activates the mitochondria-mediated apoptosis pathway .
|
-
- HY-151965
-
|
|
Parasite
|
Infection
|
|
Antimalarial agent 18 is an potent antimalarial agent, based on electronic, highly lipophilic and siderophoric properties. Antimalarial agent 18 belongs to acyloxymethyl series, as a fosmidomycin surrogate, which is potent IspC inhibitor against the non-mevalonate isoprenoid biosynthesis pathway. Antimalarial agent 18 inhibits P. falciparum (IC50=50 nM) and A. baumanii (IC50=390 nM) .
|
-
- HY-159511
-
|
|
Hedgehog
|
Cancer
|
|
Hedgehog IN-7 (Compound 8g), a purine derivative, acts as an inhibitor of Hedgehog, capable of reducing the expression of Hedgehog genes and inhibiting Hedgehog signaling. Hedgehog IN-7 has significant cytotoxicity and selectivity towards the Hedgehog pathway-dependent pancreatic cancer cell Mia-PaCa-2 cells and can be used in the research of pancreatic cancer .
|
-
- HY-W011616
-
|
CDNG1/vuc230
|
Wnt
|
Cardiovascular Disease
Cancer
|
|
Cardionogen 1 (CDNG1/vuc230) is a Wnt signaling pathway inhibitor that slows down Myc-induced liver tumorigenesis. Cardionogen 1 treatment of zebrafish embryos before gastrulation inhibits cardiomyocyte formation, whereas treatment during or after gastrulation induces cardiomyocyte formation. Cardionogen 1 has potential in research into cancer and cardiovascular disease .
|
-
- HY-170318
-
|
|
Myosin
|
Cancer
|
|
Adhibin is an allosteric inhibitor for RhoGAP class IX myosin, that inhibits Myo9 ATPase in mammalian and invertebrate with IC50 of 2.5 µM and 2.6 µM. Adhibin binds to the ATPase of myosin, interfers with its motor function, blocks the RhoGTPase related signaling pathway, and affects the cell migration, adhesion and cell division. Adhibin can be used in research about cancer metastasis .
|
-
- HY-17508
-
|
|
Bacterial
Cytochrome P450
Autophagy
Antibiotic
|
Infection
Cancer
|
|
Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
|
-
- HY-111557
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
YM-254890 is a selective Gαq/11 protein inhibitor isolated from Chromobacterium sp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by ADP by blocking the P2Y1 signal transduction pathway, with an IC50 value below 0.6 μM .
|
-
- HY-N0410R
-
|
|
Apoptosis
Reactive Oxygen Species
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Daucosterol (Standard) is the analytical standard of Daucosterol. This product is intended for research and analytical applications. Daucosterol is an orally active natural sterol compound, which has anti-inflammatory, anticancer and immunomodulatory activities. Daucosterol inhibits cancer cell proliferation by inducing autophagy through ROS-dependent manner. Daucosterol also inhibits colon cancer growth by inducing apoptosis, inhibiting cell migration and invasion and targeting caspase signalling pathway .
|
-
- HY-132305
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-3-IN-1 is a potent and selective VEGFR3 inhibitor with an IC50 of 110.4 nM. VEGFR-3-IN-1 significantly inhibits proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells by inactivating the VEGFR3 signaling pathway, and also effectively inhibits breast cancer growth .
|
-
- HY-155062
-
|
|
Mitochondrial Metabolism
Reactive Oxygen Species
β-catenin
Fluorescent Dye
PPAR
|
Cancer
|
|
IR-251 is a mitochondrion-targeting NIR fluorescent probe. IR-251 targets mitochondria via OATPs and causes mitochondrial damage in tumor cells. IR-251 IR-251 induced ROS overproduction by inhibiting PPARγ, and then inhibiting the β-catenin signaling pathway and downstream protein molecules related to the cell cycle and metastasis. IR-251 inhibits tumor proliferation and metastasis .
|
-
- HY-P990091
-
|
SAR 445088
|
Complement System
|
Inflammation/Immunology
|
|
Riliprubart (SAR445088) is an anti-C1s humanized monoclonal antibody that inhibits activated C1s in the proximal portion of the classical complement system. Riliprubart selectively inhibits activated C1s and prevents the enzymatic action of C1 on its substrates C4 and C2, thus inhibiting the formation of the classical pathway C3 convertase, C4b2a .
|
-
- HY-34544R
-
|
|
Others
|
Others
|
|
Daucosterol (Standard) is the analytical standard of Daucosterol. This product is intended for research and analytical applications. Daucosterol is an orally active natural sterol compound, which has anti-inflammatory, anticancer and immunomodulatory activities. Daucosterol inhibits cancer cell proliferation by inducing autophagy through ROS-dependent manner. Daucosterol also inhibits colon cancer growth by inducing apoptosis, inhibiting cell migration and invasion and targeting caspase signalling pathway .
|
-
- HY-155532
-
|
|
Apoptosis
|
Cancer
|
|
10m/ZS44 is a blood-brain barrier-permeable Glioblastoma (GBM) inhibitor. 10m/ZS44 significantly inhibits GBM tumor growth in a mouse xenograft model. 10m/ZS44 also activates the SIRT1/p53-mediated apoptosis pathway, thereby inhibiting the proliferation of U251 cells .
|
-
- HY-P1259A
-
|
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
|
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
|
-
- HY-125019
-
|
|
JAK
STAT
|
Inflammation/Immunology
|
|
iJak-381 is a JAK1/2 inhibitor with anti-inflammatory activity. iJak-381 blocks IL-13 signaling and also inhibits IL-4 and IL-6 signaling pathways. iJak-381 also reduced p-STAT6 levels and inhibited the influx of inflammatory cells into the lungs of mice. iJak-381 inhibits airway hyperresponsiveness (AHR) .
|
-
- HY-B1640A
-
|
Etacrynic acid sodium; Sodium etacrynate
|
NF-κB
Glutathione S-transferase
Calcium Channel
NO Synthase
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Ethacrynic acid (Etacrynic acid sodium) sodium is a diuretic. Ethacrynic acid sodium is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid sodium is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid sodium also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid sodium has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice .
|
-
- HY-15586
-
L67
1 Publications Verification
DNA Ligase Inhibitor
|
DNA/RNA Synthesis
Caspase
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
L67 (DNA Ligase Inhibitor) is a competitive DNA ligase inhibitor that effectively inhibits DNA ligases I/III (both IC50 are 10 μM). L67 can cause nuclear DNA damage by reducing levels of mitochondrial DNA and increasing levels of mitochondrially-generated ROS. L67 also activates the Caspase 1-dependent apoptosis pathway in cancer cells, can be used in cancer research .
|
-
- HY-107758
-
|
|
Prolyl Endopeptidase (PREP)
|
Cancer
|
|
Y-29794 oxalate is a selective, orally active and blood-brain barrier permeable non-peptide prolyl endopeptidase inhibitor. Y-29794 oxalate blocks the IRS1-AKT-mTORC1 pathway and inhibits tumor growth. Y-29794 oxalate is also effective in inhibiting the progression of Aβ-like deposition in the hippocampus of aging-accelerated mice (SAM) .
|
-
- HY-W371165
-
|
|
Complement System
|
Inflammation/Immunology
|
|
C1s-IN-1 trihydrochloride (Compound A1) is the selective inhibitor for C1s protease with the Ki of 5.8 μM. C1s-IN-1 trihydrochloride inhibits cleavage of C2 by C1s with an IC50 of 85 μM, inhibits the activation of classic pathway with an IC50 of 22 μM. C1s-IN-1 trihydrochloride is the competitive inhibitor for thrombin with the Ki of 51.2 μM .
|
-
- HY-17514S2
-
|
R51211-d9
|
Fungal
Hedgehog
Bacterial
Autophagy
Cytochrome P450
Antibiotic
|
Infection
|
|
Itraconazole-d9 is the deuterium labeled Itraconazole[1]. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor[2][3][4][5].
|
-
- HY-122950
-
|
|
Fungal
|
Infection
|
|
Harzianic acid, a tetramic acid derivative, with activity of antimicrobial, antibiofilm formation and biofilm disaggregation. Harzianic acid interferes with biofilm formation by limiting bacterial iron availability. Harzianic acid is also a selective inhibitor of Acetohydroxyacid synthase (AHAS), the first enzyme in the branched-chain amino acid biosynthetic pathway. Harzianic acid can used for herbicide and fungicide .
|
-
- HY-146757
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
RIPK1-IN-13 (Compound 8) is a potent inhibitor of RIPK1 with an IC50 value of 1139 nM. RIPK1-IN-13 blocks the activation of the necroptosis pathway via the inhibition of RIPK1. RIPK1-IN-13 has the potential for the research of inflammation diseases .
|
-
- HY-N2098
-
|
|
NF-κB
|
Cancer
|
|
Obtusifolin, isolated from the seeds of Cassia obtusifolia, regulates the gene expression and production of MUC5AC mucin in airway epithelial cells via inhibiting NF-kB pathway . Obtusifolin suppresses phthalate esters-induced breast cancer bone metastasis by targeting parathyroid hormone-related protein .
|
-
- HY-N2638
-
|
|
Apoptosis
|
Cardiovascular Disease
|
|
Ilexsaponin A, isolated from the root of Ilex pubescens, attenuates ischemia-reperfusion-induced myocardial injury through anti-apoptotic pathway. Ilexsaponin A can reduce myocardial infarct size, lower the serum levels of LDH, AST and CK-MB, increase cellular viability and inhibit apoptosis in hypoxia/reoxygenation cardiomyocytes .
|
-
- HY-B0094
-
|
Qinghaosu; NSC 369397
|
HCV
Parasite
Akt
Ferroptosis
|
Infection
Neurological Disease
Cancer
|
|
Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
|
-
- HY-123503
-
|
|
JNK
NF-κB
|
Neurological Disease
Inflammation/Immunology
|
|
Salicortin, a phenolic glycoside, has been isolated from many plants such as Populus and Salix species. Salicortin inhibits osteoclast differentiation and bone resorption by down-regulating JNK and NF-κB/NFATc1 signaling pathways. Salicortin has anti-amnesic, anti-adipogenic, and immune-modulatory activity .
|
-
- HY-N2110R
-
|
|
Akt
|
Inflammation/Immunology
|
|
Phellopterin (Standard) is the analytical standard of Phellopterin. This product is intended for research and analytical applications. Phellopterin is a natural product isolated from Angelica dahurica. Phellopterin reduces TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium .
|
-
- HY-P10392AF
-
|
|
β-catenin
|
Cancer
|
|
fStAx-35R TFA is the hydrocarbon-stapled peptide. fStAx-35R TFA inhibits Wnt/β-catenin signaling pathway by disrupting the β-catenin-TCF interaction. fStAx-35R TFA can be used in cancer research .
|
-
- HY-N2666
-
|
|
VEGFR
|
Cancer
|
|
5α-Hydroxycostic acid, a eudesmane-type sesquiterpene, is isolated from the herb Laggera alata. 5α-Hydroxycostic acid inhibits angiogenesis and suppresses breast cancer cell migration through regulating VEGF/VEGFR2 and Ang2/Tie2 pathways .
|
-
- HY-100037
-
NT157
1 Publications Verification
Tyrphostin NT157
|
Insulin Receptor
STAT
|
Endocrinology
Cancer
|
|
NT157 (Tyrphostin NT157) is a selective IRS-1/2 inhibitor that induces Ser-phosphorylation and consequently the degradation of IRS-1/2. NT157 (Tyrphostin NT157) is a first-in-class anti-cancer agent that also targets Stat3 signaling pathway .
|
-
- HY-N0020R
-
|
|
Wnt
Reactive Oxygen Species
|
Neurological Disease
|
|
Echinacoside (Standard) is the analytical standard of Echinacoside. This product is intended for research and analytical applications. Echinacoside, one of the phenylethanoids isolated from the stems of Cistanche deserticola, effectively inhibits Wnt/β-catenin signaling. Echinacoside elicits neuroprotection by activating Trk receptors and their downstream signal pathways. Antiosteoporotic activity .
|
-
- HY-139397
-
|
|
MyD88
|
Cardiovascular Disease
|
|
TJ-M2010-5 is a MyD88 inhibitor that binds to the TIR domain of MyD88 to interfere with its homodimerization, and the TLR/MyD88 signal pathway . TJ-M2010-5 can be used for the research of myocardial ischemia/reperfusion injury (MIRI) .
|
-
- HY-18366A
-
|
|
Hedgehog
|
Cancer
|
|
RU-SKI 43 hydrochloride is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. RU-SKI 43 hydrochloride reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway activity. RU-SKI 43 hydrochloride has anti-cancer activity .
|
-
- HY-N2112
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
Glaucocalyxin A, an ent-kauranoid diterpene from Rabdosia japonica var., induces apoptosis in osteosarcoma by inhibiting nuclear translocation of Five-zinc finger Glis 1 (GLI1) via regulating PI3K/Akt signaling pathway. Glaucocalyxin A has antitumor effect .
|
-
- HY-50055
-
|
|
ERK
|
Cancer
|
|
EtDO-P4 is a nanomolar inhibitor of glycosphingolipid (GSL) synthesis. EtDO-P4 suppresses activation of the EGFR-induced ERK pathway and various receptor tyrosine kinases (RTKs). EtDO-P4 can be used for various types of cancer, including Burkitt’s lymphoma .
|
-
- HY-18366
-
|
|
Hedgehog
|
Cancer
|
|
RU-SKI 43 is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. RU-SKI 43 reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway activity. RU-SKI 43 has anti-cancer activity .
|
-
- HY-123693
-
|
|
Insecticide
|
Inflammation/Immunology
|
|
ML358 is a first in class, potent, and selective inhibitor of the SKN-1 pathway (IC50=0.24 μM). ML358 sensitizes the model nematode C. elegans to oxidants and anthelmintic. ML358 potentially used as adjuvants to increase the efficacy and useful life of current anthelmintics .
|
-
- HY-147297
-
|
BCX9930
|
Complement System
|
Inflammation/Immunology
|
|
Pelecopan (BCX9930) is a potent, selective, orally active inhibitor of complement factor D with an IC50 value of 14.3 nM. Pelecopan can target factor D to prevent both intravascular and extravascular hemolysis in PNH. Pelecopan also be used for other alternative pathway (AP) mediated diseases .
|
-
- HY-164350
-
|
|
Ras
ERK
p38 MAPK
|
Cancer
|
|
KRAS inhibitor-27 (Compound 15h) is the inhibitor for KRAS. KRAS inhibitor-27 inhibits KRAS G12D/G12V mutated cells AsPC-1, SW620 and KRAS wildtype cell HT-29 with IC50 of 378, 0.6 and 3230 nM, respectively. KRAS inhibitor-27 inhibits ERK phosphorylation (IC50 in cell AsPC-1 and SW620 is 0.6 nM and 1 nM), reduces the expression of DUSP4, thereby inhibiting MAPK signaling pathway .
|
-
- HY-B0766
-
|
SY801
|
Autophagy
Apoptosis
HBV
HCV
HSP
Reactive Oxygen Species
Bcl-2 Family
Glutathione S-transferase
p38 MAPK
NF-κB
Microtubule/Tubulin
ERK
JNK
TNF Receptor
Interleukin Related
CDK
Cyclin G-associated Kinase (GAK)
mTOR
P-glycoprotein
Ferroptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Bicyclol (SY801) is an orally active derivative of the traditional Chinese medicine Schisandra chinensis, which has antiviral, anti-inflammatory, immunomodulatory, antioxidant, anti-steatosis, anti-fibrotic and anti-tumor activities. Bicyclol regulates the expression of heat shock proteins and plays an anti-apoptosis role in hepatocytes. Bicyclol reduces the activation of NF-κB and the levels of inflammatory factors in hepatocytes infected with hepatitis C virus (HCV) by inhibiting the activation of the ROS-MAPK-NF-κB pathway, and prevents ferroptosis in acute liver injury. Bicyclol can change the expression of Mdr-1, GSH/GST and Bcl-2, increase the intracellular concentration of anticancer drugs, and sensitize drug-resistant cells to anticancer drugs. Bicyclol inhibits the proliferation of human malignant hepatoma cells by regulating the PI3K/AKT pathway and the Ras/Raf/MEK/ERK pathway. Bicyclol can be used in the study of chronic hepatitis, acute liver injury, nonalcoholic fatty liver disease, liver fibrosis and hepatocellular carcinoma .
|
-
- HY-169413
-
|
|
Akt
|
Cancer
|
|
AKT-IN-25 (Compound 14a) is an inhibitor for Akt, that inhibits the phosphorylation of Akt, and thereby inhibits the PI3K/Akt/mTOR signaling pathway. AKT-IN-25 arrests the cell cycle at G1 phase, inhibits the cell migration of PANC-1, and inhibits the proliferation of cancer cells PANC-1, PATU-T, and SUIT-2 with IC50s of 3.05, 1.32, and 3.85 μM, respectively .
|
-
- HY-P10336
-
|
|
Serpin
|
Neurological Disease
Endocrinology
|
|
Serpinin is an agonist of the protease inhibitor Nexin-1 (PN-1). Serpinin upregulates the expression of PN-1 through the cAMP-PKA-Sp1 signaling pathway, promoting granule biogenesis in endocrine cells. Serpinin is used in research related to the regulation of secretory function . Serpinin is a selective agonist for β-adrenergic receptors. Serpinin interacts with β1-adrenergic receptors to activate the AC-cAMP-PKA pathway, which regulates myocardial systolic and diastolic function. pGlu-serpinin upregulates Bcl2 mRNA transcription and exerts neuroprotective effects .
|
-
- HY-N1356
-
-
- HY-163412
-
|
|
IKK
|
Inflammation/Immunology
|
|
IKKβ-IN-3 (Compound hit4) is a IKKβ inhibitor with an IC50 value of 30.4 nM. IKKβ is a key enzyme in the NF-κB signaling pathway and is involved in the development of many diseases. IKKβ-IN-3 can be used in the study of CAF-induced arthritis .
|
-
- HY-N0636
-
|
|
Apoptosis
|
Cancer
|
|
Eriocitrin is a flavonoid isolated from lemons that is a powerful antioxidant. Eriocitrin inhibits the proliferation of liver cancer cells by arresting the cell cycle in the S phase by upregulating p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating intrinsic signaling pathways involving mitochondria .
|
-
- HY-149370
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-60 (compound 21a) is a potent histone deacetylase (HDAC) inhibitor. HDAC-IN-60 can promote the intracellular generation of ROS, cause DNA damage, block the cell cycle at G2/M phase, and activate the mitochondria-related apoptotic pathway to induce cell apoptosis .
|
-
- HY-B0252
-
|
HCTZ
|
TGF-beta/Smad
Potassium Channel
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect .
|
-
- HY-120234
-
|
Z-Leu-Leu-Nle-CHO; GSII
|
γ-secretase
Proteasome
Apoptosis
|
Cancer
|
|
Z-LLNle-CHO (Z-Leu-Leu-Nle-CHO) is a γ-secretase inhibitor I. Z-LLNle-CHO induces caspase and ROS-dependent apoptosis by blocking the Akt-mediated pro-survival pathway. Z-LLNle-CHO can be used in cancer research, such as breast cancer and leukaemia .
|
-
- HY-W058849
-
|
|
AMPK
mTOR
Apoptosis
|
Cancer
|
|
MT 63-78 is a specific and potent direct AMPK activator with an EC50 of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects .
|
-
- HY-P3839
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a Gi/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia .
|
-
- HY-N0314
-
-
- HY-116211
-
|
WIN-25978
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
Amfonelic acid (WIN-25978) is a highly selective dopamine reuptake inhibitor. Amfonelic acid interferes with the in vitro neuronal uptake of norepinephrine in the iris of rats, but does not alter the concentrations of norepinephrine or dopamine in the whole mouse brain. Amfonelic acid can be used as a pharmacological tool to study the brain reward system, dopamine pathway and dopamine transporter .
|
-
- HY-161578
-
|
|
Others
|
Neurological Disease
|
|
Dithio-CN03 is a compound with the highest neuroprotective efficacy. Dithio-CN03 fights the progression of retinitis pigmentosa (RP) by inhibiting the cGMP mediated signaling pathway and reducing photoreceptor cell death. Dithio-CN03 can be used in research into RP and other retinal degenerative diseases .
|
-
- HY-N15274
-
|
|
GABA Receptor
Sodium Channel
Potassium Channel
|
Neurological Disease
|
|
Cicutoxin is a convulsant. Cicutoxin blocks Na + and K + channels and inhibits γ-aminobutyric acid pathways. Cicutoxin is a potent GABA antagonist that induces recurrent seizures and exerts cholinergic effects. Cicutoxin acts primarily on the brain and skeletal muscles. Cicutoxin can be isolated from Cicuta maculata (water hemlock) and Cicuta douglasii .
|
-
- HY-149369
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-59 (compound 13a) is a potent histone deacetylase (HDAC) inhibitor. HDAC-IN-59 can promote the intracellular generation of ROS, cause DNA damage, block the cell cycle at G2/M phase, and activate the mitochondria-related apoptotic pathway to induce cell apoptosis .
|
-
- HY-108473
-
|
TLR3-IN-1
|
Toll-like Receptor (TLR)
|
Cancer
|
|
CU-CPT 4a (TLR3-IN-1) is a potent, highly selective TLR3 signaling inhibitor. CU-CPT 4a represses the expression of downstream signaling pathways mediated by the TLR3/dsRNA complex, including TNF-α and IL-1β .
|
-
- HY-158017
-
|
|
PI3K
|
Cancer
|
|
WXM-1-170 (compound 10) is a Indisulam (HY-13650) derivative,and inhibits the migration of gastric cancer cells. WXM-1-170 attenuates PI3K/AKT/GSK-3β/β-catenin signaling pathway .
|
-
- HY-161362
-
|
|
PI3K
|
Cancer
|
|
SR-3-65 (compound 6) is a Indisulam (HY-13650) derivative,and inhibits the migration of gastric cancer cells. SR-3-65 attenuates PI3K/AKT/GSK-3β/β-catenin signaling pathway .
|
-
- HY-155363
-
|
|
AMPK
|
Metabolic Disease
|
|
AMPK activator 13 is a potent activator of AMPK. AMPK activator 13 inhibits mitotic clonal expansion of 3T3-L1 cells by activating AMPK pathway and enhances cell mitochondrial oxygen consumption rate. AMPK activator 13 can be used in study obesity .
|
-
- HY-118295
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Pyrimidine-indole hybrid is a compound that inhibits ciliogenesis and has the activity of antagonizing the Hedgehog signaling pathway by destabilizing microtubules. Pyrimidine-indole hybrid exerts its biological effects by inhibiting ciliogenesis and deconstructing the stable form of α-tubulin. Pyrimidine-indole hybrid has shown its unique mechanism of action in in vitro cell experiments and zebrafish embryo models, interfering with microtubule dynamics .
|
-
- HY-156112
-
|
|
Ser/Thr Protease
|
Cancer
|
|
LM2I is a derivative of Spinosyn A (SPA). LM2I is argininosuccinate synthase (ASS1) enzyme activator, and tumor inhibitor that directly interact with ASS1. LM2I has significant antiproliferative activity in seven colorectal cancer cell-lines and xenograft tumors of colorectal cancer. LM2I inhibits colorectal cancer cell growth via the EGFR pathway .
|
-
- HY-107595
-
|
|
JAK
STAT
Apoptosis
|
Cancer
|
|
SD-1008 is a potent JAK inhibitor. SD-1008 inhibits tyrosyl phosphorylation of STAT3, JAK2 and Src. SD-1008 also reduces STAT3-dependent luciferase activity. SD-1008 enhances apoptosis induced by Paclitaxel in ovarian cancer cells via directly blocking the JAK-STAT3 signaling pathway .
|
-
- HY-B1640
-
|
Etacrynic acid
|
Glutathione S-transferase
NF-κB
Calcium Channel
NO Synthase
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Ethacrynic acid has anti-inflammatory and anticancer activity. Ethacrynic acid is an orally active diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferase (GSTs) and Wnt signaling pathways. Ethacrynic acid is a radiosensitizer. Ethacrynic acid can inhibit airway smooth muscle (ASM) contraction in mice. Ethacrynic acid can increase the outflow of aqueous humor from the eye for the study of glaucoma .
|
-
- HY-12037A
-
|
ON-01910
|
Polo-like Kinase (PLK)
PI3K
Apoptosis
|
Cancer
|
|
Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
|
-
- HY-114491A
-
|
|
ERK
Raf
|
Cancer
|
|
Rineterkib hydrochloride (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
|
-
- HY-162646
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
FXIIa-IN-5 (Compound 4J) is an orally active, selective inhibitor for factor XIIa (FXIIa), with IC50 of 21 nM. FXIIa-IN-5 inhibits the intrinsic coagulation pathways, and exhibits anti-inflammatory and antithrombotic activity in Carrageenan (HY-125474)-induced mice thrombosis models. FXIIa-IN-5 exhibits moderate pharmacokinetic characteristics and slightly toxicity (at 100 mg/kg) .
|
-
- HY-172406
-
|
|
p38 MAPK
Interleukin Related
IRAK
|
Inflammation/Immunology
|
|
MAPK-IN-4 (Compound c1) is an orally active anti-inflammatory agent. MAPK-IN-4 can inhibit the expression and release of pro-inflammatory cytokines IL-6 and TNF-α induced by LPS (HY-D1056). MAPK-IN-4 can bind to IRAK4 and exert its anti-inflammatory effect by inhibiting the MAPK pathway .
|
-
- HY-167746
-
|
|
HIV
|
Infection
|
|
Nevirapine quinone methide is an active metabolite of Nevirapine, serving as a non-nucleoside reverse transcriptase inhibitor (NNRTI) for the treatment of HIV-1 infection and AIDS. Nevirapine quinone methide is associated with severe skin and liver injuries due to its metabolic activation pathways. Nevirapine quinone methide has been shown to inhibit CYP3A4, which could contribute to its hepatic toxicity.
|
-
- HY-114491
-
|
|
ERK
Raf
|
Cancer
|
|
Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
|
-
- HY-155124
-
|
|
Apoptosis
|
Cancer
|
|
Antiproliferative agent-32 (Compound 1c) inhibits the phosphorylation of PI3K/Akt/mTOR signaling pathway. Antiproliferative agent-32 inhibits Huh7 and SK-Hep-1 cells proliferation, and induce cells apoptosis, causes mitochondrial damage. Antiproliferative agent-32 can be used for research of hepatocellular carcinoma .
|
-
- HY-161266
-
-
- HY-123984
-
|
|
NF-κB
|
Metabolic Disease
|
|
LTβR-IN-1 is a potent, selective lymphotoxin β receptor (LTβR) inhibitor. LTβR-IN-1 also selectively inhibits the nuclear translocation of p52 depended on TNF12A, instead of the nuclear translocation of p65 mediated by TNF-α receptor. LTβR-IN-1 regulates the NF-kB signaling pathway IN a ligand-independent manner .
|
-
- HY-P10719A
-
|
|
MyD88
|
Infection
Inflammation/Immunology
|
|
Pepinh-MYD TFA is a MyD88 inhibitor that contains a domain sequence from MyD88 TIR and a protein transduction sequence, enabling it to penetrate the cell membrane. Pepinh-MYD TFA interferes with MyD88-mediated TLR signaling pathways, thereby inhibiting related immune responses. Pepinh-MYD TFA holds potential for studying the role of MyD88 in viral infections .
|
-
- HY-128439
-
|
|
DYRK
|
Cancer
|
|
BT173 is a potent homeodomain interacting protein kinase 2 (HIPK2) inhibitor. BT173 binds to HIPK2 does not inhibit HIPK2 kinase activity but rather, interfered allosterically with the ability of HIPK2 to associate with Smad3. BT173 attenuates renal fibrosis through suppression of the TGF-β1/Smad3 pathway .
|
-
- HY-120619
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Endocrinology
|
|
BMS-193885 is a selective neuropeptide Y1 receptor antagonist (Ki=3.3 nM) that competitively blocks the receptor to inhibit NPY-mediated appetite regulation signaling pathways, reduce food intake and inhibit weight gain. BMS-193885 has good blood-brain barrier penetration and is mainly used in the study of obesity and related metabolic diseases .
|
-
- HY-W554514
-
|
|
Bacterial
|
Infection
|
|
D-Homoserine lactone is a signaling molecule with the activity of regulating bacterial quorum sensing. The chemical structure of D-Homoserine lactone makes it a potential regulator of the AHL synthase RhlI. D-Homoserine lactone has been shown to inhibit the activity of RhlI, thereby affecting the bacterial quorum sensing signaling pathway. D-Homoserine lactone is also an enantiomer of L-homoserine lactone and is used as an inhibitor of serine hydroxymethyltransferase .
|
-
- HY-162575
-
|
|
ERK
|
Cancer
|
|
Anticancer agent 231 (Compound P5) is a tyrosine protein kinase inhibitor with a IC50 value of 3.95 μM. Anticancer agent 231 inhibits the cell viability, cell proliferation, cell migration and cancer dryness of triple negative breast cancer (TNBC) cells by targeting EGFR-ERK 1/2 signaling pathway, and is expected to play an important role in the field of TNBC disease therapy .
|
-
- HY-N3716
-
|
|
Aldose Reductase
COX
|
Metabolic Disease
Inflammation/Immunology
|
|
Dehydroglyasperin D inhibits rat and human Aldose Reductase (AR) (IC50: 62.4 μM and 176.2 μM respectively). Dehydroglyasperin D has anti-obesity, antioxidant effects. Dehydroglyasperin D shows anti-inflammatory activity by inhibiting COX-2 expression and the MLK3 signaling pathway. Dehydroglyasperin D also inhibits melanin synthesis. Dehydroglyasperin D is a prenylated flavonoid that can be isolated from Glycyrrhiza uralensi .
|
-
- HY-168070
-
|
|
COX
NF-κB
NO Synthase
|
Inflammation/Immunology
|
|
COX-2-IN-48 (5-25), a COX-2 inhibitor with an IC50 of 51.7 nM for human COX-2, exerts anti-inflammatory and analgesic effects in various rodent models by inhibiting NF-κB pathway. COX-2-IN-48 (5-25) inhibits the degradation of IκB, the phosphorylation and nuclear translocation of NF-κB p65, and the expression of COX-2 and iNOS .
|
-
- HY-145026
-
|
|
ERK
|
Inflammation/Immunology
Cancer
|
|
ERK1/2 inhibitor 5 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 5 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2020238776A1) .
|
-
- HY-103248
-
|
Vengicide
|
IRE1
Fungal
Antibiotic
Apoptosis
CDK
|
Infection
Cancer
|
|
Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an XBP1 inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC50 value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC50 value of 79 nM .
|
-
- HY-145027
-
|
|
ERK
|
Cancer
|
|
ERK1/2 inhibitor 5 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 5 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2020238776A1) .
|
-
- HY-150538
-
|
|
STAT
Apoptosis
|
Cancer
|
|
STAT3-IN-12 is a potent STAT3 signal inhibitor that can inhibit IL-6 induced JAK/STAT3 signalling pathway activation. STAT3-IN-12 inhibits cancer cell growth, migration, and induce cell apoptosis as well as cycle arrest. STAT3-IN-12 can be used in cancer-related research, such as hepatocellular carcinoma (HCC) and oesophageal carcinoma .
|
-
- HY-B0093AS
-
-
- HY-B1260
-
|
CTAB; Cetyltrimethylammonium bromide; Hexadecyltrimethylammonium bromide
|
Biochemical Assay Reagents
MMP
Apoptosis
TGF-β Receptor
|
Cancer
|
|
Cetrimonium bromide (CTAB), a quaternary ammonium, is an orally active cationic surfaetant. Cetrimonium bromide has toxicity and anticancer effect. Cetrimonium bromide inhibits cell migration and invasion through modulating the canonical and non-canonical TGF-β signaling pathways. Cetrimonium bromide can be used for DNA extraction .
|
-
- HY-144254
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor with IC50 of 2 nM. PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis in hepatocellular carcinoma models .
|
-
- HY-164413
-
|
|
VEGFR
EGFR
RET
Apoptosis
|
Cancer
|
|
CLM3, a pyrazolopyrimidine derivative, is a multiple tyrosine kinase inhibitor. CLM3 shows antiproliferative and proapoptotic activity on endothelial and cancer cells, synergistically enhanced by SN38 (HY-13704). These effects are mainly due to its inhibition of phosphorylation of VEGFR-2, EGFR and RET tyrosine kinases and their related signaling pathways .
|
-
- HY-116196
-
-
- HY-162850
-
-
- HY-113071A
-
-
- HY-170489
-
|
|
Bacterial
Fungal
Toll-like Receptor (TLR)
|
Infection
Inflammation/Immunology
|
|
Antifungal agent 123 (Compound 4b) exhibits good affinity to the oxidoreductase of Staphylococcus aureus or the membrane protein of Candida albicans, exhibits antibacterial and antifungal activities. Antifungal agent 123 scavenges free radical, exhibits antioxidant efficacy. Antifungal agent 123 inhibits the TLR signaling pathway, and exhibits anti-inflammatory efficacy .
|
-
- HY-169380
-
|
|
PINK1/Parkin
Mitophagy
|
Metabolic Disease
|
|
PARL-IN-2 (Compound 14) is a covalent inhibitor of the mitochondrial intramembrane protease PARL with an EC50 value of 0.16 μM. PARL-IN-2 leads to a robust activation of the PINK1/Parkin pathway. PARL-IN-2 promotes PINK1/Parkin-dependent mitophagy .
|
-
- HY-122534
-
|
|
Mitochondrial Metabolism
ADC Cytotoxin
Apoptosis
|
Cancer
|
|
Mensacarcin, a highly complex polyketide, strongly inhibits cell growth universally in cancer cell lines and potently induces apoptosis in melanoma cells. Mensacarcin targets to mitochondria, affects energy metabolism in mitochondria, and activates caspase-dependent apoptotic pathways. Mensacarcin, an antibiotic, can be used as a cytotoxic component of antibody-drug conjugates (ADCs) .
|
-
- HY-168903
-
|
|
STAT
|
Cancer
|
|
STAT3-IN-41 (Compound 16) is a prodrug of compound 1. STAT3-IN-41 slowly releases compound 1 inhibiting STAT3 signaling pathway. STAT3-IN-41 shows antitumor activity against lung cancer, hepatocellular carcinoma and pancreatic cancer .
|
-
- HY-142699
-
|
|
Somatostatin Receptor
|
Inflammation/Immunology
|
|
SSTR4 agonist 2 is a potent agonist of somatostatin receptor subtype 4 (SSTR4). SSTR4 pathway inhibits nociceptive and inflammatory processes. SSTR4 agonist 2 has the potential for the research of medical disorders related to SSTR4 (extracted from patent WO2014184275A1, compound 107) .
|
-
- HY-106789
-
|
CS-684
|
Bacterial
|
Infection
Inflammation/Immunology
Cancer
|
|
Plaunotol is an orally active acyclic diterpene alcohol. Plaunotol has antibacterial activity against Helicobacter pylori which causes peptic ulcer . Plaunotol inhibits tumor angiogenesis and cell proliferation. Plaunotol induces apoptosis by activation of caspase 8 and caspase 9 pathways. Plaunotol is a potential anticancer agent against colon cancer .
|
-
- HY-N11657
-
|
Sanggenone A
|
NF-κB
Keap1-Nrf2
|
Inflammation/Immunology
|
|
Sanggenon A (Sanggenone A) exerts anti-inflammatory effects by regulating NF-κB and HO-1/Nrf2 signaling pathways in BV2 and RAW264.7 cells. Sanggenon A markedly inhibits the Lipopolysaccharide (LPS; HY-D1056)-induced production of nitric oxide .
|
-
- HY-171030
-
|
|
Ferroptosis
|
Cancer
|
|
Pro-GA is a γ-Glutamylcyclotransferase (GGCT) inhibitor and a cell-permeable diester-type pro-drug with anticancer activity, GGCT is a key enzyme in glutathione metabolism and is involved in the ferroptosis pathway. Pro-GA exhibits an IC50 of 57 μM against the bladder cancer cell line T24 and can be utilized in cancer research .
|
-
- HY-N9955
-
|
|
NF-κB
p38 MAPK
NO Synthase
COX
|
Inflammation/Immunology
|
|
Isonardosinone is a nardosinone-type sesquiterpenes, which can be isolated from Valerianaceae. Isonardosinone inhibits NF-κB and MAPK signaling pathway, suppresses expression of iNOS and cyclooxygenase-2 (COX-2) in Lipopolysaccharides (HY-D1056)-induced BV2 microglia, exhibits anti-inflammatory activity .
|
-
- HY-139553A
-
|
(R)-ATI-450; (R)-CDD-450
|
Drug Isomer
|
Inflammation/Immunology
|
|
(R)-Zunsemetinib is the isomer of Zunsemetinib (HY-139553), and can be used as an experimental control. Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases .
|
-
- HY-N7128R
-
|
|
Cytochrome P450
ERK
p38 MAPK
NF-κB
MMP
PAI-1
|
Cancer
|
|
Flavanone (Standard) is the analytical standard of Flavanone. This product is intended for research and analytical applications. Flavanone is a naturally occurring flavone. Flavanone has inhibitory activity for human estrogen synthetase (aromatase). lavanone is the inhibitor for ERK/p38/NF-κB signaling pathway. Flavanone exhibits oral activity and antitumor efficacy .
|
-
- HY-N0567
-
|
Safflomin A; HSYA
|
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Hydroxysafflor yellow A (Safflomin A) is a natural product of flavonoids isolated from safflower. Hydroxysafflor yellow A can inhibit cell proliferation and promote apoptosis through the autophagy pathway. Hydroxysafflor yellow A has anti-inflammatory, antioxidant and antitumor effects. Hydroxysafflor yellow A can be used in the study of cardiovascular disease .
|
-
- HY-145584
-
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JPI-547/OCN-201
|
PARP
Apoptosis
Wnt
β-catenin
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Nesuparib (JPI-547) is an orally active PARP 1/2 and Tankyrase 1/2 inhibitor involved in the Wnt/β-catenin pathway. Nesuparib can induce cell cycle arrest and apoptosis and has anti-tumor activity. Nesuparib can be used to study cancer, neurological diseases and cardiovascular diseases .
