Search Result
Results for "
Acidogenesis pathway Inhibitors
" in MCE Product Catalog:
9888
Inhibitors & Agonists
18
Biochemical Assay Reagents
547
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-U00439
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- HY-U00439A
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- HY-136073
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- HY-135516
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Wnt pathway activator 1
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Wnt
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Cancer
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Wnt pathway activator 1 is a potent Wnt activator extracted from patent WO2012024404A1, compound 1, has an EC50s of 28-29 nM.
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- HY-117229
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- HY-136541
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YB-0158
Wnt pathway inhibitor 2
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Wnt
Apoptosis
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Cancer
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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.
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- HY-15673
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KP372-1
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PI3K
Akt
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Cancer
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KP372-1, an Akt inhibitor, block signalling through the PI3K pathway and inhibit cell proliferation while inducing apoptosis of cancer cells.
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- HY-135282
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- HY-119711
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NNGH
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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-N9474
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- HY-147789
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FPDT
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Akt
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Cancer
Neurological Disease
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FPDT is an anti-glioblastoma agent. FPDT displays the IC50 value of 45–68 μM for GBM cells and >100 μM for astrocytes. Anti-glioblastoma activity of FPDT is linked to downregulation of the AKT pathway.
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- HY-B0863
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Glyphosate
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Apoptosis
Autophagy
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Cancer
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Glyphosate is an herbicidal derivative of the amino acid glycine. Glyphosate targets and blocks a plant metabolic pathway not found in animals, the shikimate pathway, required for the synthesis of aromatic amino acids in plants.
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- HY-107595
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SD-1008
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JAK
STAT
Apoptosis
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Cancer
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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.
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- HY-12848C
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SAG dihydrochloride
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Smo
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Cancer
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SAG dihydrochloride is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG dihydrochloride activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo.
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- HY-N0247
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Saikosaponin B1
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Smo
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Cancer
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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.
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- HY-108516
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TC-E 5001
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PARP
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Cancer
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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.
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- HY-14664A
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- HY-13418
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Dorsomorphin dihydrochloride
Compound C dihydrochloride; BML-275 dihydrochloride
|
AMPK
TGF-β Receptor
Autophagy
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Cancer
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Dorsomorphin dihydrochloride (BML-275 dihydrochloride; 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 induces autophagy.
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- HY-107572
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PD 128042
CI 976
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Acyltransferase
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Metabolic Disease
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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.
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- HY-14664
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- HY-W097899
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Vanillylamine
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Others
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Others
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Vanillylamine is a derivative of vanillin is synthesized through a transaminase reaction in the phenylpropanoid pathway of capsaicinoid synthesis.
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- HY-146757
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RIPK1-IN-13
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RIP kinase
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Inflammation/Immunology
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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.
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- HY-13459
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PF-5274857
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Smo
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Cancer
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PF-5274857 is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.
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- HY-13459A
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PF-5274857 hydrochloride
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Smo
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Cancer
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PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.
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- HY-119663
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Averantin
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Fungal
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Infection
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Averantin is the minor metabolite of the fungus Cercospora arachidicola. Averantin is an aflatoxin B1 precursor that can be used in the biosynthetic pathway.
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- HY-18287A
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MRT-83 hydrochloride
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Smo
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Cancer
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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.
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- HY-123940
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SGC-AAK1-1
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Others
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Cancer
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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.
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- HY-14664DS
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(3S,5R)-Fluvastatin D6
(3S,5R)-XU 62-320 free acid D6
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Autophagy
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Cancer
Cardiovascular Disease
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(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.
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- HY-14664B
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(3R,5S)-Fluvastatin
(3R,5S)-XU 62-320 free acid
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HMG-CoA Reductase (HMGCR)
Autophagy
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Cancer
Cardiovascular Disease
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(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.
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- HY-19542
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C6 Ceramide
C6-Cer; N-Hexanoylsphingosine
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Apoptosis
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Cancer
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C6-ceramide, a ceramide pathway activator, shows activity against a variety of cancer cell lines. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects.
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- HY-138537
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NF-κB-IN-1
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IKK
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Cancer
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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.
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- HY-107753
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XRP44X
|
Ras
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Cancer
Inflammation/Immunology
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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.
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- HY-122700
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Factor D inhibitor 6
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Complement System
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Inflammation/Immunology
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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.
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- HY-145860
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PHGDH-IN-2
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Others
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Cancer
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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.
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- HY-137371
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- HY-N10405
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- HY-N0293
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Paeoniflorin
Peoniflorin
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HSP
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Neurological Disease
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Paeoniflorin (Peoniflorin), a heat shock protein-inducing compound and a pinane monoterpene glycoside with various bioactivities, such as anticancer effects, anti-oxidative stress, antiplatelet aggregation, expansion of blood vessels, reducing blood viscosity and anti-inflammatory activity. paeoniflorin protects PC12 cells from MPP + and acidic damage via autophagic pathway.
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- HY-128570
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FD-IN-1
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Complement System
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Inflammation/Immunology
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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.
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- HY-108571
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CP-775146
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PPAR
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Metabolic Disease
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CP-775146 is a selective PPARα agonist that binds strongly to the PPARα ligand. CP-775146 efficiently alleviates obesity-induced liver damage, prevents lipid accumulation by activating the liver fatty acid β-oxidation pathway.
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- HY-114295A
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Geranyl pyrophosphate triammonium
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Others
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Metabolic Disease
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Geranyl pyrophosphate triammonium is a key intermediate in the isoprenoid biosynthesis pathway (IBP). Geranyl pyrophosphate triammonium plays key roles in cellular metabolism and is responsible for the production of both sterol and non-sterol isoprenoids.
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- HY-125136
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Chaetominine
(-)-Chaetominine
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PI3K
Akt
Keap1-Nrf2
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Cancer
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Chaetominine is an alkaloidal metabolite. Chaetominine has cytotoxicity against human leukemia K562 and colon cancer SW1116 cell lines. Chaetominine reduces MRP1-mediated drug resistance via inhibiting PI3K/Akt/Nrf2 signaling pathway in K562/Adr human leukemia cells.
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- HY-121320
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Raptinal
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Caspase
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Cancer
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Raptinal, a agent that directly activates caspase-3, initiates intrinsic pathway caspase-dependent apoptosis. Raptinal is able to rapidly induce cancer cell death by directly activating the effector caspase-3, bypassing the activation of initiator caspase-8 and caspase-9.
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- HY-15496
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E6201
ER-806201
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MEK
FLT3
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Cancer
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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.
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- HY-W011209
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N6-Isopentenyladenosine
Riboprine
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Autophagy
Endogenous Metabolite
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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-129905
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L-Leucyl-L-Leucine methyl ester hydrochloride
LLOMe hydrochloride; Leu-Leu methyl ester hydrochloride; H-Leu-Leu-OMe hydrochloride
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Endogenous Metabolite
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Inflammation/Immunology
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L-Leucyl-L-Leucine methyl ester (LLOMe) hydrochloride, a dipeptide condensation product of L-leucine methyl ester generated by human monocytes or polymorphonuclear leukocytes, selectively eliminates lymphocytes with cytotoxic potential. L-Leucyl-L-Leucine methyl ester hydrochloride also can induce endolysosomal pathway stress.
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- HY-129905A
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L-Leucyl-L-Leucine methyl ester hydrobromide
LLOMe hydrobromide; Leu-Leu methyl ester hydrobromide; H-Leu-Leu-OMe hydrobromide
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Endogenous Metabolite
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Inflammation/Immunology
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L-Leucyl-L-Leucine methyl ester (LLOMe) hydrobromide, a dipeptide condensation product of L-leucine methyl ester generated by human monocytes or polymorphonuclear leukocytes, selectively eliminates lymphocytes with cytotoxic potential. L-Leucyl-L-Leucine methyl ester hydrobromide also can induce endolysosomal pathway stress.
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- HY-145532
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S-Allylmercaptocysteine
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Apoptosis
NF-κB
Keap1-Nrf2
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Cancer
Inflammation/Immunology
|
S-allylmercaptocysteine, an organic sulfur compound extracted from garlic, has anti-inflammatory and anti-oxidative effects for various pulmonary diseases. S-allylmercaptocysteine achieves its anti-cancer effect through a variety of pathways such as inducing the apoptosis of cancer cells through the TGF-β signaling pathway, or reducing the NF-κB activity and up-regulating Nrf2 to achieve the effects of anti-inflammation and anti-oxidation.