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-
- HY-150063
-
|
|
Penicillin-binding protein (PBP)
Bacterial
|
Infection
|
|
Antibacterial agent 116 is a benzophenone-containing salicylanilide compound. Antibacterial agent 116 has potent antibacterial activity by inhibiting the peptidoglycan formation. Antibacterial agent 116 is used as a photoaffinity probe to label Acinetobacter baumannii penicillin-binding protein (PBP1b), block the propagation pathway to disrupt the growth of peptidoglycan chain .
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-
- HY-W011209
-
|
Riboprine
|
Autophagy
Endogenous Metabolite
|
Cancer
|
|
N6-Isopentenyladenosine (Riboprine), an RNA modification found in cytokinins, which regulate plant growth/differentiation, and a subset of tRNAs, where it improves the efficiency and accuracy of translation. N6-Isopentenyladenosine, an end product of the mevalonate pathway, is an autophagy inhibitor with an interesting anti-melanoma activity .
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-
- HY-149087
-
-
- HY-N8847
-
|
alpha-Ionone
|
Hippo (MST)
YAP
|
Cancer
|
|
α-Ionone (alpha-Ionone) is an activator of the olfactory receptor OR10A6. α-Ionone induces apoptosis by activating OR10A6 and increasing the phosphorylation of the LATS-YAP-TAZ signaling axis in the Hippo pathway. α-Ionone can inhibit tumor formation both in vivo and in vitro .
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-
- HY-107632
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-
- HY-116532
-
|
|
Bcl-2 Family
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Cancer
|
|
YCW-E11 is a Bcl-2, and Mcl-1 inhibitor with Ki values of 0.83 and 0.33 μM, respectively. YCW-E11 induces cell apoptosis through the mitochondrial pathway and exhibits antitumor activity. YCW-E11 can be utilized in cancer research .
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-
- HY-N13123
-
|
|
Apoptosis
|
Cancer
|
|
Tenacissoside C is an anti-cancer compound that inhibits angiogenesis. Tenacissoside C induces apoptosis in cancer cells by down-regulating the expression of anti-apoptotic factors and activating caspase-9 and caspase-3. Tenacissoside C also causes cell cycle arrest in cancer cells and induces apoptosis through the mitochondrial pathway.
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-
- HY-162351
-
|
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Emopamil Binding Protein
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Metabolic Disease
|
|
EBP-IN-1 (compound 11) is an inhibitor of emopamil-binding protein (EBP), a sterol isomerase in the cholesterol biosynthetic pathway. EBP-IN-1 has a long half-life in rodents and has good metabolic turnover and brain penetration properties. EBP-IN-1 enhances oligodendrocyte formation in human cortical organoids .
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-
- HY-101546A
-
|
(+)-Cavidine
|
COX
|
Inflammation/Immunology
|
|
Cavidine ((+)-Cavidine) is a selective COX-2 inhibitor which possesses anti-inflammatory activity. Cavidine can be used for the research of skin injuries, hepatitis, cholecystitis, and scabies. Cavidine ameliorates LPS (HY-D1056)-induced acute lung injury via NF-κB signaling pathway .
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-
- HY-16397
-
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Phenethylbiguanide
|
Mitochondrial Metabolism
AMPK
Apoptosis
|
Metabolic Disease
Cancer
|
|
Phenformin (1-phenethylbiguanide) is an orally active antidiabetic and anticancer agent. Phenformin has an incidence of associated lactic acidosis. Phenformin acts through acting AMPK activation and blocking mTOR pathway. Phenformin is also a substrate of P-glycoprotein (P-gp), and an OXPHOS inhibitor. Phenformin induces cancer cell apoptosis .
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-
- HY-125035
-
|
GNF-PF-2356
|
PAK
Apoptosis
|
Cancer
|
|
LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM. LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis .
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-
- HY-139054
-
|
|
Apoptosis
|
Cancer
|
|
4'-Methoxyflavone is a flavonoid with antioxidant properties and anti-proliferative activity against cancer cells. 4'-Methoxyflavone can inhibit cycle-dependent kinases leading to cell cycle arrest and regulate cell signaling pathways to influence cell proliferation and apoptosis. 4'-Methoxyflavone can be used in cancer chemoprevention research .
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-
- HY-173002
-
|
|
DNA Methyltransferase
|
Cancer
|
|
MS9024 is the degrader for DNA methyltransferase 1 that degrades DNMT1 in cell HCT116 through the ubiquitin-proteasome pathway with a DC50 of 35 nM (DC50 in MDA-MB-468 and H1299 is 254 nM and 101 nM). MS9024 also inhibits DNMT1 with an IC50 of 0.43 μM .
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-
- HY-19893
-
|
(+)-Antroquinonol
|
Keap1-Nrf2
|
Inflammation/Immunology
Cancer
|
|
Antroquinonol ((+)-Antroquinonol), a ubiquinone derivative from the mushroom Antrodia camphorata, has hepatoprotective, anti-inflammatory, and anti-cancer effects . Antroquinonol can be used for the research of colon cancer . Antroquinonol reduces oxidative stress by enhancing the Nrf2 signaling pathway and inhibits inflammation and sclerosis in focal segmental glomerulosclerosis mice .
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-
- HY-170027
-
|
|
HIF/HIF Prolyl-Hydroxylase
AMPK
|
Cancer
|
|
LW1564 is an inhibitor for HIF-1α with an IC50 of 1.2 µM in HepG2. LW1564 inhibits mitochondrial respiration, reduces ATP production, stimulates HIF-1α degradation, and inhibits proliferation of various cancer cells with GI50 of 0.4-4.6 μM. LW1564 activates AMPK signaling pathway and inhibits lipid synthesis. LW1564 exhibits antitumor in HepG2 xenograft mouse model .
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-
- HY-N0822R
-
|
|
Chloride Channel
Pyruvate Kinase
NF-κB
TNF Receptor
HIV
AIM2
|
Cancer
|
|
Shikonin (Standard) is the analytical standard of Shikonin. This product is intended for research and analytical applications. Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM . Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway . Shikonin decreases exosome secretion through the inhibition of glycolysis . Shikonin inhibits AIM2 inflammasome activation .
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-
- HY-13065
-
|
Corylifolinin; Isobacachalcone
|
Akt
Reactive Oxygen Species
Apoptosis
Autophagy
|
Cancer
|
|
Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM). Isobavachalcone also induces Reactive Oxyen Species (ROS) generation in OVCAR-8 cells and has exhibit cancer anti-promotive and anti-proliferative activity .
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-
- HY-151429
-
|
|
Apoptosis
Ferroptosis
Bcl-2 Family
COX
|
Cancer
|
|
Antitumor agent-77 is an antitumor agent, inhibits cancer cells growth and migration. Antitumor agent-77 triggers ferroptosis by inhibiting GPx-4 and elevating COX2. Antitumor agent-77 also activates intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and hinders Epithelial-mesenchymal transition (EMT) process of cancer cells .
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-
- HY-17514S
-
|
R51211-d5
|
Fungal
Hedgehog
Cytochrome P450
Autophagy
Antibiotic
|
Infection
Cancer
|
|
Itraconazole-d5 is the deuterium labeled Itraconazole. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects[1][2][3].
|
-
- HY-121410
-
|
|
Bacterial
Apoptosis
Parasite
NF-κB
Antibiotic
|
Infection
Cancer
|
|
Narasin is a cationic ionophore antibiotic and coccidiostat agent. Narasin inhibits NF-κB signaling and induces tumor cells apoptosis. Narasin has antimicrobial, antiviral anticancer activity. Narasin inhibits tumor metastasis and growth of ERα‑positive breast cancer cells by inactivation of the TGF-β/SMAD3 and IL‑6/STAT3 signaling pathways .
|
-
- HY-N12044
-
|
|
Apoptosis
|
Cancer
|
|
Asparanin A is an apoptosis inducer with anticancer activity. Asparanin A induces cell cycle arrest in the G0/G1 phase through mitochondria and PI3K/AKT signaling pathways, inhibiting cancer cell growth. Asparanin A also demonstrated in vivo efficacy in a mouse xenograft model of Ishikawa endometrial carcinoma, significantly inhibiting tumor growth .
|
-
- HY-151428
-
|
|
Ferroptosis
Apoptosis
Bcl-2 Family
COX
|
Cancer
|
|
Antitumor agent-78 is an antitumor agent, inhibits cancer cells growth and migration. Antitumor agent-78 triggers ferroptosis by inhibiting GPx-4 and elevating COX2. Antitumor agent-78 also activates intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and hinders Epithelial-mesenchymal transition (EMT) process of cancer cells .
|
-
- HY-168023
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NOD1/-IN-1 (Compound 2) is a potent RIPK2 inhibitor with an IC50 value of 0.65 nM determined by ADP-Glo assays. NOD1/-IN-1 selectively inhibits the NOD1 pathway (with an IC50 of 33 nM for NOD1), blocking the production of pro-inflammatory cytokines and thereby reducing inflammation. NOD1/-IN-1 is applicable for research in the field of colitis .
|
-
- HY-159718
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NLRP3-IN-46 (Compound 3k) activates neuro-immunomodulatory cholinergic anti-inflammatory pathway, and thus inhibits NLRP3 inflammasome activation. NLRP3-IN-46 inhibits Uric acid sodium (HY-B2130A)-induced IL-1β production in THP-1 cells, and can be used in gouty arthritis research .
|
-
- HY-135317
-
|
CA-4948
|
IRAK
Apoptosis
FLT3
NF-κB
MyD88
|
Inflammation/Immunology
Cancer
|
|
Emavusertib is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib exhibits antitumor activity in mouse model
|
-
- HY-P1036
-
|
|
Complement System
|
Others
|
|
Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates’ complement system. Compstatin exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .
|
-
- HY-164041
-
|
|
PKC
|
Others
|
|
Staurosporine-Boc, a natural product isolated from the actinomyces Streptomyces staurosporeus, is a potent non-selective inhibitor of protein kinase. Staurosporine-Boc inhibits a variety of protein kinases, including protein kinase C (PKC), tyrosine kinase, and serine/threonine kinase. Because of its broad inhibition profile, Staurosporine-Boc is widely used as a tool compound in biological research, especially when studying cell signaling pathways .
|
-
- HY-B0097
-
|
5-Fluorouracil 2'-deoxyriboside
|
Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
Bacterial
CMV
HSV
Apoptosis
|
Infection
Cancer
|
|
Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis . Floxuridine has antiviral effects against HSV and CMV .
|
-
- HY-170765
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
ATX-IN-1 (compound 35) is an inhibitor of ATX (IC50=0.7 nM) with anti-inflammatory activity. ATX-IN-1 can inhibit TGF-β/Smad pathway and reduce collagen deposition to alleviate Bleomycin (HY-108345)-induced fibrosis in mice. ATX-IN-1 has good oral bioavailability (F=69.5%) and particle stability .
|
-
- HY-142160
-
|
|
Raf
|
Cancer
|
|
GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits Ki values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers .
|
-
- HY-101024
-
|
|
JAK
STAT
|
Inflammation/Immunology
|
|
PF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively. PF-06263276 inhibits pSTAT3 and TYK2 pathway. PF-06263276 has a protective effect against ear skin inflammation .
|
-
- HY-157740
-
|
|
HDAC
|
Cancer
|
|
XSJ-10 is a HDAC inhibitor containing a RAS/RAF protein interfering unit, with IC50s of 0.05 and 0.04 μM in PANC-1 cells and HT-29 cells. XSJ-10 can effectively induce the apoptosis of cancer cells and suppress the tumor by strongly inhibiting the RAS-RAF-MEK-ERK signaling pathway and the acetylation level of HDAC3 .
|
-
- HY-115822
-
|
|
Amino Acid Decarboxylase
Glutathione S-transferase
|
Metabolic Disease
|
|
α-Fluoromethylhistidine dihydrochloride is a potent irreversible inhibitor of histidine decarboxylase (HDC) and glutathione S-transferase, demonstrating significant potential in studying histidine metabolism and drug metabolism processes. α-Fluoromethylhistidine dihydrochloride offers an effective approach to inhibit enzymes involved in these metabolic pathways. α-Fluoromethylhistidine dihydrochloride has implications for drug development by revealing off-target effects that may influence physiological drug metabolism and elimination mechanisms.
|
-
- HY-18285
-
|
|
Casein Kinase
ERK
CDK
|
Cancer
|
|
Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of 5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively .
|
-
- HY-16146
-
|
OXi-4503 tetrasodium
|
Microtubule/Tubulin
|
Cancer
|
|
Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a proagent of Combretastatin A-1, is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 phosphate tetrasodium inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 phosphate tetrasodium exhibits anti-tumor and anti-vascular effects .
|
-
- HY-P3434A
-
|
|
Pyroptosis
|
Inflammation/Immunology
|
|
Ac-FEID-CMK TFA is a potent zebrafish-specific GSDMEb-derived peptide inhibitor.
Ac-FEID-CMK TFA can attenuate the mortality and kidney injury during septic shock. Ac-FEID-CMK TFA inhibits pyroptosis and attenuates septic AKI (acute kidney injury) in vivo. Ac-FEID-CMK TFA can suppress the caspy2-mediated noncanonical inflammasome pathway .
|
-
- HY-N4314
-
|
4',5,6,7-Tetramethoxyflavone
|
Bacterial
COX
NO Synthase
NF-κB
|
Infection
Inflammation/Immunology
Cancer
|
|
Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is a bioactive compound extracted from Eupatorium odoratum. Scutellarein tetramethyl ether exhibits anti-inflammatory, antibacterial, pro-coagulant, and anti-tumor activities. Scutellarein tetramethyl ether exerts its anti-inflammatory effects by modulating the NF-κB pathway and regulates bacterial resistance through the inhibition of efflux pumps. Additionally, Scutellarein tetramethyl ether accelerates coagulation time via the endogenous coagulation pathway. Studies have shown that Scutellarein tetramethyl ether can effectively inhibit the growth of the liver cancer cell line HepG2 (IC50= 20.08 μg/mL) .
|
-
- HY-N0563
-
|
|
AMPK
VEGFR
PI3K
Akt
NF-κB
Cytochrome P450
|
Cardiovascular Disease
Cancer
|
|
Alizarin is a natural dye. Alizarin can be extracted from the roots of madder plant. Alizarin activates AMPK and VEGFR2/eNOS pathway. Alizarin regulates PI3K/Akt and inhibits NF-κB pathway. Alizarin enhances CYP1A1 enzyme activity. Alizarin has protective effects on hypertension and vascular endothelial dysfunction. Alizarin has anti-tumor activity against multiple cancers including pancreatic cancer, breast cancer, osteosarcoma and liver cancer. Alizarin has been widely used as a pigment in textile fabrics and paintings .
|
-
- HY-104044A
-
|
BGB-290 maleate
|
Apoptosis
|
Neurological Disease
|
|
Pamiparib maleate (BGB-290 maleate) is a highly potent and selective PARP inhibitor with neurotoxicity-inducing activity. Pamiparib maleate can effectively penetrate the blood-brain barrier and cause cerebral hemorrhage, brain atrophy, and movement disorders in zebrafish embryos exposed. Pamiparib maleate exposure downregulates the activities of acetylcholinesterase (AChE) and adenosine triphosphatase (ATPase) and leads to upregulation of oxidative stress, which triggers apoptosis and interferes with the expression of neurodevelopment-related genes. The use of pamiparib maleate is also accompanied by downregulation of the Notch signaling pathway, while activation of the Notch signaling pathway can partially rescue neurodevelopmental toxicity. Therefore, pamiparib maleate provides a reference for evaluating its potential neurotoxicity during embryonic development .
|
-
- HY-N2037A
-
|
Norcoclaurine hydrochloride
|
MAP3K
MDM-2/p53
ROS Kinase
Apoptosis
|
Infection
Cardiovascular Disease
Endocrinology
Cancer
|
|
Higenamine hydrochloride is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine (Norcoclaurine) can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine hydrochloride protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine hydrochloride can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .
|
-
- HY-106263B
-
|
|
PTEN
PDK-1
MDM-2/p53
Apoptosis
Akt
|
Cancer
|
|
Tyroserleutide hydrochloride is a tripeptide isolated from the degradation products of porcine spleen with antitumor activity. Tyroserleutide hydrochloride can upregulate the expression of the tumor suppressor gene PTEN and inhibit the activity of AKT and PDK1. Tyroserleutide hydrochloride inhibits tumor cell proliferation and MDM2 phosphorylation by inhibiting the PI3K/AKT pathway, and also upregulates P21, P27, P53, and induces mitochondrial damage and cell apoptosis .
|
-
- HY-N6739
-
|
|
Bacterial
Apoptosis
Fungal
PI3K
Akt
TNF Receptor
Interleukin Related
|
Infection
Cancer
|
|
Beauvericin is a cyclohexapeptide Fusarium toxin with insecticidal, antibacterial, anticancer, antiviral and cytotoxic activities. Beauvericin causes cellular genotoxicity by producing DNA breaks, chromosomal aberrations and micronuclei, and inhibits the PI3K/AKT pathway to induce apoptosis, thereby inhibiting the growth of HCC. In addition, Beauvericin affects immune function by inhibiting lymphocyte proliferation and interfering with the differentiation process of human monocytes into macrophages .
|
-
- HY-128033R
-
|
|
Fungal
|
Infection
|
|
Fenpropimorph (Standard) is the analytical standard of Fenpropimorph. This product is intended for research and analytical applications. Fenpropimorph is a fungicide that inhibits the sterol pathway. Fenpropimorph inhibits δ8-δ7-sterol isomerase in yeast at low concentrations, with δ14-sterol reductase being blocked at higher levels, preventing the biosynthesis of ergosterol. Fenpropimorph also inhibits sterol synthesis in certain plants and mammalian cells .
|
-
- HY-108538
-
|
|
Glutathione S-transferase
NF-κB
Calcium Channel
|
Inflammation/Immunology
|
|
Ethacrynic acid D5 is a deuterium labeled Ethacrynic acid. Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice .
|
-
- HY-145025
-
|
|
ERK
|
Inflammation/Immunology
Cancer
|
|
ERK1/2 inhibitor 3 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 3 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2021218912A1, compound 1) .
|
-
- HY-168968S
-
|
|
EGFR
Histone Demethylase
|
Cancer
|
|
ZJY-54 is an orally active dual-target inhibitor of EGFR/LSD1, with IC50 values of 3.8 nM and 0.6 μM, respectively. ZJY-54 can inhibit the proliferation of non-small cell lung cancer cells, induce the accumulation of H3K4me2 and H3K9me2, and inhibit the phosphorylation of the EGFR signaling pathway. ZJY-54 has anti-tumor activity .
|
-
- HY-B0093AR
-
|
CGS14824A (Standard)
|
Angiotensin-converting Enzyme (ACE)
Apoptosis
Reactive Oxygen Species
Akt
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
Benazepril hydrochloride (Standard) is the analytical standard of Benazepril hydrochloride. This product is intended for research and analytical applications. Benazepril hydrochloride is an orally active angiotensin-converting enzyme (ACE) inhibitor to reduce angiotensin-II production. Benazepril hydrochloride inhibits oxidative stress and inhibits apoptosis by the PI3K/Akt signaling pathway. In addition, Benazepril hydrochloride improves diabetic nephropathy and decreases proteinuria. Benazepril hydrochloride can be used in the study of hypertension, heart failure and diabetic nephropathy .
|
-
- HY-124858
-
|
|
STAT
JAK
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 docks into the ATP-binding pocket of JAK2. SC99 inhibits phosphorylation of JAK2 and STAT3 with no effects on the other kinases associated with STAT3 signaling. SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities .
|
-
- HY-120646
-
|
|
PD-1/PD-L1
|
Others
|
|
BMS-242 is a small molecule PD-1/PD-L1 inhibitor with the activity of inhibiting the PD-1/PD-L1 interaction. BMS-242 can bind to the hydrophobic channel pocket between PD-L1 molecules, inhibit the PD-1/PD-L1 immune checkpoint pathway, and provide a new way for cancer inhibition.
|
-
- HY-168893
-
|
|
Src
Apoptosis
IAP
Survivin
Akt
mTOR
JAK
STAT
Ras
p38 MAPK
|
Cancer
|
|
K882 (Compound 4e) is a Src inhibitor, with KD of 0.315 μM. K882 induces Apoptosis. K882 inhibits XIAP and Survivin. K882 inhibits the activation of PI3K/Akt/mTOR, Jak1/Stat3, Ras/MAPK signaling pathways. K882 shows anti-tumor activity against non-small cell lung cancer .
|
-
- HY-17514R
-
|
|
Fungal
Hedgehog
Cytochrome P450
Autophagy
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Itraconazole (Standard) is the analytical standard of Itraconazole. This product is intended for research and analytical applications. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor .
|
-
- HY-149472
-
|
|
NF-κB
PI3K
|
Inflammation/Immunology
|
|
Anti-osteoporosis agent-4 (Compound 11h) inhibits differentiation of primary osteoclasts. Anti-osteoporosis agent-4 attenuates RANKL-induced osteoclastogenesis. Anti-osteoporosis agent-4 inhibits osteoclast formation with an IC50 value of 358.29 nM. Anti-osteoporosis agent-4 inhibits PI3K/AKT and IκBα/NF-κB signaling pathway activation .
|
-
- HY-145028
-
|
|
ERK
|
Inflammation/Immunology
Cancer
|
|
ERK1/2 inhibitor 6 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 6 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2021063335A1, compound 1) .
|
-
- HY-112440
-
|
Methuosis inducer 1
|
Others
|
Cancer
|
|
HZX-02-059 is a potent methuosis inducer and dual-target PIKfyve/tubulin inhibitor with anticancer activity. Methuosis mainly disrupts the balance of endocytosis and exocytosis, forming a large number of vesicles and inducing cell death. HZX-02-059 also induces cell vacuolization, promotes apoptosis, downregulates the p53 pathway, inhibits PI3K/AKT phosphorylation, and inhibits c-Myc and NF-κB transcription .
|
-
- HY-163479
-
|
|
Eukaryotic Initiation Factor (eIF)
MNK
|
Cancer
|
|
MNK1/2-IN-7 (compound 20j) is an orally available inhibitor of MNK1/2 with anticancer activity and hERG safety. MNK1/2-IN-7 also inhibits the phosphorylation of eIF4E, inhibiting the MNK/eIF4E signaling pathway and cancer cell proliferation. MNK1/2-IN-7 is synergistic with Ibrutinib (HY-109970) .
|
-
- HY-163538
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
TYM-3-98 is a selective inhibitor for PI3Kδ, with an IC50 of 7.1 nM. TYM-3-98 inhibits proliferationso of B-lymphoma cells. TYM-3-98 inhibits PI3K/AKT/mTOR signaling pathway through induction of apoptosis. TYM-3-98 exhibits good pahrmacokinetic characters and antitumor efficacy in mouse/rat model, without significant toxicity .
|
-
- HY-100355
-
|
|
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
C18-Ceramide is a bioactive molecule with multiple functions in cells, not a traditional agonist or inhibitor targeting a single site. It can act on multiple cellular targets, such as proteins related to endoplasmic reticulum stress (e.g., ATF-4, XBP-1, CHOP), proteins in the PI3K/AKT signaling pathway, and SNARE complex proteins. It exerts activities like inducing cell death, promoting autophagy, and regulating exocytosis through mechanisms such as activating endoplasmic reticulum stress, inhibiting the PI3K/AKT signaling pathway, and affecting lipid raft - related functions. It can be used in research on the mechanism of neuronal injury in the field of neuroscience and in the treatment research of cancers such as glioma in the field of oncology .
|
-
- HY-N0255
-
|
α-Hederin
|
Apoptosis
|
Others
Cancer
|
|
alpha-Hederin (α-Hederin), a monodesmosidic triterpenoid saponin, exhibits promising antitumor potential against a variety of human cancer cell lines. alpha-Hederin could inhibit the proliferation and induce apoptosis of gastric cancer accompanied by glutathione decrement and reactive oxygen species generation via activating mitochondrial dependent pathway .
|
-
- HY-14664AR
-
|
|
HMG-CoA Reductase (HMGCR)
Autophagy
Ferroptosis
|
Cardiovascular Disease
Cancer
|
|
Fluvastatin (sodium) (Standard) is the analytical standard of Fluvastatin (sodium). This product is intended for research and analytical applications. Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin sodium protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
|
-
- HY-107553
-
|
|
HSP
Apoptosis
|
Cancer
|
|
Chetomin, an active component of Chaetomium globosum, is a heat shock protein 90/hypoxia-inducible factor 1 alpha (Hsp90/HIF1α) pathway inhibitor. Chetomin is a potent, nontoxic non-small cell lung cancer cancer stem cells (NSCLC CSC)-targeting molecule .
|
-
- HY-B1971
-
-
- HY-150755
-
|
|
Topoisomerase
COX
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Topo I/COX-2-IN-2 (Compound W10) is a potent dual-target inhibitor of Topo I and COX-2 with IC50 values of 0.90 μM and 2.31 μM, respectively. Topo I/COX-2-IN-2 induces cancer cell apoptosis through the mitochondrial pathway .
|
-
- HY-126248
-
|
|
PARP
|
Cancer
|
|
Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model .
|
-
- HY-B0497CR
-
|
|
STAT
Parasite
Antibiotic
|
Infection
Cancer
|
|
Crocin (Standard) is the analytical standard of Crocin. This product is intended for research and analytical applications. Crocin (Crocin I) is an orally active natural product that can be isolated from the stigma of Crocus sativus. Crocin inhibits tumor cell proliferation and promotes apoptosis through JAK pathway. Crocin has anti-inflammatory, antioxidant and antitumor activities .
|
-
- HY-N2095
-
|
Atractylon
|
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
Atractylone (Atractylon) is a sesquiterpenoid extracted from Atractylodis Rhizoma. Atractylone (Atractylon) alleviates influenza A virus (IAV)-induced lung injury via regulating the TLR7 signaling pathway, and acts as a promising agent for IAV treatment. Atractylone (Atractylon) inhibits the degranulation of mast cell and exhibits potential for the treatment of mast cell-mediated allergic reactions .
|
-
- HY-P0119
-
|
|
GCGR
MEK
Akt
MMP
JNK
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Lixisenatide is a GLP-1 receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of proinflammatory cytokines, and blocks of cellular signaling pathways. Lixisenatide decreases atheroma plaque size and instability in Apoe −/− Irs 2+/− mice by reprogramming macrophages towards an M2 phenotype, which leads to reduced inflammation .
|
-
- HY-168951
-
|
|
Annexin A
Apoptosis
|
Cancer
|
|
(R)-SL18 is a degrader of ANXA3 and can degrade ANXA3 protein through the ubiquitination pathway. (R)-SL18 inhibits the proliferation, migration, invasion, and colony formation of breast cancer cells and induces apoptosis. (R)-SL18 can be used in the research of triple-negative breast cancer .
|
-
- HY-155747
-
|
|
Autophagy
Akt
mTOR
|
Cancer
|
|
FDW028 a potent and highly selective FUT8 inhibitor. FUT8 exhibits potent anti-tumor activity by defucosylation and impelling lysosomal degradation of B7-H3 through the chaperone-mediated autophagy (CMA) pathway. FDW028 can be used for metastatic colorectal cancer (mCRC) research .
|
-
- HY-133556
-
|
|
AMPK
|
Metabolic Disease
|
|
IQZ23 inhibits adipocyte differentiation via AMPK pathway activation. IQZ23 exerts a high efficacy in decreasing the triglyceride level (EC50=0.033 μM) in 3T3-L1 adipocytes. IQZ23 could be used for the research of obesity and related metabolic disorders .
|
-
- HY-W042416
-
|
DMAc
|
NF-κB
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
N,N-Dimethylacetamide (DMAc) is an organic solvent with blood-brain transmissibility and an FDA-approved drug excipient. N, N-dimethylacetamide exerts anti-inflammatory activity by inhibiting the NF-κB signaling pathway. N, N-dimethylacetamide can be used in studies of weight gain caused by a high-fat diet and neuroinflammation in Alzheimer's disease .
|
-
- HY-B0185
-
|
Lignocaine
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence . Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia .
|
-
- HY-19528S
-
|
SAH (S-Adenosylhomocysteine)-d4
|
Endogenous Metabolite
|
Metabolic Disease
|
|
SAH-d4 is the deuterium labeled SAH. SAH (S-Adenosylhomocysteine) is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine[1]. SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 µM[2].
|
-
- HY-141523
-
|
RMC-4630; SHP2-IN-7
|
SHP2
Phosphatase
|
Cancer
|
|
Vociprotafib (RMC-4630) is an orally active, selective and potent phosphatase SHP2 inhibitor, which blocks activation of the RAS-RAF-MEK-ERK signaling pathway with antitumor activity. Vociprotafib accelerates the time to, and increases the magnitude of, tumor regressions in Osimertinib (HY-15772)-sensitive EGFR-mutant tumors of mice .
|
-
- HY-129236
-
|
|
Na+/K+ ATPase
Apoptosis
|
Cancer
|
|
Hellebrin is a bufadienolide compound extracted from plants that can inhibit tumor cell growth. Hellebrigenin shows potential in overcoming cancer cells' resistance to apoptosis stimuli and has also demonstrated anti-proliferation effects in multidrug-resistant (MDR) cancer cell models. Hellebrin can act on Na+/K+-ATPase to regulate intracellular signaling pathways .
|
-
- HY-112801
-
|
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
|
Cancer
|
|
F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALK WT, ROS1 WT, ALK L1196M and ALK G1202R, respectively .
|
-
- HY-118032
-
|
|
Apoptosis
Autophagy
JNK
ERK
|
Cancer
|
|
Bozepinib is a PKR (RNA-dependent protein kinase) activator and potently inhibits the HER-2 signaling pathway as well as JNK and ERK kinases. Bozepinib induces PKR-mediated apoptosis and synergizes with IFNα to trigger apoptosis, autophagy and senescence. Bozepinib also demonstrates in vivo antitumor and antimetastatic efficacy in xenografted nude mice .
|
-
- HY-N3071
-
|
|
Apoptosis
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Picrasidine I is an anti-inflammatory and anti-osteoclastogenic dimeric alkaloid that can be isolated from Picrasma quassioides. Picrasidine I inducs cell cycle arrest, and triggers cell apoptosis by downregulats ERK and Akt pathways. Picrasidine I inhibits the activation of MAPKs, NF-κB and ROS generation, and suppresses the expression of c-Fos and NFATc1 .
|
-
- HY-N0284
-
|
|
PI3K
Akt
|
Inflammation/Immunology
Cancer
|
|
Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities .
|
-
- HY-B0464R
-
|
|
Bcl-2 Family
Caspase
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Hydralazine (hydrochloride) (Standard) is the analytical standard of Hydralazine (hydrochloride). This product is intended for research and analytical applications. Hydralazine hydrochloride is an antihypertensive agent. Hydralazine hydrochloride can inhibit mitochondrial fission and human peritoneal mesothelial cell proliferation. Hydralazine hydrochloride has immunomodulation and anti-migratory effect. Hydralazine hydrochloride activates the intrinsic pathway of apoptosis and causes DNA damage .
|
-
- HY-134245
-
|
Tubercidin 5'-phosphate; 7-Deaza-AMP
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
7-Deazaadenosine 5'-phosphate (Tubercidin 5'-phosphate; 7-Deaza-AMP) is a potential substrate or competitive inhibitor of enzymes that interact with 5′-adenylic acid monophosphate. As a nucleotide derivative, 7-Deazaadenosine 5'-phosphate can regulate cellular functions by affecting intracellular signaling pathways, especially in signaling involving AMP .
|
-
- HY-100538A
-
|
|
DNA/RNA Synthesis
JNK
|
Cancer
|
|
DTP3 TFA is a potent and selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway .
|
-
- HY-N0697R
-
|
|
Endogenous Metabolite
JAK
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Crocin (Standard) is the analytical standard of Crocin. This product is intended for research and analytical applications. Crocin (Crocin I) is an orally active natural product that can be isolated from the stigma of Crocus sativus. Crocin inhibits tumor cell proliferation and promotes apoptosis through JAK pathway. Crocin has anti-inflammatory, antioxidant and antitumor activities .
|
-
- HY-N0717
-
|
Valine
|
Bacterial
Arginase
Akt
|
Infection
|
|
L-Valine (Valine) is a new nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
|
-
- HY-13968
-
JW 55
3 Publications Verification
|
PARP
|
Cancer
|
|
JW 55 is a potent and selective β-catenin signaling pathway inhibitor, which functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). JW 55 decreases auto-PARsylation of TNKS1/2 in vitro with IC50s of 1.9 μM and 830 nM respectively.
|
-
- HY-P99618
-
|
IBI-315; BH2950
|
EGFR
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
Fidasimtamab (IBI-315; BH2950) is a recombinant human IgG1 bispecific antibody that targets, binds and inhibits both HER2 and PD-1 and their downstream signalling pathways, and links PD-1 expressing T cells to HER2 expressing tumour cells. Fidasimtamab has potential immunosuppressive and antitumor activity .
|
-
- HY-170989
-
|
|
Epigenetic Reader Domain
Autophagy
|
Cancer
|
|
BRD4 degrader-5 (Compound 23) is a hydrophobic tag (HyTag)-based protein degrader for BRD4 (DC50 = 24.7 μM) through ER stress and autophagy-lysosome pathway. BRD4 degrader-5 inhibits the proliferation of cancer cell 4T1 with an IC50 of 20.6 μM .
|
-
- HY-N13164
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
Polygalacin D3 is a triterpenoid saponin compound that can be extracted from the roots of the balloon flower. Polygalacin D3 can inhibit the proliferation of non-small cell lung cancer (NSCLC) cell lines by blocking the PI3K/Akt pathway, and it induces cell cycle arrest and cell apoptosis .
|
-
- HY-N1381
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Periplocin is a cardiotonic steroid isolated from root-bark Periploca sepium Bunge. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase .
|
-
- HY-169190
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-53 (compound B3) is an inhibitor targeting PD-1/PD-L1 and VISTA signaling pathways. PD-1/PD-L1-IN-53 can be used in anti-cancer research .
|
-
- HY-146971
-
|
|
NO Synthase
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 38 (compound 23d) is a potent Nrf2/HO-1 pathway inhibitor, with an IC50 value of 0.38 μM for NO. Anti-inflammatory agent 38 can significantly reduce the level of ROS in cells. Anti-inflammatory agent 38 can be used for researching anti-inflammatory .
|
-
- HY-160514
-
|
|
Phosphatase
|
Metabolic Disease
|
|
LXQ46 is an orally active inhibitor for protein tyrosine phosphatase 1B (PTP1B), with an IC50 of 0.190 μM. LXQ46 enhances insulin and leptin signaling pathways in insulin-resistant C2C12. LXQ46 ameliorates type 2 diabetes and increases insulin tolerance in mouse models .
|
-
- HY-161816
-
|
|
Apoptosis
Autophagy
PI3K
Akt
|
Cancer
|
|
PI3K/AKT-IN-3 (compound 8C) can induce autophagy and apoptosis by inhibiting the PI3K/AKT signaling pathway. PI3K/AKT-IN-3 can be used in cancer research .
|
-
- HY-N2963
-
|
|
ERK
p38 MAPK
JAK
STAT
TNF Receptor
Interleukin Related
COX
Arginase
|
Inflammation/Immunology
|
|
Broussonin E is a phenolic compound and shows anti-inflammatory activity. Broussonin E can suppress inflammation by modulating macrophages activation statevia inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway. Broussonin E can be used for the research of inflammation-related diseases such as atherosclerosis .
|
-
- HY-N6704
-
|
|
ERK
Apoptosis
|
Cancer
|
|
Enniatin A1 isolated from Fusarium mycotoxins is a cyclic hexadepsipeptide consisting of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids. Enniatin A1 possesses anticarcinogenic properties by induction of apoptosis and disruption of ERK signalling pathway. Enniatin A1 inhibits ACAT with an IC50 of 49 μM in rat liver microsomes .
|
-
- HY-N0072R
-
|
|
Apoptosis
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Brazilin (Standard) is the analytical standard of Brazilin. This product is intended for research and analytical applications. Brazilin is a red dye precursor obtained from the heartwood of several species of tropical hardwoods. Brazilin inhibits the cells proliferation, promotes apoptosis, and induces autophagy through the AMPK/mTOR pathway. Brazilin shows chondroprotective and anti-inflammatory activities .
|
-
- HY-115902
-
|
|
FGFR
Apoptosis
|
Cancer
|
|
FGFR4-IN-7 (Compound C3) is a covalent reversible FGFR4 inhibitor with an IC50 value of 0.42 μM. FGFR4-IN-7 induces apoptosis via the FGFR4 signaling pathway blockage. FGFR4-IN-7 can be used for the research of hepatocellular carcinoma (HCC) .
|
-
- HY-N0047
-
|
|
JNK
mTOR
Akt
PDK-1
Autophagy
Apoptosis
|
Cancer
|
|
Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis .
|
-
- HY-12068
-
|
XL-147 derivative 1
|
PI3K
|
Cancer
|
|
PI3K-IN-1 (XL-147 derivative 1) is a potent inhibitor of PI3K. PI3K-IN-1 (25 μM) blocks PI3K/Akt signaling pathways .
|
-
- HY-14621
-
|
Vanillylacetone; Gingerone
|
NF-κB
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Zingerone (Vanillylacetone) is a nontoxic methoxyphenol isolated from Zingiber officinale, with potent anti-inflammatory, antidiabetic, antilipolytic, antidiarrhoeic, antispasmodic and anti-tumor properties . Zingerone alleviates oxidative stress and inflammation, down-regulates NF-κB mediated signaling pathways . Zingerone acts as an anti-mitotic agent, and inhibits the growth of neuroblastoma cells .
|
-
- HY-149205
-
|
|
PI3K
ERK
|
Inflammation/Immunology
|
|
CXJ-2 is a cyclic peptide, and exhibits moderate affinity toward elastin derived peptides (EDPs). CXJ-2 exhibits potent activities to inhibit the PI3K/ERK pathway and decrease hepatic stellate cell proliferation and migration. CXJ-2 possesses potent antifibrotic efficacy .