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- HY-19345
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Vacquinol-1
NSC13316
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Others
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Cancer
|
Vacquinol-1 (NSC13316) is a MKK4-specific activator that activates MAPK pathways. Vacquinol-1 specifically induces human glioblastoma cell (GC) death, attenuates tumor progression and prolongs survival in a glioblastoma multiforme (GBM) mouse model. Vacquinol-1 also induces apoptosis in hepatocellular carcinoma (HCC)cell.
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- HY-146751
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PI3K/Akt/mTOR-IN-2
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PI3K
Akt
mTOR
Apoptosis
|
Cancer
|
PI3K/Akt/mTOR-IN-2 is a PI3K/AKT/mTOR pathway inhibitor. PI3K/Akt/mTOR-IN-2 possess anti-cancer effects and selectivity against MDA-MB-231 cells with IC50 value of 2.29 μM. PI3K/Akt/mTOR-IN-2 can induce cancer cell cycle arrest and apoptosis.
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- HY-139793
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UDP-glucosamine disodium
UDP-GlcNAc disodium
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Endogenous Metabolite
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Metabolic Disease
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UDP-glucosamine (UDP-GlcNAc) disodium is a substrate for O-GlcNAc transferase, which catalyzes the attachment of O-GlcNAc to proteins. O-GlcNAcase catalyzes the removal of O-GlcNAc from proteins. UDP-glucosamine (UDP-GlcNAc) disodium is the end product of the hexosamine biosynthesis pathway, which is regulated primarily by glucose-6-phosphate-Glutamine:fructose-6-phosphate amidotransferase (GFAT).
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- HY-144806
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PI3K/AKT-IN-1
|
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.
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- HY-115902
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FGFR4-IN-7
|
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).
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- HY-143472
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PI3Kδ-IN-11
|
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.
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- HY-147670
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TPB15
|
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.
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- HY-F0003
-
NADPH tetrasodium salt
|
Ferroptosis
Endogenous Metabolite
|
Cancer
|
NADPH tetrasodium salt functions as an important cofactor in a variety of metabolic and biosynthetic pathways. NADPH tetrasodium salt plays a vital role in the biosynthesis of drugs, chiral alcohols, fatty acids and biopolymers, while also being required for lipid biosynthesis, biomass formation, and cell replication. The demand for NADPH tetrasodium salt is particularly high in proliferating cancer cells, where it acts as a cofactor for the synthesis of nucleotides, proteins, and fatty acids. NADPH tetrasodium salt is also essential for the neutralization of the dangerously high levels of reactive oxygen species (ROS) generated by increased metabolic activity. NADPH tetrasodium salt is an endogenous inhibitor of ferroptosis.
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- HY-P1626
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Acetyl tetrapeptide-15
|
Opioid Receptor
|
Neurological Disease
|
Acetyl tetrapeptide-15 is a synthetic peptide used in the cosmetics for sensitive skin. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioid receptor via an endorphin-like pathway.
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- HY-147082
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GA-017
|
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.
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- HY-113410
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3-Methylglutaric acid
|
Endogenous Metabolite
|
Metabolic Disease
|
3-Methylglutaric acid, a leucine metabolite, is a conspicuous C6 dicarboxylic organic acid classically associated with two distinct leucine pathway enzyme deficiencies, 3-hydroxy-3-methylglutaryl CoA lyase (HMGCL) and 3-methylglutaconyl CoA hydratase (AUH).
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- HY-133558
-
VII-31
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
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-146483
-
Anti-Aβ agent 1A
|
Amyloid-β
|
Inflammation/Immunology
Neurological Disease
|
Anti-Aβ agent 1A (compound M15) has potent activity against amyloid-β. Anti-Aβ agent 1A possesses can significantly inhibit LPS-induced levels of IL-1β, IL-6 and TNF-α, and reduces the apoptosis of SH-SY5Y induced by H2O2 through mitochondria pathway. Anti-Aβ agent 1A possesses antioxidant, anti-inflammatory, anti-Aβ toxicity and neuroprotective activities. Anti-Aβ agent 1A can be used for researching Alzheimer’s disease (AD).
|
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- HY-115924
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CDK1-IN-1
|
CDK
|
Cancer
|
CDK1-IN-7 is a potent CDK1 inhibitor (CDK1/CycB IC50=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-7 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-7 is a potential targeted antitumor agent.
|
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- HY-131005
-
-
- HY-107408
-
SANT 2
|
Hedgehog
|
Cancer
|
SANT 2 is a potent antagonist of Hh-signaling pathway. Hedgehog (Hh) signaling plays an important role in cell signaling of embryonic development and adult tissue homeostasis. SANT 2 has the potential for the research of several malignancies including Gorlin syndrome (a disorder predisposing to basal cell carcinoma, medulloblastoma and rhabdomyosarcoma), prostate, pancreatic and breast cancers.
|
-
- HY-119720
-
-
- HY-112670
-
-
- HY-123548
-
ML148
|
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-142437
-
-
- HY-142433
-
-
- HY-135145
-
CB-103
|
Notch
|
Cancer
|
CB-103 is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. CB-103 has anti-tumor activity.
|
-
- HY-108277
-
Ginsenoside F5
|
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.
|
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- HY-146444
-
Anticancer agent 56
|
Apoptosis
ROS
Bcl-2 Family
Caspase
|
Cancer
|
Anticancer agent 56 (compound 4d) is a potent anti-cancer agent with drug-likeness properties, possessing anticancer activity against several cancer cell lines (IC50<3 μM). Anticancer agent 56 induces cell cycle arrest at G2/M phase and triggers mitochondrial apoptosis pathway. Anticancer agent 56 acts by accumulation of ROS, up regulation of BAX, down regulation of Bcl-2 and activation of caspases 3, 7, 9.
|
-
- HY-N0498
-
Nitidine chloride
|
Parasite
Apoptosis
STAT
Topoisomerase
ERK
FAK
p38 MAPK
NF-κB
|
Cancer
Inflammation/Immunology
|
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.
|
-
- HY-N0177
-
Diosgenin
|
STAT
|
Metabolic Disease
|
Diosgenin, a steroidal saponin, can inhibit STAT3 signaling pathway. Diosgenin is an exogenous activator of Pdia3/ERp57.
|
-
- HY-N1469
-
-
- HY-146709
-
-
- HY-N3188
-
Niloticin
|
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-145231
-
FGFR2-IN-2
|
FGFR
|
Cancer
|
FGFR2-IN-2 (Compound 38) is a selective FGFR2 inhibitor with IC50s of 389, 29, and 758 nM for FGFR1, FGFR2, and FGFR3, respectively.
|
-
- HY-N1382
-
Asperuloside
|
NO Synthase
|
Inflammation/Immunology
|
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-145826
-
-
- HY-101275
-
-
- HY-10412
-
-
- HY-12238
-
IWR-1
endo-IWR 1; IWR-1-endo
|
Wnt
|
Cancer
|
IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.
|
-
- HY-13324
-
Bardoxolone methyl
RTA 402; NSC 713200; CDDO Methyl ester
|
Keap1-Nrf2
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
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.
|
-
- HY-N6017
-
Bakkenolide A
|
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-145302
-
Mycobactin-IN-2
|
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-N2051
-
Zeylenone
|
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-W001174
-
-
- HY-W096600
-
2F-Peracetyl-Fucose
1,3,4-Tri-O-acetyl-2-deoxy-2-fluoro-L-fucopyranos
|
Others
|
Cancer
|
2F-Peracetyl-Fucose (1,3,4-Tri-O-acetyl-2-deoxy-2-fluoro-L-fucopyranos) acts as a potent fucosyltransferase (FUT) inhibitor.
|
-
- HY-N10227
-
-
- HY-A0293
-
Pyrvinium pamoate
Pyrvinium embonate
|
Wnt
|
Cancer
|
Pyrvinium pamoate is an FDA-approved antihelmintic drug that inhibits WNT pathway signaling.
|
-
- HY-108437
-
exo-IWR-1
|
Wnt
|
Cancer
Infection
|
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-142834
-
-
- HY-118933
-
Calpain Inhibitor VI
SJA6017
|
Proteasome
|
Others
|
Calpain Inhibitor VI (SJA6017) is a synthesized peptide aldehyde inhibitor of calpain. Calpain Inhibitor VI inhibits purified m-calpain with the IC50 of 80 nM. Calpain Inhibitor VI can be used for the research of cataract.