|
-
- HY-147770
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
NF-κB-IN-6 (Compound 3d) is an anti-inflammatory agent through the mechanism of decreasing the protein expressions of iNOS and COX-2 by suppressing NF-κB signaling pathway. NF-κB-IN-6 inhibits NO production in LPS-induced RAW264.7 cells with an IC50 of 23.1 μM .
|
-
- HY-P5559
-
|
|
PROTACs
|
Cancer
|
|
ND1-YL2 is a PROTAC that selectively degrades SRC-1 via the N-degron pathway. ND1-YL2 significantly inhibits cancer invasion and migration in vitro and in vivo. ND1-YL2 can be used in cancer research .
|
-
- HY-B0185B
-
|
Lignocaine hydrochloride hydrate
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Lidocaine (Lignocaine) hydrochloride hydrate inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride hydrate decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride hydrate is an amide derivative and has potential for the research of ventricular arrhythmia .
|
-
- HY-17595R
-
|
|
Parasite
Apoptosis
Microtubule/Tubulin
|
Infection
Cancer
|
|
Mebendazole (Standard) is the analytical standard of Mebendazole. This product is intended for research and analytical applications. Mebendazole is a highly effective, broad-spectrum antihelmintic against nematode infestations. Mebendazole also exhibits inhibitory effect against glioblastoma multiforme (GBM), inhibits Hedgehog pathway and tubulin polymerization. Mebendazole is orally active and can cross CNS penetration .
|
-
- HY-N0405
-
|
|
TNF Receptor
Interleukin Related
|
Neurological Disease
Cancer
|
|
Orientin is a neuroprotective agentinhibits which has anti-inflammation, anti-oxidative, anti-tumor, and cardio protection properties. Orientin inhibits the levels of IL-6, IL-1β and TNF-α. Orientin increases IL-10 level. Orientin exhibits neuroprotective effect by inhibits TLR4 and NF-kappa B signaling pathway. Orientin can used in study neuropathic pain .
|
-
- HY-B0185AS1
-
|
Lignocaine-d6 hydrochloride
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Lidocaine-d6 (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor[2].
|
-
- HY-110070
-
|
2-Amino-4-phosphonobutyric acid sodium
|
mGluR
|
Others
Neurological Disease
|
|
DL-AP4 sodium (2-Amino-4-phosphonobutyric acid sodium) is an agonist for metabotropic glutamate receptors (mGluR). DL-AP4 sodium binds to mGluR4, activates the signaling pathway that is negatively correlated with adenylate cyclase, and inhibits the Forskolin (HY-15371)-induced production of cAMP. DL-AP4 sodium is also an inhibitor for ON channel, that reduces the sensitivity of photoreceptors to brightness changes .
|
-
- HY-W005379
-
|
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
DGM is an inhibitor of the TGF-β1/Smad signaling pathway with significant antifibrotic effects. DGM inhibits the epithelial-mesenchymal transition (EMT) process in alveolar epithelial cells and slows the progression of pulmonary fibrosis in vivo by reducing lung inflammation, improving lung function, and decreasing extracellular matrix (ECM) remodeling. DGM can be used in research on idiopathic pulmonary fibrosis (IPF) and EMT-related diseases .
|
-
- HY-W438351
-
|
|
RANKL/RANK
|
Metabolic Disease
|
|
1,3-Dibenzyl-5-fluorouracil is a chemical inhibitor of osteoclastogenesis. 1,3-Dibenzyl-5-fluorouracil inhibits the expression of osteoclast markers by downregulating the receptor activator of NF-κB ligand (RANKL) and macrophage colony-stimulating factor (M-CSF) signaling pathways. 1,3-Dibenzyl-5-fluorouracil can be used in the study of metabolic bone diseases .
|
-
- HY-168328
-
|
|
NF-κB
Interleukin Related
|
Inflammation/Immunology
|
|
FKK6 is a selective agonist for pregnane X receptor (PXR) with an EC50 of 1.2 µM. FKK6 exhibits good affinity with plasma proteins, and good metabolic metabolism in human microsomes. FKK6 inhibits PXR-related NF-κB signaling pathway, inhibits the expression of inflammatory factors, and exhibits anti-inflammatory activity against DSS (HY-116282)-induced colitis in mouse model .
|
-
- HY-111172
-
|
|
MMP
NF-κB
|
Cancer
|
|
Inotilone is an inhibitor of matrix metalloproteinase MMP-2 and MMP-9, to against metastatic in lung cancer cells. Inotilone enhances the activity of the antioxidant enzymes to support its anti-metastatic activity. Inotilone also inhibits IκBα phosphorylation and NFκB p65 nuclear translocation, involving in FAK, PI3K/AKT, MAPKs and NFκB pathways .
|
-
- HY-124284
-
-
- HY-113618A
-
|
|
CRAC Channel
Interleukin Related
|
Cardiovascular Disease
|
|
RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 hydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 hydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways .
|
-
- HY-P1036A
-
|
|
Complement System
|
Others
|
|
Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin TFA binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin TFA inhibits only the activation of primates’ complement system. Compstatin TFA exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .
|
-
- HY-12873
-
|
|
Ras
p38 MAPK
JNK
|
Cancer
|
|
RBC8 is a selective and allosteric RALA and RALB inhibitor. RBC8 stabilizes the inactive GDP-bound state of Ral, preventing its activation. RBC8 promotes the phosphorylation of proteins related to the MAPK/JNK pathway. RBC8 has the activity of inhibiting tumor cell proliferation, migration and invasion. RBC8 is used in the study of various cancers such as lung cancer, gastric cancer, and multiple myeloma .
|
-
- HY-107466
-
|
|
MDM-2/p53
|
Cancer
|
|
WK298 is a potent inhibitor of the MDM2/MDMX-p53 interaction with good anti-tumor activity. WK298 can fully activate the p53 pathway by inhibiting the binding of MDM2 and MDMX to p53. The development of WK298 benefited from a deep understanding of the key elements of the p53-MDM2/MDMX interaction structure .
|
-
- HY-128570
-
|
|
Complement System
|
Inflammation/Immunology
|
|
FD-IN-1 (Compound 12) is an orally bioavailable and selective factor D (FD) inhibitor with an IC50 of 12 nM. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system. FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC50s of 7.7 and 6.5 µM, respectively .
|
-
- HY-137381
-
|
N6-Benzoyl-cAMP
|
Potassium Channel
|
Others
|
|
6-Bnz-cAMP (N6-Benzoyl-cAMP), a derivative of cyclic adenosine monophosphate (cAMP), is a potent inhibitor of the bTREK-1 potassium channel. 6-Bnz-cAMP can strongly inhibit the bTREK-1 potassium channel through a protein kinase A (PKA) independent mechanism. 6-Bnz-cAMP can be used to explore potential signal transduction proteins in the cAMP signaling pathway .
|
-
- HY-I0447AR
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Sodium 4-aminosalicylate (dihydrate) (Standard) is the analytical standard of Sodium 4-aminosalicylate (dihydrate). This product is intended for research and analytical applications. Sodium 4-aminosalicylate (Sodium para-Aminosalicylic acid) dihydrate is para-aminosalicylic acid (PAS), a dihydrofolate reductase (DHFR) inhibitor and antituberculous agent. PAS is incorporated into the folate pathway via dihydropteroate synthase (DHPS) and dihydrofolate synthase (DHFS) to generate the hydroxydihydrofolate antimetabolite, which in turn inhibits DHFR enzyme activity .
|
-
- HY-12037
-
|
ON-01910 sodium
|
Polo-like Kinase (PLK)
PI3K
Apoptosis
|
Cancer
|
|
Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
|
-
- HY-18329
-
|
|
MDM-2/p53
STAT
Apoptosis
|
Cancer
|
|
TDP-665759 is an inhibitor for HDm2:p53 complex, and thus activates p53, inhibits STAT3 signaling pathway (EC50 of 5.90 μM) and the cell viability of p53 expressing A549R (IC50 of 7.02 μM). TDP-665759 induces apoptosis in HepG2. TDP-665759 exhibits antitumor efficacy in mouse models .
|
-
- HY-168892
-
|
|
ATTECs
Atg8/LC3
Autophagy
|
Cancer
|
|
LC3B recruiter 2 (34R) is an LC3B recruiter and a component of the autophagy-lysosome pathway degradation system (ATTEC, Autophagy-Tethering Compounds), which directly binds to LC3B. LC3B recruiter 2 binds to CDK9 inhibitor SNS-032 (HY-10008) through a linker, forming an ATTEC that targets the degradation of the CDK9 and Cyclin T1 complex (with inhibitory effects on both). Therefore, LC3B recruiter 2 exerts activity through the LC3B-dependent autophagy-lysosome pathway, interfering with the cell cycle of cancer cells, thus exhibiting antitumor activity .
|
-
- HY-110228
-
|
1,1-Dimethylbiguanide-d6 hydrochloride
|
AMPK
Autophagy
Mitophagy
Apoptosis
mTOR
|
Cardiovascular Disease
Metabolic Disease
|
|
Metformin-d6 hydrochloride is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo .
|
-
- HY-N1181
-
-
- HY-N10612
-
|
|
AMPK
PPAR
TRP Channel
Mitochondrial Metabolism
|
Metabolic Disease
Cancer
|
|
Petasin inhibits adipogenesis in cell 3T3-F442A with an IC50 of 0.95 μM. Petasin inhibits the expression of lipid synthesis factors ACC1, FAS and SCD1 by inhibiting transcription factors PPARγ and C/EBPα, as well as targeting TRPA1 and TRPV1 channels . Petasin inhibits mitochondrial complex I, thereby inhibiting tumor growth and metastasis. Petasin activates AMPK signaling pathway, participating in regulation of glucose and lipid metabolism. Petasin is orally active .
|
-
- HY-111137
-
|
XC-302 free base
|
Akt
|
Cancer
|
|
Puquitinib (XC-302 free base) is a multi-target inhibitor with the activity of inducing autophagy in nasopharyngeal carcinoma cells by inhibiting the PI3K/AKT/mTOR signaling pathway. Puquitinib was able to inhibit the proliferation of CNE-2 cells, showing a dose-dependent antiproliferative effect. Puquitinib induced the formation of autophagosomes and autolysosomes in CNE-2 cells, which were observed by fluorescence microscopy and electron microscopy. Puquitinib promoted the formation of LC3-II and increased the expression of beclin 1, while reducing the level of p62. Puquitinib inhibited the PI3K/AKT/mTOR pathway by reducing the expression of p-AKT and p-mTOR. Puquitinib also induced apoptosis in CNE-2 cells, and when autophagy was inhibited, the apoptosis rate was reduced, which means that autophagy may interact with apoptosis to induce cell death .
|
-
- HY-169100
-
|
|
VEGFR
PI3K
Akt
mTOR
p38 MAPK
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Antiproliferative agent-57 (compound M2) is a tumor angiogenesis inhibitor. Antiproliferative agent-57 inhibits the secretion of VEGF in SiHa cells under hypoxic conditions (IC50=0.68 μM) without inducing cytotoxicity. Antiproliferative agent-57 can modulate the PI3K/AKT/mTOR and MAPK signaling pathways in tumor cells to inhibit the expression of HIF-1α and VEGF in tumor tissues .
|
-
- HY-W010995
-
|
|
Wnt
Survivin
β-catenin
|
Cancer
|
|
2,5-Dimethylcelecoxib is an analogue of celecoxib (HY-14398) with anticancer activity but without COX-2 inhibitory activity. 2,5-Dimethylcelecoxib exerts its anti-cancer cell proliferation effect by inhibiting the core mechanism of the Wnt/β-catenin signaling pathway. 2,5-Dimethylcelecoxib also inhibits T-cell factor-dependent transcriptional activity and inhibits expression of the Wnt/β-catenin target gene products cyclin D1 and survivin .
|
-
- HY-129284
-
|
|
COX
|
Cancer
|
|
APHS is a specific and covalent COX-2 inhibitor with neuroprotective effects. COX-2 is a prostaglandin (PG) synthetase overexpressed in colorectal cancer (CRC) and has pleiotropic cancer-promoting effects. APHS modifies COX-2 by acetylating the active site (serine 516), thereby inhibiting prostaglandin production. The neuroprotective activity of APHS is inhibited by prostaglandin E2. APHS also co-inhibits the WNT pathway, an anti-tumor mechanism in addition to COX-2 inhibition .
|
-
- HY-W424851
-
|
6,7-Dimethoxy-2-(1-piperazinyl)-4-quinazolinamine hydrochloride
|
PARP
|
Infection
Inflammation/Immunology
|
|
DPQ hydrochloride is a blood-brain barrier permeable and selective PARP-1 inhibitor that blocks PARP-1-mediated DNA damage repair and NAD +/ATP consumption, thereby inhibiting excessive inflammatory responses. DPQ hydrochloride inhibits NF-κB pathway activation, reduces the expression of pro-inflammatory factors (such as TNF-α, IL-6) and oxidative stress. DPQ hydrochloride can be used in inflammation-related studies of acute lung injury, myocardial infarction, and neurodegenerative diseases .
|
-
- HY-114869
-
DPQ
1 Publications Verification
|
PARP
|
Neurological Disease
|
|
DPQ is a blood-brain barrier permeable and selective PARP-1 inhibitor that blocks PARP-1-mediated DNA damage repair and NAD +/ATP consumption, thereby inhibiting excessive inflammatory responses. DPQ inhibits NF-κB pathway activation, reduces the expression of pro-inflammatory factors (such as TNF-α, IL-6) and oxidative stress. DPQ can be used in inflammation-related studies of acute lung injury, myocardial infarction, and neurodegenerative diseases .
|
-
- HY-B1640R
-
|
Etacrynic acid (Standard)
|
Glutathione S-transferase
NF-κB
Calcium Channel
|
Inflammation/Immunology
Cancer
|
|
Ethacrynic acid (Standard) is the analytical standard of Ethacrynic acid. This product is intended for research and analytical applications. Ethacrynic acid (Etacrynic acid) is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice .
|
-
- HY-146261
-
|
|
Microtubule/Tubulin
Indoleamine 2,3-Dioxygenase (IDO)
Apoptosis
|
Cancer
|
|
HI5 is a potent tublin and IDO inhibitor, with an IC50 value of 70 nM in HeLa cells. HI5 inhibit IDO expression and decrease kynurenine production, leading to stimulating T cells activation and proliferation. HI5 can inhibit tubulin polymerization and cell migration, cause G2/M phase arrest, and induce apoptosis via the mitochondrial dependent apoptosis pathway and cause reactive oxidative stress generation in HeLa cells. HI5 can be used for researching anticancer .
|
-
- HY-163677
-
|
|
PROTACs
PI3K
Akt
|
Cancer
|
|
ARM165 is a heterobifunctional molecule. ARM165 degrades the PIK3CG proteins, inhibits PI3Kγ-Akt signaling pathway, and thus exhibits antileukemia efficacy. ARM165 inhibits proliferations of AML cells, with IC50 <1 μM. (Pink: ligand for target protein PI3Kγ inhibitor AZ2 (HY-111570); Black: linker; Blue: ligand for E3 ligase Pomalidomide (HY-10984))
|
-
- HY-169436
-
|
|
PD-1/PD-L1
|
|
|
Lon-TK is a glycolysis inhibitor + linker conjugate of LTB (HY-169434). LTB is an intelligent responsive prodrug that connects Lonidamine (Lon) (HY-B0486) and a PD-L1 inhibitor (BMS-1, HY-19991) through a thioketal linker. It significantly inhibits the glycolytic metabolism of tumor cells and blocks the PD-1/PD-L1 immune escape pathway. Lon-TK shows potential for application in photodynamic-enhanced immunotherapy research .
|
-
- HY-10412
-
|
KT7515
|
JNK
Mixed Lineage Kinase
MDM-2/p53
|
Neurological Disease
|
|
CEP-1347 is an inhibitor of the JNK/SAPK pathway with neuroprotective effects. CEP-1347 blocks JNK1 activation induced by members of the mixed lineage kinase (MLK) family (MLK3, MLK2, MLK1, dual leucine zipper kinase, and leucine zipper kinase). As an inhibitor of MDM4, CEP-1347 can more effectively inhibit the growth of glioma cells expressing wild-type p53 .
|
-
- HY-B1232
-
|
Su-4885
|
Endogenous Metabolite
Cytochrome P450
Autophagy
|
Neurological Disease
Metabolic Disease
Endocrinology
Cancer
|
|
Metyrapone (Su-4885) is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone can be used for researching Cushing's syndrome and depression .
|
-
- HY-168925
-
|
|
PARP
β-catenin
|
Cancer
|
|
EXQ-2d is the inhibitor for tankyrase and inhibits TNKS1 and TNKS2 with an IC50 of 48.8 nM and 13.8 nM (pIC50=7.31 and 7.86). EXQ-2d inhibits WNT/β-catenin signaling pathway with IC50 of 515 nM. EXQ-2d exhibits anti-proliferative activity in cancer cells COLO 320DM and RKO with GI50 of 4.9 μM and 77 μM .
|
-
- HY-B0678
-
|
AHR438; NSC170959
|
NF-κB
PGC-1α
|
Neurological Disease
Inflammation/Immunology
|
|
Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia .
|
-
- HY-137092
-
|
|
SHP2
Phosphatase
|
Cancer
|
|
IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers .
|
-
- HY-10971A
-
|
MLN 8237 sodium
|
Aurora Kinase
Autophagy
Apoptosis
|
Cancer
|
|
Alisertib (MLN 8237) sodium is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib sodium induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity .
|
-
- HY-128872
-
|
EHP-101; VCE-004.8
|
PPAR
Cannabinoid Receptor
HIF/HIF Prolyl-Hydroxylase
|
Metabolic Disease
Inflammation/Immunology
|
|
Etrinabdione (EHP-101; VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist. Etrinabdione inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. Etrinabdione, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. Etrinabdione attenuates adipogenesis and prevents diet-induced obesity .
|
-
- HY-156279
-
|
|
Apoptosis
HDAC
|
Cancer
|
|
HDAC6-IN-22 (compound 30) is a inhibitor of HDAC6, with the IC50 of 4.63 nM. HDAC6-IN-22 has antiproliferative effects in vitro and in vivo towards multiple myeloma. HDAC6-IN-22
induces cell cycle arrest in the G2 phase and promotes apoptosis through the mitochondrial pathway .
|
-
- HY-167843
-
|
|
Akt
PI3K
Autophagy
|
Neurological Disease
|
|
Alborixin is an inhibitor of the PI3K-AKT pathway that induces autophagy. It promotes the clearance of intracellular and extracellular amyloid-β by upregulating autophagy-related proteins (such as BECN1, ATG5, ATG7) and enhancing lysosomal activity, thereby reducing amyloid-β-mediated neurotoxicity. Alborixin shows potential for research in Alzheimer's disease .
|
-
- HY-124418
-
SBI-477
1 Publications Verification
|
Fluorescent Dye
|
Metabolic Disease
|
|
SBI-477 is a chemical probe stimulated insulin signaling by deactivating the transcription factor MondoA, leading to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain–containing 4 (ARRDC4). SBI-477 coordinately inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes .
|
-
- HY-139504
-
|
CC-99677
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
|
|
Gamcemetinib (CC-99677) is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC50=156.3 nM) and cell based assays (EC50=89 nM). Gamcemetinib is extracted from patent WO2020236636, compound 1 .
|
-
- HY-N0292
-
|
|
Cytochrome P450
PPAR
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity . Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase .
|
-
- HY-100408
-
|
|
Porcupine
|
Cardiovascular Disease
Cancer
|
|
GNF-6231 is a porcupine (IC50= 0.8 nM), Pron, and endoplasmic reticulum protein inhibitor with oral activity. GNF-6231 has anticancer activity. GNF-6231 can prevent the activation of the Wnt pathway by blocking the secretion of all Wnt ligands. GNF-6231 can be used in the study of myocardial infarction .
|
-
- HY-N0076
-
|
(-)-Bilobalide
|
Apoptosis
Autophagy
Endogenous Metabolite
|
Neurological Disease
|
|
Bilobalide, a sesquiterpene trilactone constituent of Ginkgo biloba, inhibits the NMDA-induced efflux of choline with an IC50 value of 2.3 µM. Bilobalide prevents apoptosis through activation of the PI3K/Akt pathway in SH-SY5Y cells. Exerts protective and trophic effects on neurons .
|
-
- HY-19528R
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
SAH (Standard) is the analytical standard of SAH. This product is intended for research and analytical applications. SAH (S-Adenosylhomocysteine) is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine . SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 μM .
|
-
- HY-142686
-
|
|
SGK
|
Inflammation/Immunology
|
|
SGK1-IN-3 (compound 3a) is a potent and orally active inhibitor of SGK1. The serine/threonine kinase SGK1 is an activator of the β-catenin pathway and a powerful stimulator of cartilage degradation that is found to be upregulated under genomic control in diseased osteoarthritic cartilage. SGK1-IN-3 has the potential for the research of osteoarthritis .
|
-
- HY-113071C
-
|
(S)-MVA
|
Endogenous Metabolite
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
|
|
(S)-Mevalonic acid is the isomer of Mevalonic acid (HY-113071). Mevalonic acid ((S)-DCIT) is a precursor substance of the mevalonate pathway，which is essential for cell growth and proliferation. Mevalonic acid is effective in inhibiting Simvastatin (HY-17502)-induced decrease in C2C12 cell viability in vitro. Mevalonic acid can be used in studies of myopathy and heart failure .
|
-
- HY-19528S1
-
|
SAH (S-Adenosylhomocysteine)-13C5
|
Endogenous Metabolite
|
Metabolic Disease
|
|
SAH- 13C5 is the 13C-labeled SAH. SAH (S-Adenosylhomocysteine) is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine[1]. SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 µM[2].
|
-
- HY-162265
-
|
|
Apoptosis
|
Cancer
|
|
UCM-13369 (Compound 4b) is a NPM1 inhibitor. UCM-13369 downregulates the pathway associated with mutant NPM1 C+, and specifically recognizes the C-end DNA-binding domain of NPM1 C+. UCM-13369 induces apoptosis in AML cell lines and primary cells, that can be used for the research of AML .
|
-
- HY-138301
-
Miclxin
1 Publications Verification
DS37262926
|
β-catenin
|
Cancer
|
|
Miclxin (DS37262926) is a potent inhibitor of mutant β-catenin, involving in Wnt signaling pathway. Miclxin induces β-catenin-dependent apoptosis, leads to severe mitochondrial damage with the loss of mitochondrial membrane. Miclxin kills tumor via targeting to MIC60, a major components of the mitochondrial contact site and cristae organizing system (MICOS) complex .
|
-
- HY-107811
-
Harmol
1 Publications Verification
|
α-synuclein
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Harmol is a TFEB activator, an orally active monoamine oxidase inhibitor that has anti-tumor, anti-depressant, and anti-aging effects. Harmol can induce cell mitosis, autophagy and apoptosis. Harmol promotes the degradation of α-synuclein through the regulation of the autophagy-lysosomal pathway, improving motor deficits in mouse models of Parkinson's disease .
|
-
- HY-14930A
-
-
- HY-14930
-
-
- HY-14928
-
-
- HY-116269
-
|
|
Ras
Apoptosis
PAK
ERK
|
Cancer
|
|
AZA197 is a selective small molecule inhibitor of Cdc42.AZA197 suppresses colon cancer cell proliferation, cell migration, invasion and increases apoptosis by down-regulating the PAK1 and ERK signaling pathways in vitro. AZA197 reduces tumor growth and significantly increases mouse survival in SW620 tumor xenografts .
|
-
- HY-160864
-
|
HWA 448
|
Phosphodiesterase (PDE)
|
Cancer
|
|
Torbafylline is a PDE inhibitor. Torbafylline mitigates protein breakdown in rat skeletal muscle following burns by activating the PDE4/cAMP/EPAC/PI3K/Akt signaling pathway. Torbafylline suppresses the increased ubiquitin-proteasome-dependent protein degradation observed in the skeletal muscles of rats susceptible to cancer and sepsis .
|
-
- HY-W012980R
-
|
|
Endogenous Metabolite
AMPK
PKA
|
Metabolic Disease
|
|
Isovaleric acid (Standard) is the analytical standard of Isovaleric acid. This product is intended for research and analytical applications. Isovaleric acid is an oral active short-chain fatty acid that inhibits osteoclast differentiation by stimulating AMPK phosphorylation and promotes colonic smooth muscle relaxation by activating the cAMP/PKA pathway. Isovaleric acid can be used in research on skeletal diseases (such as osteoporosis) and intestinal disorders .
|
-
- HY-N15315
-
|
|
Apoptosis
MAP3K
NF-κB
|
Others
|
|
Triptriolide inhibits Puromycin aminonucleoside PAN (HY-15695)-induced apoptosis in mouse podocytes through regulation of Bcl-2 family proteins and inhibition of Caspase-3. Triptriolide promotes the cell survival, protects and restores the podocyte function through activation of TAK1-NF-κB signaling pathway and upregulation of podocin .
|
-
- HY-N6636R
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Valencene (Standard) is the analytical standard of Valencene. This product is intended for research and analytical applications. Valencene is a sesquiterpene isolated from Cyperus rotundus, possesses antiallergic, antimelanogenesis, anti-infammatory, and antioxidant activitivies. Valencene inhibits the exaggerated expression of Th2 chemokines and proinflammatory chemokines through blockade of the NF-κB pathway. Valencene is used to flavor foods and drinks .
|
-
- HY-144778
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
Apoptosis
Bcl-2 Family
|
Cancer
|
|
IDO1/TDO-IN-1 (30) is a potent dual IDO1 (uncompetitive, Ki of 0.23 μM) and TDO (competitive, Ki of 0.73 μM) inhibitor. IDO1/TDO-IN-1 (30) significantly promotes cell apoptosis through the potential mitochondria-mediated Bcl-2/Bax pathway .
|
-
- HY-12470A
-
|
|
Casein Kinase
|
Cancer
|
|
PF-4800567 hydrochloride is a potent and selective inhibitor of?casein kinase?1? (CK1?), with an?IC50?of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM). PF-4800567 hydrochloride is useful in probing unique roles between these two kinases in multiple signaling pathways .
|
-
- HY-117857
-
-
- HY-W706180
-
|
|
Isotope-Labeled Compounds
Fungal
|
Infection
|
|
(±)-Triadimefon-d4 is deuterium labeled Triadimefon. Triadimefon is a triazole fungicide used to control powdery mildew, rusts, and other fungal pests on grains, fruit and vegetable crops, turf, shrubs, and trees. Triadimefon inhibits lanosterol 14α-demethylase, interfering with oxidative demethylation reactions in the ergosterol biosynthesis pathway of fungi, and also blocks gibberellin biosynthesis .
|
-
- HY-N0634
-
|
Cimitin
|
NF-κB
|
Inflammation/Immunology
|
|
Cimifugin (Cimitin) is a bioactive component of Cimicifuga racemosa, a Chinese herb. Cimifugin suppresses allergic inflammation by reducing epithelial derived initiative key factors via regulating tight junctions . Cimifugin reduces the migration and chemotaxis of RAW264.7 cells and inhibits the release of inflammatory factors and activation of MAPKs and NF-κB signaling pathways induced by LPS .
|
-
- HY-116145
-
|
|
Tyrosinase
NF-κB
|
Inflammation/Immunology
|
|
MHY884 is a tyrosinase inhibitor that suppresses UVB-induced activation of NF-κB signaling pathway through the downregulation of oxidative stress. MHY884 suppresses oxidative stress in the melanoma cells and attenuates UVB-induced oxidative stress, resulting in reduced NF-κB activity in irradiated mice. MHY884 is promising for research of UVB-induced skin damage .
|
-
- HY-Y0669
-
-
- HY-113965
-
|
|
Hedgehog
Smo
Apoptosis
|
Inflammation/Immunology
|
|
CUR61414 is a novel, potent and cell permeable Hedgehog signaling pathway inhibitor (IC50 =100-200 nM). CUR61414 is a small-molecule aminoproline class compound and selectively binds to smoothened (Smo) with a Ki value of 44 nM. CUR-61414 can induce apoptosis in cancer cells without affecting neighboring non-tumor cells .
|
-
- HY-N0366R
-
|
|
PDGFR
|
Cancer
|
|
Sennoside B (Standard) is the analytical standard of Sennoside B. This product is intended for research and analytical applications. Sennoside B is an anthraquinone glycoside, found in large quantities in leaves and pods of Senna (Cassia angustifolia) . Sennoside B can inhibit PDGF-stimulated cell proliferation by binding to PDGF-BB and its receptor and by down-regulating the PDGFR-beta signaling pathway .
|
-
- HY-N13080
-
|
|
Others
|
Cancer
|
|
3-Oxo-bufalin is an active compound that can be isolated from cultured toad liver tissue. 3-Oxo-bufalin can be produced through a metabolic pathway, and it is a metabolite of Bufalin (HY-N0877) catalyzed by the stereoselective 3β-dehydrogenase. Bufalin is a Na+/K+-ATPase inhibitor and has anti-tumor activity .
|
-
- HY-142686A
-
|
|
SGK
|
Inflammation/Immunology
|
|
SGK1-IN-3 hydrochloride (compound 3a) is a potent and orally active inhibitor of SGK1. The serine/threonine kinase SGK1 is an activator of the β-catenin pathway and a powerful stimulator of cartilage degradation that is found to be upregulated under genomic control in diseased osteoarthritic cartilage. SGK1-IN-3 hydrochloride has the potential for the research of osteoarthritis .
|
-
- HY-114395A
-
|
|
Drug Isomer
|
Inflammation/Immunology
|
|
(R)-NVS-ZP7-4 is the R-isomer of NVS-ZP7-4. NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel agentgable node in the Notch pathway.
|
-
- HY-155753
-
|
|
NF-κB
COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 50 (compound a1) is a Fusidic acid derivative with anti-inflammatory effects. Anti-inflammatory agent 50 inhibits inflammatory factor NO, IL-6 and TNF-α. Anti-inflammatory agent 50 alleviates acute lung injury by regulating inflammatory mediators and suppressing the MAPK, NF-κB and NLRP3 inflammasome signaling pathways .
|
-
- HY-P10899
-
|
|
TGF-beta/Smad
PROTACs
|
Endocrinology
|
|
ETTAC-2 is a LRG1 PROTAC degrader. ETTAC-2 promotes ubiquitination and degradation of LRG1 (DC50 of 8.38 µM). ETTAC-2 inhibits the TGF-β-Smad3 signaling pathway and diminishes the secretion of fibrosis-associated proteins. ETTAC-2 attenuates the progression of renal fibrosis .
|
-
- HY-100507A
-
|
CC 122 hydrochloride
|
E1/E2/E3 Enzyme
Apoptosis
Molecular Glues
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Avadomide hydrochloride (CC 122 hydrochloride) is the hydrochloride form of Avadomide (HY-100507). Avadomide hydrochloride is an orally active cereblon modulator. Avadomide hydrochloride modulates cereblon E3 ligase activity, inhibits NF-κB pathway, arrests the cell cycle at G1 phase, and thus induces apoptosis in cancer cell PDAC. Avadomide hydrochloride exhibits potent antitumor and immunomodulatory activities .
|
-
- HY-124083
-
|
|
Microtubule/Tubulin
Apoptosis
Caspase
Mitochondrial Metabolism
|
Cancer
|
MPT0B214 is a microtubule inhibitor that strongly binds to the colchicine binding site of tubulin, preventing tubulin polymerization. MPT0B214 induces apoptosis through a mitochondrial/caspase 9 dependent pathway and shows cytotoxicity across various human tumor cell lines. MPT0B214 can be used for cancer research .
|
-
- HY-N0022
-
-
- HY-156618
-
|
ABSK011
|
FGFR
|
Cancer
|
|
Irpagratinib (ABSK011) is an orally active inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinase, targeting to FGFR4 (IC50<10 nM). Irpagratinib inhibits the auto-phosphorylation of FGFR4 and blocks signal transduction from FGFR4 to downstream pathway activation. Irpagratinib exhibits high exposure in PK study in mouse, rat and dog, and also shows antineoplastic/anti-tumor activity in subcutaneous xenograft tumor models .
|
-
- HY-16126
-
|
L-651582; CAI
|
Calcium Channel
NF-κB
p38 MAPK
NO Synthase
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Carboxyamidotriazole (L-651582) is an orally active cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole inhibits NF-κB, MAPK activation and NO production. Carboxyamidotriazole has anti-angiogenic and anti-inflammatory activities. Carboxyamidotriazole has anticancer activity against liver cancer, lung cancer and leukemia .
|
-
- HY-147165
-
|
|
YAP
|
Cancer
|
|
VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids . VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-149351
-
|
|
NF-κB
|
Cardiovascular Disease
|
|
NF-κB-IN-10 (compound E1) is an NF-κB inhibitor that can improve heart failure by reducing oxidative stress and inflammation by regulating Nrf2/NF-κB signaling pathway. NF-κB-IN-10 inhibits LPS-induced NO production and expression of iNOS and COX-2 in RAW264.7 cells. NF-κB-IN-10 can be used in the research of cardiovascular diseases .
|
-
- HY-163535
-
|
|
HDAC
DNA Methyltransferase
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
J208 is a dual inhibitor for histone deacetylase (HDAC) and DNA methyltransferase (DNMT). J208 inhibits proliferation of cancer cells, as well as the migration/invasion of triple-negative breast cancer (TNBC) cells. J208 induces apoptosis, arrests the cell cycle at G0/G1 phase. J2008 activates the innate immune signalling pathway in TNBC, by inducing the expression of endogenous retroviruses (ERVs) .
|
-
- HY-149652
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
IRF5-IN-1 (compound C5) is an IRF5 pathway-specific inhibitor. IRF5-IN-1 significantly reduces IRF5 nuclear translocation without affecting the activation of NF-κB p65. IRF5-IN-1 acts through SLC15A4 to selectively inhibit TLR7/8-induced IRF5 responses in cells .
|
-
- HY-121607
-
|
|
AP-1
Apoptosis
|
Cancer
|
|
INI-43 is an inhibitor of Kpnβ1, interfering with the nuclear localization of Kpnβ1 and known Kpnβ1 cargo proteins, NFAT, NFκB, AP-1, and NFY. INI-43 can inhibit the proliferation of cancer cells, cause G2-M cell cycle arrest in cancer cells, and induce the intrinsic apoptosis pathway .
|
-
- HY-117702
-
|
|
Prolyl Endopeptidase (PREP)
Aminopeptidase
|
Metabolic Disease
|
|
RB 101 is an active mixed inhibitor against two enzymes which metabolize the enkephalins neutral endopeptidase and aminopeptidase N. RB 101 has rather long-lasting antinociceptive effects. RB 101 inhibits the in vivo [ 3H]DPN binding both under basal conditions and after swim stress in mice. RB 101 can be used to determine the precise in vivo localization of enkephalinergic pathways recruited by various stimuli .
|
-
- HY-N2510
-
|
Myristicine
|
5-HT Receptor
EGFR
ERK
Apoptosis
Bacterial
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Myristicine is an orally bioavailable serotonin receptor antagonist and weak monoamine oxidase (MAO) inhibitor. Myristicine also exerts anti-cancer effects on gastric cancer cells by inhibiting the EGFR/ERK signaling pathway. Myristicine is the main component of nutmeg essential oil and has anti-cancer, anti-proliferative, antibacterial, anti-inflammatory and apoptosis-inducing effects. Myristicine abuse can produce hallucinogenic effects, organ damage, etc .
|
-
- HY-163029
-
|
|
Cathepsin
SARS-CoV
|
Infection
|
|
CTSLCTSB-IN-1 (compound 212-148) is a bispecific inhibitor of host viral spike cleaver proteins CTSL/CTSB and TMPRSS2 with IC50s of 2.13/64.07 nM and 1.38 μM, respectively. CTSLCTSB-IN-1 blocks two relevant SARS-CoV-2 viral entry pathways by inhibiting the viral spike cleavage and can be applied to anti-SARS-CoV-2 research .
|
-
- HY-B0004R
-
|
|
Adenosine Receptor
Phosphodiesterase (PDE)
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Doxofylline (Standard) is the analytical standard of Doxofylline. This product is intended for research and analytical applications. Doxofylline is an orally active PDE IV inhibitor and A1AR antagonist. Doxofylline reduces inflammation in epithelial cells via inhibiting mitochondrial ROS production and amelioration of multiple cellular pathways (NLRP3-TXNIP inflammasome activation). Doxophylline can be used in studies of asthma, chronic obstructive pulmonary disease, and bronchospasm .
|
-
- HY-164483
-
|
|
Akt
Trk Receptor
|
Cancer
|
|
HS-345 is a TrkA/Ak inhibitor with significant anti-pancreatic cancer effects. HS-345 inhibits the growth and proliferation of pancreatic cancer cells by targeting the TrkA/Akt signaling pathway, while also inducing apoptosis. Additionally, HS-345 suppresses blood vessel formation by decreasing the expression of HIF-1α and VEGF. HS-345 holds promise for research in pancreatic cancer .
|
-
- HY-N4107R
-
|
|
TGF-beta/Smad
|
Infection
Inflammation/Immunology
Cancer
|
|
Phyllanthin (Standard) is the analytical standard of Phyllanthin. This product is intended for research and analytical applications. Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .
|
-
- HY-N9481
-
-
- HY-117051
-
|
|
HSP
|
Cancer
|
|
STA-2842 is an inhibitor of heat shock protein HSP90 with potential to inhibit autosomal dominant polycystic kidney disease (ADPKD). ADPKD is caused by inherited mutations in the PKD1 or PKD2 genes that abnormally activate multiple signaling proteins and pathways that regulate cell proliferation. STA-2842 can significantly reduce initial renal cyst formation and kidney growth in mice, and slow disease progression in mice with existing cysts.
|
-
- HY-16558
-
Butein
4 Publications Verification
2’,3,4,4’-tetrahydroxy Chalcone
|
EGFR
Autophagy
Apoptosis
Phosphodiesterase (PDE)
|
Cancer
|
|
Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4 . Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells . Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a . Butein is a SIRT1 activator (STAC).