|
-
- HY-112914
-
-
- HY-131592
-
-
- HY-112108
-
Chitosan oligosaccharide
COS
|
AMPK
|
Cancer
Metabolic Disease
|
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.
|
-
- HY-N4202
-
-
- HY-145301
-
Mycobactin-IN-1
|
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-N1447
-
-
- HY-17602
-
Amcasertib
BBI503
|
Others
|
Cancer
|
Amcasertib (BBI503) is an orally active and small-molecule multi-kinase inhibitor. Amcasertib exhibits inhibitory activity against the NANOG and CD133 expression and cell viability in PC-9/GR cells. As an orally available cancer cell stemness kinase inhibitor with potential antineoplastic activity, it is currently being studied in phase I clinical trials in a number of cancers.
|
-
- HY-144708
-
-
- HY-13307
-
JK184
|
Hedgehog
|
Cancer
|
JK184 is a potent Hedgehog (Hh) pathway inhibitor with IC50 of 30 nM in mammalian cells.
|
-
- HY-13901
-
-
- HY-N10175
-
Berkeleyacetal C
|
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-121879
-
-
- HY-N1404
-
Sodium aescinate
|
NF-κB
|
Cancer
Inflammation/Immunology
|
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-142706
-
-
- HY-100538
-
DTP3
|
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-125168
-
-
- HY-128588
-
STAT3-IN-3
|
STAT
Apoptosis
|
Cancer
|
STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. STAT3-IN-3 induces apoptosis in breast cancer cells. STAT3-IN-3 acts as a promising mitochondria-targeting STAT3 inhibitor for cancer research.
|
-
- HY-132167
-
AZD5305
|
PARP
|
Cancer
|
AZD5305 is a potent, selective and oral active PARP inhibitor. AZD5305 is potent and efficacious in animal xenografts and PDX models.
|
-
- HY-110156
-
YZ9
|
Others
|
Cancer
|
Y29 is a potent PFKFB3 inhibitor with an IC50 of 0.183 µM, and acts as a competitive inhibitor against Fru-6-P with a Ki of 0.094 µM. Y29 also inhibits the HeLa cell growth with a GI50 of 2.7 µM.
|
-
- HY-101098
-
-
- HY-16587
-
Saridegib
IPI-926; Patidegib
|
Smo
|
Cancer
|
Saridegib is a potent and specific inhibitor of Smoothened (Smo), a key signaling transmembrane protein in the Hedgehog (Hh) pathway.
|
-
- HY-N0371
-
Pachymic acid
3-O-Acetyltumulosic acid
|
Akt
ERK
|
Cancer
|
Pachymic acid is a lanostrane-type triterpenoid from P. cocos. Pachymic acid inhibits Akt and ERK signaling pathways.
|
-
- HY-135899
-
SIRT7 inhibitor 97491
|
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-126390
-
(E/Z)-BCI
NSC 150117
|
Phosphatase
Apoptosis
|
Cancer
Inflammation/Immunology
|
(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-117997
-
UMB-32
|
Epigenetic Reader Domain
|
Cancer
|
UMB-32, a potent, selective BRD4 inhibitor, binds BRD4 with the Kd of 550 nM, and IC50 of 637 nM. UMB-32 also shows potency against TAF1, a bromodomain-containing transcription factor.
|
-
- HY-128923
-
SKF-34288 hydrochloride
3-Mercaptopicolinic acid hydrochloride
|
Others
|
Metabolic Disease
|
SKF-34288 hydrochloride (3-Mercaptopicolinic acid) is a phosphoenolpyruvate carboxykinase (PEPCK) inhibitor.
SKF-34288 hydrochloride is a potent hypoglycemic agent via inhibition of glucose synthesis through the specific inhibition of PEPCK in the gluconeogenesis pathway. SKF-34288 hydrochloride inhibits Asn metabolism and results in an increase in amino acids and amides.
|
-
- HY-18981
-
Decursin
(+)-Decursin
|
PKC
Apoptosis
|
Cancer
Inflammation/Immunology
|
Decursin ((+)-Decursin) is a cytotoxic agent and a potent protein kinase C activator from the Root of Angelica gigas. Decursin inhibits tumor growth, migration, and invasion in gastric cancer by down-regulating CXCR7 expression. Decursin inhibits the growth of HepG2 cells via Hippo/YAP signaling pathway.
|
-
- HY-135231
-
NL-1
|
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-126200
-
-
- HY-15412
-
HhAntag
|
Smo
|
Cancer
|
HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway.
|
-
- HY-146739
-
-
- HY-110077
-
API-1
|
Akt
Apoptosis
|
Cancer
|
API-1, a potent Akt/PKB inhibitor, binds to the PH domain and inhibits Akt membrane translocation. API-1 efficiently reduces the phosphorylation levels of Akt with an IC50 of ∼0.8 μM. API-1 is selective for PKB and does not inhibit the activation of PKC, and PKA. API-1 also induces apoptosis by synergizing with TNF-related apoptosis-inducing ligand (TRAIL).
|
-
- HY-119823
-
PGP-4008
|
P-glycoprotein
|
Cancer
|
PGP-4008 is a specific P-glycoprotein (Pgp) inhibitor. PGP-4008 inhibits tumor growth in a murine syngeneic Pgp-mediated multiple drug resistance (MDR) solid tumor model when given in combination with Doxorubicin.
|
-
- HY-N0651
-
Spinosin
|
Others
|
Neurological Disease
|
Spinosyn a C-glycoside flavonoid isolated from the seeds of Zizyphus jujube, with neuroprotective effects. Spinosin inhibits Aβ1-42 production and aggregation via activating Nrf2/HO-1 pathway.
|
-
- HY-15735
-
c-Met inhibitor 1
|
c-Met/HGFR
|
Cancer
|
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.
|
-
- HY-103269
-
BAI1
|
Bcl-2 Family
Apoptosis
|
Cancer
|
BAI1 is a selective and allosteric inhibitor of BAX, an apoptosis regulator. BAI1 directly binds to BAX and allosterically inhibits BAX activation. BAI1 has the potential for the research of diseases mediated by BAX-dependent cell death.
|
-
- HY-46568
-
CDK7/12-IN-1
|
CDK
|
Cancer
|
CDK7/12-IN-1 is a selective CDK7/12 inhibitor with IC50s of 3 and 277 nM for CDK7 and CDK 12, respectively. CDK7 and CDK12 inhibition is an effective strategy to inhibit tumour growth.
|
-
- HY-N1745
-
-
- HY-129390
-
Orelabrutinib
ICP-022
|
Btk
|
Cancer
|
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.
|
-
- HY-N0486
-
-
- HY-122098
-
-
- HY-N3354
-
Lupiwighteone
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-N0366
-
Sennoside B
|
PDGFR
|
Cancer
|
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-125666
-
-
- HY-144700
-
-
- HY-16343
-
NB-598
|
Others
|
Metabolic Disease
|
NB-598 is a potent and competitive inhibitor of squalene epoxidase (SE), and suppresses triglyceride biosynthesis through the farnesol pathway.
|
-
- HY-16343C
-
NB-598 Maleate
|
Others
|
Metabolic Disease
|
NB-598 Maleate is a potent and competitive inhibitor of squalene epoxidase (SE), and suppresses triglyceride biosynthesis through the farnesol pathway.
|
-
- HY-143535
-
HG122
|
Androgen Receptor
|
Cancer
|
HG122 promotes androgen receptor (AR) degradation through the proteasome pathway inhibiting the castration-resistant prostate cancer.
|
-
- HY-121118
-
-
- HY-16343A
-
-
- HY-17024
-
-
- HY-100960
-
Dioctanoylglycol
Ethylene glycol dicaprylate; Ethylene glycol dioctanoate; Ethylenedioctanoate
|
Others
|
Cardiovascular Disease
|
Dioctanoylglycol (Ethylene glycol dicaprylate), a diacylglycerol analog, is a diacylglycerol kinase (DGK) inhibitor (Ki of 58 μM).
|
-
- HY-136497
-
-
- HY-142922
-
BCR-ABL-IN-4
|
Bcr-Abl
|
Cancer
|
BCR-ABL-IN-4 is a BCR-ABL inhibitor with anticancer effects. BCR-ABL-IN-4 inhibits the cancer cell growth with IC50 values of 0.67 nM and 16 nM for K562 cells and BCR-ABL T315I transfected Ba/F3 cells, respectively (WO2021143927A1; compound 11).
|
-
- HY-N10234
-
-
- HY-146752
-
-
- HY-D1084
-
-
- HY-N2573A
-
Corydalmine hydrochloride
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-103381
-
NSC693868
|
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-116364
-
AZT triphosphate
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-N6843
-
Arnicolide D
|
Caspase
PI3K
Akt
mTOR
STAT
|
Cancer
|
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.
|
-
- HY-146367
-
VEGFR-2-IN-19
|
VEGFR
Apoptosis
ROS
|
Cancer
|
VEGFR-2-IN-19 (Compound 15b) is a potent VEGFR2 inhibitor. VEGFR-2-IN-19 induces cell apoptosis and increases intracellular reactive oxygen species level. VEGFR-2-IN-19 can be used as an anticancer agent.
|
-
- HY-142460
-
KRAS G12C inhibitor 28
|
Ras
|
Cancer
|
KRAS G12C inhibitor 28 is a KRAS G12C inhibitor with an IC50 of 57 nM. KRAS G12C inhibitor 28 has antitumor effects (WO2021113595A1; Example 1).
|
-
- HY-115880
-
KRAS G12D inhibitor 3
|
Ras
|
Cancer
|
KRAS G12D inhibitor 3 is a KRAS G12D inhibitor with an IC50 of <500 nM. KRAS G12D inhibitor 3 has antitumor effects (WO2022002102A1; compound 146).
|
-
- HY-115880A
-
KRAS G12D inhibitor 3 TFA
|
Ras
|
Cancer
|
KRAS G12D inhibitor 3 TFA is a KRAS G12D inhibitor with an IC50 of <500 nM. KRAS G12D inhibitor 3 TFA has antitumor effects (WO2022002102A1; compound 146).
|
-
- HY-145882
-
BOD-NH-NP
|
Others
|
Others
|
BOD-NH-NP is an activatable fluorescent probe for imaging endogenous nitric oxide via the eNOS enzymatic pathway.
|
-
- HY-N1423
-
-
- HY-N0479
-
Licarin B
(-)-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-10590
-
-
- HY-142458
-
-
- HY-142457
-
-
- HY-N0822
-
Shikonin
C.I. 75535; Isoarnebin 4
|
Chloride Channel
Pyruvate Kinase
NF-κB
TNF Receptor
HIV
|
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-144983
-
-
- HY-144980
-
-
- HY-N1346
-
Robinin
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
Robinin is present in flavonoid fraction of Vigna unguiculata leaf. Robinin inhibits upregulated expression of TLR2 and TLR4. Robinin ameliorates oxidized low density lipoprotein (Ox-LDL) induced inflammatory insult through TLR4/NF-κB pathway.
|
-
- HY-19373
-
-
- HY-N0791
-
Tectoridin
|
Estrogen Receptor/ERR
|
Cancer
|
Tectoridin is a isoflavone isolated from Maackia amurensis. Tectoridin is a phytoestrogen and activates estrogen and thyroid hormone receptors. Tectoridin exerts the estrogenic effects via ER-dependent genomic pathway and GPR30-dependent nongenomic pathway.
|
-
- HY-118160
-
PPM-18
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-N2573
-
Corydalmine
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-147007
-
β-catenin-IN-3
|
β-catenin
Wnt
|
Cancer
|
β-catenin-IN-3 (compound C2) is a potent and selective β-catenin inhibitor with a KD value of 54.96 nM. β-catenin-IN-3 acts by targeting a cryptic allosteric modulation site of β-catenin. β-catenin-IN-3 can significantly reduce viability of β-catenin-driven cancer cells.
|
-
- HY-101130
-
-
- HY-112181
-
KO-947
|
ERK
|
Cancer
|
KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential utility in MAPK pathway dysregulated tumors.
|
-
- HY-U00460
-
-
- HY-142967
-
TGFβ-IN-1
|
TGF-β Receptor
|
Cancer
|
TGFβ-IN-1 is an antitumor growth and metastasis agent through inhibiting the transforming growth factor‑β signaling pathway.
|
-
- HY-N2666
-
5α-Hydroxycostic acid
|
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-16274
-
Lapaquistat acetate
TAK-475
|
Others
|
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-122404
-
Xantocillin
Xanthocillin X
|
MEK
ERK
Autophagy
|
Cancer
|
Xantocillin (Xanthocillin X) is a marine agent extracted from Penicillium commune, induces autophagy through inhibition of the MEK/ERK pathway.
|
-
- HY-144985
-
-
- HY-N10198
-
-
- HY-19726
-
NSC59984
|
MDM-2/p53
|
Cancer
|
NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway. NSC59984 acts by targeting GOF-mutant p53 and stimulates p73 to restore the p53 pathway signaling.
|
-
- HY-116364A
-
AZT triphosphate TEA
3'-Azido-3'-deoxythymidine-5'-triphosphate TEA
|
HIV
DNA/RNA Synthesis
HBV
Reactive Oxygen Species
Apoptosis
|
Infection
|
AZT triphosphate TFA (3'-Azido-3'-deoxythymidine-5'-triphosphate TFA) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TFA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TFA also inhibits the DNA polymerase of HBV. AZT triphosphate TFA activates the mitochondria-mediated apoptosis pathway.
|
-
- HY-117930
-
Danicopan
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).
|
-
- HY-N2098
-
Obtusifolin
|
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-N0314
-
-
- HY-139397
-
TJ-M2010-5
|
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-12068
-
PI3K-IN-1
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-N10199
-
-
- HY-N7814
-
-
- HY-143431
-
Cdc7-IN-17
|
CDK
|
Cancer
|
Cdc7-IN-17 is a potent CDC7 inhibitor with an IC50 of <10 μM, extracted from patent WO2018217439A1. Cdc7-IN-17 can be used for cancer research.
|
-
- HY-N6002
-
3'-Hydroxypterostilbene
|
Apoptosis
Autophagy
|
Cancer
|
3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 µM for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the PI3K/Akt/mTOR/p70S6K, and p38MAPK pathways and activates the ERK1/2, JNK1/2 MAPK pathways.
|
-
- HY-145046
-
SOS1-IN-3
|
Ras
|
Cancer
|
SOS1-IN-3 is a potent SOS1 (son of sevenless homolog 1) inhibitor with an IC50 of 5 nM. SOS1-IN-3 has anticancer effects (WO2019122129A1; compound I-1).
|
-
- HY-126539
-
UBE2T/FANCL-IN-1
|
Others
|
Cancer
|
UBE2T/FANCL-IN-1 is a potent inhibitor of UBE2T/FANCL-mediated FANCD2 monoubiquitylation that sensitizes cells to the DNA cross-linking agent, Carboplatin.
|
-
- HY-146741
-
SDR-04
|
Epigenetic Reader Domain
|
Cancer
|
SDR-04 is a BET inhibitor and exhibits strong BRD4-BD1 affinity and inhibition activity. SDR-04 potently suppresses MV4;11 cancer cell line proliferation.
|
-
- HY-142853
-
-
- HY-142849
-
-
- HY-142467
-
-
- HY-N0255
-
alpha-Hederin
α-Hederin
|
Apoptosis
|
Others
|
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-100538A
-
DTP3 TFA
|
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-144690
-
-
- HY-136386
-
-
- HY-N4231
-
-
- HY-137454
-
-
- HY-100790
-
Ciliobrevin A
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-N10232
-
Agistatin E
|
Others
|
Infection
|
Agistatin E is a pyranacetal originally isolated from a Fusarium sp. that inhibits the cholesterol biosynthesis.
|
-
- HY-N10231
-
-
- HY-108356
-
NS3694
|
Apoptosis
|
Cancer
|
NS3694, a diarylurea compound, is an apoptosome inhibitor. NS3694 inhibits apoptosome formation and caspase activation.
|
-
- HY-117287
-
Deucravacitinib
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.
|
-
- HY-100534
-
IDE 2
|
TGF-beta/Smad
|
Others
|
IDE2 is a small molecule cell-permeable inducer of definitive endoderm formation in mouse and human embryonic stem cells (ESCs) by activating the TGF-βsignaling pathway.
|
-
- HY-103322
-
6-Bnz-cAMP sodium salt
|
PKA
|
|
6-Bnz-cAMP sodium salt is a cell-permeable cAMP analog. 6-Bnz-cAMP selectively activates cAMP-dependent PKA but not Epac signaling pathways.