|
-
- HY-147165A
-
|
|
YAP
|
Cancer
|
|
VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids . VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-W806047
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 Inhibitor-37 is a compound with anticancer activity that has inhibitory activity against BRD4. BRD4 Inhibitor-37 has an IC50 of approximately 0.05-0.1 μM in binding assays and shows a GI50 of 0.1-0.3 μM in cell-based assays. The effect of BRD4 Inhibitor-37 on c-Myc, a downstream protein of BRD4, has been validated, demonstrating its ability to intervene in this signaling pathway. BRD4 Inhibitor-37 exhibits selectivity among five different bromodomain proteins, enhancing its potential as a BET protein inhibitor .
|
-
- HY-N2037AS1
-
|
Norcoclaurine-d4-1 hydrochloride; Demethyl-Coclaurine-d4-1 hydrochloride
|
Isotope-Labeled Compounds
MAP3K
MDM-2/p53
Apoptosis
ROS Kinase
|
Infection
Cardiovascular Disease
Endocrinology
Cancer
|
|
Higenamine-d4-1 (Norcoclaurine-d4-1) hydrochloride is deuterium labeled Higenamine (hydrochloride). Higenamine hydrochloride is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine (Norcoclaurine) can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine hydrochloride protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine hydrochloride can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .
|
-
- HY-N2037AR
-
|
|
MAP3K
MDM-2/p53
ROS Kinase
Apoptosis
|
Infection
Cardiovascular Disease
Endocrinology
Cancer
|
|
Higenamine (hydrochloride) (Standard) is the analytical standard of Higenamine (hydrochloride). This product is intended for research and analytical applications. Higenamine hydrochloride is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine (Norcoclaurine) can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine hydrochloride protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine hydrochloride can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .
|
-
- HY-N4314R
-
|
|
Bacterial
COX
NO Synthase
NF-κB
|
Infection
Inflammation/Immunology
Cancer
|
|
Scutellarein tetramethyl ether (Standard) is the analytical standard of Scutellarein tetramethyl ether. This product is intended for research and analytical applications. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is a bioactive compound extracted from Eupatorium odoratum. Scutellarein tetramethyl ether exhibits anti-inflammatory, antibacterial, pro-coagulant, and anti-tumor activities. Scutellarein tetramethyl ether exerts its anti-inflammatory effects by modulating the NF-κB pathway and regulates bacterial resistance through the inhibition of efflux pumps. Additionally, Scutellarein tetramethyl ether accelerates coagulation time via the endogenous coagulation pathway. Studies have shown that Scutellarein tetramethyl ether can effectively inhibit the growth of the liver cancer cell line HepG2 (IC50= 20.08 μg/mL) .
|
-
- HY-117037
-
|
|
Apoptosis
ERK
|
Cardiovascular Disease
Cancer
|
|
FR900359 is a depsipeptide selective inhibitor of Gαq/11/14 in mammalia, can inhibits ERK pathway. FR900359 suppresses the proliferation of melanoma cells and decreases of blood pressure. FR900359 also protected against airway hyperreactivity in murine models of allergen sensitization in Ovalbumins(HY-W250978)–induced sensitization model of asthma. FR900359 can be used for cancer and cardiovascular disease research .
|
-
- HY-17508R
-
|
|
Bacterial
Cytochrome P450
Autophagy
Antibiotic
|
Infection
Cancer
|
|
Clarithromycin (Standard) is the analytical standard of Clarithromycin. This product is intended for research and analytical applications. Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
|
-
- HY-17473
-
Embelin
4 Publications Verification
Embelic acid; Emberine; NSC 91874
|
IAP
NF-κB
Apoptosis
Autophagy
|
Cancer
|
|
Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells .
|
-
- HY-N1372A
-
|
|
HIV
FAK
Apoptosis
Autophagy
|
Infection
Cancer
|
|
Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing . Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK . Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer .
|
-
- HY-155784
-
|
|
Sirtuin
Reactive Oxygen Species
Keap1-Nrf2
|
Cancer
|
|
SPC-180002 is a SIRT1/3 dual inhibitor, with IC50 values of 1.13 and 5.41 μM, respectively. SPC-180002 disturbs redox homeostasis via ROS generation, which leads to an increase in both p21 protein stability and mitochondrial dysfunction. SPC-180002 strongly inhibits cell cycle progression and cancer cell growth. SPC-180002 activates the Nrf2 signaling pathway .
|
-
- HY-173084
-
|
|
Phosphatase
MDM-2/p53
|
Cancer
|
|
BRD6257 is an orally active inhibitor for protein phosphatase, Mg2+/Mn2+ dependent 1D PPM1D with an IC50 of 5 nM. BRD6257 activates p53 signaling pathway with an EC50 of 51 nM, increases the p21 expression, inhibits the proliferation of cancer cell MOLM13 (IC50=2.8 μM). BRD6257 exhibits good metabolic stability in human and rat liver microsomes .
|
-
- HY-100035
-
|
|
ROCK
ERK
CDK
Apoptosis
|
Cancer
|
|
PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity .
|
-
- HY-107592
-
|
|
IKK
STAT
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
ACHP (compound 4j) is a selective and orally active IκB kinase inhibitor with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. ACHP can effectively inhibit the STAT3 signaling pathway and induce cancer cell cycle arrest and apoptosis. ACHP shows anti-inflammatory activity in a mouse ear edema model. ACHP can be used in anti-inflammatory and anti-cancer (such as multiple myeloma and leukemia) studies .
|
-
- HY-149485
-
|
|
JNK
|
Inflammation/Immunology
|
|
JNK2-IN-1 (Compound J27) is a JNK2 inhibitor (Kds: 79.2 μM). JNK2-IN-1 has anti-inflammatory activity. JNK2-IN-1 decreases the release of TNF-α and IL-6 through inhibiting the activation of NF-κB/MAPK pathway. JNK2-IN-1 alleviates the symptoms of LPS-induced acute lung injury (ALI) and sepsis .
|
-
- HY-171272
-
|
|
Reactive Oxygen Species
MDM-2/p53
|
Cancer
|
|
PRDX1-IN-3 (compound 19-048) is a PRDX1 covalent inhibitor with anti-colorectal cancer activity. PRDX1-IN-3 can effectively inhibit the proliferation of colorectal cancer cells, and its antitumor effect on nude mice with colorectal cancer carrying PRDX1 gene knockout is significantly reduced. PRDX1-IN-3 also upregulates the downstream genes of the p53 signaling pathway to exert an anticancer effect .
|
-
- HY-168924
-
|
|
Wnt
β-catenin
|
Metabolic Disease
|
|
Wnt/β-catenin activator 1 (Compound 5m) is the orally active activator for Wnt/β-catenin signaling pathway, that arrests cell cycle at G1 phase, inhibits early proliferation of adipocytes, and inhibits adipogenesis in cell 3T3-L1 with an IC50 of 330 nM. Wnt/β-catenin activator 1 exhibits anti-adipogenic and anti-dyslipidemic activities in high-fat diet fed Syrian golden hamster model .
|
-
- HY-125026
-
|
|
Endogenous Metabolite
|
Others
|
|
MyomiRs-IN-1 is a myomiRs inhibitor with activity to inhibit myoD translation in C2C12 cells. MyomiRs-IN-1 does not change the expression level of myoD mRNA, while downregulating the expression of differentiation markers. MyomiRs-IN-1 affects the expression of myomiRs in muscle cells by regulating the regulatory pathway between miR-221/222 and myoD. The application of MyomiRs-IN-1 can facilitate research on muscle development and related diseases .
|
-
- HY-169555
-
|
|
ASK1
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
ASK1-IN-7 (Compound 4c) is an ASK1 inhibitor and a derivative of the ASK1 inhibitor scaffold 5-(5-Phenyl-furan-2-ylmethylene)-2-thioxo-thiazolidin-4-one. ASK1-IN-7 holds promise for research related to the ASK1 signaling pathway, such as cell stress responses, inflammation, neurodegenerative diseases, and cardiovascular diseases .
|
-
- HY-115893A
-
|
|
CDK
|
Cancer
|
|
P18IN005 hydrochloride is a novel inhibitor of p18, exhibiting potent activity in negatively regulating haematopoietic stem cell (HSC) self-renewal. P18IN005 hydrochloride has been shown to be more effective than p27 in inhibiting HSC self-renewal in mouse models. P18IN005 hydrochloride promotes the expansion of functional HSCs in short-term cultures. P18IN005 hydrochloride serves as a valuable tool for dissecting the signaling pathways involved in stem cell self-renewal.
|
-
- HY-14162
-
|
|
FLAP
|
Inflammation/Immunology
|
AM103 (free acid) is a selective FLAP inhibitor that can block the first step of the LT pathway, which is 5-LO activation. AM103 (free acid) can inhibit the production of LTB4 and cysteinyl leukotrienes (CysLT). AM103 (free acid) has anti-inflammatory activity in a mouse model of chronic lung inflammation and can extend the survival time of mice injected with platelet-activating factor. AM103 (free acid) can be used for research on respiratory diseases such as asthma .
|
-
- HY-164853
-
|
|
Pyroptosis
NOD-like Receptor (NLR)
ERK
FGFR
AMPK
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Kanglexin is an orally active and novel anthraquinone compound. Kanglexin inhibits NLRP3 inflammatory body activation and cell pyroptosis, and has a cardioprotective effect. Kanglexin promotes angiogenesis through FGFR1/ERK signaling pathway and accelerates diabetic wound healing. In addition, Kanglexin has the effect of lipid-lowering and inhibiting the dedifferentiation of vascular smooth muscle cells, and can be used in the study of hyperlipidemia, fatty liver and atherosclerosis .
|
-
- HY-149331
-
|
|
TNF Receptor
Caspase
NF-κB
|
Inflammation/Immunology
|
|
TNF-α-IN-11 (Compound 10) is a TNF-α inhibitor with a KD value of 12.06 μM. TNF-α-IN-11 binds to TNF-α and blocks the activation of TNF-α-trigged caspase and NF-κB signaling pathway. TNF-α-IN-11 inhibits the phosphorylation of IκBα, as well as the nuclear translocation of NF κB p65. TNF-α-IN-11 can be used for research of TNF-α-mediated autoimmune diseases .
|
-
- HY-N0108
-
|
Parietin; Rheochrysidin
|
Bacterial
Toll-like Receptor (TLR)
NF-κB
Apoptosis
Autophagy
Antibiotic
|
Infection
Inflammation/Immunology
Cancer
|
|
Physcion (Parietin), an anthraquinone derivative derived from the traditional Chinese medicine rhubarb, is an effective oral active 6-phosphogluconate dehydrogenase inhibitor with blood-brain barrier permeability, with IC50 and Kd values of 38.5 μM and 26.0 μM, respectively. Additionally, Physcion is an inhibitor of the <>bTLR4/NF-κB signaling pathway, exhibiting anti-inflammatory, antibacterial, and anticancer effects, and can induce Apoptosis and Autophagy in cancer cells .
|
-
- HY-B0736AR
-
|
|
Fungal
Autophagy
Apoptosis
p38 MAPK
Microtubule/Tubulin
|
Infection
|
|
Sertaconazole (nitrate) (Standard) is the analytical standard of Sertaconazole (nitrate). This product is intended for research and analytical applications. Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole nitrate is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells .
|
-
- HY-103645
-
|
|
Bacterial
Aurora Kinase
Apoptosis
|
Infection
Cancer
|
|
GW779439X is a pyrazolopyridazine identified in an inhibitor of the S. aureus PASTA kinase Stk1. GW779439X potentiates the activity of β-lactam antibiotics against various MRSA and MSSA isolates, some even crossing the breakpoint from resistant to sensitive. GW779439X is an AURKA inhibitor and induces apoptosis by the caspases 3/7 pathway . MRSA:methicillin-resistant S. aureus; MSSA: methicillin-sensitive S. aureus
|
-
- HY-162647
-
|
|
PI3K
|
Inflammation/Immunology
|
|
PI3Kδ-IN-22 (Compound 26) is a selective inhibitor for PI3Kδ with pKi of 9.3. PI3Kδ-IN-22 inhibits PI3Kδ-AKT signaling pathway in THP-1 cells, with pIC50 of 9.4. PI3Kδ-IN-22 exhibits good pharmacokinetic characters in rats .
|
-
- HY-113289
-
|
|
Akt
Androgen Receptor
Bacterial
Drug Metabolite
HSV
|
Infection
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Brassicasterol is a metabolite of Ergosterol and has cardiovascular protective effects. Brassicasterol exerts anticancer effects in prostate cancer through dual targeting of AKT and androgen receptor signaling pathways. Brassicasterol inhibits HSV-1 (IC50=1.2 μM) and Mycobacterium tuberculosis. Brassicasterol also inhibits sterol δ 24-reductase, slowing the progression of atherosclerosis. Brassicasterol is also a cerebrospinal fluid biomarker for Alzheimer's disease .
|
-
- HY-103399R
-
|
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
|
|
Clarithromycin (Standard) is the analytical standard of Clarithromycin. This product is intended for research and analytical applications. Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
|
-
- HY-17508S1
-
|
|
Isotope-Labeled Compounds
Bacterial
Antibiotic
Autophagy
Cytochrome P450
|
Others
|
|
Clarithromycin-d3 is the deuterium labeled Clarithromycin (HY-17508) . Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .
|
-
- HY-W012977
-
-
- HY-168044
-
|
|
AMPK
|
Cancer
|
|
ALKBH1-IN-3 is a potent DNA N6-methyladenine (6mA) demethylase ALKBH1 inhibitor. ALKBH1-IN-3 increases the abundance of 6mA, inhibits cell viability and upregulates the AMP-activated protein kinase (AMPK) signaling pathway in gastric cancer cell lines HGC27 and AGS. ALKBH1-IN-3 is promising for research of cancers, including gastric cancer .
|
-
- HY-113509
-
|
LXA4
|
Interleukin Related
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties . Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways . Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC50 value of 25.74 nM .
|
-
- HY-120604
-
|
NVP_BVB808
|
JAK
STAT
|
Cancer
|
|
BVB808 (NVP_BVB808) is a selective JAK2 inhibitor with approximately 10-fold selectivity for JAK2 over other JAK family members (such as JAK1, JAK3 or TYK2) in vitro. BVB808 inhibits the activity of JAK2 and reduces the phosphorylation of STAT5, thereby blocking the JAK2-dependent cell proliferation and survival signaling pathways. BVB808 can be used in cancer research .
|
-
- HY-113756AR
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Latanoprost acid (Standard) is the analytical standard of Latanoprost acid. This product is intended for research and analytical applications. Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor . Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes .
|
-
- HY-143248
-
|
|
G Protein-coupled Receptor Kinase (GRK)
HDAC
|
Cardiovascular Disease
|
|
KR-39038 is an orally active and potent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC50 of 0.02 μM. KR-39038 significantly inhibits angiotensin II-induced cellular hypertrophy through suppression of HDAC5 pathway in neonatal cardiomyocytes. KR-39038 shows profound anti-hypertrophic effects and improved cardiac function. KR-39038 can be used for heart failure research .
|
-
- HY-169131
-
|
|
AMPK
|
Cancer
|
|
ALKBH1-IN-4 prodrug (Compound 29E) is a prodrug of a DNA N6-methyladenine demethylase ALKBH1 inhibitor that significantly increases the abundance of 6mA in cells and upregulates the AMPK signaling pathway, thereby inhibiting the viability of gastric cancer cells. ALKBH1-IN-4 prodrug exhibits excellent cellular activity and favorable metabolic exposure in vivo, and holds promise for research in gastric cancer .
|
-
- HY-117938
-
|
|
Aminoacyl-tRNA Synthetase
|
Cancer
|
|
T-3861174 is an inhibitor of prolyl-tRNA synthetase (PRS, Aminoacyl-tRNA Synthetase) without completely inhibiting its translation process. T-3861174 activates the GCN2-ATF4 pathway and induces death in multiple tumor cell lines, including SK-MEL-2. T-3861174 demonstrated significant antitumor activity in multiple xenograft models without significantly affecting body weight .
|
-
- HY-113618B
-
|
|
CRAC Channel
Interleukin Related
|
Cardiovascular Disease
|
|
RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways .
|
-
- HY-162147
-
|
|
mTOR
Autophagy
|
Inflammation/Immunology
|
|
Nur77 modulator 3 (9e) can bind to Nur77 and inhibit TGF-β1-induced α-SMA and COLA1 expression in a Nur77-dependent manner. Nur77 modulator 3 induces Nur77 expression and enhances autophagic flux by inhibiting the mTORC1 signaling pathway in vitro and in vivo. Nur77 modulator 3 blocks the progression of hepatic fibrosis .
|
-
- HY-162703
-
|
|
AMPK
|
Metabolic Disease
|
|
Lipid-lowering agent-2 (Compound 14d) is an orally active lipid-lowering agent with an EC50 of 0.06 μM. Lipid-lowering agent-2 inhibits the lipid synthesis, activates the AMPK signaling pathway, and exhibits anti-obesity effect. Lipid-lowering agent-2 inhibits food intake, improves the glucose metabolism, and reduces the body weight and adipose tissue in high-fat diet (HFD)-induced obese mice .
|
-
- HY-161140
-
|
|
PI3K
Wnt
|
Cancer
|
|
PI3Kα-IN-16 (Z86) is a novel PI3Kα inhibitor with an IC50 value of 4.28 μM. PI3Kα-IN-16 has potent inhibitory efficiency on PI3K-mediated CRCs growth and migration. PI3Kα-IN-16 also inhibits the Wnt signaling pathway .
|
-
- HY-149275
-
|
|
Pyruvate Kinase
PDK-1
Akt
EGFR
Apoptosis
|
Cancer
|
|
PKM2/PDK1-IN-1, one of shikonin thioether derivatives, is a dual inhibitor of PKM2/PDK1. PKM2/PDK1-IN-1 inhibits the proliferation of NSCLC cells, and induces apoptosis. PKM2/PDK1-IN-1 induces intercellular ROS production, and regulates the apoptotic proteins, to involves in mitochondrial and death receptor pathway .
|
-
- HY-144761
-
|
|
JNK
|
Cancer
|
|
TOPK-p38/JNK-IN-1 (Compound B12) is an orally active TOPK-p38/JNK signaling pathway inhibitor with the IC50 value of 2.14 µM for NO production. TOPK-p38/JNK-IN-1 shows anti-inflammatory activities. TOPK-p38/JNK-IN-1 also inhibits phosphorylate downstream related proteins and avoids degradation of TOPK .
|
-
- HY-158045
-
|
|
PROTACs
PARP
|
Inflammation/Immunology
Cancer
|
|
PROTAC PARP1 degrader-1 (Compound CN0) is a PROTAC degrader of PARP1. PROTAC PARP1 degrader-1 activates the cGAS/STING immunity pathway and eventually enhances T cell killing of tumor cells. PROTAC PARP1 degrader-1 inhibits DNA damage repair, resulting in highly efficient accumulation of cytosolic DNA fragments (Blue: CRBN ligand, Black: linker; Pink: PARP1 inhibitor) .
|
-
- HY-145963
-
|
|
GLUT
|
Cancer
|
|
DRB18 is a potent pan-class GLUT inhibitor. DRB18 alters energy-related metabolism in A549 cells by changing the abundance of metabolites in glucose-related pathways. DRB18 can eventually lead to G1/S phase arrest and increase oxidative stress and necrotic cell death. DRB18 has anti-tumor activity .
|
-
- HY-B0679
-
|
RU-0211; SPI-0211
|
Chloride Channel
CFTR
Glutathione Peroxidase
NO Synthase
TNF Receptor
|
Metabolic Disease
|
|
Lubiprostone (SPI-0211; RU0211) increases intestinal fluid secretion through generation of CIC-2/CFTR and activation of cAMP signaling pathway. Lubiprostone inhibits myeloperoxidase (MPO) activity, downregulates Indomethacin (HY-14397)-induced iNOS and TNFα expression. Lubiprostone can be used for chronic constipation research .
|
-
- HY-162265A
-
|
|
Apoptosis
|
Cancer
|
|
UCM-13369 (Compound 4b) is a NPM1 inhibitor. UCM-13369 downregulates the pathway associated with mutant NPM1 C+, and specifically recognizes the C-end DNA-binding domain of NPM1 C+. UCM-13369 induces apoptosis in AML cell lines and primary cells. UCM-13369 can be used for leukemia research .
|
-
- HY-115620
-
|
|
Phosphatase
PI3K
TNF Receptor
|
Inflammation/Immunology
|
|
AQX-016A is an orally active and potent SHIP1 agonist. AQX-016A can activate recombinant SHIP1 enzyme in vitro and stimulate SHIP1 activity. AQX-016A also can inhibit the PI3K pathway and TNFa production, can be useful for various inflammatory diseases research .
|
-
- HY-W015883R
-
|
|
Endogenous Metabolite
NF-κB
p38 MAPK
|
Metabolic Disease
Inflammation/Immunology
|
|
Fumaric acid (Standard) is the analytical standard of Fumaric acid. This product is intended for research and analytical applications. Fumaric acid is an unsaturated dicarbonic acid, an intermediate product of the citric acid cycle that provides intracellular energy in the form of ATP. Fumaric acid exerts anti-inflammatory effects by inhibiting the NF-κB signaling pathway dependent on p38 MAPK. Fumaric acid can be used in the study of pregnancy-induced hypertension .
|
-
- HY-N2425
-
|
|
Cholinesterase (ChE)
|
Metabolic Disease
|
|
Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC50 for CYP2D6 is 0.761 μM, and the Ki is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system
|
-
- HY-N12726
-
|
|
p38 MAPK
MMP
|
Infection
Inflammation/Immunology
Cancer
|
Halociline, a derivative of alkaloids, that can be isolated from the marine fungus Penicillium griseofulvum.
Halociline targets MAPK1, MMP-9, and PIK3CA in gastric cancer cells, potentially mediated by diverse pathways including cancer, lipid metabolism, atherosclerosis, and EGFR tyrosine kinase inhibitor resistance. Halociline possesses antimicrobial, antioxidant and biofilm inhibitory activities .
|
-
- HY-N7171
-
|
4,4'-DiOMEA; Nasutin C
|
Wnt
|
Cancer
|
|
4,4'-Di-O-methylellagic acid (4,4'-DiOMEA; Nasutin C) can be isolated from the Australian termites. 4,4'-Di-O-methylellagic acid is blue-fluorescent under ultra-violet light . 4,4'-Di-O-methylellagic acid inhibits colon cancer cell proliferation via the wnt signal pathway .
|
-
- HY-147942
-
|
|
PROTACs
EGFR
|
Cancer
|
|
MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer .
|
-
- HY-19972
-
|
|
Wnt
|
Cancer
|
|
ML243 is a selective small-molecule inhibitor of breast cancer stem cells. ML243 has 32-fold greater selective inhibition in the breast CSC-like cell line HMLE_shECad than the control cell line HMLE_shGFP. ML243 may target the Wnt pathway at the protein level without altering RNA expression levels .
|
-
- HY-155807
-
|
|
STAT
JAK
Apoptosis
|
Cancer
|
|
DPP is a Platinum(IV) complex, bearing pterostilbene-derived axial ligand. DPP inhibit the JAK2-STAT3 pathway in breast cancer (BC) cells with antiproliferative activity, and activates caspase-3 and cleaved poly ADP-ribose polymerase to induces apoptosis. DPP promotes the maturation and antigen presentation of dendritic cells, and exhibits in vivo safety .
|
-
- HY-N0253R
-
|
|
Bacterial
p38 MAPK
NF-κB
Apoptosis
|
Infection
Inflammation/Immunology
|
|
Hederacoside C (Standard) is the analytical standard of Hederacoside C. This product is intended for research and analytical applications. Hederacoside C (Kalopanaxsaponin B) is an ingredient that can be obtained mainly from ivy leaves. Hederacoside C mediates inflammation by inhibiting activation of MAPK/NF-κB and its downstream signaling pathway. Hederacoside C has anti-inflammatory and antibacterial activity .
|
-
- HY-N0404R
-
|
|
p38 MAPK
AMPK
|
Metabolic Disease
Inflammation/Immunology
|
|
Sinigrin (Standard) is the analytical standard of Sinigrin. This product is intended for research and analytical applications. Sinigrin is a major glucosinolate present in plants of the Brassicaceae family. Sinigrin inhibits early-stage adipogenesis of 3T3-L1 adipocytes through the AMPK and MAPK signaling pathways. Sinigrin has potent anti-oxidant, anti-tumor and anti-inflammatory effects .
|
-
- HY-19528S2
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
SAH- 13C10 is the 13C labeled SAH[1]. SAH (S-Adenosylhomocysteine) is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine[2]. SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 μM[3].
|
-
- HY-117903A
-
|
|
Smo
Hedgehog
|
Cancer
|
|
MRT-92 is a Smoothened (Smo) antagonist (Ki=0.7 nM) with anticancer activity. MRT-92 inhibits Hedgehog signaling pathway and rodent cerebellar granule cell proliferation by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor (IC50=0.4 nM). MRT-92 can be used in the study of cerebellar glioma .
|
-
- HY-B0252S
-
|
HCTZ-d2
|
TGF-beta/Smad
Potassium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
Hydrochlorothiazid-d2 is the deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[1][2][3].
|
-
- HY-N1414A
-
|
|
Bcl-2 Family
Apoptosis
|
Neurological Disease
|
|
3′,6-Disinapoylsucrose is a type of oligosaccharide that's effective when taken orally, and it has antidepressant, anti-anxiety, and antioxidant properties. 3′,6-Disinapoylsucrose inhibits neuronal apoptosis by lowering the ratio of Bax to Bcl-2 in hippocampal neurons, and it enhances cognitive function in APP/PS1 transgenic mice by activating the CREB/BDNF signaling pathway .
|
-
- HY-12557
-
|
|
CaSR
Wnt
TNF Receptor
|
Inflammation/Immunology
|
|
γ-Glutamylvaline is an activator of CaSR with anti-inflammatory activity. γ-Glutamylvaline inhibits TNF-α-induced proinflammatory cytokine production and increases Wnt5a expression. γ-Glutamylvaline activates calcium-sensing receptor pathways in adipocytes of 3T3-L1 mice and prevents low-grade chronic inflammation .
|
-
- HY-P10710
-
|
|
IFNAR
Interleukin Related
COX
|
Inflammation/Immunology
|
|
BMP-4 is a penetrating heparin-binding peptide with anti-inflammatory and anti-chondrogenic functions. In murine chondrocytes and macrophages, BMP-4 regulates the iNOS-IFN-IL6 signaling pathway to inhibit the expression of inflammatory proteins such as iNOS, COX2, IFN, and IL6 in a dose-dependent manner, effectively suppressing inflammation and alleviating various arthritis symptoms .
|
-
- HY-P10839
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
NBD peptide inhibits NF-κB signaling pathway through inhibition of the NEMO-IKK complex combination. NBD peptide exhibits anti-inflammatory efficacy through block of pro-inflammatory cytokines production. NBD peptide exhibits immunosuppressive activity through regulation of immune cells. NBD peptide enhances its transmembrane ability by combining with cell-penetrating peptide HIV-TAT .
|
-
- HY-111125
-
|
|
Parasite
Reactive Oxygen Species
Apoptosis
|
Infection
Cancer
|
|
AMRI-59 is a potent inhibitor of PrxI used for parasitic infections. AMRI-59 can increase cellular ROS, leading to activation of signaling pathways mediated by mitochondria and apoptosis signal-regulated kinase 1, thereby leading to apoptosis in A549 human lung adenocarcinoma. AMRI-59 exhibits significant antitumor activity without apparent acute toxicity .
|
-
- HY-W762011R
-
|
|
Apoptosis
Reactive Oxygen Species
JNK
Oxidative Phosphorylation
|
Neurological Disease
Cancer
|
|
BDE 47 (Standard) is the analytical standard of BDE 47. This product is intended for research and analytical applications. BDE 47 targets mitochondria, inhibits mitochondrial oxidative phosphorylation (OXPHOS), decreases mitochondrial membrane potential (MMP) and induces apoptosis in embryonic cell. BDE 47 induces the generation of ROS, and activates the JNK signaling pathway. BDE 47 exhibits embryonic developmental toxicity in zebrafish .
|
-
- HY-163775
-
|
|
MyD88
NF-κB
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 88 (compound 6) is a carbazole derivative with anti-inflammatory activity found in marine Streptomyces. It exerts its anti-inflammatory effect by inhibiting pro-inflammatory factors and enhancing the expression of anti-inflammatory factors in the Myd88/Nf-κB pathway. Anti-inflammatory agent 88 can be used for the development of anti-inflammatory drugs .
|
-
- HY-123037R
-
|
|
Fungal
|
Infection
|
|
Triadimefon (Standard) is the analytical standard of Triadimefon. This product is intended for research and analytical applications. Triadimefon is a triazole fungicide used to control powdery mildew, rusts, and other fungal pests on grains, fruit and vegetable crops, turf, shrubs, and trees. Triadimefon inhibits lanosterol 14α-demethylase, interfering with oxidative demethylation reactions in the ergosterol biosynthesis pathway of fungi, and also blocks gibberellin biosynthesis.
|
-
- HY-116035
-
|
|
NF-κB
CDK
Apoptosis
|
Cancer
|
|
Nimbolide is a triterpene compound that can be isolated from neem (Azadirachta indica), possesses anticancer and antiproliferative activity. Nimbolide induces tumor cell apoptosis by inhibiting NF-κB and CDK4/CDK6 kinase. Nimbolide suppresses the Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways .
|
-
- HY-10971
-
|
MLN 8237
|
Aurora Kinase
Autophagy
Apoptosis
|
Cancer
|
|
Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity .
|
-
- HY-132242
-
|
SFN-NAC
|
HDAC
Apoptosis
Drug Metabolite
|
Cancer
|
|
DL-Sulforaphane N-acetyl-L-cysteine (SFN-NAC) is an orally active HDAC inhibitor and metabolite of sulforaphane (HY-13755) with longer half-life and better blood-brain barrier permeability. DL-Sulforaphane N-acetyl-L-cysteine activates autophagy-mediated downregulation of α-tubulin expression through the ERK pathway and can be used in cancer research .
|
-
- HY-B1371
-
|
Spiroperidol
|
Dopamine Receptor
5-HT Receptor
Wnt
|
Neurological Disease
|
|
Spiperone (Spiroperidol) is a potent dopamine D2, serotonin 5-HT1A, and serotonin 5-HT2A antagonist. Spiperone is also a labelled ligand for neuroleptic receptors. Spiperone enhances intracellular calcium level and inhibits the Wnt signaling pathway. Spiperone has the potential for the research of neurology diseases .
|
-
- HY-111954
-
-
- HY-N6896
-
|
|
TGF-beta/Smad
|
Cancer
|
|
Isoviolanthin, a flavonoid glycoside, could markedly inhibit TGF-β1-mediated migration and invasion by deactivating epithelial-mesenchymal transition (EMT) via the TGF-β/Smad and PI3K/Akt/mTOR pathways in HCC cells. Isoviolanthin exhibits no cytotoxic effects on normal liver LO2 cells .
|
-
- HY-N13208
-
|
|
MMP
TGF-beta/Smad
|
Others
|
Stevia Powder is a natural sweetener with antioxidant activity. Stevia Powder can downregulate pro fibrotic pathways in cirrhotic rats, including reduced hepatic myofibroblasts and decreased expression of matrix metalloproteinases MMP2 and MMP13, upregulate anti fibrotic molecule Smad7, prevent serum necrosis and elevated bile stasis markers, thereby inhibiting the development of liver fibrosis .
|
-
- HY-B0094S
-
|
Qinghaosu-d3; NSC 369397-d3
|
Akt
Ferroptosis
HCV
Parasite
|
Infection
Neurological Disease
Cancer
|
|
Artemisinin-d3 is the deuterium labeled Artemisinin. Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants[1]. Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects[2].
|
-
- HY-B0627
-
|
1,1-Dimethylbiguanide
|
AMPK
Autophagy
Mitophagy
Apoptosis
mTOR
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Metformin (1,1-Dimethylbiguanide) inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo .
|
-
- HY-17471A
-
|
1,1-Dimethylbiguanide hydrochloride
|
AMPK
Autophagy
Mitophagy
Apoptosis
mTOR
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Metformin (1,1-Dimethylbiguanide) hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo .
|
-
- HY-124843
-
|
CLT-005
|
STAT
Apoptosis
|
Cancer
|
|
LLL3 (CLT-005) is a STAT3 inhibitor. LLL3 inhibits dimerization and phosphorylation of STAT3, thereby preventing intraconuclear transfer of STAT3 and inhibits the expression of STAT3 dependent genes, which encode proteins such as Bcl-xL and cyclin D1. In addition, LLL3 can induce cell growth inhibition and apoptosis in human breast cancer and rhabdomyosarcoma cells via the caspase pathway. LLL3 can be used in the study of STAT3 persistent activation types of cancer .
|
-
- HY-B1232A
-
|
Su-4885 Tartrate
|
Endogenous Metabolite
Cytochrome P450
Autophagy
mTOR
|
Neurological Disease
Endocrinology
|
|
Metyrapone (Su-4885) Tartrate is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone Tartrate inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone Tartrate increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone Tartrate can be used for researching Cushing's syndrome and depression .
|
-
- HY-107825
-
|
|
Endogenous Metabolite
Bacterial
Cholinesterase (ChE)
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Flavonol is a cholinesterase (ChE) inhibitor, with an IC50 value of 120 μM and a Ki value of 74 μM. Flavonol has antioxidant, free radical-scavenging, antibacterial properties, and immune modulation functions. Flavonol inhibits the PriA helicase of Staphylococcus aureus. Flavonol can suppress the production of NO in LPS-activated RAW 264.7 cells by inhibiting the expression of the iNOS enzyme. Flavonol shows protective and analgesic effects in mice through various neuronal pathways. Flavonol can be used in research related to tumors and atherosclerosis diseases .
|
-
- HY-152079
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP1B1-IN-3 is a potent and selective CYP1B1 inhibitor with IC50 values of 6.6, 347.3, >10000 nM for CYP1B1, CYP1A1, CYP1A2, respectively. CYP1B1-IN-3 inhibits cell migration and invasion. CYP1B1-IN-3 inhibits P-gp, AKT/ERK, FAK/SRC, and EMT pathways .
|
-
- HY-155391
-
|
|
Carbonic Anhydrase
P-glycoprotein
Wnt
β-catenin
|
Cancer
|
|
hCA/Wnt/β-catenin-IN-1 (Compd 15) is an inhibitor of hCA (Ki: 33.6, 24.1, 6.8 nM for hCA II, hCA IX, hCA XII). hCA/Wnt/β-catenin-IN-1 reduces P-gp activity. hCA/Wnt/β-catenin-IN-1 also inhibits Wnt/β-catenin signaling pathway. hCA/Wnt/β-catenin-IN-1 inhibits cancer cell viability, including the NCI/ADR-RES DOX-resistant cell line .
|
-
- HY-162268
-
|
|
MALT1
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
MALT1-IN-13 (compound 10m) is inhibitor for mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1), which to binds MALT1 protease covalently and irreversibly, inhibits MALT1 with the IC50 of 1.7 μM. MALT1-IN-13 inhibits proliferation against ABC-DLBCL and induces apoptosis in ABC-DLBCL HBL1. MALT1-IN-13 regulates mTOR and PI3K-Akt pathways .
|
-
- HY-110294
-
|
A37
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
CM037 is a highly selective and competitive ALDH1A1 inhibitor (IC50=4.6 μM). CM037 blocks the catalytic activity of ALDH1A1, thereby inhibiting the activation of the downstream HIF-1α/VEGF pathway. CM037 is mainly used to study the ALDH1A1-mediated regulation of cancer stem cells (CSCs) and angiogenesis, especially in breast cancer, showing the potential to inhibit tumor angiogenesis and stem cell characteristics .
|
-
- HY-171174
-
|
|
CDK
STAT
Wnt
|
Cancer
|
|
CDK8-IN-16 (Compound 51) is an orally active dual inhibitor for CDK8 and CDK19 wih IC50 of 5.1 nM and 5.6 nM. CDK8-IN-16 inhibits the phospho-STAT1 SER727 with an IC50 of 17.9 nM in SW620 cell, inhibits WNT signaling pathway with an IC50 of 7.2 nM in 7dF3 cell. CDK8-IN-16 exhibits good pharmacokinetic characteristics in rat models with an oral bioavailability of 57% .
|
-
- HY-169403
-
|
|
STAT
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
NW16 is an orally active inhibitor for STAT3 with Kd of 11.0 μM. NW16 arrests the cell cycle at S phase, induces apoptosis in HCT116, and inhibits the proliferation of cancer cell HCT116, A549, and B16 with IC50s of 0.28, 1.22, and 9.86 μM, respectively. NW16 induces the production of ROS, inhibits the PI3K/AKT signaling pathway, and thus exhibits antitumor efficacy in mouse model .
|
-
- HY-105349
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC50=0.23 nM). T-0156 inhibits PDE6 (IC50=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC50>10 μM). T-0156 enhances the nitric oxide (NO)/cGMP pathway .
|
-
- HY-155847
-
|
|
Phosphatase
|
Cancer
|
|
LYP-IN-3 (compound D34) is a selective inhibitor of Lymphoid-tyrosine phosphatase (LYP) (Ki=0.93 μM), and regulates T-cell receptor (TCR) signaling pathway in tumor progress. LYP-IN-3 activates T-cell and inhibits M2 macrophage polarization, but upregulates PD-1/PD-L1 expression. LYP-IN-3 can be leveraged with PD-1/PD-L1 inhibitor, for futher cancer immunotherapy .
|
-
- HY-147613
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-6 (Compound 19c) is a potent and dual inhibitor of PI3K/mTOR. PI3K/mTOR Inhibitor-6 displays better stability in artificial gastric fluids than gedatolisib. PI3K/mTOR Inhibitor-6 significantly suppresses the PI3K/Akt/mTOR signaling pathway at 10 μM. PI3K/mTOR Inhibitor-6 has the potential for the research of cancer diseases .
|
-
- HY-147941
-
|
|
PROTACs
EGFR
|
Cancer
|
|
MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer .
|
-
- HY-153855
-
|
RXC004
|
Wnt
Acyltransferase
Porcupine
|
Cancer
|
|
Zamaporvint (RXC004) is an orally active and selective inhibitor of Wnt. Zamaporvint targete membrane-bound o-acyltransferase Porcupine and inhibited Wnt ligand palmitoylation, secretion, and pathway activation. Zamaporvint displays a favorable pharmacokinetic profile and shows potent antiproliferative effects in Wnt ligand-dependent colorectal and pancreatic cell lines. Zamaporvint possesses multiple antitumor mechanisms and can be used in cancer research .
|
-
- HY-14928A
-
|
|
PPAR
ERK
JNK
TGF-beta/Smad
NO Synthase
COX
NF-κB
Interleukin Related
|
Metabolic Disease
|
|
Lobeglitazone sulfate is a new type of thiazolidinedione. Lobeglitazone sulfate is the orally active agonist for PPAR with EC50 of 137.4 nM and 546.3 nM for PPARγ and PPARα. Lobeglitazone sulfate is the inhibitor for ERK/JNK/Smad/NF-κB signaling pathway. Lobeglitazone sulfate exhibits anti-inflammatory, anti-diabetic, anti-fibrotic and anti-atherosclerotic properties .
|
-
- HY-133865
-
|
|
Interleukin Related
|
Metabolic Disease
Inflammation/Immunology
|
|
Diacetoxy-6-gingerdiol is a gingerol isolated with anti-inflammatory and antioxidant effects, which is found in the dichloromethane extract of rhizomes of ginger (Zingiber officinale Roscoe). Diacetoxy-6-gingerdiol protects the extracellular matrix of nucleus pulposus cells and ameliorates intervertebral disc degeneration by inhibiting the IL-1β-mediated NLRP3 pathway .
|
-
- HY-B0094R
-
|
|
HCV
Parasite
Akt
Ferroptosis
|
Infection
Neurological Disease
Cancer
|
|
Artemisinin (Standard) is the analytical standard of Artemisinin. This product is intended for research and analytical applications. Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
|
-
- HY-115888
-
|
|
Macrophage migration inhibitory factor (MIF)
|
Cancer
|
|
MIF2-IN-1 (compound 5d) is a potent inhibitor of MIF2 tautomerase with an IC50 of 1.0 μM. MIF2-IN-1 suppresses the proliferation of non-small cell lung cancer cells by the induction of cell cycle arrest via deactivation of the MAPK pathway. MIF2-IN-1 has the potential for the research of cancer diseases .
|
-
- HY-P9931
-
|
CNTO 1959
|
Interleukin Related
|
Inflammation/Immunology
|
|
Guselkumab is a recombinant human IgG1 monoclonal antibody against the IL-23p19 subunit. Guselkumab binds to human and cynomolgus monkey IL-23 with Kd values of 3.3 and 1.9 pmol/L, respectively. Guselkumab inhibits production of cytokines lying downstream of the IL-23 signaling pathway and can be used for psoriatic arthritis research .
|
-
- HY-N2638R
-
|
|
Apoptosis
|
Cardiovascular Disease
|
|
Ilexsaponin A (Standard) is the analytical standard of Ilexsaponin A. This product is intended for research and analytical applications. Ilexsaponin A, isolated from the root of Ilex pubescens, attenuates ischemia-reperfusion-induced myocardial injury through anti-apoptotic pathway. Ilexsaponin A can reduce myocardial infarct size, lower the serum levels of LDH, AST and CK-MB, increase cellular viability and inhibit apoptosis in hypoxia/reoxygenation cardiomyocytes .
|
-
- HY-B0252R
-
|
HCTZ (Standard)
|
TGF-beta/Smad
Potassium Channel
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Hydrochlorothiazide (Standard) is the analytical standard of Hydrochlorothiazide. This product is intended for research and analytical applications. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect .
|
-
- HY-163030
-
|
|
Elastase
NF-κB
p38 MAPK
Bacterial
|
Infection
Inflammation/Immunology
|
|
LasB-IN-1 (compound 5f) is a potent and orally active inhibitor of LasB (IC50 = 8.7 μM). LasB-IN-1 effectively attenuates elastase production and biofilm formation by P. aeruginosa while alleviating the inflammatory response through downregulating MAPK and NF-κB pathways. LasB-IN-1 is potential to be a novel anti-infective candidate against drug-resistant infections .
|
-
- HY-124124
-
|
|
Endogenous Metabolite
Drug Metabolite
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
N-Methylnicotinamide is an endogenous metabolite with antithrombotic effect. N-Methylnicotinamide via production/release of prostacyclin inhibits arterial thrombosis development. N-Methylnicotinamide is also the N-methylation product from nicotinamide catalyzed by N-methyltransferase within nicotinate and nicotinamide metabolism pathway. N-Methylnicotinamide is a potential biomarker in miR-1291-altered pancreatic cell metabolism and tumorigenesis .
|
-
- HY-N0636R
-
|
|
Apoptosis
|
Cancer
|
|
Eriocitrin (Standard) is the analytical standard of Eriocitrin. This product is intended for research and analytical applications. Eriocitrin is a flavonoid isolated from lemons that is a powerful antioxidant. Eriocitrin inhibits the proliferation of liver cancer cells by arresting the cell cycle in the S phase by upregulating p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating intrinsic signaling pathways involving mitochondria .
|
-
- HY-130723
-
|
|
AMPK
|
Cancer
|
|
AMPK activator 2 (compound 7a), a fluorine-containing proguanil derivative, up-regulates AMPK signal pathway and downregulates mTOR/4EBP1/p70S6K. AMPK activator 2 inhibits proliferation and migration of human cancer cell lines (UMUC3, T24, A549) .
|
-
- HY-130723A
-
|
|
AMPK
|
Cancer
|
|
AMPK activator 2 (compound 7a) hydrochloride, a fluorine-containing proguanil derivative, up-regulates AMPK signal pathway and downregulates mTOR/4EBP1/p70S6K. AMPK activator 2 hydrochloride inhibits proliferation and migration of human cancer cell lines (UMUC3, T24, A549) .
|
-
- HY-N10623
-
|
|
Tyrosinase
|
Cancer
|
|
5-epi-Arvestonate A is a sesquiterpenoid isolated from the whole plants of Seriphidium transiliense. 5-epi-Arvestonate A promotes melanogenic production by activating the transcription of microphthalmia-associated transcription factor (MITF) and tyrosinase family genes. 5-epi-Arvestonate A inhibits the expression of IFN-γ-chemokine through the JAK/STAT signaling pathway in immortalized human keratinocyte (HaCaT) cells .
|
-
- HY-N0626
-
|
|
Fungal
Bacterial
Endogenous Metabolite
Antibiotic
IGF-1R
|
Infection
|
|
Sorbic acid is an effective, safe, and non-toxic food preservative. It can effectively inhibit most molds, yeasts, and certain bacteria. Sorbic acid is orally active and can enhance the growth performance of economically important animals (Duroc × Landrace × Yorkshire piglets) by activating the insulin-like growth factor system (IGF), and it can also lead to lipid accumulation by disrupting lipid clearance pathways 。
|
-
- HY-N2908
-
|
Methyl atrarate
|
Androgen Receptor
NO Synthase
p38 MAPK
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases .
|
-
- HY-B0337B
-
|
Sulphadimethoxine 1000 µg/mL in methanol
|
Antibiotic
|
Infection
|
|
Sulfadimethoxine 1000 μg/mL in methanol (Sulphadimethoxine 1000 μg/mL in methanol) is a sulfonamide antibiotic that inhibits the enzyme dihydropteroate synthase, thereby blocking dihydrofolic acid synthesis and disrupting folic acid production in prokaryotic organisms. Its antimicrobial activity extends to both Gram-positive and Gram-negative bacteria, as well as Chlamydia. Resistance to this compound may arise through alterations in dihydropteroate synthase or the activation of alternative pathways for folic acid synthesis.
|
-
- HY-103164
-
|
|
Adenosine Receptor
Monoamine Oxidase
|
Neurological Disease
|
|
(E)-8-(3-Chlorostyryl)caffeine is a selective adenosine A2A receptor antagonist. (E)-8-(3-Chlorostyryl)caffeine inhibits monoamine oxidase B (MAO-B) with a Ki value of 70 nM by a pathway that is independent of its actions on the A2A receptor. (E)-8-(3-Chlorostyryl)caffeine has the potential for Parkinson's disease research .
|
-
- HY-N2259
-
|
(+)-Curcumenol
|
Cytochrome P450
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Curcumenol ((+)-Curcumenol) is a potent CYP3A4 inhibitor with an IC50 of 12.6 μM, which is one of constituents in the plants of medicinally important genus of Curcuma zedoaria, with neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. Curcumenol ((+)-Curcumenol) suppresses Akt-mediated NF-κB activation and p38 MAPK signaling pathway in LPS-stimulated BV-2 microglial cells .
|
-
- HY-N2996
-
|
|
HIV Protease
|
Infection
|
|
Ganodermanondiol is a melanogenesis inhibitor isolated from the Ganoderma lucidum .Ganodermanondiol exhibits potent cytoprotective effects on tert-butyl hydroperoxide-induced hepatotoxicity . Ganodermanondiol shows significant anti-HIV-1 protease activity with an IC50 of 90 μM . Ganodermanondiol exhibits a strong anticomplement activity against the classical pathway of the complement system with an IC50 of 41.7μM .
|
-
- HY-N0314R
-
|
|
Interleukin Related
Prostaglandin Receptor
Apoptosis
|
Inflammation/Immunology
|
|
Pectolinarin (Standard) is the analytical standard of Pectolinarin. This product is intended for research and analytical applications. Pectolinarin possesses anti-inflammatory activity . Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin suppresses cell proliferation and inflammatory response and induces apoptosis via inactivation of the PI3K/Akt pathway .
|
-
- HY-124896
-
|
6-Geranylnaringenin; Mimulone
|
Phosphatase
Apoptosis
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Bonannione A (6-Geranylnaringenin; Mimulone), a prenylflavonoid, is an orally active and potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 14 µM. Bonannione A triggers caspase-dependent apoptosis. Bonannione A induces autophagy through p53-mediated AMPK/mTOR pathway. Bonannione A shows anti-inflammatory, antiradical and anti-cancer activity .
|
-
- HY-113853
-
|
|
Akt
Apoptosis
|
Others
|
|
WF-10129 is a cytotoxic steroidal compound isolated from the plant Physalis. WF-10129 inhibits liver cancer cell proliferation, induces apoptosis, interferes with metabolism, and significantly reduces lactate production in vitro and in vivo. WF-10129 can also exert anti-tumor activity by regulating the expression of related genes and proteins through the AKT-p53 pathway.
|
-
- HY-170943
-
|
|
AMPK
GLUT
|
Metabolic Disease
|
Antidiabetic agent 7 (Compound 5m) is hyperglycemic inhibitor. Antidiabetic agent 7 exhibits promising potency to stimulate GLUT4 translocation in skeletal muscle cells via activating AMPK-dependent pathway. Antidiabetic agent 7 reduces blood glucose levels. Antidiabetic agent 7 shows favorable pharmacokinetic properties. Antidiabetic agent 7 is potential to be used for anti-hyperglycemic research .
|
-
- HY-114413
-
|
|
HSP
Apoptosis
|
Cancer
|
|
YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathway against glioblastoma, directly binding to heat shock protein 90 (HSP90) with an IC50 of 820 nM on NFAT nuclear translocation. YZ129-induced GBM cell-cycle arrest at the G2/M phase promotes apoptosis and inhibited tumor cell proliferation and migration .
|
-
- HY-N8263
-
|
|
Bacterial
Fungal
NF-κB
|
Infection
Inflammation/Immunology
|
|
Nepetoidin B, an anti-inflammatory agent, inhibits inflammation by modulating the NF-κB and Nrf2/HO-1 signaling pathways. Nepetoidin B also has antifungal and antibacterial activity. Nepetoidin B is a natural product that can be obtained from Salvia plebeia R. Br. Nepetoidin B can be used in anti-inflammatory and anti-infectious research .
|
-
- HY-100487
-
|
MLN7243
|
E1/E2/E3 Enzyme
NF-κB
Apoptosis
|
Cancer
|
|
TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis .
|
-
- HY-N2098R
-
|
|
NF-κB
|
Cancer
|
|
Obtusifolin (Standard) is the analytical standard of Obtusifolin. This product is intended for research and analytical applications. Obtusifolin, isolated from the seeds of Cassia obtusifolia, regulates the gene expression and production of MUC5AC mucin in airway epithelial cells via inhibiting NF-kB pathway . Obtusifolin suppresses phthalate esters-induced breast cancer bone metastasis by targeting parathyroid hormone-related protein .
|
-
- HY-148305
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-28 (compound 3) is an immune checkpoint inhibitor of PD-1/PD-L1 signaling pathway (IC50=0.744 µM). PD-1/PD-L1-IN-28 shows good research potential in tumor immunity .
|
-
- HY-W009776
-
|
Suberohydroxamic acid; SBHA
|
HDAC
Apoptosis
|
Cancer
|
|
Suberoyl bis-hydroxamic acid (Suberohydroxamic acid; SBHA) is a competitive and cell-permeable HDAC1 and HDAC3 inhibitor with ID50 values of 0.25 μM and 0.30 μM, respectively .Suberoyl bis-hydroxamic acid renders MM cells susceptible to apoptosis and facilitates the mitochondrial apoptotic pathways .Suberoyl bis-hydroxamic acid can be used for the study of medullary thyroid carcinoma (MTC) .
|
-
- HY-124089
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
Eicosapentaenoyl ethanolamide, an omega-3 fatty acid, is one of N-acylethanolamines (NAEs). Eicosapentaenoyl ethanolamide is cannabinoid CB1/CB2 receptor agonist. Eicosapentaenoyl ethanolamide acts as a metabolic signal. Eicosapentaenoyl ethanolamide inhibits dietary restriction (DR)-induced lifespan extension in wild type animals and suppresses lifespan extension in a TOR pathway mutant .
|
-
- HY-N11420
-
|
|
Bacterial
Phytohormone
|
Others
|
|
Coronatine is a plant growth regulator that mimicks the jasmonic acid-isoleucine conjugate (JA-Ile), targets the jasmonic acid receptor COI1, activates the jasmonic acid signaling pathway, thereby inhibiting salicylic acid (SA)-dependent defense responses. Coronatine antagonizes the stomatal closure, induces plant cell necrosis and chlorosis, interfers with plant hormone balance, thereby promoting pathogen infection .
|
-
- HY-122198
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation .
|
-
- HY-167931
-
|
|
Drug Derivative
|
Metabolic Disease
|
|
Cinnamohydrazide, an unsaturated carboxylic acid derivative, serves as a precursor to aspartame through enzyme-mediated amination to phenylalanine. This compound may offer potential benefits in the prevention and treatment of diabetes by facilitating insulin secretion, enhancing pancreatic β-cell function, inhibiting hepatic gluconeogenesis, promoting glucose uptake, amplifying insulin signaling pathways, delaying carbohydrate digestion and glucose absorption, and reducing protein glycation and insulin fibrillation.
|
-
- HY-123718
-
|
|
Parasite
|
Others
|
|
6-Benzylthioinosine is a compound with antileukemic activity that increases cytotoxicity against acute myeloid leukemia cells when combined with Metformin (HY-B0627), modulating cellular metabolism and signaling pathways through multiple mechanisms. 6-Benzylthioinosine is also a potential precursor inhibitor of mammalian nucleoside transporter ENT1 (es), and its derivatives have anti-Toxoplasma activity .
|
-
- HY-50868
-
|
INNO-406; NS-187
|
Bcr-Abl
Src
Apoptosis
|
Cancer
|
|
Bafetinib is an orally active Lyn/Bcr-Abl tyrosine kinase inhibitor. Bafetinib enhances the activity of several pro-apoptotic Bcl-2 homology (BH) 3-pure proteins (Bim, Bad, Bmf, and Bik) through intrinsic apoptotic pathways regulated by the Bcl-2 family, and induces apoptosis of Ph + leukemia cells. Bafetinib has antitumor activity .
|
-
- HY-151622
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-11 is an orally active PI3K/mTOR inhibitor (IC50: 3.5, 4.6, and 21.3 nM for PI3Kα, PI3Kδ, and mTOR). PI3K/mTOR Inhibitor-11 regulates the PI3K/AKT/mTOR signaling pathway by inhibiting the phosphorylation of AKT and S6 proteins. PI3K/mTOR Inhibitor-11 can be used in the research of cancers .
|
-
- HY-N2360
-
|
|
E1/E2/E3 Enzyme
Apoptosis
MMP
ClpP
|
Infection
Inflammation/Immunology
Cancer
|
|
Hinokiflavone is a novel modulator of pre-mRNA splicing activity extracted from plants with anti-inflammatory, anti-tumor and antiviral activities. Hinokiflavone is also a potent inhibitor for matrix metalloproteinases (MMPs). Hinokiflavone attenuates the virulence of Methicillin (HY-121544)-resistant staphylococcus aureus by inhibiting caseinolytic protease P (ClpP) with an IC50 value of 34.36 mg/mL. Hinokiflavone induces apoptosis via the reactive oxygen species-mitochondria-mediated apoptotic pathway and inhibits tumor cell migration and invasion. Hinokiflavone is a SUMO protease inhibitor against sentrin-specific protease 1 (SENP1) activity .
|
-
- HY-168718
-
|
|
FAK
JAK
Aurora Kinase
PI3K
Akt
Apoptosis
|
Cancer
|
|
FAK-IN-22 (Compound 26) is an inhibitor of FAK, JAK3, and Aurora B, with IC50 values of 50.94 nM, 9.99 nM, and 0.49 nM, respectively, effectively inhibiting tumor occurrence and metastasis in pancreatic ductal adenocarcinoma (PDAC). FAK-IN-22 effectively inhibits the proliferation of PANC-1 cells, with an IC50 value of 0.15 μM. FAK-IN-22 induces apoptosis and G2/M phase arrest in PANC-1 cells by inhibiting the FAK/PI3K/Akt signaling pathway .
|
-
- HY-B0627A
-
|
1,1-Dimethylbiguanide (glycinate)
|
AMPK
Autophagy
Mitophagy
Apoptosis
mTOR
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Metformin (1,1-Dimethylbiguanide) glycinate inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin glycinate also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin glycinate regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo .
|
-
- HY-N1181R
-
|
|
Endogenous Metabolite
ClpP
Bacterial
Apoptosis
Akt
Interleukin Related
COX
JNK
p38 MAPK
Reactive Oxygen Species
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Tamarixetin (Standard) is the analytical standard of Tamarixetin. This product is intended for research and analytical applications. Tamarixetin (4'-O-Methyl Quercetin) is an orally active natural flavonoid derivative of quercetin and caseinolytic protease p (ClpP) inhibitor with anti-inflammatory, antioxidant and antitumor effects. Tamarixetin inhibits the hydrolytic activity of ClpP to the fluorescent substrate Suc-LY-AMC with an IC50 of 49.73 μM, which can be used for the study of Staphylococcus aureus infection. Tamarixetin inhibits tumor cell growth, induces apoptosis, and cell cycle arrest. Tamarixetin prevents cardiac hypertrophy by inhibiting the NFAT and AKT pathways .
|
-
- HY-122214
-
AC-73
5 Publications Verification
|
Autophagy
|
Cancer
|
|
AC-73 is a first specific, orally active inhibitor of cluster of differentiation 147 (CD147), which specifically disrupts CD147 dimerization, thereby mainly suppressing the CD147/ERK1/2/STAT3/MMP-2 pathways. AC-73 inhibits the motility and invasion of hepatocellular carcinoma cells . AC-73 is also an anti-proliferative agent and an inducer of autophagy in leukemic cells .
|
-
- HY-A0081
-
|
|
Dopamine Receptor
SARS-CoV
Sodium Channel
|
Neurological Disease
Cancer
|
|
Fluphenazine dihydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dihydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine dihydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dihydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dihydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-135317F
-
|
CA-4948 phosphate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib phosphate (CA-4948 phosphate) is the phosphate salt form of Emavusertib (HY-135317). Emavusertib phosphate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib phosphate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib phosphate exhibits antitumor activity in mouse model .
|
-
- HY-119980B
-
|
|
Dopamine Receptor
Sodium Channel
SARS-CoV
|
Neurological Disease
Cancer
|
|
Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-N2334A
-
|
Chenodeoxycholylglycine sodium salt; Sodium glycochenodeoxycholate
|
Endogenous Metabolite
Apoptosis
STAT
BCL6
Interleukin Related
Caspase
|
Metabolic Disease
Cancer
|
|
Glycochenodeoxycholic acid sodium salt (Sodium glycochenodeoxycholate) is a relatively toxic bile salt generated in the liver from chenodeoxycholic acid and glycine. Glycochenodeoxycholic acid sodium salt inhibits Autophagosome formation and impairs lysosomal function by inhibiting lysosomal proteolysis and increasing lysosomal pH in human normal liver cells, leading to the Apoptosis of human hepatocyte cells. Glycochenodeoxycholic acid sodium salt induces stemness and chemoresistance via activating STAT3 signaling pathway in hepatocellular carcinoma cells (HCC). Glycochenodeoxycholic acid sodium salt is promising for research in the field of cholestasis desease, hepatocellular carcinoma and primary sclerosing cholangitis (PSC) .
|
-
- HY-135317E
-
|
CA-4948 maleate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib maleate (CA-4948 maleate) is the maleate salt form of Emavusertib (HY-135317). Emavusertib maleate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib maleate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib maleate exhibits antitumor activity in mouse model .
|
-
- HY-13811
-
|
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity .
|
-
- HY-B0808A
-
|
Oxaprozinum potassium; Wy21743 potassium
|
COX
NF-κB
Akt
IKK
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Oxaprozin potassium is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin potassium also inhibits the activation of NF-κB. Oxaprozin potassium induces cell apoptosis. Oxaprozin potassium shows anti-inflammatory activity. Oxaprozin potassium-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties .
|
-
- HY-156027
-
-
- HY-171006
-
|
|
Caspase
PARP
Pyroptosis
Interleukin Related
IFNAR
|
Infection
Inflammation/Immunology
|
|
IRF1-IN-1 (Compound I-2) is an IRF1 inhibitor. IRF1-IN-1 decreases the recruitment of IRF1 to the promoter of CASP1. IRF1-IN-1 inhibits cell death signaling pathway (i.e., cleavage of Caspase 1, GSDMD, IL-1 and PARP1). IRF1-IN-1 has a protective effect on ionizing radiation-induced inflammatory skin injury .
|
-
- HY-162936
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
SILA-123 is a FLT3 inhibitor (FLT3-WT: IC50=2.1 nM; FLT3-ITD: IC50=1.0 nM). SILA-123 inhibits FLT3 phosphorylation and downstream signaling pathways, leading to apoptosis by arresting cell cycle progression at the G0/G1 phase. SILA-123 can be used in the study of acute myeloid leukemia .
|
-
- HY-124122
-
|
|
VEGFR
Checkpoint Kinase (Chk)
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
|
BPTQ is a potent inhibitor against VEGFR1 and CHK2 with IC50 values of 0.54 and 1.70 µmol/L, respectively. BPTQ is also an intercalator of DNA with anticancer activities. BPTQ inhibits the proliferation of HL-60 cells by arresting cells at S and G2/M phase with an IC50 value of 12 µmol/L. BPTQ also activates the mitochondria-mediated Apoptosis pathway by a decrease in mitochondrial membrane potential, increase in the Bax:Bcl-2 ratio and activation of caspases .
|
-
- HY-121537
-
|
|
COX
Akt
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities .
|
-
- HY-155821
-
|
|
NF-κB
NO Synthase
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 55 (compound 9j) is a derivative of Coixol and has anti-inflammatory activity. Anti-inflammatory agent 54 inhibits the NF-κB pathway and downregulates the expression of iNOS, TNF-α, IL-6 and IL-1β. Anti-inflammatory agent 54 inhibits LPS-induced nitric oxide (NO) production in RAW264.7 macrophages (IC50: 0.8 μM) and exerts in vivo anti-inflammatory activity in a mouse auricular edema model .
|
-
- HY-119980
-
|
|
Sodium Channel
Dopamine Receptor
SARS-CoV
|
Infection
Neurological Disease
Cancer
|
|
Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-155820
-
|
|
NF-κB
NO Synthase
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 54 (compound 9c) is a derivative of Coixol and has anti-inflammatory activity. Anti-inflammatory agent 54 inhibits the NF-κB pathway and downregulates the expression of iNOS, TNF-α, IL-6 and IL-1β. Anti-inflammatory agent 54 inhibits LPS-induced nitric oxide (NO) production in RAW264.7 macrophages (IC50: 2.4 μM) and exerts in vivo anti-inflammatory activity in a mouse auricular edema model .
|
-
- HY-B0097R
-
|
5-Fluorouracil 2'-deoxyriboside (Standard)
|
Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
Bacterial
CMV
HSV
Apoptosis
|
Infection
Cancer
|
|
Floxuridine (Standard) is the analytical standard of Floxuridine. This product is intended for research and analytical applications. Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis . Floxuridine has antiviral effects against HSV and CMV .
|
-
- HY-119948
-
|
|
Cyclin G-associated Kinase (GAK)
MDM-2/p53
|
Cancer
|
AKCI is a type of AURKC-IκBα interaction inhibitor, with an IC50 value of 24.9 μM. In MDA-MB-231 cells, AKCI can induce G2/M cell cycle arrest by regulating the p53/p21/CDC2/cyclin B1 pathway, inhibit cell migration and invasion, and reduce colony formation and tumor growth. AKCI can be used for research on breast cancer .
|
-
- HY-135317C
-
|
CA-4948 tosylate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib tosylate (CA-4948 tosylate) is the tosylate salt form of Emavusertib (HY-135317). Emavusertib tosylate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib tosylate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib tosylate exhibits antitumor activity in mouse model .
|
-
- HY-B0319
-
|
UK-20349
|
Fungal
Antibiotic
Parasite
Akt
PI3K
mTOR
Autophagy
|
Infection
Cancer
|
|
Tioconazole (UK-20349) is a broad-spectrum antifungal imidazole derivative. Tioconazole inhibits several dermatophytes and yeasts, with MIC50 values of less than 3.12 mg/L and 9 mg/L, respectively. Additionally, Tioconazole exhibits anti-parasitic activity. Tioconazole exerts anticancer activity by inhibiting the PI3K/AKT/mTOR signaling pathway and blocking autophagy. Tioconazole is applicable for research in the fields of anti-infection and anticancer therapy .
|
-
- HY-N0405R
-
|
|
TNF Receptor
Interleukin Related
|
Neurological Disease
Cancer
|
|
Orientin (Standard) is the analytical standard of Orientin. This product is intended for research and analytical applications. Orientin is a neuroprotective agentinhibits which has anti-inflammation, anti-oxidative, anti-tumor, and cardio protection properties. Orientin inhibits the levels of IL-6, IL-1β and TNF-α. Orientin increases IL-10 level. Orientin exhibits neuroprotective effect by inhibits TLR4 and NF-kappa B signaling pathway. Orientin can used in study neuropathic pain .
|
-
- HY-N2334
-
|
Chenodeoxycholylglycine
|
Endogenous Metabolite
Apoptosis
STAT
BCL6
Interleukin Related
Caspase
|
Metabolic Disease
Cancer
|
|
Glycochenodeoxycholic acid (Chenodeoxycholylglycine) is a relatively toxic bile salt generated in the liver from chenodeoxycholic acid and glycine. Glycochenodeoxycholic acid inhibits Autophagosome formation and impairs lysosomal function by inhibiting lysosomal proteolysis and increasing lysosomal pH in human normal liver cells, leading to the Apoptosis of human hepatocyte cells. Glycochenodeoxycholic acid induces stemness and chemoresistance via activating STAT3 signaling pathway in hepatocellular carcinoma cells (HCC). Glycochenodeoxycholic acid is promising for research in the field of cholestasis desease, hepatocellular carcinoma and primary sclerosing cholangitis (PSC) .
|
-
- HY-13065R
-
|
|
Akt
Reactive Oxygen Species
Apoptosis
Autophagy
|
Cancer
|
|
Isobavachalcone (Standard) is the analytical standard of Isobavachalcone. This product is intended for research and analytical applications. Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM). Isobavachalcone also induces Reactive Oxyen Species (ROS) generation in OVCAR-8 cells and has exhibit cancer anti-promotive and anti-proliferative activity .
|
-
- HY-168929
-
|
|
Fluorescent Dye
Phosphatase
STAT
Apoptosis
|
Cancer
|
|
SHP1 activator 1 (Compound 3n) is an activator for src homology-2 domain-containing protein tyrosine phosphatase 1(SHP1) with an EC50 of 17.66 μM. SHP1 activator 1 inhibits the proliferation of ABC-DLBCL cells, induces apoptosis by inhibiting STAT3 signaling pathway. SHP1 activator 1 emitts blue and green fluorescence signalis in MDA-MB-231 cell, and can be used as a cell imaging agent .
|
-
- HY-163472
-
|
|
Stearoyl-CoA Desaturase (SCD)
|
Metabolic Disease
Cancer
|
|
PR280 is a potent inhibitor of dihydroceramide desaturase 1 (Des1) (IC50=700 nM). PR280 forms hydrogen bonds with the amino acid residues of Des1, and its cyclopropenone group may form a coordination with the iron center, thus stabilizing the binding to the active site of Des1 and inhibiting the sphingosine lipid synthesis pathway of dihydroceramide (dhCer) to form ceramide. PR280 can be used in the study of diseases related to sphingosine lipid metabolism, such as cancer and metabolic diseases .
|
-
- HY-N12959
-
|
DDR
|
PI3K
Akt
NF-κB
|
Cancer
|
|
5,4'-Dihydroxy-6,8-dimethoxy-7-O-rhamnosyl flavone (DDR) is an anticancer agent that can be extracted from Indigofera ovata. 5,4'-Dihydroxy-6,8-dimethoxy-7-O-rhamnosyl flavone can inhibit the PI3K/AKT and NF-кB pathways, inhibit the invasion and migration of cancer cells, and has anticancer activity .
|
-
- HY-B0808
-
|
Oxaprozinum; Wy21743
|
COX
NF-κB
Akt
IKK
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Oxaprozin is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB. Oxaprozin induces cell apoptosis. Oxaprozin shows anti-inflammatory activity. Oxaprozin-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties .
|
-
- HY-N8931
-
|
Lithospermic acid monomethyl ester
|
Akt
|
Neurological Disease
|
|
Monomethyl lithospermate activates the PI3K/AKT pathway, which plays a protective role in nerve injury. Monomethyl lithospermate can improve the survival ability of SHSY-5Y cells, inhibit the breakdown of mitochondrial membrane potential (MMOP) and inhibit cell apoptosis. Monomethyl lithospermate also reduced the level of oxidative stress in the brain tissue of rats with middle artery occlusion (MCAO) and improved nerve damage in rats with ischemic stroke (IS) .
|
-
- HY-144765
-
|
|
NF-κB
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
|
NF-κB-IN-4 (compound 17) is a potent and BBB-penetrated NF-κB pathway inhibitor with blood brain barrier (BBB) permeability. NF-κB-IN-4 exhibits potential anti-neuroinflammatory activity with low toxicity. NF-κB-IN-4 can block the activation and phosphorylation of IκBα, reduce expression of NLRP3, and thus inhibit NF-κB activation. NF-κB-IN-4 can be used for neuroinflammation related diseases research .
|
-
- HY-168030
-
|
|
Apoptosis
Ferroptosis
Carbonic Anhydrase
Reactive Oxygen Species
Caspase
Mitochondrial Metabolism
|
Cancer
|
|
hCAIX-IN-23 (Compound 27) is a human carbonic anhydrase (hCA) inhibitor with Ki values of 10.4 and 8.5 nM for hCA IX and hCA XII, respectively. In addition to inhibiting hCA activity, hCAIX-IN-23 releases NO, exhibiting dual antitumor activity. hCAIX-IN-23 induces apoptosis by regulating mitochondrial caspase activity and the ferroptosis pathway (ferroptosis) through the downregulation of hCA IX and iron-regulatory protein expression. hCAIX-IN-23 is useful for renal cancer research .
|
-
- HY-135317B
-
|
CA-4948 hydrochloride
|
IRAK
FLT3
Apoptosis
NF-κB
MyD88
|
Inflammation/Immunology
Cancer
|
|
Emavusertib hydrochloride (CA-4948 tosylate) is the hydrochloride salt form of Emavusertib (HY-135317). Emavusertib hydrochloride is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib hydrochloride inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib hydrochloride exhibits antitumor activity in mouse model .
|
-
- HY-122292
-
|
|
Antibiotic
Bacterial
|
Infection
Inflammation/Immunology
|
|
Celastramycin A is an antibiotic isolated from Streptomyces MaB-QuH-8, which exhibits antimicrobial activity against series of gram-negative bacteria and mycobacteria, with MICs between 0.05-3.1 μg/ml . Celastramycin A exhibits immunosuppressing efficacy in ex vivo Drosophila through immune deficiency pathway (IC50 of 0.008 μg/ml), inhibits the immunoresponse in human innate immunity through TNF-α signaling, inhibits IL-8 production in HUEVCs with IC50 of 0.06 μg/ml .
|
-
- HY-135317D
-
|
CA-4948 mesylate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib mesylate (CA-4948 mesylate) is the mesylate salt form of Emavusertib (HY-135317). Emavusertib mesylate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib mesylate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib mesylate exhibits antitumor activity in mouse model .
|
-
- HY-W587878
-
|
|
Cytochrome P450
Pyruvate Kinase
Fungal
Apoptosis
Insecticide
|
Infection
Cancer
|
|
Thujopsene is the inhibitor for cytochrome P450, that inhibits CYP2B6, CYP3A4, CYP2C19, CYP2C8, CYP2C9 with IC50s of 1.3, 12.6, 13.6, 29.8, and 44.9 μM, respectively. Thujopsene binds to PKM2, inhibits the metabolism pathway of cancer cell, induces apoptosis in MKN45, thereby exhibiting antitumor efficacy. Thujopsene exhibits anti-termite and antifungal activities through autoxidation .
|
-
- HY-115529
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
(-)BI97D6 is a broad-spectrum inhibitor of the Bcl-2 protein family, inhibiting Mcl-1, Bcl-2, Bcl-xL and Bcl-1 with IC50 values of 0.025, 0.031, 0.076 and 0.122 μM, respectively. (-)BI97D6 stimulates cell death through the Bak and Bax mediated mitochondrial apoptosis pathway. In addition, (-)BI97D6 inhibits Mcl-1 and can effectively induce apoptosis in acute myeloid leukemia (AML) cells .
|
-
- HY-13404A
-
|
INC280 dihydrochloride; INCB28060 dihydrochloride
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (INC280; INCB28060) dihydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-B1232R
-
|
|
Endogenous Metabolite
Cytochrome P450
Autophagy
|
Neurological Disease
Metabolic Disease
Endocrinology
Cancer
|
|
Metyrapone (Standard) is the analytical standard of Metyrapone. This product is intended for research and analytical applications. Metyrapone (Su-4885) is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone can be used for researching Cushing's syndrome and depression .
|
-
- HY-173038
-
|
|
EGFR
ERK
STAT
Apoptosis
|
Cancer
|
|
EGFR-IN-151 (Compound 10) inhibits EGFR and its downstream signaling pathways ERK/STAT3. EGFR-IN-151 inhibits the proliferation of a variety lung cancer cells (IC50s for NCI-H1781, HCC827, NCI-H3255 and NCI-H1975 is 11.7, 5.19, 7.32 and 1.53 μM, respectively), inhibits the colony formation and migration of H1975, arrests the cell cycle at G1 phase, and induces apoptosis in H1975 .
|
-
- HY-N0194
-
|
|
Apoptosis
Parasite
|
Inflammation/Immunology
Cancer
|
|
Asiatic acid, a pentacyclic triterpene found in Centella asiatica (Centella asiatica), has anticancer activity. Asiatic acid induces apoptosis in melanoma cells and has barrier protective effects on human aortic endothelial cells (HAEC). Asiatic acid also has anti-inflammatory activity and inhibits tumor necrosis factor (TNF)-α-induced endothelial barrier dysfunction. Asiatic acid also inhibits NLRP3 inflammasome activation and NF-κB pathway, effectively inhibits inflammation in rats, and has neuroprotective effects in rat spinal cord injury (SCI) model .
|
-
- HY-N0028
-
|
|
Others
|
Inflammation/Immunology
|
|
Forsythiaside A is an orally active phenylethanoid glycoside isolated from the dried fruits of Forsythia suspensa. Forsythiaside A is also an inhibitor of COX-2 and has anti-inflammatory, antioxidant and neuroprotective effects. Forsythiaside A prevents neuroinflammation and apoptosis caused by Aβ25-35 damage and may be used in Alzheimer's disease (AD) research. Forsythiaside A also activates the Nrf2/HO-1 signaling pathway and inhibits OVA-induced asthma in mice. Forsythiaside A inhibits the interaction between KLRB1 and CLEC2D .
|
-
- HY-13404C
-
|
INC280 dihydrochloride hydrate; INCB-28060 dihydrochloride hydrate
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (INC280; INCB28060) dihydrochloride hydrate is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride hydrate can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride hydrate potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride hydrate is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-B0678S
-
|
|
Isotope-Labeled Compounds
NF-κB
PGC-1α
|
Neurological Disease
Inflammation/Immunology
|
|
Metaxalone-d3 is the deuterium labeled Metaxalone. Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia .
|
-
- HY-169019
-
|
|
PI3K
Apoptosis
|
Cancer
|
XJTU-L453 is a PI3Kα inhibitor with an IC50 value of 0.4 nM. XJTU-L453 can inhibit the proliferation of breast cancer cell lines T47D and MCF7, with IC50 values of 0.2 μM and 0.5 μM, respectively. XJTU-L453 can inhibit the PI3K pathway, induce cell cycle arrest, and trigger cell apoptosis (apoptosis). XJTU-L453 also has antitumor activity in MCF7 xenograft mice .