|
-
- HY-N0636
-
Eriocitrin
|
Apoptosis
|
Cancer
|
Eriocitrin is a flavonoid isolated from lemon, which is a strong antioxidant agent. Eriocitrin could inhibit the proliferation of hepatocellular carcinoma cell lines by arresting cell cycle in S phase through up-regulation of p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating mitochondria-involved intrinsic signaling pathway.
|
-
- HY-112179
-
GSK180
|
Others
|
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-N7695
-
Physalin B
|
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-50868
-
Bafetinib
INNO-406; NS-187
|
Bcr-Abl
Src
Apoptosis
|
Cancer
|
Bafetinib is a potent and orally active Lyn/Bcr-Abl tyrosine kinase inhibitor. Bafetinib augments the activities of several proapoptotic Bcl-2 homology (BH)3-only proteins (Bim, Bad, Bmf and Bik) and induces apoptosis in Ph + leukemia cells via Bcl-2 family-regulated intrinsic apoptosis pathway.
|
-
- HY-50730
-
Asparagusic acid
|
Parasite
|
Infection
|
Asparagusic acid is a sulfur-containing flavor component produced by asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.
|
-
- HY-147513
-
AKT-IN-12
|
Akt
Apoptosis
|
Cancer
|
AKT-IN-12 (compound 3e) is a potent Akt kinase inhibitor with an IC50 value of 0.55 μM. AKT-IN-12 induces G0/G1 cell cycle arrest and apoptosis. AKT-IN-12 also inhibits p-AKT, p-ERK, and activates p-JNK, JNK. AKT-IN-12 can be used for researching leukemia.
|
-
- HY-N0486S11
-
-
- HY-136476G
-
Pt(II) protoporphyrin IX
|
Others
|
Others
|
Pt(II) protoporphyrin IX is a protoporphyrin IX. Protoporphyrin IX is a heterocyclic organic compound, which consists of four pyrrole rings, and is the final intermediate in the heme biosynthetic pathway.
|
-
- HY-N0486S4
-
-
- HY-N0486S
-
-
- HY-N0486S12
-
-
- HY-N0486S9
-
-
- HY-136476F
-
Cd(II) protoporphyrin IX
|
Others
|
Others
|
Cd(II) protoporphyrin IX is a protoporphyrin IX. Protoporphyrin IX is a heterocyclic organic compound, which consists of four pyrrole rings, and is the final intermediate in the heme biosynthetic pathway.
|
-
- HY-136476E
-
Cr(III) protoporphyrin IX
|
Others
|
Others
|
Cr(III) protoporphyrin IX is a protoporphyrin IX. Protoporphyrin IX is a heterocyclic organic compound, which consists of four pyrrole rings, and is the final intermediate in the heme biosynthetic pathway.
|
-
- HY-N6812
-
Karacoline
|
Others
|
Endocrinology
|
Karacoline, a diterpene alkaloid found in the plant Aconitum kusnezoffii, reduces degradation of the extracellular matrix (ECM) in intervertebral disc degeneration (IDD) via the NF-κB signaling pathway.
|
-
- HY-N0399
-
-
- HY-16776A
-
(2S,5S)-Censavudine
(2S,5S)-OBP-601; (2S,5S)-BMS-986001
|
HIV
|
Infection
|
(2S,5S)-Censavudine ((2S,5S)-OBP-601) is the (2S,5S)-enantiomer of Censavudine. Censavudine, a nucleoside reverse transcriptase inhibitor, is a potent HIV inhibitor.
|
-
- HY-119874
-
Alkannin
|
Ras
|
Cancer
Inflammation/Immunology
|
Alkannin is a potent and specific inhibitor of tumor-specific pyruvate kinase-M2 (PKM2). Alkannin does not inhibit PKM1 and pyruvate kinase-L (PKL). Alkannin acts as a potential anticancer agent.
|
-
- HY-W012037
-
8-Hydroxyquinoline hemisulfate
8-Quinolinol hemisulfate
|
Bacterial
Antibiotic
|
Infection
|
8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
|
-
- HY-113618A
-
RO2959 hydrochloride
|
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-115497
-
BRD5529
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
BRD5529 is a selective CARD9-E3 ubiquitin ligase TRIM62 protein-protein interaction inhibitor with an IC50 of 8.6 μM. BRD5529 directly and selectively binds CARD9, disrupts TRIM62 recruitment, inhibits TRIM62-mediated ubiquitinylation and activation of CARD9, and demonstrates cellular activity and selectivity in CARD9-dependent pathways.
|
-
- HY-144681
-
LY3372689
|
Others
|
Neurological Disease
|
LY3372689 is an orally active O-GlcNAcase (OGA) enzyme inhibitor. LY3372689 can be used for tauopathies research, including Alzheimer’s disease.
|
-
- HY-N6673
-
-
- HY-N2281
-
-
- HY-N1423S1
-
Glycocholic acid-d5
|
Endogenous Metabolite
|
Cancer
|
Glycocholic acid-d5 is the deuterium labeled Glycocholic acid. Glycocholic acid is a bile acid with anticancer activity, targeting against pump resistance-related and non-pump resistance-related pathways.
|
-
- HY-N0901
-
Corynoxine
|
Autophagy
|
Cancer
Neurological Disease
|
Corynoxine, a tetracyclic oxindole alkaloid, is isolated from the hooks of Uncaria macrophylla. Corynoxine is a natural autophagy enhancer that promotes the clearance of alpha-synuclein via Akt/mTOR pathway.
|
-
- HY-P3255
-
-
- HY-N0432
-
Astragaloside I
Astrasieversianin IV; Cyclosieversioside B
|
Wnt
β-catenin
|
Metabolic Disease
|
Astragaloside I, one of the main active ingredients in Astragalus membranaceus, has osteogenic properties. Astragaloside I stimulates osteoblast differentiation through the Wnt/β-catenin signaling pathway.
|
-
- HY-N0901B
-
Corynoxine hydrochloride
|
Autophagy
|
Cancer
Neurological Disease
|
Corynoxine hydrochloride, a tetracyclic oxindole alkaloid, is isolated from the hooks of Uncaria macrophylla. Corynoxine hydrochloride is a natural autophagy enhancer that promotes the clearance of alpha-synuclein via Akt/mTOR pathway.
|
-
- HY-112412
-
PDGFR Tyrosine Kinase Inhibitor III
PDGF Receptor Tyrosine Kinase Inhibitor III
|
PDGFR
|
Neurological Disease
|
PDGFR Tyrosine Kinase Inhibitor III (PDGF Receptor Tyrosine Kinase Inhibitor III), a multikinase inhibitor, inhibits PDGFR, EGFR, FGFR, PKA, and PKC, respectively. PDGFR Tyrosine Kinase Inhibitor III can be used for the research of amyotrophic lateral sclerosis.
|
-
- HY-143437
-
TNIK-IN-5
|
Wnt
|
Cancer
|
TNIK-IN-5 is an efficient TNIK inhibitor with IC50 of 0.05 μM. TNIK-IN-5 efficiently inhibits Wnt signaling in intact cells. TNIK-IN-5 shows excellent in vitro anti-colorectal cancer activity.
|
-
- HY-138558
-
-
- HY-N0436
-
Engeletin
|
NF-κB
|
Infection
Inflammation/Immunology
|
Engeletin is a flavanonol glycoside isolated from hymenaea martiana, inhibits NF-κB signaling-pathway activation, and possesses anti-inflammatory, analgesic, diuresis, detumescence, and antibiosis effects.
|
-
- HY-139844
-
-
- HY-N0587
-
Demethylzeylasteral
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
Demethylzeylasteral is a triterpene compound isolated from Tripterygium wilfordii Hook F, with anti-inflammatory, immunosuppressive and anti-tumor activities. Demethylzeylasteral can significantly alleviates atherosclerosis (AS). Demethylzeylasteral inhibits triple-negative breast cancer invasion by blocking the canonical and non-canonical TGF-β signaling pathways.
|
-
- HY-144778
-
-
- HY-116035
-
Nimbolide
|
NF-κB
CDK
Apoptosis
|
Cancer
|
Nimbolide is a triterpene derived from the leaves and flowers of neem (Azadirachta indica L). Nimbolide induces apoptosis through inactivation of NF-κB. Nimbolide inhibits CDK4/CDK6 kinase activity. Nimbolide suppresses the NF-κB, Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways.
|
-
- HY-14621
-
Zingerone
Vanillylacetone; Gingerone
|
NF-κB
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
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-143471
-
PLK1/BRD4-IN-1
|
Polo-like Kinase (PLK)
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
PLK1/BRD4-IN-1 (9b) is an orally active dual PLK1 and BRD4 inhibitor with IC50 values of 22 nM and 109 nM against PLK1 and BRD4, respectively. PLK1/BRD4-IN-1 induces cell cycle arrest and apoptosis, downregulates the transcription of several proliferation-related oncogenes, and exhibits favorable in vivo antitumor activity.
|
-
- HY-15609
-
-
- HY-N6684
-
Deoxynivalenol
|
Others
|
Metabolic Disease
|
Deoxynivalenol, a 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-143475
-
POP-IN-2
|
Others
|
Cancer
Neurological Disease
|
POP-IN-2 (Compound 7k) is a potent, covalent prolyl oligopeptidase (POP) inhibitor with a Ki of 6 nM. POP-IN-2 can be used for studying neurodegenerative diseases and cancer.
|
-
- HY-143474
-
Y-29794
|
Others
|
Cancer
Neurological Disease
|
Y-29794 (Compound 2) is a potent, covalent prolyl oligopeptidase (POP) inhibitor with a Ki of 0.95 nM. Y-29794 can be used for studying neurodegenerative diseases and cancer.
|
-
- HY-144292
-
HDAC-IN-30
|
HDAC
|
Cancer
|
HDAC-IN-30 is a novel multi-target HDAC inhibitor, including HDAC1 (IC50=13.4 nM),HDAC2 (IC50=28.0 nM), HDAC3 (IC50=9.18 nM), HDAC6 (IC50=42.7 nM), HDAC8 (IC50=131 nM). HDAC-IN-30 exhibits potent antitumor efficacy.
|
-
- HY-101144
-
RSM-932A
TCD-717
|
Others
|
Cancer
|
RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC50s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles.
|
-
- HY-N7029
-
3',4',5',5,7-Pentamethoxyflavone
|
Others
|
Cancer
|
3',4',5',5,7-Pentamethoxyflavone, a natural flavonoid extracted from Rutaceae plants, sensitizes chemoresistant cancer cells to chemotherapeutic drugs by inhibition of Nrf2 pathway.
|
-
- HY-142687
-
-
- HY-108607
-
PACOCF3
Palmityltrifluoromethylketone
|
Phospholipase
|
Inflammation/Immunology
|
PACOCF3 (Palmityltrifluoromethylketone) is a selective phospholipase A2 inhibitor with an IC50 of 3.8 μM. PACOCF3 alters Ca 2+ signaling in renal tubular cells.
|
-
- HY-101364A
-
CHPG sodium salt
|
mGluR
NF-κB
ERK
Akt
|
Inflammation/Immunology
Neurological Disease
|
CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways..
|
-
- HY-101364
-
CHPG
|
mGluR
NF-κB
ERK
Akt
|
Inflammation/Immunology
Cardiovascular Disease
|
CHPG is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways.
|
-
- HY-15672
-
FM19G11
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
Neurological Disease
|
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-103645
-
GW779439X
|
Bacterial
Aurora Kinase
Apoptosis
|
Cancer
Infection
|
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-113618B
-
RO2959 monohydrochloride
|
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-14373
-
CB30865
ZM 242421
|
NAMPT
|
Cancer
|
CB30865 (ZM 242421) is a nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with potent cytotoxicity. CB30865 is highly potent against a variety of human tumour cell lines (IC50 values in the 1-10 nM range).
|
-
- HY-132168
-
RMC-5552
|
mTOR
|
Cancer
|
RMC-5552 is a potent and selective inhibitor of mTORC1. RMC-5552 inhibits phosphorylation of mTORC1 pS6K and p4EBP1 with IC50s of 0.14 nM and 0.48 nM, respectively. RMC-5552 has anti-cancer activity.
|
-
- HY-108623
-
-
- HY-N0298
-
-
- HY-141807
-
MS21
|
PROTACs
|
Cancer
|
MS21, a novel degrader of AKT, selectively inhibits the growth of PI3K/PTEN pathway-mutant cancers with wild-type KRAS and BRAF.
|
-
- HY-N2877
-
-
- HY-128606
-
-
- HY-N5134
-
5'-Guanylic acid
5'-GMP; 5'-guanosine monophosphate
|
Endogenous Metabolite
|
Metabolic Disease
|
5'-Guanylic acid (5'-GMP) is involved in several metabolic disorders, including the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and the 2-hydroxyglutric aciduria pathway.
|
-
- HY-N0486S1
-
-
- HY-107818
-
4-Hydroxychalcone
|
NF-κB
|
Inflammation/Immunology
Cardiovascular Disease
|
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-101776
-
Desmethyl-VS-5584
Desmethyl-SB2343
|
mTOR
PI3K
|
Cancer
|
Desmethyl-VS-5584 is a dimethyl analog of VS-5584 which is an potent and selective mTOR/PI3K dual inhibitor with pyrido [2,3-d] pyrimidine structure.
|
-
- HY-145289
-
Antitumor agent-37
|
Apoptosis
|
Cancer
|
Antitumor agent-37 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-37 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-37 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-37 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues.
|
-
- HY-145288
-
Antitumor agent-36
|
Apoptosis
|
Cancer
|
Antitumor agent-36 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-36 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-36 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-36 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues.
|
-
- HY-B1247
-
-
- HY-W001171
-
-
- HY-N2460
-
Aloesin
Aloeresin
|
Others
|
Cancer
Inflammation/Immunology
|
Aloesin (Aloeresin) is an active constituent of the herb aloe vera and displays anti-inflammatory activity, ultraviolet protection, and antibacterium effects. Aloesin exerts its anticancer effect through the MAPK signaling pathway.
|
-
- HY-N1472
-
Levistolide A
|
Apoptosis
|
Cancer
|
Levistolide A (LA), a natural compound isolated from the traditional Chinese herb Ligusticum chuanxiong Hort, is used for treating cancer. Levistolide A can induce apoptosis via ROS-mediated ER stress pathway.
|
-
- HY-130239
-
14(S)-HDHA
14(S)-HDoHE
|
Drug Metabolite
|
Neurological Disease
|
14(S)-HDHA (14(S)-HDoHE) is an oxygenation product of Docosahexaenoic acid (DHA). 14(S)-HDHA is a marker reflecting activation of a Docosahexaenoic acid carbon 14-lipoxygenation pathway.
|
-
- HY-N6826
-
Asatone
|
NF-κB
|
Inflammation/Immunology
|
Asatone is an active component isolated from Radix et Rhizoma Asari, with anti-inflammatory effect via activation of NF-κB and donwn regulation of p-MAPK (ERK, JNK and p38) pathways.
|
-
- HY-N0486S5
-
-
- HY-N2005
-
-
- HY-119989
-
Cyclopyrimorate
|
Others
|
Infection
|
Cyclopyrimorate, a highly effective bleaching herbicide for weed control in rice fields, targets homogentisate solanesyltransferase (HST). HST is a downstream enzyme of 4-hydroxyphenylpyruvate dioxygenase in the plastoquinone (PQ) biosynthesis pathway.
|
-
- HY-N0486S3
-
-
- HY-50289
-
Sorbinil
|
Aldose Reductase
|
Metabolic Disease
|
Sorbinil, is an Aldose reductase inhibitor (ARI).