|
-
- HY-126876
-
|
|
Apoptosis
AMPK
Reactive Oxygen Species
|
Cancer
|
|
GL-V9 inhibits proliferation of HepG2 cell (IC50 is 35.2 μM) through induction of apoptosis and cell cycle arrest at G2/M phase. GL-V9 regulates mitochondrial membrane potential and increases the production of intracellular reactive oxygen species. GL-V9 inhibits the pentose phosphate pathway (PPP), enhances fatty acid oxidation (FAO) through activation of AMPK, and thus inhibits the metastasis of cancer cells. GL-V9 exhibits antitumor efficacy in mouse model .
|
-
- HY-116522
-
-
- HY-13404
-
|
INC280; INCB28060
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-13404B
-
|
INC280 hydrochloride; INCB-28060 hydrochloride
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (INC280; INCB28060) hydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib hydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib hydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib hydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-171007
-
-
- HY-B0678S1
-
|
AHR438-d6; NSC170959-d6
|
Isotope-Labeled Compounds
NF-κB
PGC-1α
|
Neurological Disease
Inflammation/Immunology
|
|
Metaxalone-d6 is deuterium labeled Metaxalone. Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia .
|
-
- HY-121012
-
|
|
NF-κB
Akt
|
Endocrinology
|
|
(rac)-AG-205 is a potent inhibitor of progesterone receptor membrane component 1 (Pgrmc1) that induces genes involved in sterol synthesis, including the INSIG1 protein, which forms a complex with PGRMC1. (rac)-AG-205 prevents neuronal resistance to hypoxic ischaemia by blocking NF-kB signalling and activation of the BDNF/PI3K/AKT pathway .
|
-
- HY-Y0669S
-
-
- HY-P10897
-
-
- HY-128749AR
-
|
|
Endogenous Metabolite
|
Cancer
|
|
D-Glucaric acid (tetrahydrate) (Standard) is the analytical standard of D-Glucaric acid (tetrahydrate). This product is intended for research and analytical applications. D-Glucaric acid tetrahydrate is the end-products of the D-glucuronic acid pathway in mammals. D-Glucaric acid tetrahydrate is also found in fruits and vegetables. D-Glucaric acid tetrahydrate can be used to reduce cholesterol and inhibits tumor development. D-Glucaric acid tetrahydrate also enhances human immunity and reduce cancer risks .
|
-
- HY-N0236
-
Corylin
5 Publications Verification
|
Antibiotic
STAT
|
Infection
Metabolic Disease
Cancer
|
|
Corylin is an orally active flavonoid anti-inflammatory and osteogenic agent that inhibits IL-6-induced STAT3 promoter activity and STAT3 phosphorylation. Corylin also has anticancer, antiatherosclerotic, and ameliorating activity in hyperlipidemia and insulin resistance, inducing adipocyte browning and lipolysis through SIRT1 or β3-AR-dependent pathways .
|
-
- HY-113439
-
12-HETE
1 Publications Verification
|
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
|
|
12-HETE, a major metabolic product of arachidonic acid using 12-LOX catalysis, inhibits cell apoptosis in a dose-dependent manner. 12-HETE promotes the activation and nuclear translocation of NF-κB through the integrin-linked kinase (ILK) pathway .12-HETE has both anti-thrombotic and pro-thrombotic effects . 12-HETE is a neuromodulator .
|
-
- HY-115924
-
|
|
CDK
|
Cancer
|
|
CDK1-IN-1 is a potent CDK1 inhibitor (CDK1/CycB IC50=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-1 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-1 is a potential targeted antitumor agent .
|
-
- HY-155542
-
|
|
ROR
|
Cancer
|
|
RORγ antagonist 1 (compound 22), a potent betulinic acid derivative, is an antagonist of RORγ (KD=0.18 μM). RORγ antagonist 1 exhibits anti-proliferative activity in HPAF-II pancreatic cancer xenograft model. RORγ antagonist 1 inhibits RAS/MAPK and AKT/mTORC1 pathway, and induces caspase-dependent apoptosis in pancreatic cancer cells .
|
-
- HY-N1818
-
|
3-Deoxysappanone B
|
p38 MAPK
|
Neurological Disease
Inflammation/Immunology
|
|
Deoxysappanone B (3-Deoxysappanone B) is a homoisoflavone compound isolated from Caesalpinia sappan L (Lignum Sappan). Deoxysappanone B has anti-neuroinflammatory and neuroprotective effects and inhibits the production of neuroinflammatory mediators by blocking the IκB kinase (IKK)-NF-κB and p38/ERK MAPK pathways. Deoxysappanone B can be used in disease studies of neuritis and inflammation-related neurological damage .
|
-
- HY-B0185AS
-
|
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Lidocaine-d10 (hydrochloride) is the deuterium labeled Lidocaine hydrochloride. Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride, an amide derivative, has the potential for the research of the ventricular arrhythmia[2].
|
-
- HY-P1556
-
|
|
PKG
|
Cardiovascular Disease
|
|
Vasonatrin Peptide (VNP) is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway .
|
-
- HY-146287
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Zn(BQTC) is a highly potent mitochondrial DNA (mtDNA) and nuclear DNA (nDNA) inhibitor. Zn(BQTC) causes severe damage to the mtDNA and nDNA, sequentially disruptes mitochondrial and nuclear functions. Zn(BQTC) promotes the DNA damage-induced apoptotic signaling pathway. Zn(BQTC) has selectively antiproliferative activity against A549R cells. Zn(BQTC) can be used for researching anticancer .
|
-
- HY-168517
-
|
|
Pim
Casein Kinase
Apoptosis
|
Cancer
|
|
PIM-1/CK2-IN-2 (compound 3aA) is a PIM-1/CK2 inhibitor. PIM-1/CK2-IN-2 can induce the mitochondrial apoptotic pathway in CCRF-CEM cells. PIM-1/CK2-IN-2 can be used in cancer research .
|
-
- HY-N0631
-
|
|
p38 MAPK
NF-κB
|
Inflammation/Immunology
|
|
Cornuside is a secoiridoid glucoside isolated from the fruit of Cornus officinalis Sieb. et Zucc., which is a traditional oriental medicine for treating inflammatory diseases and invigorating blood circulation. Cornuside inhibits mast cell-mediated allergic response by down-regulating MAPK and NF-κB signaling pathways. Cornuside has anti-allergic effects in vivo and in vitro which suggests a therapeutic application of this agent in inflammatory allergic diseases .
|
-
- HY-113691
-
|
|
Lipoxygenase
|
Others
|
|
(E)-L-652343 is a compound with potent cyclooxygenase and 5-lipoxygenase inhibitory activity. (E)-L-652343 can effectively inhibit the synthesis of products of these two pathways in vivo. (E)-L-652343 showed high sensitivity and specificity in the detection of geometric isomers in canine and human plasma. (E)-L-652343 showed selective metabolism in vivo, and the elimination rate of the E isomer was faster than that of the Z isomer .
|
-
- HY-146743
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-53 is a potent antitumor agent. Antitumor agent-53 induces cell cycle arrest at the G2/M phase. Antitumor agent-53 inhibits the PI3K/AKT pathway to induce the apoptosis of HGC-27 cells. Antitumor agent-53 has the potential for the research of gastrointestinal tumors .
|
-
- HY-W017212
-
|
Methyl 3-phenylpropenoate
|
Tyrosinase
Bacterial
AMPK
|
Infection
Metabolic Disease
|
|
Methyl cinnamate (Methyl 3-phenylpropenoate), an active component of Zanthoxylum armatum, is a widely used natural flavor compound. Methyl cinnamate (Methyl 3-phenylpropenoate) possesses antimicrobial activity and is a tyrosinase inhibitor that can prevent food browning. Methyl cinnamate (Methyl 3-phenylpropenoate) has antiadipogenic activity through mechanisms mediated, in part, by the CaMKK2-AMPK signaling pathway .
|
-
- HY-111875
-
|
|
SNIPERs
Epigenetic Reader Domain
|
Cancer
|
|
SNIPER(BRD)-1, consists of an IAP antagonist LCL-161 derivative and a BET inhibitor, (+)-JQ-1, connected by a linker. SNIPER(BRD)-1 induces the degradation of BRD4 via the ubiquitin-proteasome pathway. SNIPER(BRD)-1 also degrades cIAP1 , cIAP2 and XIAP with IC50s of 6.8 nM, 17 nM, and 49nM, respectively .
|
-
- HY-14266A
-
|
|
Apoptosis
Reverse Transcriptase
Autophagy
HIV
|
Infection
|
|
Dapivirine hydrochloride is a non-nucleoside reverse transcriptase inhibitor with antitumor activity. Dapivirine hydrochloride attenuates the proliferation of glioblastoma cells and induces apoptosis. Dapivirine hydrochloride modulates autophagy and activates Akt, Bad, and SAPK/JNK signaling pathways. Dapivirine hydrochloride has shown inhibitory effects on glioma cell growth both in vitro and in vivo. Dapivirine hydrochloride is also a promising drug candidate for topical microbial agents for the prevention of sexual transmission of HIV-1 .
|
-
- HY-B0252S2
-
|
HCTZ-13C6
|
TGF-beta/Smad
Potassium Channel
|
Metabolic Disease
|
|
Hydrochlorothiazide- 13C6 is the 13C labeled Hydrochlorothiazide[1]. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[2][3][4].
|
-
- HY-B0185S1
-
|
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Lidocaine-d10 is the deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia[2].
|
-
- HY-N0270
-
|
Ononoside; Formononetin 7-O-β-D-glucopyranoside
|
ERK
JNK
p38 MAPK
PI3K
Akt
mTOR
Apoptosis
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Ononin is an orally active isoflavone. Ononin inhibits the ERK/JNK/p38 and PI3K/Akt/mTOR pathways. Ononin regulates Apoptosis. Ononin has anti-tumor effects on laryngeal cancer and lung cancer. Ononin has neuroprotective effects. Ononin alleviates endoplasmic reticulum stress and diabetic nephropathy .
|
-
- HY-N0408
-
-
- HY-14664B
-
|
(3R,5S)-XU 62-320 free acid
|
HMG-CoA Reductase (HMGCR)
Autophagy
|
Cardiovascular Disease
Cancer
|
|
(3R,5S)-Fluvastatin is the 3R,5S-isomer Fluvastatin. Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
|
-
- HY-115625
-
|
|
Progesterone Receptor
Apoptosis
|
Cancer
|
|
AG-205 is a progesterone receptor membrane component-1 (PGRMC1) inhibitor with anti-mitotic, anti-migratory and anti-invasive activities. AG-205 increases expression of genes coding enzymes of the cholesterol biosynthetic pathway or of steroidogenesis. AG-205 promotes Apoptosis modified regulation of the cell cycle and reduces cell migration and invasion capacities in ovary and breast cancer cells .
|
-
- HY-N0265
-
|
|
Caspase
Apoptosis
|
Cardiovascular Disease
|
|
Asperosaponin VI, A saponin component from Dipsacus asper, induces osteoblast differentiation through BMP‐2/p38 and ERK1/2 pathway . Asperosaponin Ⅵ inhibits apoptosis in hypoxia-induced cardiomyocyte by increasing the Bcl-2/Bax ratio and decreasing active caspase-3 expression, as well as enhancing of p-Akt and p-CREB .
|
-
- HY-151966
-
|
|
PROTACs
IAP
Caspase
|
Cancer
|
|
TD1092 is a pan-IAP degrader, degrades cIAP1, cIAP2, and XIAP. TD1092 activates Caspase 3/7, and promotes cancer cells apoptosis via IAP degradation. TD1092 inhibits TNFα mediated NF-κB pathway and reduces the phosphorylation of IKK, IkBα, p65, and p38. TD1092 can act as PROTAC, and is used for cancer research .
|
-
- HY-N2535
-
|
4-Hydroxy-3-methoxycinnamaldehyde
|
Keap1-Nrf2
Apoptosis
|
Inflammation/Immunology
|
|
Coniferaldehyde (4-Hydroxy-3-methoxycinnamaldehyde) is an effective inducer of heme oxygenase-1 (HO-1). Coniferaldehyde inhibits LPS-induced apoptosis through the PKCα/β II/Nrf-2/HO-1 dependent pathway in RAW264.7 macrophage cells. Coniferaldehyde has antioxidant and anti-inflammatory activities .
|
-
- HY-158016
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
Antiproliferative agent-49 (Compound 5a) is a EGFR-TK inhibitor with an IC50 of 0.09 μM. Antiproliferative agent-49 is a anti-proliferative agent. Antiproliferative agent-49 displays good activities against HER3 and HER4 with IC50 values 0.18 and 0.37 µM. Antiproliferative agent-49 induces mitochondrial apoptotic pathway and increased accumulation of ROS .
|
-
- HY-135564A
-
|
|
Phosphatase
Phospholipase
HIV Protease
ERK
Autophagy
|
Infection
Cancer
|
|
RK-682 is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 inhibits the dephosphorylation of CD45 (IC50 is 54 μM) and VHR (IC50 is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC50s of 78.2, 43.2 and 145 nM, respectively, arrests the cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24 .
|
-
- HY-172256
-
|
|
PI4K
|
Cancer
|
|
PI4KIII beta inhibitor 5 is a PI4KIIIβ inhibitor with an IC50 of 19 nM. PI4KIII beta inhibitor 5 can induce cancer cell apoptosis (Apoptosis), cell cycle arrest at the G2/M phase, and autophagy (Autophagy) by inhibiting the PI3K/AKT pathway. PI4KIII beta inhibitor 5 has also demonstrated significant antitumor activity in the H446 xenograft model of small cell lung cancer. PI4KIII beta inhibitor 5 can be used for research in the field of cancer therapy .
|
-
- HY-168858
-
|
|
Trk Receptor
ERK
PI3K
Apoptosis
|
Cancer
|
|
TRK-IN-30 (Compound C11) is the inhibitor for tropomyosin receptor kinase (TRK) that inhibits TRKA, TRKB and TRKC and drug resistant mutant TRKA G595R with an IC50 of 1.8, 0.98, 3.8, and 54 nM, respectively. TRK-IN-30 inhibits the activation of the downstream PI3K/AKT and MEK/ERK signaling pathways. TRK-IN-30 inhibits the colony formation and cell migration of Km-12, arrests the cell cycle at G0/G1 phase, and induces apoptosis in Km-12 .
|
-
- HY-168207
-
|
|
Toll-like Receptor (TLR)
NF-κB
|
Inflammation/Immunology
|
|
TH023 is an inhibitor for the TLR4 signaling pathway, that targets especially the formation of TLR4 homodimer. TH023 inhibits secreted embryonic alkaline phosphatase in cell HEK-Blue hTLR4 with an IC50 of 0.354 μM, and inhibits the NO expression in RAW264.7 with an IC50 of 1.61μM. TH023 also inhibits the activation of NF-κB, reduces the nuclear translocation of NF-κB p65. TH023 exhibits anti-inflammatory efficacy in LPS (HY-D1056)-induced mouse acute sepsis model, and ameliorates the mouse lung injury .
|
-
- HY-17471AR
-
|
1,1-Dimethylbiguanide (hydrochloride) (Standard)
|
AMPK
Autophagy
Mitophagy
Apoptosis
mTOR
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Metformin hydrochloride (Standard) is the analytical standard of Metformin (hydrochloride). This product is intended for research and analytical applications. Metformin (1,1-Dimethylbiguanide) hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo .
|
-
- HY-N0373
-
|
|
Amyloid-β
Apoptosis
NOD-like Receptor (NLR)
|
Neurological Disease
|
|
Licochalcone B is an extract from the root of Glycyrrhiza uralensis. Licochalcone B inhibits amyloid β (42) self-aggregation (IC50=2.16 μM) and disaggregate pre-formed Aβ42 fibrils, reduce metal-induced Aβ42 aggregation through chelating metal ionsLicochalcone B inhibits phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone B inhibits growth and induces apoptosis of NSCLC cells. Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7‐NLRP3 interaction .
|
-
- HY-113071AR
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
|
|
Mevalonic acid (lithium salt) (Standard) is the analytical standard of Mevalonic acid (lithium salt). This product is intended for research and analytical applications. Mevalonic acid (MVA) lithium salt is a precursor substance of the mevalonate pathway, which is essential for cell growth and proliferation. Mevalonic acid lithium salt is effective in inhibiting Simvastatin (HY-17502)-induced decrease in C2C12 cell viability in vitro. Mevalonic acid lithium salt can be used in studies of myopathy and heart failure .
|
-
- HY-P2088
-
|
Des-N-tetramethyltriostin A
|
Antibiotic
|
Cancer
|
|
TANDEM (Des-N-tetramethyltriostin A) is a synthetic antibiotic drug that has the activity of inhibiting the growth of tumor cells. TANDEM can be used in combination with chemotherapy to enhance the inhibitory effect. TANDEM has shown significant inhibitory effects on a variety of cancer cell lines in in vitro experiments. The structure of TANDEM allows it to effectively target tumor cells during the inhibition process. TANDEM's mechanism of action involves interfering with cell proliferation and survival pathways .
|
-
- HY-W105318
-
|
PBP
|
TGF-beta/Smad
Apoptosis
|
Cancer
|
|
Pentabromophenol (PBP) is a brominated flame retardant (BFR) widely used in various consumer products to reduce the flammability of materials used in different utility items. Pentabromophenol can accelerate the degradation of transforming growth factor-β (TGF-β) receptors by promoting clathrin-mediated endocytosis, thereby inhibiting the TGF-β signaling pathway. Additionally, Pentabromophenol can also induce apoptosis in peripheral blood mononuclear cells (PBMCs) .
|
-
- HY-160851
-
|
AK3287; AKEX0011
|
ASK1
p38 MAPK
|
Inflammation/Immunology
|
|
GDC-3280 (AK3287; AKEX0011) is an orally active compound based on Pirfenidone (HY-B0673)'s phenyl pyridone scaffold. GDC-3280 alleviates the inflammatory and fibrotic reaction of silicosis by inhibiting the ASK1-p38 MAPK pathway and regulating macrophage polarization. GDC-3280 exhibits anti-inflammatory and anti-fibrotic effects .
|
-
- HY-116619
-
|
(E/Z)-NVP-LAQ824; (E/Z)-LAQ824
|
HDAC
Apoptosis
|
Others
|
|
(E/Z)-Dacinostat ((E/Z)-NVP-LAQ824) is a histone deacetylase inhibitor that has the ability to induce apoptosis and enhance the activity of fludarabine in killing leukemia cells. (E/Z)-Dacinostat can trigger the production of reactive oxygen species (ROS) and DNA damage, enhance the killing effect of fludarabine on leukemia cells, and induce apoptosis. Its mechanism is related to the regulation of DNA repair processes and intracellular signaling pathways.
|
-
- HY-N0567R
-
|
|
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Hydroxysafflor yellow A (Standard) is the analytical standard of Hydroxysafflor yellow A. This product is intended for research and analytical applications. Hydroxysafflor yellow A (Safflomin A) is a natural product of flavonoids isolated from safflower. Hydroxysafflor yellow A can inhibit cell proliferation and promote apoptosis through the autophagy pathway. Hydroxysafflor yellow A has anti-inflammatory, antioxidant and antitumor effects. Hydroxysafflor yellow A can be used in the study of cardiovascular disease .
|
-
- HY-124151
-
|
2'-AMP; Adenosine 2'-phosphate; AMP 2'-phosphate
|
Adenosine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation .
|
-
- HY-B0185S
-
|
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
N-Oxide Lidocaine-d10 is the deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia[2].
|
-
- HY-158210
-
|
|
Wnt
β-catenin
MDM-2/p53
|
Cancer
|
|
Wnt/β-catenin-IN-3 (compound 17) is a Wnt/β-catenin inhibitor with low micromolarGI50s against various cancer cells. Wnt/β-catenin-IN-3triggers G2/M cell cycle arrest though activation of p53-p21 pathway as well as intrinsic and extrinsic apoptotic death of colon cancer cells .
|
-
- HY-N0202
-
|
Asterolide
|
ERK
Apoptosis
p38 MAPK
Akt
Src
STAT
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Atractylenolide II (Asterolide) is a sesquiterpenoid compound. Atractylenolide II can induce G1 phase cell cycle arrest and apoptosis in B16 melanoma cells. Atractylenolide II is an orally effective anticancer agent that can exert anti-melanoma effects by inhibiting the STAT3 signaling pathway. In addition, Atractylenolide II has been shown to ameliorate myocardial fibrosis, oxidative stress, and neuroprotective activity .
|
-
- HY-162004
-
|
|
NF-κB
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
NF-κB-IN-14 (compound 5e) significantly inhibits nitric oxide production in LPS-induced macrophages (IC50: 6.4 μM). NF-κB-IN-14 disrupts the TLR4-MyD88 protein interaction, leading to the suppression of the NF-κB signaling pathway suppression. NF-κB-IN-14 reduces ear edema and inflammation in an atopic dermatitis mouse model .
|
-
- HY-B0965A
-
|
|
Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Neurological Disease
Cancer
|
|
Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
- HY-103018
-
|
ASN-002
|
JAK
Syk
|
Inflammation/Immunology
Cancer
|
|
Gusacitinib (ASN-002) is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma .
|
-
- HY-13735H
-
|
Acriquine acetate
|
Parasite
Sodium Channel
DNA Stain
Apoptosis
|
Cancer
|
|
Quinacrine (Acriquine) acetate is a small molecule modulator of the cGAS-STING-TBK1 signaling pathway, possessing immune stimulatory activity. Quinacrine acetate has been explored for its potential therapeutic applications in enhancing anti-tumor immunity. Quinacrine acetate can improve the effectiveness of cancer immunotherapies by addressing the poor immunogenicity of various tumors. Quinacrine acetate also presents a promising strategy for overcoming the limitations associated with immune checkpoint inhibitors in cancer treatment.
|
-
- HY-P1823
-
|
|
Akt
mTOR
Caspase
|
Infection
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
C-Reactive Protein (CRP) is an anti-pneumococcal plasma protein that can serve as an inflammatory marker. C-Reactive protein can protect mice from pneumococcal infection by activating complement. C-Reactive protein can inhibit the activation of caspase-3/9 through the CD64/AKT/mTOR pathway, thereby promoting chemotherapy resistance in mice with tongue squamous cell carcinoma .
|
-
- HY-N6064
-
|
|
Apoptosis
IAP
|
Cancer
|
|
Polygalacin D (PGD) is a bioactive compound isolated from Platycodon grandiflorum with anticancer and anti-proliferative properties.
PGD suppresses the expression of the IAP family of proteins including survivin, cIAP-1 and cIAP-2 and blocks the PI3K/Akt pathway by inhibiting the phosphorylation of GSK3β, Akt and the expression of PI3K. Polygalacin D induces apoptosis
|
-
- HY-B0185R
-
|
Lignocaine (Standard)
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Lidocaine (Standard) is the analytical standard of Lidocaine. This product is intended for research and analytical applications. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence . Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia .
|
-
- HY-133033
-
|
|
Mitochondrial Metabolism
|
Metabolic Disease
|
|
COQ7-IN-1, a highly potent inhibitor of human coenzyme Q (COQ7), interferes with ubiquinone (UQ) synthesis. COQ7-IN-1 does not disturb physiological cell growth of human normal culture cells. COQ7-IN-1 can be used for the research of the balance between UQ supplementation pathways: de novo UQ synthesis and extracellular UQ uptake .
|
-
- HY-146006
-
|
|
Microtubule/Tubulin
MMP
|
Cancer
|
|
Tubulin/MMP-IN-1 (compound 15g) is a potent inhibitor of tubulin and MMP. Tubulin/MMP-IN-1 has the potential for the research of cancer diseases. Tubulin/MMP-IN-1 suppresses tubulin polymerization, induces cell cycle arrest at the G2/M phase, leads to reactive oxidative stress (ROS) generation of HepG2 cells, and results in apoptosis by the mitochondrial-dependent apoptotic pathway .
|
-
- HY-N0743
-
|
|
α-synuclein
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Senkyunolide A is a phthalide, anti-tumor cell proliferation agent with anticancer activity. Senkyunolide A protects neurons from corticosterone (HY-B1618)-induced apoptosis by decreasing protein phosphatase PP2A and α-synuclein phosphorylation and protein level. Senkyunolide A also inhibits osteoarthritis through the NLRP3 signaling pathway and suppresses the expression of CD137, a diagnostic biomarker for atherosclerosis .
|
-
- HY-Y0669R
-
-
- HY-14621R
-
|
|
NF-κB
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Zingerone (Standard) is the analytical standard of Zingerone. This product is intended for research and analytical applications. Zingerone (Vanillylacetone) is a nontoxic methoxyphenol isolated from Zingiber officinale, with potent anti-inflammatory, antidiabetic, antilipolytic, antidiarrhoeic, antispasmodic and anti-tumor properties . Zingerone alleviates oxidative stress and inflammation, down-regulates NF-κB mediated signaling pathways . Zingerone acts as an anti-mitotic agent, and inhibits the growth of neuroblastoma cells .
|
-
- HY-108959
-
|
|
ERK
PI3K
mTOR
|
Cancer
|
|
D-87503 is a potent inhibitor of PI3k/Akt/mTOR, with the IC50s of 62 nM and 0.76 μM, respectively for PI3k and Erk2. D-87503 effectively suppressed the target downstream substrates Akt and Rsk1 kinase of the PI3k/Akt/mTOR signaling pathway .
|
-
- HY-147941A
-
|
|
PROTACs
EGFR
|
Cancer
|
|
MS9427 TFA is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 TFA selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 TFA potently inhibits the proliferation of NSCLC cells. MS9427 TFA can be used for researching anticancer .
|
-
- HY-B0252S1
-
|
HCTZ-13C,d2
|
Isotope-Labeled Compounds
TGF-beta/Smad
Potassium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
Hydrochlorothiazid- 13C,d2 is the 13C- and deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[1][2][3].
|
-
- HY-B1971R
-
-
- HY-N12887
-
|
|
Mitochondrial Metabolism
|
Others
Cancer
|
|
Mycothiazole is an inhibitor for mitochondrial electron transport chain (ETC) complex I. Mycothiazole exhibits cytotoxicity in cancer cells Huh7 (IC50 is 55.8 μM), U87 and MCF7. Mycothiazole induces apoptosis in Huh7. Mycothiazole utilizes the unfolded protein response (UPR) and heat shock response (HSR) pathway involved transcription factors ATFS-1 and HSF1, to extend the lifespan of C. elegans .
|
-
- HY-103018A
-
|
ASN-002 hydrochloride
|
JAK
Syk
|
Inflammation/Immunology
Cancer
|
|
Gusacitinib (ASN-002) hydrochloride is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib hydrochloride rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib hydrochloride can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma .
|
-
- HY-N0284R
-
|
|
PI3K
Akt
|
Inflammation/Immunology
Cancer
|
|
Esculetin (Standard) is the analytical standard of Esculetin. This product is intended for research and analytical applications. Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities .
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-
- HY-P1556A
-
|
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PKG
|
Metabolic Disease
|
|
Vasonatrin Peptide (VNP) TFA is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide TFA possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide TFA protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway .
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-
- HY-N1381R
-
|
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Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Periplocin (Standard) is the analytical standard of Periplocin. This product is intended for research and analytical applications. Periplocin is a cardiotonic steroid isolated from root-bark Periploca sepium Bunge. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase .
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-
- HY-B0185BR
-
|
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Lidocaine (hydrochloride hydrate) (Standard) is the analytical standard of Lidocaine (hydrochloride hydrate). This product is intended for research and analytical applications. Lidocaine (Lignocaine) hydrochloride hydrate inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride hydrate decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride hydrate is an amide derivative and has potential for the research of ventricular arrhythmia .
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-
- HY-122464
-
|
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Herbicide
|
Others
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|
(±)-Jasmonic acid is an endogenous growth regulator closely related to plant resistance to abiotic stresses, used to activate defense responses to wounding, herbivory, and pathogen attacks. (±)-Jasmonic acid does not play an independent regulatory role, but works in a complex signaling network with other plant hormone signaling pathways. In addition, (±)-Jasmonic acid can also reduce chlorophyll levels in green and etiolated barley leaf segments and inhibit the elongation of rice seedlings .
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-
- HY-B1901S
-
|
|
Isotope-Labeled Compounds
|
Neurological Disease
|
|
Eperisone-d10 (hydrochloride) is the deuterium labeled Eperisone hydrochloride. Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is an antispastic agent used for treatment of diseases characterized by muscle stiffness and pain. It works by relaxing both skeletal muscles and vascularsmooth muscles, thus demonstrating avariety of effects such as reduction ofmyotonia, improvement of circulationand suppression of the pain reflex. Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is a centrally acting muscle relaxant inhibiting the pain reflex pathway, having a vasodilator effect[1][2 [3].
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-
- HY-162280
-
|
|
PROTACs
RANKL/RANK
Nuclear Factor of activated T Cells (NFAT)
Btk
|
Cancer
|
|
PROTAC BTK Degrader-9 (compound 23) is a PROTAC degrader that effectively targets BTK. PROTAC BTK Degrader-9 downregulates the BTK-PLCγ2-Ca 2+-NFATc1 signaling pathway activated by RANKL. Thus, PROTAC BTK Degrader-9 was able to inhibit osteoclastogenesis and attenuate alveolar bone resorption in a mouse periodontitis model .
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-
- HY-151483
-
|
|
Histone Demethylase
|
Cardiovascular Disease
|
|
TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC50=44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. TK-129 reduces ang II-induced activation of cardiac fibroblasts in vitro and reduces isoprenaline-induced myocardial remodelling and fibrosis in vivo. TK-129 can be used in studies of cardiovascular disease .
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-
- HY-16558R
-
|
|
EGFR
Autophagy
Apoptosis
Phosphodiesterase (PDE)
|
Cancer
|
|
Butein (Standard) is the analytical standard of Butein. This product is intended for research and analytical applications. Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4 . Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60c-src in HepG2 cells . Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a . Butein is a SIRT1 activator (STAC).
|
-
- HY-168491
-
|
|
Phosphodiesterase (PDE)
STING
PD-1/PD-L1
|
Cancer
|
|
Enpp-1-IN-25 (Compound 30) is an ENPP1 inhibitor with an IC50 of 8.05 nM and low oral bioavailability. Enpp-1-IN-25 can effectively activate the intracellular STING pathway by inhibiting cGAMP degradation. Enpp-1-IN-25 can enhance immune cell infiltration in the tumor microenvironment and type I interferon responses, and potentiate the antitumor efficacy of the anti-PD-L1 antibody. Enpp-1-IN-25 can be used in the research of cancer immunotherapy .
|
-
- HY-14536
-
|
Basic Blue 9; CI-52015; Methylthioninium chloride
|
Guanylate Cyclase
Monoamine Oxidase
NO Synthase
Microtubule/Tubulin
|
Infection
Neurological Disease
Cancer
|
|
Methylene blue (Basic Blue 9) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue is a Tau aggregation inhibitor. Methylene blue reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation .
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-
- HY-161849
-
|
|
Histone Demethylase
|
Metabolic Disease
|
|
LSD1-IN-31 (compound 11e) can directly bind to LSD1/CoREST complex to reduce LSD1 demethylation enzymatic activity. LSD1-IN-31 inhibits LSD1 demethylation activity and influences its downstream IκB/NF-κB signaling pathway. LSD1-IN-31 inhibits osteoclastic bone loss in vitro and in vivo. LSD1-IN-31 can be used for osteoporosis research .
|
-
- HY-141431
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Inflammation/Immunology
Cancer
|
|
Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent .
|
-
- HY-164480
-
|
|
IKK
NF-κB
|
Inflammation/Immunology
Cancer
|
|
GTCpFE inhibits IKKα/β in the NF-κB pathway with anti-inflammatory activities and blocks p65 nuclear entry, which consists of Dimethyl fumarate (DMF) (HY-17363) linked to Aspirin (ASA) (HY-14654). GTCpFE exhibits selective anti-cancer stem-like cell (CSC) activity by reducing mammosphere growth and the CD44 + CD24 - immunophenotype. GTCpFE inhibits breast cancer stem cells, an important NFκB- and PGE2-dependent phenotype in aggressive cancers .
|
-
- HY-161323
-
|
|
FLT3
Bcr-Abl
Apoptosis
|
Cancer
|
|
FLT3-ITD/D835Y-IN-1 (Compound 1) is a FLT3-ITD and BCR-ABL inhibitor. FLT3-ITD/D835Y-IN-1 mediates proapoptosis by inhibiting the FLT3 and BCR-ABL pathways, as well as other possible targets. FLT3-ITD/D835Y-IN-1 can be used in the study of acute myeloid leukemia (AML) .
|
-
- HY-D0958
-
|
Basic Blue 9 hydrate; CI-52015 hydrate; Methylthioninium chloride hydrate
|
Guanylate Cyclase
Monoamine Oxidase
NO Synthase
Microtubule/Tubulin
|
Infection
Inflammation/Immunology
Cancer
|
|
Methylene blue (Basic Blue 9) hydrate is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue hydrate through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue hydrate is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue hydrate is a Tau aggregation inhibitor. Methylene blue hydrate reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation .
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-
- HY-168024
-
|
|
RIP kinase
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NOD1/2-IN-1 (Compound 18) is a potent RIPK2 inhibitor with an IC50 value of 1.4 nM, as determined by the ADP-Glo assay. NOD1/2-IN-1 blocks the production of pro-inflammatory cytokines by inhibiting the NOD1/NOD2 pathways, with IC50 values of 18 nM and 170 nM for NOD1 and NOD2, respectively, thereby reducing inflammatory responses. NOD1/2-IN-1 can be used in studies related to colitis .
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-
- HY-164102
-
|
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
|
TNF-α-IN-18 (Compound 61) is an inhibitor for TNF-α (IC50 of 1.8 μM), that inhibits TNF signaling pathway through block of NF-kB migration from cytoplasm to nucleus. TNF-α-IN-18 exhibits slight cytotoxicity to mouse fibroblast LM cell, with a CC50 >50 μM. TNF-α-IN-18 ameliorates the TNF- or Lipopolysaccharide (HY-D1056)-induced sepsis in mouse models. TNF-α-IN-18 protects mice from rheumatoid arthritis .
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-
- HY-108464A
-
|
|
Sodium Channel
TRP Channel
|
Metabolic Disease
Inflammation/Immunology
|
|
Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM . Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca 2+ transport with an IC50 of 140 nM in a Ca 2+ uptake assay . Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway . Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease .
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-
- HY-N2510R
-
|
|
5-HT Receptor
EGFR
ERK
Apoptosis
Bacterial
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Myristicin (Standard) is the analytical standard of Myristicin. This product is intended for research and analytical applications. Myristicine is an orally bioavailable serotonin receptor antagonist and weak monoamine oxidase (MAO) inhibitor. Myristicine also exerts anti-cancer effects on gastric cancer cells by inhibiting the EGFR/ERK signaling pathway. Myristicine is the main component of nutmeg essential oil and has anti-cancer, anti-proliferative, antibacterial, anti-inflammatory and apoptosis-inducing effects. Myristicine abuse can produce hallucinogenic effects, organ damage, etc .
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-
- HY-19671
-
|
SR-45023A; SR 9223i; SK&F-99085
|
Apoptosis
|
Cancer
|
|
Apomine (SR-45023A) is an antineoplastic agent that inhibits the mevalonate/isoprenoid pathway in cholesterol synthesis.