Sorbinil plays therapeutic role in treating diabetes and diabetic complications, decreases AR activity and inhibits polyol pathway, it to be found comparatively safer than other ARIs for human use.
|
-
- HY-N2523
-
Gigantol
|
Wnt
|
Cancer
|
Gigantol is a bibenzyl compound derived from several medicinal orchids. Giganto shows promising therapeutic potential against cancer cells. Gigantol is a novel inhibitor of the Wnt/β-catenin pathway.
|
-
- HY-144882
-
-
- HY-130702
-
-
- HY-103663A
-
MAK683 hydrochloride
|
Histone Methyltransferase
|
Cancer
|
MAK683 hydrochloride is an embryonic ectoderm development (EED) inhibitor extracted from patent US20160176882 A1, compound example 2. MAK683 exhibits IC50s of 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay.
|
-
- HY-119046
-
SNX-0723
|
HSP
Parasite
|
Infection
|
SNX-0723 is a potent Hsp90 Inhibitor with anti-Plasmodium activity. SNX-0723 shows high binding affinity for HsHsp90 and PfHsp90 with Kis of 4.4 and 47 nM, respectively. SNX-0723 inhibits liver-stage P. berghei ANKA parasites with the EC50 of 3.3 μM.
|
-
- HY-136521
-
AZ13824374
|
Epigenetic Reader Domain
|
Cancer
|
AZ13824374 is a highly potent and selective ATAD2 bromodomain inhibitor which shows cellular target engagement and antiproliferative activity in a range of breast cancer models. AZ13824374 inhibits ATAD2 with pIC50s of 8.2 and 6.2 in ATAD2 FRET assay and ATAD2 NanoBRET assay, respectively.
|
-
- HY-N7126
-
Citronellal
|
Others
|
Neurological Disease
|
Citronellal is a monoterpenea from the essential oils in various aromatic species of plants, with depressant, and antinociceptive properties. Citronellal attenuates mechanical nociception, mediated in part by the NO-cGMP-ATP-sensitive K ⁺ channel pathway.
|
-
- HY-B0141
-
-
- HY-N6012
-
(-)-Alkannin
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
(-)-Alkannin, found in Alkanna tinctoria, is used as a food coloring. (-)-Alkannin shows anticancer activity, arrests cell cycle, and induces apoptosis. (-)-Alkannin improves hepatic inflammation in a Rho-kinase pathway.
|
-
- HY-N0486S10
-
-
- HY-N0819
-
Raddeanin A
|
Apoptosis
|
Cancer
|
Raddeanin A is a natural triterpenoid saponin component of Anemone raddeana, with anti-cancer activities. Raddeanin A exerts anticancer effect on human osteosarcoma via the ROS/JNK and NF-κB signal pathway.
|
-
- HY-113509
-
Lipoxin A4
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-145159
-
-
- HY-144824
-
-
- HY-N7674A
-
Angoline hydrochloride
|
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-N7674
-
Angoline
|
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-N1098
-
Velutin
|
Others
|
Inflammation/Immunology
|
Velutin is an aglycone extracted from Korean Mistletoe, with inhibitory activity against melanin biosynthesis. Velutin reduces osteoclast differentiation and down-regulates HIF-1α through the NF-κB pathway.
|
-
- HY-N2031
-
Parishin
|
Others
|
Neurological Disease
|
Parishin is a phenolic glucoside isolated from Gastrodia elata. Parishin exhibits antiaging effects and extends the lifespan of yeast via regulation of Sir2/Uth1/TOR signaling pathway.
|
-
- HY-N8773
-
3,5,7-Trihydroxychromone
|
Others
|
Others
|
3,5,7-Trihydroxychromone is the analogue of galangin. 3,5,7-Trihydroxychromone is also the binder of bovine serum albumin. 3,5,7-Trihydroxychromone undergoes multiple antioxidant pathways.
|
-
- HY-N0008
-
Orcinol glucoside
|
Others
|
Neurological Disease
|
Orcinol glucoside (OG) is an active constituent isolated from Rhizoma Curculiginis, with antidepressant effects. Orcinol glucoside facilitates the shift of MSC fate to osteoblast and prevents adipogenesis via Wnt/β-catenin signaling pathway.
|
-
- HY-P1784
-
Secretin, canine
|
Src
|
Endocrinology
|
Secretin, canine is an endocrine hormone that stimulates the secretion of bicarbonate-rich pancreatic fluids. Secretin, canine can regulates gastric chief cell function and paracellular permeability in canine gastric monolayers by a Src kinase-dependent pathway.
|
-
- HY-18770B
-
-
- HY-143872
-
Bcl-2-IN-4
|
Bcl-2 Family
|
Cancer
|
Bcl-2-IN-4 is a potent, orally active and selective Bcl-2 inhibitor with an IC50 of 1.5 nM. Bcl-2-IN-4 displays >200-fold selectivity over Bcl-xL (IC50 of 411 nM). Bcl-2-IN-4 inhibits RS4; 11 cell proliferation with an IC50 of 2.7 nM (WO2021180040A1; compound 2).
|
-
- HY-144031S
-
Tyk2-IN-8
|
JAK
|
Inflammation/Immunology
|
Tyk2-IN-8 (Compound 3) is a selective Tyk-2 inhibitor with an IC50 of 5.7 nM for TYK2-JH2. Tyk2-IN-8 inhibits JAK1-JH1 with IC50 of 3.0 nM. Tyk2-IN-8 can be used for the research of autoimmune disease.
|
-
- HY-113439
-
12-HETE
|
Apoptosis
|
Inflammation/Immunology
Cardiovascular Disease
|
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-W017212
-
Methyl cinnamate
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-W009776
-
Suberoyl bis-hydroxamic acid
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-14664CS
-
(3S,5R)-Fluvastatin D6 sodium
(3S,5R)-XU 62-320 D6
|
HMG-CoA Reductase (HMGCR)
|
Cancer
Cardiovascular Disease
|
(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.
|
-
- HY-142031
-
-
- HY-105349
-
T-0156
|
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-116804
-
ZLD1039
|
Histone Methyltransferase
|
Cancer
|
ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis.
|
-
- HY-N0279
-
-
- HY-B0863S
-
Glyphosate-d2
|
Apoptosis
Autophagy
|
|
Glyphosate-d2 is the deuterium labeled Glyphosate. Glyphosate is an herbicidal derivative of the amino acid glycine. Glyphosate targets and blocks a plant metabolic pathway not found in animals, the shikimate pathway, required for the synthesis of aromatic amino acids in plants.
|
-
- HY-N10106
-
-
- HY-N2135
-
-
- HY-N4019
-
Maohuoside A
|
TGF-β Receptor
|
Metabolic Disease
|
Maohuoside A, a single compound isolated from the E. koreanum that potently promotes osteogenesis. Maohuoside A enhances the osteogenesis of bone marrow-derived mesenchymal stem cells via bone morphogenetic protein (BMP) and MAPK signaling pathways.
|
-
- HY-137443
-
Ipivivint
|
CDK
Wnt
|
Cancer
|
Ipivivint (compound 38) is a 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-108441
-
CCT031374 hydrobromide
|
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-10440
-
Vismodegib
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-144032
-
Tyk2-IN-9
|
JAK
|
Inflammation/Immunology
|
Tyk2-IN-9 (Compound 26) is a selective Tyk-2 inhibitor with IC50s of 0.076 and 1.8 nM for TYK2-JH2 and JAK1-JH2, respectively. Tyk2-IN-9 can be used for the research of inflammatory or autoimmune disease.
|
-
- HY-135813
-
LtaS-IN-1
|
Bacterial
|
Infection
|
LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
|
-
- HY-144264
-
Human carbonic anhydrase II-IN-1
|
Carbonic Anhydrase
|
Endocrinology
|
Human carbonic anhydrase II-IN-1 (Compound S-13) is a potent human carbonic anhydrase II (hCA II) inhibitor with a Ki of 4.4 nM. Human carbonic anhydrase II-IN-1 also inhibits other hCAs isoforms I, IV and IX, with Ki values of 9.2 nM, 480.2 nM and 14.7 nM, respectively. Human carbonic anhydrase II-IN-1 can be used for glaucoma research.
|
-
- HY-144087
-
TYK2-IN-11
|
JAK
|
Inflammation/Immunology
|
TYK2-IN-11 (Compound 5B) is a selective Tyk-2 inhibitor with IC50s of 0.016 and 0.31 nM for TYK2-JH2 and JAK1-JH2, respectively. TYK2-IN-11 can be used for the research of inflammatory or autoimmune disease.
|
-
- HY-117726
-
-
- HY-14804A
-
Tasisulam sodium
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-N0738
-
-
- HY-14804
-
Tasisulam
LY 573636
|
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
-
-
- HY-N6794
-
10Z-Hymenialdisine
(Z)-Hymenialdisine; Hymenialdisine
|
AMPK
VEGFR
PDGFR
|
Cancer
|
10Z-Hymenialdisine ((Z)-Hymenialdisine) is a natural bioactive pyrrole alkaloid. 10Z-Hymenialdisine is a pan kinase inhibitor, and has anticancer activities.
|
-
- HY-146137
-
-
- HY-113277
-
-
- HY-115576
-
-
- HY-N1419
-
Vaccarin
|
AMPK
|
Metabolic Disease
|
Vaccarin is an active flavonoid glycoside associated with various biological functions. Vaccarin significantly promote wound healing and endothelial cells and fibroblasts proliferation in the wound site. Vaccarin ameliorates insulin resistance and steatosis by activating the AMPK signaling pathway.
|
-
- HY-N0188
-
Esculin
|
p38 MAPK
|
Inflammation/Immunology
Cancer
|
Esculin, a fluorescent coumarin glucoside, is an active ingredient of ash bark. Esculin ameliorates cognitive impairment in experimental diabetic nephropathy (DN), and exerts anti‑oxidative stress and anti‑inflammatory effects, via the MAPK signaling pathway.
|
-
- HY-N0705
-
-
- HY-121827
-
LH21
|
Cannabinoid Receptor
|
Metabolic Disease
|
LH-21 is a potent in vivo neutral cannabinoid CB1 receptor antagonist. LH-21 reduces food intake and body weight gain in obese Zucker rats.