Apomine can accelerate the degradation of 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR). Apomine can also inhibit the growth of various types of cancer cells, including lung cancer, colon cancer, breast cancer, and skin cancer. In addition, Apomine is able to induce apoptosis in tumor cell lines derived from leukemia, colon cancer, liver cancer, ovarian cancer, and breast cancer .
|
-
- HY-169408
-
|
|
Cytochrome P450
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-137 (Compound 4c) is an inhibitor for aromatase and EGFR with IC50s of 1.67 μg/mL and 0.08 μg/mL. EGFR-IN-137 inhibits the proliferation of cancer cell MCF-7 and MDA-MB-231 with IC50s of 1.62 µM and 4.14 µM. EGFR-IN-137 arrests the cell cycle at G0/G1 phase in MDA-MB-231, and induces apoptosis through caspase-dependent pathway .
|
-
- HY-172409
-
|
|
Cannabinoid Receptor
p38 MAPK
NF-κB
|
Inflammation/Immunology
|
|
CB1R antagonist 2 (Compound 11g) is the antagonist for cannabinoid receptor 1 (CB1R), that inhibits MAPK/NF-κB signaling pathway and exhibits anti-inflammatory activity. CB1R antagonist 2 inhibits LPS (HY-D1056)-induced IL-6, IL-1β and TNF-α expressions in RAW264.7. CB1R antagonist 2 ameliorates OVA-induced allergic rhinitis in mouse models .
|
-
- HY-P9930
-
|
AMG 145
|
NF-κB
Ser/Thr Protease
Toll-like Receptor (TLR)
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Evolocumab (AMG 145) is a human monoclonal antibody that inhibits PCSK9. Evolocumab is used in the study of hypercholesterolemia and atherosclerotic cardiovascular disease. Evolocumab binds to circulating PCSK9 protein and inhibits its binding to LDLR. Evolocumab has antioxidant and cytoprotective activities against H2O2-induced oxidative damage to endothelial cells. Evolocumab may also negatively regulate activation of the TLR-4/NF-κB signaling pathway to prevent inflammation .
|
-
- HY-170867
-
|
|
Keap1-Nrf2
Heme Oxygenase (HO)
Reactive Oxygen Species
|
Cardiovascular Disease
|
|
Nrf2/HO-1 activator 3 (Compound C3a) is the activator for Nrf2 signaling pathway that promotes the Nrf2 translocation into nuclei and upregulates the expression of heme oxygenase-1 HO-1. Nrf2/HO-1 activator 3 inhibits the overespression of ROS and MDA in H2O2- or glucose-stimulated H9c2 cardiomyocytes, inhibits the cell viability and colony formation, thereby exhibiting antioxidant efficacy .
|
-
- HY-151443
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo .
|
-
- HY-117287
-
|
BMS-986165
|
JAK
Interleukin Related
IFNAR
|
Inflammation/Immunology
|
|
Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways. Deucravacitinib, the FDA's world first de novo deuterium, is available for study in moderate to severe plaque psoriasis .
|
-
- HY-168589
-
|
|
Apoptosis
Cytochrome P450
Caspase
Reactive Oxygen Species
|
Cancer
|
|
Apoptosis inducer 30 (Compound 15a) is an anticancer agent. Apoptosis inducer 30 induces MCF-7 cells apoptosis through mitochondrial pathway. Apoptosis inducer 30 induces intracellular reactive oxygen species levels and decreases mitochondrial membrane potential, and blocks the cell cycle in the G0/G1 phase. Apoptosis inducer 30 inhibits cell growth, with an IC50 value of 0.32 μM against MCF-7 cells, and inhibits tumor growth in a mouse model of breast cancer .
|
-
- HY-172171
-
|
|
GSK-3
β-catenin
|
Neurological Disease
|
|
GSK3β-IN-2 (Compound S01) is the inhibitor for GSK3β with an IC50 of 0.35 nM. GSK3β-IN-2 activates Wnt/β-catenin signaling pathway, promotes neurogenesis and neurite growth. GSK3β-IN-2 inhibits Aβ-induced tau hyperphosphorylation at Ser396, reduces the formation of neurofibrillary tangles. GSK3β-IN-2 ameliorates Alzheimer's Disease in zebrafish model .
|
-
- HY-162729
-
|
|
Histone Demethylase
Monoamine Oxidase
TGF-beta/Smad
|
Cardiovascular Disease
|
|
LSD1-IN-34 (Compound 7d) is the orally active inhibitor for Lysine-specific demethylase (LSD) and monoamine oxidase (MAO), with IC50 of 4.51 and 18.46 nM, for LSD1 and MAO A. LSD1-IN-34 inhibits the Ang II-induced neonatal rat myocardial fibroblasts (NRCFs) activation, without significant toxicity (20 μM). LSD1-IN-34 inhibits TGFβ/Smad signaling pathway, and ameliorates heart failure in mice. LSD1-IN-34 exhibits good pharmacokinetic characteristics in rats .
|
-
- HY-170839
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
TRPV1-IN-3 (compound 14) is a TRPV1 inhibitor that can be used for the research of idiopathic pulmonary fibrosis. TRPV1-IN-3 affects the expression of fibrosis markers collagen I and 伪-SMA by inhibiting the TGF-β/Smads and MAPK pathways, thereby exerting antifibrotic activity in vitro (IC50=0.51 μM). TRPV1-IN-3 significantly inhibits collagen deposition in lung tissue, improves the alveolar structure, and also increases the survival rate of mice with pulmonary fibrosis induced by Bleomycin (HY-108345) .
|
-
- HY-120793
-
|
TRB-N0224
|
Ras
Apoptosis
MMP
|
Inflammation/Immunology
Cancer
|
|
CMC2.24 (TRB-N0224), an orally active tricarbonylmethane agent, is effective against pancreatic tumor in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs with IC50s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis .
|
-
- HY-155731
-
|
|
Influenza Virus
|
Infection
|
|
Antiviral agent 35 (compound 4d) is an orally active and potent influenza virus inhibitor, acting function in the early stage of virus replication. Antiviral agent 35 inhibits ROS accumulation, autophagy and apoptosis induced by influenza virus, and also inhibits inflammatory response mediated by RIG-1 pathway in mouse model with pulmonary infection. Antiviral agent 35 shows little cytotoxicity with CC50 >800 μM in MDCK cells, and anti-H1N1 (A/Weiss/43) activity with EC50 of 2.28 μM .
|
-
- HY-161858
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
EpskA21 is an inhibitor for PI3K/AKT signaling pathway, and inhibits the proliferation of cancer cells MCF-7, A549, MIA-PaCa-2, Panc-1 and HepG2, with IC50 of 1.3-7.24 μM. EpskA21 inhibits the cell migration, arrests the cell cycle at G2/M (MCF-7) and S (MIA-PaCa-2) phase, and induces apoptosis in MCF-7 and MIA-PaCa-2. EpskA21 causes the mitochondrial dysfunction .
|
-
- HY-N0272R
-
|
|
Others
|
Inflammation/Immunology
|
|
Eleutheroside E (Standard) is the analytical standard of Eleutheroside E. This product is intended for research and analytical applications. Eleutheroside E is an important component of Eleutheroside and has antioxidant, anti-fatigue, anti-inflammatory, antibacterial, immunomodulatory and cardioprotective effects. Eleutheroside E may inhibit the MAPK signaling pathway, thereby inhibiting H/R-induced NF-κB activation and oxidative stress, reducing metabolic reprogramming, and protecting myocardium from ischemia-reperfusion (I/R) injury. Eleutheroside E also counteracts the effects of high altitude hypobaric hypoxia (HAHI) by inhibiting inflammation and pyroptosis .
|
-
- HY-W753806
-
|
UK 33274 hydrochloride
|
Akt
|
Cardiovascular Disease
|
|
Doxazosin hydrochloride (UK 33274 hydrochloride) is a compound used to inhibit hypertension and prostate hyperplasia, with activity that inhibits postsynaptic α1-adrenoceptors on vascular smooth muscle. Doxazosin hydrochloride can cause vasodilation, thereby reducing peripheral vascular resistance. Doxazosin hydrochloride was found to inhibit the proliferation and migration of hepatic stellate cells in a mouse liver fibrosis model. Doxazosin hydrochloride regulates fibrosis, autophagy, and apoptosis of hepatic stellate cells by activating the PI3K/Akt/mTOR signaling pathway. Doxazosin hydrochloride also blocks autophagic flux and induces apoptosis of hepatic stellate cells .
|
-
- HY-163527
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC50=0.20±0.02 nM) and FGFR4(IC50=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity .
|
-
- HY-164685
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
T-0156 free base is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 free base specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC50=0.23 nM). T-0156 free base inhibits PDE6 (IC50=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC50>10 μM). T-0156 free base enhances the nitric oxide (NO)/cGMP pathway .
|
-
- HY-B0678R
-
|
AHR438 (Standard); NSC170959 (Standard)
|
NF-κB
PGC-1α
|
Neurological Disease
Inflammation/Immunology
|
|
Metaxalone (Standard) is the analytical standard of Metaxalone. This product is intended for research and analytical applications. Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia .
|
-
- HY-144450
-
|
|
PI3K
Akt
|
Cancer
|
|
PI3K-IN-29 is a potent PI3K inhibitor. PI3K-IN-29 displays good inhibition potencies against U87MG, HeLa and HL60 cells with IC50 values of 0.264, 2.04 and 1.14 µM, respectively. PI3K-IN-29 inhibits PI3K/Akt pathway by inhibiting phosphorylation of Akt that is catalyzed by PI3K .
|
-
- HY-147614
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-7 (Compound 19i) is a potent and dual inhibitor of PI3K/mTOR. PI3K/mTOR Inhibitor-7 shows 4.7-fold higher potency than the positive control gedatolisib (0.3 vs. 1.4 μM, IC50 values). PI3K/mTOR Inhibitor-7 significantly suppresses the PI3K/Akt/mTOR signaling pathway at 10 μM. PI3K/mTOR Inhibitor-7 has the potential for the research of cancer diseases .
|
-
- HY-N0634R
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Cimifugin (Standard) is the analytical standard of Cimifugin. This product is intended for research and analytical applications. Cimifugin (Cimitin) is a bioactive component of Cimicifuga racemosa, a Chinese herb. Cimifugin suppresses allergic inflammation by reducing epithelial derived initiative key factors via regulating tight junctions . Cimifugin reduces the migration and chemotaxis of RAW264.7 cells and inhibits the release of inflammatory factors and activation of MAPKs and NF-κB signaling pathways induced by LPS .
|
-
- HY-100490B
-
|
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- HY-N0076R
-
|
|
Apoptosis
Autophagy
Endogenous Metabolite
|
Neurological Disease
|
|
Bilobalide (Standard) is the analytical standard of Bilobalide. This product is intended for research and analytical applications. Bilobalide, a sesquiterpene trilactone constituent of Ginkgo biloba, inhibits the NMDA-induced efflux of choline with an IC50 value of 2.3 μM. Bilobalide prevents apoptosis through activation of the PI3K/Akt pathway in SH-SY5Y cells. Exerts protective and trophic effects on neurons .
|
-
- HY-158196
-
|
|
PERK
Apoptosis
|
Cancer
|
|
PERK/eIF2α activator 1 (compound V8) is a flavonoid with an anti-tumor activity. PERK/eIF2α activator 1 induces apoptosis and activates the PERK-eIF2α-ATF4 pathway. PERK/eIF2α activator 1 inhibits HepG2 cell proliferation with an IC50 value of 23 μM .
|
-
- HY-155974
-
|
|
MDM-2/p53
|
Cancer
|
|
MeOIstPyrd is an anti-skin cancer agent. MeOIstPyrd inhibits cell proliferation, migration, and spheroid formation by activating the mitochondrial intrinsic apoptotic pathway. MeOIstPyrd induces DNA damage. MeOIstPyrd activates p53, and increases the half-life of p53 and stabilizes p53 by phosphorylating it at ser15. MeOIstPyrd binds to MDM2 in the p53 sub-pocket and blocks p53-MDM2 interaction .
|
-
- HY-N0022R
-
-
- HY-W998345
-
|
|
PROTACs
PDK-1
Akt
|
Cancer
|
SMART1 is a highly specific and CRBN-dependent PROTAC that can effectively degrade Smurf1. SMART1 can block the PDK1-Akt signaling pathway in KRAS mutant colorectal cancer. SMART1 can inhibit tumor growth in KRAS mutant colorectal cancer (CRC) xenograft models.(Blue: CRBN ligand; Black: linker; Pink: Smurf1 ligand (Smurf1-L)) .
|
-
- HY-B0094S3
-
|
Qinghaosu-13C,d4; NSC 369397-13C,d4
|
Ferroptosis
Akt
Parasite
HCV
Isotope-Labeled Compounds
|
Infection
Neurological Disease
Cancer
|
|
Artemisinin- 13C,d4 is 13C and deuterated labeled Artemisinin (HY-B0094). Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
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-
- HY-P10793
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
Cyclic(YCDGFYACYMDV) is a HER2 signaling pathway inhibitor with anti-cancer activity. This compound self-assembles into nanoparticles in aqueous solution and transforms into nanofibers upon specific binding to HER2 on cancer cells. This transformation disrupts HER2 dimerization and subsequent downstream signaling events, leading to cancer cell apoptosis (Apoptosis). The inhibitory effects on HER2 positive breast cancer have been demonstrated to be effective in a murine xenograft model .
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-
- HY-B0965
-
|
|
Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Infection
Neurological Disease
Cancer
|
|
Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
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-
- HY-N8847R
-
|
|
Hippo (MST)
YAP
|
Cancer
|
|
α-Ionone (Standard) is the analytical standard of α-Ionone. This product is intended for research and analytical applications. α-Ionone (alpha-Ionone) is an activator of the olfactory receptor OR10A6. α-Ionone induces apoptosis by activating OR10A6 and increasing the phosphorylation of the LATS-YAP-TAZ signaling axis in the Hippo pathway. α-Ionone can inhibit tumor formation both in vivo and in vitro .
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-
- HY-118912
-
|
|
Orphan Receptor
|
Inflammation/Immunology
Cancer
|
|
BMH-9 (Compound Z54) is a modulator for nuclear receptor subfamily 2, group F, member 6 (NR2F6) (also known as nuclear orphan receptor Ear2) . BMH-9 is an activator for p53 signaling pathway through interaction with DNA. BMH-9 inhibits proliferation of human cancer cells, exhibits antitumor efficacy in NOD-SCID mouse models .
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-
- HY-E70390
-
|
masp-2, c1 esterase, c1-esterase
|
Wnt
|
Cardiovascular Disease
Inflammation/Immunology
|
|
C1s Enzyme is a subunit of the complement C1 complex, which activates the complement as a serine protease. C1s Enzyme cleaves LRP5 and LRP6, and thus activates the Wnt/β-Catenin signaling pathway. C1s Enzyme promotes the macrophage M2 polarization and inhibits M1 polarization. C1s Enzyme enhances efferocytosis, exhibits anti-inflammatory activity .
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-
- HY-112671
-
|
RTA dh404
|
Keap1-Nrf2
NF-κB
|
Cardiovascular Disease
Inflammation/Immunology
|
|
CDDO-dhTFEA (RTA dh404) is a synthetic oleanane triterpenoid compound which potently activates Nrf2 and inhibits the pro-inflammatory transcription factor NF-κB . CDDO-dhTFEA restores hypertension (MAP), increases Nrf2 and expression of its target genes, attenuates activation of NF-κB and transforming growth factor-β pathways, and reduces glomerulosclerosis, interstitial fibrosis and inflammation in the chronic kidney disease (CKD) rats .
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-
- HY-W015590R
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
Polyphyllin I (Standard) is the analytical standard of Polyphyllin I. This product is intended for research and analytical applications. Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis .
|
-
- HY-100490
-
|
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
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-
- HY-B1899S
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
Apoptosis
|
Others
|
|
Taurodeoxycholic acid-d5 is the deuterium labeled Taurodeoxycholic acid (HY-B1899) . Taurodeoxycholic acid, a bile acid, stabilizes the mitochondrial membrane, decreases free radical formation. Taurodeoxycholic acid inhibits apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid exhibits neuroprotective effect in 3-nitropropionic acid induced mouse model or genetic mouse model of Huntington's disease (HD) .
|
-
- HY-N0047R
-
|
|
JNK
mTOR
Akt
PDK-1
Autophagy
Apoptosis
|
Cancer
|
|
Polyphyllin I (Standard) is the analytical standard of Polyphyllin I. This product is intended for research and analytical applications. Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis .
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-
- HY-170813
-
|
|
CDK
|
Infection
|
|
P162-0948 is a selective CDK8 inhibitor with an IC50 value of 50.4 nM. P162-0948 reduces cell migration and protein expression of EMT-related proteins in A549 human alveolar epithelial cell lines. P162-0948 reduces phosphorylation of Smad, which suggests disruption of the TGF-β/Smad signaling pathway. P162-0948 is promising for research of pulmonary fibrosis .
|
-
- HY-N0270R
-
|
|
Others
|
Others
Neurological Disease
Cancer
|
|
Ononin (Standard) is the analytical standard of Ononin. Ononin is an orally active isoflavone. Ononin inhibits the ERK/JNK/p38 and PI3K/Akt/mTOR pathways. Ononin regulates Apoptosis. Ononin has anti-tumor effects on laryngeal cancer and lung cancer. Ononin has neuroprotective effects. Ononin alleviates endoplasmic reticulum stress and diabetic nephropathy .
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-
- HY-B0863
-
|
|
Apoptosis
Autophagy
Necroptosis
|
Neurological Disease
|
|
Glyphosate, a non-selective systemic biocide with broad-spectrum activity, is an herbicidal derivative of the amino acid glycine. Glyphosate inhibits the enzymatic activity of the 5-endopyruvylshikimate 3-phosphate synthase (EPSPS) in the shikimic acid pathway, preventing the synthesis of the aromatic amino acids tyrosine, phenylalanine, and tryptophan. Glyphosate induces oxidative stress, neuroinflammation, and mitochondrial dysfunction, processes that lead to neuronal death by autophagia, necrosis, or apoptosis, as well as the appearance of behavioral and motor disorders .
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-
- HY-N0292R
-
|
|
Cytochrome P450
PPAR
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Oleuropein (Standard) is the analytical standard of Oleuropein. This product is intended for research and analytical applications. Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity . Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase .
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-
- HY-159125
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-47 (MolPort-001-742-690) is a PH-selective PD-1/PD-L1 signaling pathway inhibitor with significant affinity for PD-L1 under acidic conditions and lower toxicity. PD-1/PD-L1-IN-47 can be used in the study of tumors .
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-
- HY-N13248
-
|
|
Glycosidase
|
Metabolic Disease
|
|
Mulberry Leaf Extract is a mulberry leaf extract, and its components include: 1-Deoxynojirimycin. Mulberry Leaf Extract can effectively alleviate the adverse effects of high-fat diet on blood lipids and renal function, regulate lipid metabolism abnormalities, and significantly inhibit the accumulation of glycosylated substances in glomeruli. Mulberry Leaf Extract can regulate the key signaling pathways of diabetic nephropathy, but does not directly affect blood glucose levels. .
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-
- HY-P10869
-
|
|
Natriuretic Peptide Receptor (NPR)
|
Inflammation/Immunology
Cancer
|
|
dCNP binds to NPR-B/C receptor, activates cGMP signaling pathway, and regulates vascular function. dCNP exhibits anti-hypoxia property through downregulation of hypoxia-related genes expressions like HIF1α and HIF2α. dCNP inhibits the induction of tumor stroma and exhibits anti-fibrosis activity. dCNP upregulates CTLs, NK cells, and conventional type 1 dendritic cells in tumors, and activates immune responses .
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-
- HY-167704
-
|
|
Apoptosis
|
Cancer
|
|
NF023 is a compound that inhibits X-BIR1/TAB1 assembly activity. NF023 can affect cell survival signaling pathways by interfering with XIAP-mediated NF-κB activation. NF023 also shows potential as a selective P2X1 adenylate receptor antagonist. This compound has the potential to synergize with existing pro-apoptotic drugs and play an important role in cancer suppression .
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-
- HY-139066
-
|
Trichosanic acid
|
TNF Receptor
GLUT
Proteasome
Tau Protein
PKC
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Punicic acid is a bioactive compound of pomegranate seed oil. Punicic acid is an isomer of conjugated α-linolenic acid and ω-5 polyunsaturated fatty acids. Punicic acid has anti-inflammatory and antioxidant activities and can inhibit the expression of inflammatory mediators such as tumor necrosis factor α (TNF-α). Punicic acid can also reduce the formation of β-amyloid deposits and hyperphosphorylation of tau by increasing the expression of GLUT4 protein and inhibiting the overactivation of calpain, and is used to prevent and treat neurodegenerative diseases. In addition, punicic acid also has breast cancer inhibitor properties that depend on lipid peroxidation and PKC pathways .
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-
- HY-N2132
-
-
- HY-129115
-
|
|
Reactive Oxygen Species
Caspase
|
Others
|
|
S1QEL1.1 is a small molecule inhibitor that specifically inhibits the generation of superoxide and hydrogen peroxide at the IQ site during reverse electron transfer in mitochondrial respiratory chain complex I (Complex I), with an IC50 of 0.07 μM. S1QEL1.1 can significantly reduce the activation of cysteine-aspartic protease (caspase) triggered by endoplasmic reticulum stress. S1QEL1.1 helps to decrease excessive proliferation of stem cells by inhibiting the Reactive Oxygen Species signaling pathway initiated by endoplasmic reticulum stress .
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-
- HY-155998
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
NF-κB-IN-11 (Compound 3i) is a NF-κB inhibitor. NF-κB-IN-11 inhibits TNF-α induced activation of NF-κB pathway, and inhibits nuclear translocation of NF-κB. NF-κB-IN-11 down-regulates the expression levels of phosphor-IKK, IκBα, and NF-κB p65. NF-κB-IN-11 has anti-inflammatory activity, and alleviates dextran sulfate sodium-induced colitis in mice. NF-κB-IN-11 (p.o.) shows a MTD more than 1852 mg/kg in mice acute toxicity assay .
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-
- HY-W251428
-
|
Egg PG
|
Biochemical Assay Reagents
|
Others
|
|
Phosphatidylglycerols (PG) is a selective inhibitor targeting the TLR4 accessory protein CD14/MD-2 complex, inhibiting LPS or virus (such as RSV)-mediated inflammatory signaling pathways through competitive binding. Phosphatidylglycerols directly bind to viral particles to block infection, inhibit COX-2 expression to reduce the release of inflammatory factors (IL-6, IL-8), and improve oxidative stress by regulating mitochondrial membrane phospholipid remodeling. Phosphatidylglycerols can be taken orally or by inhalation and can be used in the study of chronic inflammatory diseases (such as atherosclerosis) and respiratory viral infections (such as RSV) .
|
-
- HY-N0194R
-
|
|
Apoptosis
Parasite
|
Inflammation/Immunology
Cancer
|
|
Asiatic acid (Standard) is the analytical standard of Asiatic acid. This product is intended for research and analytical applications. Asiatic acid, a pentacyclic triterpene found in Centella asiatica (Centella asiatica), has anticancer activity. Asiatic acid induces apoptosis in melanoma cells and has barrier protective effects on human aortic endothelial cells (HAEC). Asiatic acid also has anti-inflammatory activity and inhibits tumor necrosis factor (TNF)-α-induced endothelial barrier dysfunction. Asiatic acid also inhibits NLRP3 inflammasome activation and NF-κB pathway, effectively inhibits inflammation in rats, and has neuroprotective effects in rat spinal cord injury (SCI) model .
|
-
- HY-164384
-
|
|
PI3K
Akt
mTOR
Apoptosis
|
Cancer
|
|
DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC50s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice .
|
-
- HY-N10009
-
|
|
NF-κB
TNF Receptor
COX
ERK
p38 MAPK
Sirtuin
|
Inflammation/Immunology
|
|
Cudraflavone B is a prenylated flavonoid with anti-inflammatory and anti-tumor properties. Cudraflavone B is also a dual inhibitor of COX-1 and COX-2. Cudraflavone B blocks the translocation of nuclear factor κB (NF-κB) from the cytoplasm to the nucleus in macrophages. Thus, Cudraflavone B inhibits tumor necrosis factor α (TNFα) gene expression and secretion. Cudraflavone B also triggers the mitochondrial apoptotic pathway, activates NF-κB, the MAPK p38, and ERK, and induced the expression of SIRT1. Thus Cudraflavone B inhibits the growth of human oral squamous cell carcinoma cells .
|
-
- HY-163288
-
|
|
Histone Methyltransferase
HSP
Apoptosis
|
Cancer
|
|
EZH2/HSP90-IN-29 is a dual inhibitor for EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively. EZH2/HSP90-IN-29 increases apoptosis/necrosis-related gene expression, induces cell cycle arrest at M phase and inhibits reactive oxygen species (ROS) catabolism pathway. EZH2/HSP90-IN-29 is able to cross the blood-brain-barrier (BBB) .
|
-
- HY-149539
-
|
|
FLT3
RET
|
Cancer
|
|
PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po) .
|
-
- HY-146323
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-58 (Compound C18) is an anti-tumor agent. Antitumor agent-58 effectively inhibits colony formation and cell migration of MGC-803 cells. Antitumor agent-58 induces apoptosis of MGC-803 cells through activation of the p38 and JNK signaling pathways. Antitumor agent-58 induces mitochondrial dysfunction of MGC-803 cells. Antitumor agent-58 effectively inhibits tumor growth of xenograft model bearing MGC-803 cells .
|
-
- HY-N1904
-
-
- HY-N6002
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
3'-Hydroxypterostilbene is a Pterostilbene (HY-N0828) analogue. 3'-Hydroxypterostilbene inhibits the growth of COLO 205, HCT-116 and HT-29 cells with IC50s of 9.0, 40.2 and 70.9 µM, respectively. 3'-Hydroxypterostilbene significantly down-regulates PI3K/Akt and MAPKs signaling pathways and effectively inhibits the growth of human colon cancer cells by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene can be used for the research of cancer .
|
-
- HY-164468
-
|
|
Bcl-2 Family
Apoptosis
Autophagy
|
Cancer
|
|
Ch282-5 is an orally active inhibitor targeting the Bcl-2 protein, inducing mitochondria-dependent apoptosis (Apoptosis) by disrupting mitophagy and the mTOR pathway. Ch282-5 exhibits antiproliferative activity against colorectal cancer cells both in vitro and in vivo, and it also inhibits metastasis. Additionally, Ch282-5 enhances Oxaliplatin (HY-17371)-induced autophagy (Autophagy) by downregulating the Mcl-1 protein and increasing platelet count, alleviating adverse effects of Navitoclax (HY-10087) .
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-
- HY-17473R
-
|
|
IAP
NF-κB
Apoptosis
Autophagy
|
Cancer
|
|
Embelin (Standard) is the analytical standard of Embelin. This product is intended for research and analytical applications. Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells .
|
-
- HY-B0808R
-
|
Oxaprozinum (Standard); Wy21743 (Standard)
|
COX
NF-κB
Akt
IKK
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Oxaprozin (Standard) is the analytical standard of Oxaprozin. This product is intended for research and analytical applications. Oxaprozin is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB. Oxaprozin induces cell apoptosis. Oxaprozin shows anti-inflammatory activity. Oxaprozin-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties .
|
-
- HY-N1372AR
-
|
|
HIV
FAK
Apoptosis
Autophagy
|
Infection
Cancer
|
|
Fangchinoline (Standard) is the analytical standard of Fangchinoline. This product is intended for research and analytical applications. Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing . Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK . Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer .
|
-
- HY-N5112B
-
|
Isoarnebin I
|
HIF/HIF Prolyl-Hydroxylase
Apoptosis
Notch
NO Synthase
Bcl-2 Family
|
Cancer
|
|
β,β-Dimethylacrylshikonin (Isoarnebin I) is a naphthoquinone derivative that can be isolated from Lithospermum erythrorhizon Sieb. et Zucc. β,β-Dimethylacrylshikonin promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway. β,β-Dimethylacrylshikonin inhibits Notch-1 activation. β,β-Dimethylacrylshikonin inhibtis tumor cell proliferation, induces tumor cell apoptosis, and inhibits tumor growth .
|
-
- HY-117746
-
|
|
Bacterial
|
Infection
|
|
KSK120 is a potent inhibitor of drug-resistant infections with specific activity against Chlamydia trachomatis (C. trachomatis). KSK120 inhibits the developmental cycle of C. trachomatis, thereby reducing the infectivity of progeny bacteria. KSK120 targets the glucose-6-phosphate (G-6P) metabolic pathway of C. trachomatis, showing its potential application in antimicrobial inhibition. The mechanism of KSK120 may involve inhibition of the transcriptional machinery, which provides new ideas for the development of specific drugs against C. trachomatis infection .
|
-
- HY-N0028R
-
|
|
Others
|
Inflammation/Immunology
|
|
Forsythiaside A (Standard) is the analytical standard of Forsythiaside A. This product is intended for research and analytical applications. Forsythiaside A is an orally active phenylethanoid glycoside isolated from the dried fruits of Forsythia suspensa. Forsythiaside A is also an inhibitor of COX-2 and has anti-inflammatory, antioxidant and neuroprotective effects. Forsythiaside A prevents neuroinflammation and apoptosis caused by Aβ25-35 damage and may be used in Alzheimer's disease (AD) research. Forsythiaside A also activates the Nrf2/HO-1 signaling pathway and inhibits OVA-induced asthma in mice .
|
-
- HY-119980BS
-
|
|
Isotope-Labeled Compounds
Dopamine Receptor
Sodium Channel
SARS-CoV
|
Neurological Disease
Cancer
|
|
Fluphenazine-d6 (hydrochloride) is deuterium labeled Fluphenazine (hydrochloride). Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-119980A
-
|
|
Dopamine Receptor
Sodium Channel
SARS-CoV
|
Infection
Neurological Disease
Cancer
|
|
Fluphenazine dimaleate is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dimaleate blocks neuronal voltage-gated sodium channels. Fluphenazine dimaleate acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dimaleate can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dimaleate can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-119980S
-
|
|
Isotope-Labeled Compounds
Sodium Channel
Dopamine Receptor
SARS-CoV
|
Others
|
|
Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-168895
-
|
|
AP-1
ERK
Apoptosis
|
Cancer
|
|
c-Fos-IN-1 (Compound P16) is a c-Jun inhibitor, and decreases mRNA levels and protein levels of c-Fos. c-Fos-IN-1 also inhibits the phosphorylation activity of ERK and the transcriptional activity of AP-1. c-Fos-IN-1 shows anticancer activity by inhibiting ERK/c-Fos/Jun pathway. c-Fos-IN-1 inhibits the proliferation and migration of gastric cancer cells (IC50: 2.31 μM for MGC-803 cell). c-Fos-IN-1 arrests cell cycle at G2/M phase and induces cancer cell apoptosis. c-Fos-IN-1 inhibits gastric cancer tumor growth .
|
-
- HY-P9974
-
|
OMP-18R5
|
Wnt
|
Cancer
|
|
Vantictumab (OMP-18R5) is a fully human IgG2 monoclonal antibody. Vantictumab inhibits Wnt pathway signaling by binding to FZD1/2/5/7/8 receptors. Vantictumab can be studied against cancers through direct actions on tumor cells, including CSCs, and effects on the stroma, such as metastatic HER2-negative breast cancer and metastatic pancreatic adenocarcinoma .
|
-
- HY-N0255R
-
|
|
Apoptosis
|
Others
|
|
alpha-Hederin (Standard) is the analytical standard of alpha-Hederin. This product is intended for research and analytical applications. alpha-Hederin (α-Hederin), a monodesmosidic triterpenoid saponin, exhibits promising antitumor potential against a variety of human cancer cell lines. alpha-Hederin could inhibit the proliferation and induce apoptosis of gastric cancer accompanied by glutathione decrement and reactive oxygen species generation via activating mitochondrial dependent pathway .
|
-
- HY-N2425R
-
|
|
Cholinesterase (ChE)
|
Metabolic Disease
|
|
Rhodiosin (Standard) is the analytical standard of Rhodiosin. This product is intended for research and analytical applications. Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC50 for CYP2D6 is 0.761 μM, and the Ki is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system
|
-
- HY-143718
-
|
|
JAK
Btk
|
Inflammation/Immunology
|
|
JAK3/BTK-IN-3 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-3 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 009)
|
-
- HY-N6896R
-
|
|
TGF-beta/Smad
|
Cancer
|
|
Isoviolanthin (Standard) is the analytical standard of Isoviolanthin. This product is intended for research and analytical applications. Isoviolanthin, a flavonoid glycoside, could markedly inhibit TGF-β1-mediated migration and invasion by deactivating epithelial-mesenchymal transition (EMT) via the TGF-β/Smad and PI3K/Akt/mTOR pathways in HCC cells. Isoviolanthin exhibits no cytotoxic effects on normal liver LO2 cells .
|
-
- HY-146033
-
|
|
HPV
|
Cancer
|
|
HPV18-IN-1 (Compound H1) is a potent inhibitor of HPV18. HPV18-IN-1 prevents cervical cancer cells from premature cell procession and abnormal proliferation. HPV18-IN-1 supresses E7-Rb-E2F cellular pathway and DNA methylation. HPV18-IN-1 has the potential for the research of cancer diseases .
|
-
- HY-W380450
-
|
Viloxazin; Emovit
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Viloxazine (Viloxazin) is a norepinephrine reuptake inhibitor, also a potent 5-HT2C agonist and 5-HT2B antagonist with an EC50 of 32 μM and an IC50 of 27 μM for 5-HT2C and 5-HT2B, respectively. The mechanism of action of Viloxazine predominantly involves serotonergic and noradrenergic pathways. Viloxazine can be used for researching depression .
|
-
- HY-143472
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
PI3Kδ-IN-11 is a highly potent and selective PI3Kδ inhibitor with IC50 value of 27.5 nM. PI3Kδ-IN-11 dose-dependently blocks the activity of PI3K/Akt pathway. PI3Kδ-IN-11 can be used for researching B or T cell-related malignancies .
|
-
- HY-164492
-
|
|
Raf
|
Cancer
|
|
LSN3074753, an analog of LY3009120 (HY-12558), is a pan-RAF and Raf dimer inhibitor. LSN3074753 demonstrates activity against tumor cells with MAPK pathway activation driven by BRAF monomer or RAF dimers including BRAF- or KRAS-mutant colorectal cancer. LSN3074753 combined with Cetuximab (HY-P9905) shows additive and synergistic effects for colorectal cancer PDX models, particularly those with KRAS or BRAF mutation .
|
-
- HY-163343
-
|
|
Phosphodiesterase (PDE)
STING
|
Cancer
|
|
Enpp-1-IN-20 (Compound 31) is an ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) inhibitor, with an IC50 of 0.09 nM. Enpp-1-IN-20 has strongest inhibitory activity in the cell-based assay, with an IC50 of 8.8 nM. Enpp-1-IN-20 has significant potency in both ENPP1 inhibition and STING pathway stimulation in vitro. Enpp-1-IN-20 can be used for the research of cancer .
|
-
- HY-124089S
-
|
|
Isotope-Labeled Compounds
Cannabinoid Receptor
|
Metabolic Disease
|
|
Eicosapentaenoyl ethanolamide-d4 is the deuterium labeled Eicosapentaenoyl ethanolamide. Eicosapentaenoyl ethanolamide, an omega-3 fatty acid, is one of N-acylethanolamines (NAEs). Eicosapentaenoyl ethanolamide is cannabinoid CB1/CB2 receptor agonist. Eicosapentaenoyl ethanolamide acts as a metabolic signal. Eicosapentaenoyl ethanolamide inhibits dietary restriction (DR)-induced lifespan extension in wild type animals and suppresses lifespan extension in a TOR pathway mutant[1][2].
|
-
- HY-144323
-
|
|
PROTACs
PERK
|
Cancer
|
|
YF135 is an efficient and reversible-covalent KRAS G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway .
|
-
- HY-107661
-
|
ONO-2506; (R)-2-Propyloctanoic acid
|
Others
|
Neurological Disease
|
|
Arundic acid (ONO-2506) is an astrocyte-modulating agent, which delays the expansion of cerebral infarcts by modulating the activation of astrocytes through inhibition of S-100β synthesis. Arundic acid also increases the expression level of EAAT1 by activating the Akt, ERK, and NF-κB signaling pathways, which has the potential to eliminate excess glutamate and inhibit excitotoxic brain damage or death. Arundic acid has the potential for stroke and Alzheimer’s disease research .
|
-
- HY-P10838
-
|
|
PD-1/PD-L1
Apoptosis
|
Inflammation/Immunology
|
|
PL120131 is a PD-1/PD-L1 inhibitory peptide that can interfere with the interaction of PD-1/PD-L1 by binding to PD-1. PL120131 is capable of inhibiting the PD-1-mediated apoptotic signaling pathway, protecting Jurkat cells and primary lymphocytes from apoptosis. PL120131 aids in the antitumor activity of cytotoxic T lymphocytes (CTLs) .
|
-
- HY-50907
-
|
|
Bcl-2 Family
Apoptosis
Autophagy
Mitophagy
|
Cancer
|
|
ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research .
|
-
- HY-136310
-
|
|
PI5P4K
|
Cancer
|
|
PIP4K-IN-a131 is PIP4K lipid kinases inhibitor, with IC50s of 1.9?μM and 0.6?μM for purified PIP4K2A and PIP4Ks, respectively. PIP4K-IN-a131 exhibits cancer-selective lethality via dual blockade of the lipid kinase PIP4Ks and mitotic pathways .
|
-
- HY-152860
-
|
HRX-0215
|
p38 MAPK
JNK
NF-κB
MDM-2/p53
|
Cancer
|
|
Darizmetinib (HRX-0215) is an orally active, potent and selective inhibitor of mitogen-activated protein kinase kinase 4 (MKK4). Darizmetinib leads to enhancement of the MKK7 and JNK1 signaling pathways, thereby activating the transcription factors ATF2 and ELK1, promoting cell proliferation and liver regeneration. Darizmetinib is promising for research of preventing liver failure after extensive oncological liver resections or transplantation of small liver grafts .
|
-
- HY-159965
-
|
|
NOD-like Receptor (NLR)
RIP kinase
Interleukin Related
|
Inflammation/Immunology
|
|
NOD1-RIPK2-IN-1 (Compound 37) is a NOD1-RIPK2 signaling pathway inhibitor with IC50 values of 42 nM and 1.52 nM for NOD1 and RIPK2, respectively. NOD1-RIPK2-IN-1 reduces the secretion of the pro-inflammatory cytokine IL-8 and can be used in the research of inflammation and immune-related diseases .
|
-
- HY-N0717R
-
|
|
Arginase
Akt
Bacterial
|
Others
|
|
L-Valine (Standard) is the analytical standard of L-Valine. This product is intended for research and analytical applications. L-Valine (Valine) is a new nonlinear semiorganic material. L-Valine standrd causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine standrd inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
|
-
- HY-164595
-
|
|
Hippo (MST)
Apoptosis
AMPK
|
Metabolic Disease
|
|
IHMT-MST1-39 is an orally active inhibitor for MST kinase, with IC50 of 42 nM and 109 nM, for MST1 and MST2. IHMT-MST1-39 activates the AMPK signaling pathway in liver cells, reduces apoptosis of pancreatic β-cells. IHMT-MST1-39 ameliorates diabetes in Streptozotocin (HY-13753)-induced type 1 diabetes (T1D) mouse models .
|
-
- HY-B0493
-
|
|
Chloride Channel
COX
|
Inflammation/Immunology
Cancer
|
|
Niflumic acid is a calcium-activated chloride channel blocker and COX-2 inhibitor with the IC50 value of 100 nM. Niflumic acid induces apoptosis through caspase-8/Bid/Bax pathway in lung cancer cells. Niflumic acide exhibits anti-tumor activity by affecting the expression of ERK1/2 and the activity of MMP2 and MMP9. Niflumic acid has orally bioactivity. Niflumic acid acts on rheumatoid arthritis .
|
-
- HY-100490A
-
|
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- HY-143717
-
|
|
JAK
Btk
|
Inflammation/Immunology
|
|
JAK3/BTK-IN-2 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-2 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 004)
|
-
- HY-P1698
-
|
AB-103
|
Bacterial
CD28
|
Infection
Inflammation/Immunology
Cancer
|
|
Reltecimod (AB-103) is a T-cell-specific surface glycoprotein CD28 (TP44) antagonist. Reltecimod has beneficial effects against different bacterial infections, their exotoxins and endotoxins, and ionizing radiation. Reltecimod modulates the inflammatory response by targeting and attenuating the critical CD28/B7-2 co-stimulatory pathway, without inhibiting it. Reltecimod can be used to research necrotizing soft-tissue infections (NSTIs) .
|
-
- HY-170594
-
|
|
Atg7
Autophagy
|
Cancer
|
|
Antitumor agent-192 (Compound 2f) is a β-carboline antitumor agent. Antitumor agent-192 induces autophagy in HCT116 cells via the ATG5/ATG7 pathway. Antitumor agent-192 has an IC50 of less than 5 μM for human tumor cell lines and significantly inhibits tumor development and reduces tumor weight in a mouse colorectal cancer model transplanted with allografts [1].
|
-
- HY-161857
-
|
|
Akt
mTOR
Caspase
CDK
|
Cancer
|
|
Akt/mTOR-IN-1 (Compound 8r) is an AKT/mTOR signaling pathway inhibitor exhibiting an IC50 value of 0.8 µM with anticancer activity. Akt/mTOR-IN-1 can decrease the expression of Caspase 3 and increase the expression of the autophagic protein Cyclin B1, thereby inducing cell autophagy and apoptosis. Akt/mTOR-IN-1 can be used in research related to non-small cell lung cancer (NSCLC) .
|
-
- HY-155751
-
-
- HY-14664C
-
|
(3S,5R)-XU 62-320
|
HMG-CoA Reductase (HMGCR)
|
Cardiovascular Disease
Cancer
|
|
(3S,5R)-Fluvastatin sodium ((3S,5R)-XU 62-320) is the (3S,5R)-enantiomer of Fluvastatin. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
|
-
- HY-N6973
-
Boldine
1 Publications Verification
|
RANKL/RANK
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Boldine is an apomorphine isoquinoline alkaloid extracted from the root of the pheasant pepper (Litsea cubeba). Boldine is an oral effective antioxidant, anti-inflammatory, antitumor agent, and can inhibit osteoclast formation. Boldine induces apoptosis of human bladder cancer cells by regulating ERK, AKT and GSK-3β. Boldine ameliorates bone destruction by down-regulating the OPG/RANKL/RANK signaling pathway. It can be used in rheumatoid arthritis research .
|
-
- HY-168090
-
|
|
p38 MAPK
NF-κB
RANKL/RANK
|
Endocrinology
|
|
Anti-osteoporosis agent-11 (compound 3k) is an anti-osteoporosis compound targeting osteoclasts. Anti-osteoporosis agent-11 has the most significant inhibitory effect on osteoclast differentiation, with an IC50 value of 0.36 μM. In addition, Anti-osteoporosis agent-11 inhibits osteoclast formation, bone resorption, and the expression of osteoclast-specific genes by blocking rankl-induced mitogen-activated protein kinase (MAPK) and NF-κB signaling pathways .
|
-
- HY-W042416R
-
|
|
NF-κB
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
N,N-Dimethylacetamide (Standard) is the analytical standard of N,N-Dimethylacetamide. This product is intended for research and analytical applications. N,N-Dimethylacetamide (DMAc) is an organic solvent with blood-brain transmissibility and an FDA-approved drug excipient. N, N-dimethylacetamide exerts anti-inflammatory activity by inhibiting the NF-κB signaling pathway. N, N-dimethylacetamide can be used in studies of weight gain caused by a high-fat diet and neuroinflammation in Alzheimer's disease .
|
-
- HY-D0168
-
|
3,5-Dihydroxytoluene
|
Fluorescent Dye
Tyrosinase
p38 MAPK
ERK
|
Metabolic Disease
Cancer
|
|
Orcinol (3,5-Dihydroxytoluene) is an organic compound used in biological dyeing and proteomics research. Orcinol inhibits melanogenesis in B16F10 cells by upregulating the MAPK/ERK signaling pathway, and suppresses the expression of MITF, tyrosinase (TYR), TRP1, and DCT. Orcinol exhibits certain DPPH radical scavenging activity. In addition, Orcinol can alter nitrogen balance in animals. Orcinol holds promise for research in cancer and metabolic diseases .
|
-
- HY-B0252S3
-
|
HCTZ-15N2,13C,d2
|
Potassium Channel
TGF-beta/Smad
Isotope-Labeled Compounds
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Hydrochlorothiazide- 15N2, 13C,d2 is 15N and deuterated labeled Hydrochlorothiazide (HY-B0252). Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect .
|
-
- HY-N0106
-
|
(Rac)-Danshensu sodium; (Rac)-Tanshinol sodium
|
Keap1-Nrf2
NF-κB
Mitochondrial Metabolism
Apoptosis
|
Infection
Cardiovascular Disease
Inflammation/Immunology
|
|
(Rac)-Salvianic acid A sodium is the racemic form of Salvianic acid A (HY-N1913). Salvianic acid A is an orally active phenolic compound that induces Nrf2/HO-1 activation and inhibits the NF-κB pathway, and it also activates the mitochondrial antioxidant defense system (Mitochondrial Metabolism). Salvianic acid A exhibits anti-inflammatory, antioxidant, and anti-apoptotic properties (Apoptosis), demonstrating potential for research into inflammation and cardiovascular diseases .
|
-
- HY-143720
-
|
|
JAK
Btk
|
Inflammation/Immunology
|
|
JAK3/BTK-IN-5 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-5 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147953A1, example 35)
|
-
- HY-173165
-
|
3-O-(6-Bromo-D-mannosyl)-28-acylamino-n-caproate methyl oleanolic acid
|
Phosphatase
Apoptosis
|
Cancer
|
|
OA-Br-1 is an orally active and selective inhibitor of PTP1B with an IC50 value of 7.08 μM. OA-Br-1 induces apoptosis. OA-Br-1 has broad spectrum anti-proliferative activity against cancer cells, and plays an anti-breast cancer role through the PTP1B/PI3K/AKT signaling pathway both in vitro and in vivo .
|
-
- HY-B0863B
-
|
|
Apoptosis
Autophagy
Necroptosis
|
Neurological Disease
|
|
Glyphosate isopropylammonium, a non-selective systemic biocide with broad-spectrum activity, is an herbicidal derivative of the amino acid glycine. Glyphosate isopropylammonium inhibits the enzymatic activity of the 5-endopyruvylshikimate 3-phosphate synthase (EPSPS) in the shikimic acid pathway, preventing the synthesis of the aromatic amino acids tyrosine, phenylalanine, and tryptophan. Glyphosate isopropylammonium induces oxidative stress, neuroinflammation, and mitochondrial dysfunction, processes that lead to neuronal death by autophagia, necrosis, or apoptosis, as well as the appearance of behavioral and motor disorders .
|
-
- HY-N13218
-
|
|
Others
|
Cardiovascular Disease
|
|
Pueraria Extract is a kudzu extract, and its components include: Isoflavones. Pueraria Extract (ethanol extract) can significantly improve cardiac damage in rats with acute myocardial infarction. Pueraria Extract improves bile acid levels by increasing the expression of CYP7A1 and restoring the diversity of intestinal microbiota. Pueraria Extract can also inhibit the FXR-FGF15 signaling pathway and increase the expression of OST-α to increase bile acid reabsorption and fecal excretion. .
|
-
- HY-143719
-
|
|
JAK
Btk
|
Inflammation/Immunology
|
|
JAK3/BTK-IN-4 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-4 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147953A1, compound 003)
|
-
- HY-N0751
-
|
|
STAT
Akt
HIV
|
Infection
Cancer
|
|
Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. Scutellarin is active against HIV-1IIIB, HIV-1(74V) and HIV-1KM018 with EC50s of 26 μM, 253 μM and 136 μM, respectively.
|
-
- HY-P10810
-
|
|
Wnt
β-catenin
|
Cancer
|
|
QPH-FR, a quinoa peptide, is a leucine-rich repeat-containing G-protein-coupled receptor 5 (LGR5) inhibitor. QPH-FR competitively suppresses the formation of the LGR5/RSPO1 complex by binding to LGR5. QPH-FR causes RNF43/ZNRF3 to ubiquitinate the FZD receptor, thereby suppressing the Wnt/β-catenin signaling pathway and exerting stemness inhibition .
|
-
- HY-143241
-
|
|
HDAC
MDM-2/p53
Apoptosis
|
Cancer
|
|
HDAC-IN-34 (compound 27) is a potent HDAC inhibitor, with IC50 values of 0.022 and 0.45 μM for HDAC1 and HDAC6, respectively. HDAC-IN-34 can bind to DNA and cause DNA damage. HDAC-IN-34 causes cells apoptosis through p53 signaling pathway. HDAC-IN-34 exhibits significant anti-proliferation effect against HCT-116 cells, with an IC50 of 1.41 μM .
|
-
- HY-P10401
-
|
|
Apoptosis
iGluR
|
Cardiovascular Disease
Neurological Disease
|
|
TAT-GluR6-9c is a GluR6-PSD95 interaction blocker. By regulating the GluR6 mediated signaling pathway, TAT-GluR6-9c inhibits the activation of JNK and phosphorylation of c-Jun, reduces the expression of Fas L and thus reduces the occurrence of apoptosis. TAT-GluR6-9c can be used to study cerebral ischemia and neuroprotective strategies .
|
-
- HY-139567
-
|
BMS-986256
|
Toll-like Receptor (TLR)
NF-κB
Apoptosis
|
Inflammation/Immunology
|
|
Afimetoran (BMS-986256) is an orally active, selective, and highly bioavailable TLR7/8 antagonist. Afimetoran (BMS-986256) can inhibit TLR7/8 activation of the NF-κB pathway and reverse TLR7 mediated resistance to steroid induced apoptosis in plasma cell like dendritic cells (pDCs). Afimetoran (BMS-986256) can be used for research on inflammation and autoimmune diseases (systemic lupus erythematosus) .
|
-
- HY-111952
-
|
CID 16016685
|
Endogenous Metabolite
|
Others
|
|
SR-4995 (CID 16016685) is a highly effective and selective ligand for α-β-hydrolase domain-containing 5 (ABHD5), facilitating the activation of adipose triglyceride lipase (ATGL) by displacing ABHD5 from its inhibitory regulators, perilipin-1 (PLIN1) and PLIN5. It directly interacts with ABHD5, inhibiting its association with PLIN1, and promotes lipolysis in adipocytes and muscle tissues while circumventing PKA-dependent signaling pathways.
|
-
- HY-143716
-
|
|
JAK
Btk
|
Inflammation/Immunology
|
|
JAK3/BTK-IN-1 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-1 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 002) .
|
-
- HY-N9541
-
|
|
Others
|
Inflammation/Immunology
|
|
Chaetoglobosin Vb is a novel cytotoxic alkaloid with anti-inflammatory and antioxidant activities. Chaetoglobosin Vb can inhibit oxidative stress induced by LPS stimulation, reduce the production of reactive oxygen species and increase the expression of the antioxidant enzyme superoxide dismutase (SOD). Chaetoglobosin Vb significantly reduced the gene and protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) induced by LPS, and alleviated the production of proinflammatory cytokines such as TNF-α, IL-6 and IL-1β. Chaetoglobosin Vb exerts its biological activity through the TLR4-mediated MyD88-dependent signaling pathway and the TRIF-dependent signaling pathway, which is specifically manifested by inhibiting the phosphorylation of p38, ERK, and JNK MAPK and the translocation of NF-κB p65 subunit to the nucleus. Chaetoglobosin Vb showed no cytotoxic effect in the concentration range of 25-100 μM and promoted SOD enzyme activity and phosphorylation of p38, ERK1/2 and JNK in a dose-dependent manner .
|
-
- HY-130413
-
|
Neuroprotectin D1; NPD1
|
Endogenous Metabolite
PI3K
Akt
HIF/HIF Prolyl-Hydroxylase
Reactive Oxygen Species
Caspase
Interleukin Related
MicroRNA
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Protectin D1, a neuroprotectin D1 produced by neuronal cells, is a member of a newly discovered family of bioactive products derived from docosahexaenoic acid. Protectin D1 also serves as a specialized pro-resolving mediator, exhibiting effective in vivo pro-resolving activity in various human disease models. Additionally, Protectin D1 is an inhibitor of NALP3 inflammasomes and regulates the PI3K/AKT and HIF-1α signaling pathways. Protectin D1 exerts anti-inflammatory effects by reducing ROS levels, inhibiting the expression of NALP3, ASC, and Caspase-1, and consequently decreasing the release of pro-inflammatory cytokines IL-1β and IL-18. Furthermore, Protectin D1 enhances miRNA-210 expression, activates the PI3K/AKT signaling pathway, and exerts cardioprotective effects. Protectin D1 holds promise for research in cardiovascular diseases and inflammatory disorders .
|
-
- HY-110333
-
|
|
EGFR
|
Cancer
|
|
BMS-599626 dihydrochloride is a small molecule pan-HER (human epidermal growth factor receptor) kinase inhibitor. BMS-599626 dihydrochloride primarily targets HER1 (IC50=20 nmol/L) and HER2 (IC50=30 nmol/L) kinase activity in the HER family. BMS-599626 inhibits the kinase activity of HER1 and HER2 by competing with their ATP-binding sites, and can inhibit the downstream signaling pathway by blocking the heterodimer formation of HER1 and HER2. BMS-599626 dihydrochloride can be used to study the antitumor effects of multiple HER1 or HER2 overexpressed tumor models .
|
-
- HY-N0763
-
|
Isopsoralen
|
Apoptosis
Virus Protease
NF-κB
p38 MAPK
JNK
Caspase
|
Infection
Inflammation/Immunology
Cancer
|
|
Angelicin is a furanocoumarin compound that functions as an inhibitor of NF-κB and MAPK signaling pathways, exhibiting anti-inflammatory, antiviral, and antitumor activities. It suppresses the lytic replication of γ-herpesviruses, such as MHV-68, early during viral infection, potentially inhibiting RTA gene expression (IC50=28.95 μM). Angelicin also mitigates inflammation by inhibiting the phosphorylation and nuclear translocation of NF-κB, and the phosphorylation of p38 and JNK. Furthermore, it induces apoptosis in neuroblastoma cells by downregulating anti-apoptotic proteins like Bcl-2, Bcl-xL, and Mcl-1, while activating caspase-9 and caspase-3.
|
-
- HY-N0226
-
|
|
Cholinesterase (ChE)
Beta-secretase
|
Neurological Disease
Metabolic Disease
|
|
Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and can be used for the research of Alzheimer disease . Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberinecan be used for the research of diabetic disease .
|
-
- HY-162895
-
|
|
Polo-like Kinase (PLK)
Akt
CDK
Caspase
Apoptosis
|
Cancer
|
NL13 is a Polo-like kinase 4 (PLK4) inhibitor with an IC50 value of 2.32 μM. NL13 can inhibit the viability of PC3 and DU145 prostate cancer cells, with IC50 values of 3.51 μM and 2.53 μM, respectively. NL13 can lead to the inactivation of the AKT signaling pathway by downregulating CCNB1/CDK1, inducing G2/M cell cycle arrest, and triggering apoptosis through the cleavage of caspase-9/caspase-3. In prostate cancer mice, NL13 can inhibit tumor growth .
|
-
- HY-162641
-
|
|
IRAK
NF-κB
p38 MAPK
TNF Receptor
|
Inflammation/Immunology
|
|
AF-45 inhibits IRAK4 and IRAK1, with IC50s of 128 nM and 1765 nM. AF-45 inhibits the release of IL-6 and TNF-α in macrophages, with IC50s of 0.53-1.54 μM and 0.6-2.75 μM. AF-45 is also an inhibitor for NF-κB/MAPK signaling pathway. AF-45 exhibits anti-inflammatory activities against DSS-induced ulcerative colitis and Lipopolysaccharide (HY-D1056)-induced acute lung injury in mouse model. AF-45 exhibits good pharmacokinetic characteristics in rat models .
|
-
- HY-170877
-
|
|
SHP2
PI3K
Akt
Autophagy
|
Cancer
|
|
SHP2-IN-35 (Compound 3f) is the inhibitor for SHP2. SHP2-IN-35 exhibits antiproliferative activity in cancer cells RKO, SW480 and CT26 with IC50 of 5.72 μM, 3.71 μM and 1.42 μM, respectively. SHP2-IN-35 inhibits the PI3K-Akt signaling pathway, regulates the cell cycle associated gene expressions, and induces mitochondrial-related autophagy. SHP2-IN-35 inhibits the expression of certain cytokines and chemokines in the tumor microenvironment (TME), thereby regulating the tumor progression .
|
-
- HY-13404R
-
|
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Capmatinib (Standard) is the analytical standard of Capmatinib. This product is intended for research and analytical applications. Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-119009
-
|
|
JAK
STAT
NF-κB
Bcl-2 Family
|
Cancer
|
|
TM-233 is an inhibitor of the JAK/STAT and NF-κB signaling pathways, exhibiting significant antitumor activity. TM-233 reduces the expression of the anti-apoptotic protein Mcl-1 by inhibiting the phosphorylation of JAK2 and STAT3, and regulates its transcription by directly binding to the Mcl-1 gene promoter. Additionally, TM-233 prevents the translocation of NF-κB from the cytoplasm to the nucleus by inhibiting its DNA-binding activity, thereby reducing nuclear NF-κB expression. TM-233 shows potential in overcoming Bortezomib (HY-10227) resistance and can be applied in research related to multiple myeloma .
|
-
- HY-164411
-
|
|
c-Met/HGFR
|
Cancer
|
|
KRC-00715 is an effective oral c-Met inhibitor with an IC50 of 9.0 nM, demonstrating high selectivity in gastric cancer cells. KRC-00715 specifically inhibits the growth of c-Met-highly expressed cell lines by inducing G1/S phase arrest, leading to a reduction in downstream signaling pathways, including Akt and Erk, as well as c-Met activity. KRC-00715, in the gastric cancer cell line Hs746, is characterized by an IC50 of 39 nM, and it selectively inhibits the proliferation of c-Met-highly expressed cell lines. KRC-00715 reduces tumor size in Hs746T xenograft mouse models .
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-
- HY-121435
-
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RAR/RXR
PI3K
Akt
Apoptosis
|
Cancer
|
|
K-8012, a sulindac (HY-B0008) analog, is a potent antagonist of RXRa. The IC50 value for K-8012 to inhibit 9-cis-RA-induced Gal4-RXRa-LBD trans-activation were about 9.2 μM. K-8012 exerts improved anticancer activity over sulindac in a RXRa-dependent manner. K-8012 exhibits activity in inhibiting the tRXRa-mediated PI3K/AKT signaling pathway. K-8012 induces apoptosis and inhibits AKT activation by preventing tRXRa from binding to p85a .
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-
- HY-155169
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
hLTA4H/hLTA4S-IN-1 is a possible dual inhibitor that has the activity of inhibiting both human leukotriene hydrolase (hLTA4H) and human leukotriene C4 synthase (hLTC4S). hLTA4H/hLTA4S-IN-1 was identified by computer-assisted methods and is able to effectively interfere with the leukotriene biosynthesis pathway in cells. hLTA4H/hLTA4S-IN-1 can be used to study inflammatory responses .
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- HY-108543
-
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Phosphatase
Apoptosis
|
Cancer
|
|
NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor (Ki=32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C); IC50=22.3 nM (human Cdc25A), 56.9 nM (human Cdc25C), 125 nM (Cdc25B)) . NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway .
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-
- HY-163784
-
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Aldose Reductase
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Cancer
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|
AKR1C3-IN-14 (compound 4) is an AKR1C3 inhibitor (IC50=0.122 μM) that reduces the overproduction of androgens by inhibiting the activity of the AKR1C3 enzyme, thereby regulating hormone-mediated signaling. AKR1C3-IN-14 also plays a role in the biosynthesis of the prostaglandin PGF2α, regulating cell proliferation by affecting this pathway. AKR1C3-IN-14 can be used in the study of prostate cancer .
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- HY-A0081R
-
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Dopamine Receptor
SARS-CoV
Sodium Channel
|
Neurological Disease
Cancer
|
|
Fluphenazine (dihydrochloride) (Standard) is the analytical standard of Fluphenazine (dihydrochloride). This product is intended for research and analytical applications. Fluphenazine dihydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dihydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine dihydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dihydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dihydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
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- HY-19744
-
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MyD88
|
Inflammation/Immunology
|
|
T6167923 is a selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with IC50s of 2.7 μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively .
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- HY-138813R
-
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Drug Metabolite
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Cancer
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|
Glycochenodeoxycholic acid sodium salt (Standard) is the analytical standard of Glycochenodeoxycholic acid sodium salt. This product is intended for research and analytical applications. Glycochenodeoxycholic acid sodium salt (Sodium glycochenodeoxycholate) is a relatively toxic bile salt generated in the liver from chenodeoxycholic acid and glycine. Glycochenodeoxycholic acid sodium salt inhibits Autophagosome formation and impairs lysosomal function by inhibiting lysosomal proteolysis and increasing lysosomal pH in human normal liver cells, leading to the Apoptosis of human hepatocyte cells. Glycochenodeoxycholic acid sodium salt induces stemness and chemoresistance via activating STAT3 signaling pathway in hepatocellular carcinoma cells (HCC). Glycochenodeoxycholic acid sodium salt is promising for research in the field of cholestasis desease, hepatocellular carcinoma and primary sclerosing cholangitis (PSC) .
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- HY-N0316
-
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JAK
NF-κB
Reactive Oxygen Species
Apoptosis
VEGFR
c-Myc
|
Cancer
|
|
Mollugin is an orally active and potent NF-κB inhibitor. Mollugin induces S-phase arrest of HepG2 cells, and increased intracellular reactive oxygen species (ROS) levels. Mollugin induces DNA damage in HepG2 cells, as well as an increase in the expression of p-H2AX. Mollugin shows anti-cancer effect by inhibiting TNF-α-induced NF-κB activation. Mollugin enhances the osteogenic action of BMP-2 (bone morphogenetic protein 2) via the p38-Smad signaling pathway .
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- HY-N2334AR
-
|
|
Endogenous Metabolite
Apoptosis
STAT
BCL6
Interleukin Related
Caspase
|
Metabolic Disease
Cancer
|
|
Glycochenodeoxycholic acid sodium salt (Standard) is the analytical standard of Glycochenodeoxycholic acid sodium salt. This product is intended for research and analytical applications. Glycochenodeoxycholic acid sodium salt (Sodium glycochenodeoxycholate) is a relatively toxic bile salt generated in the liver from chenodeoxycholic acid and glycine. Glycochenodeoxycholic acid sodium salt inhibits Autophagosome formation and impairs lysosomal function by inhibiting lysosomal proteolysis and increasing lysosomal pH in human normal liver cells, leading to the Apoptosis of human hepatocyte cells. Glycochenodeoxycholic acid sodium salt induces stemness and chemoresistance via activating STAT3 signaling pathway in hepatocellular carcinoma cells (HCC). Glycochenodeoxycholic acid sodium salt is promising for research in the field of cholestasis desease, hepatocellular carcinoma and primary sclerosing cholangitis (PSC) .
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- HY-151262
-
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JAK
STING
NF-κB
STAT
|
Inflammation/Immunology
|
|
JAK-IN-23 is an orally active double inhibitor of JAK/STAT and NF-κB. JAK-IN-23 can inhibit JAK1/2/3 with IC50 values of 8.9 nM, 15 nM and 46.2 nM, respectively. JAK-IN-23 has potent inhibitory activities against interferon-stimulated genes (ISG) and NF-κB pathways with IC50 values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 has great anti-inflammatory that decreases the release of various proinflammatory factors. JAK-IN-23 can be used for the research of inflammatory bowel disease (IBD) .
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-
- HY-169703
-
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RANKL/RANK
p38 MAPK
Akt
NF-κB
|
Inflammation/Immunology
|
|
SPA0355 is a thiourea derivative that has antioxidant and anti-inflammatory properties. SPA0355 inhibits the RANKL (receptor activator of nuclear factor κB ligand) induced osteoclast formation in primary bone marrow-derived macrophages. SPA0355 also suppresses the activation of the MAPKs, Akt, and NF-κB pathways. Additionally, SPA0355 promotes osteoblast differentiation, increases alkaline phosphatase activity, and enhances mineral nodule formation. SPA0355 can protect ovariectomized mice from bone loss by stimulating osteoblast differentiation and inhibiting osteoclast resorption, making it useful for studying postmenopausal osteoporosis .
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-
- HY-W050154
-
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|
Parasite
Tyrosinase
NF-κB
CDK
|
Infection
Inflammation/Immunology
Cancer
|
|
Kojic acid is a substance produced by Aspergillus oryzae that is orally effective and can also be absorbed transdermally. Kojic acid exhibits various biological activities, including anti-aging, anti-nematode, antimicrobial, antioxidant, and anti-inflammatory effects. Kojic acid is a Tyrosinase inhibitor with an Mushroom Tyrosinase IC50 of 182.7 μM. Kojic acid prevents melanin production by capturing copper ions that bind to the tyrosinase active site, thus inhibiting its activation. Kojic acid also suppresses the NF-κB and p21 signaling pathways in human keratinocytes. Kojic acid derivatives have anticancer activity .
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-
- HY-N7204
-
|
|
Monoamine Oxidase
Dopamine β-hydroxylase
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
|
4-Hydroxyderricin, the major active ingredients of Angelica keiskei Koidzumi, is an orally active, potent selective MAO-B (Monoamine oxidase inhibitors) inhibitor with an IC50 of 3.43 μM. 4-Hydroxyderricin also mildly inhibits dopamine β (DBH)-hydroxylase activity. 4-Hydroxyderricin has antidepressant activity, anti-allergic, anti-diabetic, anti-oxidant, and antitumor effects. 4-Hydroxyderricin promotes apoptosis and cell cycle arrest through regulating PI3K/AKT/mTOR pathway in hepatocellular cells. 4-Hydroxyderricin inhibits osteoclast formation and accelerates osteoblast differentiation . 4-Hydroxyderricin is promising for research of inflammatory diseases .
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-
- HY-N0373R
-
|
|
Amyloid-β
Apoptosis
NOD-like Receptor (NLR)
|
Neurological Disease
|
|
Licochalcone B (Standard) is the analytical standard of Licochalcone B. This product is intended for research and analytical applications. Licochalcone B is an extract from the root of Glycyrrhiza uralensis. Licochalcone B inhibits amyloid β (42) self-aggregation (IC50=2.16 μM) and disaggregate pre-formed Aβ42 fibrils, reduce metal-induced Aβ42 aggregation through chelating metal ionsLicochalcone B inhibits phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone B inhibits growth and induces apoptosis of NSCLC cells. Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7‐NLRP3 interaction .
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-
- HY-122575
-
|
|
P2X Receptor
Influenza Virus
Topoisomerase
MicroRNA
Apoptosis
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively . Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase . Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis . Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway . Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM . Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM .
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-
- HY-162944
-
|
|
Ferroptosis
Mitochondrial Metabolism
STING
Autophagy
|
Cancer
|
|
NA-Ir is a Ferroptosis inducer. NA-Ir targets mitochondrial DNA (mtDNA) and activates the cGAS-STING pathway to induce ferritinophagy (Autophagy), while also generating reactive oxygen species (ROS) through photodynamic therapy (PDT), depleting glutathione (GSH), and downregulating glutathione peroxidase 4 (GPX4), thereby triggering lipid peroxidation and Ferroptosis. NA-Ir exhibits higher anticancer activity under light exposure and selectively inhibits cancer cells with high H2S levels .
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-
- HY-N0265R
-
|
|
Caspase
Apoptosis
|
Cardiovascular Disease
|
|
Asperosaponin VI (Standard) is the analytical standard of Asperosaponin VI. This product is intended for research and analytical applications. Asperosaponin VI, A saponin component from Dipsacus asper, induces osteoblast differentiation through BMP‐2/p38 and ERK1/2 pathway . Asperosaponin Ⅵ inhibits apoptosis in hypoxia-induced cardiomyocyte by increasing the Bcl-2/Bax ratio and decreasing active caspase-3 expression, as well as enhancing of p-Akt and p-CREB .
|
-
- HY-113224
-
-
- HY-10182B
-
|
CHIR-99021 trihydrochloride; CT99021 trihydrochloride
|
Organoid
GSK-3
Wnt
β-catenin
Autophagy
|
Cancer
|
|
Laduviglusib (CHIR-99021) trihydrochloride is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib trihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib trihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib trihydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib trihydrochloride induces autophagy .
|
-
- HY-15113
-
|
|
Prolyl Endopeptidase (PREP)
|
Neurological Disease
Cancer
|
|
Y-29794 is a selective, orally active inhibitor for non-peptide prolyl endopeptidase (PREP), with an IC50 of 3 nM and a Ki of 0.95 nM. Y-29794 enhances the effect of thyrotropin-releasing hormone (TRH) on the release of ACh in the rat hippocampus, exhibits potential neuroprotective efficacy. Y-29794 exhibits anticancer activity through inhibition of the IRS1-AKT-mTORC1 pathway. Y-29794 penetrates the brain-blood barrier (BBB) .
|
-
- HY-P990025
-
|
ARGX-117
|
Complement System
|
Inflammation/Immunology
|
|
Empasiprubar (ARGX-117) is a humanized inhibitory monoclonal antibody targeting complement C2. Empasiprubar binds to the Sushi-2 domain of C2, preventing the formation of C3 pre convertase and inhibiting the activation of classical and lectin pathways upstream of C3 activation. Empasiprubar can prevent complement mediated autoimmune hemolytic anemia and antibody mediated organ transplant rejection. Empasiprubar can prevent neuroglial lymphoconjunctival injury in GM1 antibody mediated mouse models .
|
-
- HY-107632G
-
-
- HY-B1690AR
-
|
|
Antibiotic
Bacterial
Histamine Receptor
|
Infection
|
|
Thioridazine (Standard) is the analytical standard of Thioridazine. This product is intended for research and analytical applications. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
- HY-131972
-
|
|
PI3K
|
Cancer
|
|
PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy .
|
-
- HY-P99437
-
|
KN-026
|
EGFR
|
Cancer
|
|
Anbenitamab (KN-026) is a bispecific antibody simultaneously targeting the extracellular domains II and IV of the human HER2. Anbenitamab blocks both ligand-dependent and ligand-independent HER2 signaling pathway. The IgG1 Fc fragment of Anbenitamab binds FcRγIIIa mediates potent antibody dependent cell-mediated cytotoxicity (ADCC) and inhibits tumor cell proliferation. Anbenitamab has the potential for HER2-positive metastatic breast cancer (MBC) research .
|
-
- HY-124379
-
TPCK
1 Publications Verification
L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK
|
Ser/Thr Protease
HPV
Apoptosis
PDK-1
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is an effective serine protease inhibitor and also a blocker of the PDK1/Akt pathway. TPCK can modify the E7 protein in actively keratinocyte cells. TPCK can induce cellular apoptosis, suppress tumor growth, reduce hypoxic-ischemic brain injury in rat pups, and affect vascular permeability in inflamed rats .
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-
- HY-N0631R
-
|
|
p38 MAPK
NF-κB
|
Inflammation/Immunology
|
|
Cornuside (Standard) is the analytical standard of Cornuside. This product is intended for research and analytical applications. Cornuside is a secoiridoid glucoside isolated from the fruit of Cornus officinalis Sieb. et Zucc., which is a traditional oriental medicine for treating inflammatory diseases and invigorating blood circulation. Cornuside inhibits mast cell-mediated allergic response by down-regulating MAPK and NF-κB signaling pathways. Cornuside has anti-allergic effects in vivo and in vitro which suggests a therapeutic application of this agent in inflammatory allergic diseases .
|
-
- HY-15113A
-
|
|
Prolyl Endopeptidase (PREP)
|
Neurological Disease
Cancer
|
|
Y-29794 tosylate is a selective, orally active inhibitor for non-peptide prolyl endopeptidase (PREP), with an IC50 of 3 nM and a Ki of 0.95 nM. Y-29794 tosylate enhances the effect of thyrotropin-releasing hormone (TRH) on the release of ACh in the rat hippocampus, exhibits potential neuroprotective efficacy. Y-29794 tosylate exhibits anticancer activity through inhibition of the IRS1-AKT-mTORC1 pathway. Y-29794 tosylate penetrates the brain-blood barrier (BBB) .
|
-
- HY-133095
-
|
|
STAT
PPAR
|
Inflammation/Immunology
|
|
BML-260 is a potent inhibitor of dual-specific phosphatases JSP-1 and DUSP22. BML-260 can activate UCP1 and thermogenesis in adipocytes in a JSP-1-independent manner. The effect of BML-260 on adipocytes is partially achieved through the activation of CREB, STAT3, and PPAR signaling pathways. BML-260 can be used in the research of inflammatory and proliferative disorders associated with JNK signaling dysfunction as well as obesity .
|
-
- HY-10182
-
|
CHIR-99021; CT99021
|
Organoid
GSK-3
Wnt
β-catenin
Autophagy
|
Metabolic Disease
Cancer
|
|
Laduviglusib (CHIR-99021) is a potent, selective and orally active GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib enhances mouse and human embryonic stem cells self-renewal. Laduviglusib induces autophagy .
|
-
- HY-N2535R
-
|
|
Keap1-Nrf2
Apoptosis
|
Inflammation/Immunology
|
|
Coniferaldehyde (Standard) is the analytical standard of Coniferaldehyde. This product is intended for research and analytical applications. Coniferaldehyde (4-Hydroxy-3-methoxycinnamaldehyde) is an effective inducer of heme oxygenase-1 (HO-1). Coniferaldehyde inhibits LPS-induced apoptosis through the PKCα/β II/Nrf-2/HO-1 dependent pathway in RAW264.7 macrophage cells. Coniferaldehyde has antioxidant and anti-inflammatory activities .
|
-
- HY-101349
-
|
|
Dopamine Receptor
Apoptosis
|
Neurological Disease
Cancer
|
|
L 741742 is a dopamine receptor D4 (DRD4) antagonist that selectively inhibits glioblastomas (GBM) growth in vitro and in vivo, synergyed with Temozolomide (TMZ) (HY-17364). L 741742 disrupts in effectors PDGFRβ/ERK1/2 and mTOR signaling. Additionally, L 741742 disrupts endolysosmal function compromising the autophagy-lysosomal degradation pathway, followed by G0/G1 cell cycle arrest and Apoptosis. L 741742 is promising for research of GBM and neurogenesis .
|
-
- HY-100490S
-
|
|
Isotope-Labeled Compounds
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Rilmenidine-d4 is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].
|
-
- HY-18318
-
|
|
Raf
VEGFR
PERK
|
Cancer
|
|
Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC50 values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity .
|
-
- HY-146228
-
|
|
HSP
Apoptosis
Topoisomerase
EGFR
VEGFR
|
Cancer
|
|
HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway .
|
-
- HY-107737
-
|
1,2-Dilauroyl-sn-glycero-3-phosphocholine
|
Liposome
Apoptosis
TNF Receptor
PPAR
|
Metabolic Disease
|
|
1,2-DLPC (1,2-Dilauroyl-sn-glycero-3-phosphocholine) is a ligand for LRH-1 agonists. 1,2-DLPC is a phospholipid used in the synthesis of liposomes. 1,2-DLPC enhances fat breakdown and apoptosis in fat cells through a TNFα-dependent pathway, while also inhibiting palmitate-induced insulin resistance through PPARα-mediated inflammation in muscle cells .
|
-
- HY-161520
-
|
|
Glucocorticoid Receptor
NF-κB
|
Inflammation/Immunology
|
|
Glucocorticoid receptor/NF-κB modulator-1 (Compound 20) is a derivative of ocotillol. Glucocorticoid receptor/NF-κB modulator-1 suppresses the degradation of glucocorticoid receptor (GR) mRNA and GR protein, inhibits the activation of NF-κB signaling pathway. Glucocorticoid receptor/NF-κB modulator-1 downregulates levels of NO, interleukin-6 and tumor necrosis factor-alpha (TNF-α). Glucocorticoid receptor/NF-κB modulator-1 ameliorates sepsis in mouse model .
|
-
- HY-146725
-
|
|
FBPase
|
Metabolic Disease
|
|
FBPase-IN-1 is a potent FBPase (Fructose-1,6-bisphosphatase) inhibitor for Type 2 diabetes (T2D) study with an IC50 of 0.22 μM. FBPase-IN-1 can reduce blood glucose levels and ameliorate glucose tolerance. FBPase-IN-1 modifies the C128 site, regulates the N125-S124-S123 allosteric pathway of FBPase and affects the catalytic activity of FBPase .
|
-
- HY-153896
-
|
|
c-Met/HGFR
|
Cancer
|
|
LMTK3-IN-1 (compound C28) is an ATP-competitive inhibitor of lemur tyrosine kinase 3 (LMTK3) (Kd=2.5 μM)，that acts by degrading LMTK3 via the ubiquitin-proteasome pathway. LMTK3-IN-1 shows anticancer activity in a variety of cancer cell lines and in vivo BC mouse models. LMTK3-IN-1 induces apoptosis in BC cell lines at 10-20 μM .
|
-
- HY-N8016S2
-
|
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
|
Nonanal-d2 is deuterated labeled Methyl cinnamate (HY-W017212). Methyl cinnamate (Methyl 3-phenylpropenoate), an active component of Zanthoxylum armatum, is a widely used natural flavor compound. Methyl cinnamate (Methyl 3-phenylpropenoate) possesses antimicrobial activity and is a tyrosinase inhibitor that can prevent food browning. Methyl cinnamate (Methyl 3-phenylpropenoate) has antiadipogenic activity through mechanisms mediated, in part, by the CaMKK2-AMPK signaling pathway .
|
-
- HY-I0746
-
|
m-Aminobenzoic acid; 3ABA
|
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
|
|
3-Aminobenzoic acid (3-ABA) is an orally active anti-inflammatory agent targeting the tight junction (TJ) regulatory pathways in intestinal epithelial cells. 3-Aminobenzoic acid improves intestinal inflammation by enhancing intestinal barrier integrity and reducing epithelial permeability. It can be used in studies related to improving gut health. Additionally, 3-Aminobenzoic acid analogs can act as γ-aminobutyric acid transaminase (GABA-AT) inhibitors, exhibiting anticonvulsant effects .
|
-
- HY-12383S
-
|
|
Isotope-Labeled Compounds
COX
|
Neurological Disease
Inflammation/Immunology
|
|
Pelubiprofen- 13C,d3 is the 13C- and deuterium labeled Pelubiprofen. Pelubiprofen, an orally active and non-steroidal anti-inflammatory drug, is a member of the 2-arylpropionic acid family and has relatively selective effects on COX-2 activity. Pelubiprofen inhibits COX activity and the transforming growth factor-β activated kinase 1-IκB kinase β-NF-κB pathway, and has significant anti-inflammatory and analgesic effects[1].
|
-
- HY-168551
-