, and displays efficacy as a feeding inhibitor.
|
-
- HY-145809
-
-
- HY-143886
-
AD011
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
AD011 is a dual inhibitor of cACE/NEP. AD011 is synthesized based on the previously reported C-domain selective ACE inhibitor lisinopril-tryptophan. AD011 has the potential for providing the potent antihypertensive and cardioprotective benefits.
|
-
- HY-143888
-
AD013
|
Angiotensin-converting Enzyme (ACE)
|
Others
|
AD013 is a dual inhibitor of cACE/NEP. AD013 is synthesized based on the previously reported C-domain selective ACE inhibitor lisinopril-tryptophan. AD013 has the potential for providing the potent antihypertensive and cardioprotective benefits.
|
-
- HY-143887
-
AD012
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
AD012 is a dual inhibitor of cACE/NEP. AD012 is synthesized based on the previously reported C-domain selective ACE inhibitor lisinopril-tryptophan. AD012 has the potential for providing the potent antihypertensive and cardioprotective benefits.
|
-
- HY-N0883
-
Gamabufotalin
Gamabufagin
|
|
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-N2959
-
Brevilin A
|
JAK
STAT
Apoptosis
Autophagy
|
Cancer
|
Brevilin A is a sesquiterpene lactone isolated from Centipeda minima with anti-tumor activity. Brevilin A is a selective inhibitor of JAK-STAT signal pathway by attenuating the JAKs activity and blocking STAT3 signaling (IC50 = 10.6 µM) in Cancer Cells. Brevilin A induces apoptosis and autophagy via mitochondrial pathway and PI3K/AKT/mTOR inactivation in colon adenocarcinoma cell CT26.
|
-
- HY-146006
-
Tubulin/MMP-IN-1
|
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-N0265
-
Asperosaponin VI
|
Caspase
Apoptosis
|
Cardiovascular Disease
|
Asperosaponin VI, A saponin component from Dipsacus asper wall, 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-101918
-
DS-1040 Tosylate
|
Others
|
Cardiovascular Disease
|
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
|
-
- HY-113066
-
-
- HY-N0595
-
Genistin
Genistine; Genistoside; Genistein 7-O-β-D-glucopyranoside
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
Metabolic Disease
|
Genistin (Genistine), an isoflavone belonging to the phytoestrogen family, is a potent anti-adipogenic and anti-lipogenic agent. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of ERalpha signaling pathway.
|
-
- HY-B1287
-
Citalopram hydrobromide
(±)-Citalopram hydrobromide; Lu 10-171
|
Serotonin Transporter
Autophagy
|
Neurological Disease
Cancer
|
Citalopram hydrobromide is a selective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with an IC50 of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC50 of 14 nM. Antidepressant effect.
|
-
- HY-116934
-
5-Pentadecylresorcinol
Adipostatin A
|
Others
|
Cancer
Infection
|
5-Pentadecylresorcinol (Adipostatin A) is a glycerol-3-phosphate dehydrogenase (GPDH) inhibitor with an IC50 of 4.1 µM. Adipostatin A shows good larvicidal activity against Aedes aegypti.
|
-
- HY-115937
-
c-Met-IN-9
|
c-Met/HGFR
Apoptosis
|
Cancer
|
c-Met-IN-9, a 4-phenoxypyridine derivative, is a c-Met kinas inhibitor with an IC50 of 12 nM. c-Met-IN-9 induces cells apoptosis, and has antitumor activities.
|
-
- HY-16126
-
-
- HY-N3925
-
-
- HY-P2203A
-
SAHM1 TFA
|
Notch
|
|
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-119683
-
Epoxiconazole
|
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-15879
-
-
- HY-103358
-
KF38789
|
Others
|
Inflammation/Immunology
|
KF38789 is a selective inhibitor of P-selectin-PSGL-1 binding. KF38789 inhibits the binding of U937 cells to immobilized P-selectin immunoglobulin G chimeric protein (P-selectin-Ig) with an IC50 value of 1.97 μM.
|
-
- HY-N10332
-
Leptosphaerodione
|
Proteasome
|
Cancer
|
Leptosphaerodione, isolated from Remotididymella sp. Fungus, is a potent ubiquitin-proteasome system (UPS) inhibitor. Leptosphaerodione exhibits cytotoxicity in HeLa cells with IC50 value of 3.2 μM. Anti-tumor agent.
|
-
- HY-W006230
-
Anthraflavic acid
|
Others
|
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-141891
-
M435-1279
|
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-W012241
-
-
- HY-N10150
-
-
- HY-144870
-
STAT3-IN-7
|
STAT
|
Cancer
|
STAT3-IN-7, an aryl sulfonamido azetidine compound, is an orally active STAT3 inhibitor. STAT3-IN-7 has anticancer activities (WO2021016333A1, H182).
|
-
- HY-N0486S6
-
-
- HY-137864
-
Amifostine thiol
WR-1065
|
MDM-2/p53
|
Cancer
|
Amifostine thiol (WR-1065) is an active metabolite of the cytoprotector Amifostine (HY-B0639). Amifostine thiol is a cytoprotective agent with radioprotective abilities. Amifostine thiol activates p53 through a JNK-dependent signaling pathway.
|
-
- HY-113066A
-
-
- HY-N0486S8
-
-
- HY-131055
-
Mytoxin B
|
ADC Cytotoxin
PI3K
Apoptosis
|
Cancer
|
Mytoxin B is an ADC cytotoxin. Mytoxin B is a satratoxin-type trichothecene macrolide and is similar to the effect of LY294002 (HY-10108). Mytoxin B induces cell apoptosis via PI3K/Akt pathway.
|
-
- HY-N0486S7
-
-
- HY-144323
-
YF135
|
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-136310
-
PIP4K-IN-a131
|
Others
|
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-14664C
-
(3S,5R)-Fluvastatin sodium
(3S,5R)-XU 62-320
|
HMG-CoA Reductase (HMGCR)
|
Cancer
Cardiovascular Disease
|
(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-113976A
-
Endothall
Endothal
|
Phosphatase
|
|
Endothall (Endothal) is a protein phosphatase 2A (PP2A) inhibitor with IC50s of 90 nM and 5 µM for PP2A and PP1, respectively. Endothall can be used as an herbicide. Endothall also is useful in cancer chemotherapy.
|
-
- HY-115292
-
Simvastatin hydroxy acid sodium
Tenivastatin sodium; Simvastatin Impurity A sodium
|
HMG-CoA Reductase (HMGCR)
|
Cancer
|
Simvastatin hydroxy acid sodium (Tenivastatin sodium; Simvastatin Impurity A sodium) is an active hydrolytic metabolite of Simvastatin (HY-17502). Simvastatin shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM.
|
-
- HY-107550
-
HDAC6-IN-7
|
HDAC
|
Cancer
|
TCS HDAC6 20b is a HDAC6-selective inhibitor. TCS HDAC6 20b blocks the growth of estrogen receptor α-positive breast cancer MCF-7 cells.
|
-
- HY-N0637
-
-
- HY-B1468
-
-
- HY-144448
-
FAK-IN-2
|
FAK
Apoptosis
|
Cancer
|
FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC50= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis.
|
-
- HY-N5001
-
Euphorbia Factor L2
|
Apoptosis
|
Cancer
|
Euphorbia factor L2, a lathyrane diterpenoid isolated from caper euphorbia seed (the seeds of Euphorbia lathyris L.), has been traditionally applied to treat cancer. Euphorbia factor L2 shows potent cytotoxicity and induces apoptosis via a mitochondrial pathway.
|
-
- HY-120696
-
SR9186
ML368
|
Cytochrome P450
Parasite
|
Infection
|
SR9186 (ML368) is a potent CYP3A4 inhibitor with IC50 s for inhibition of midazolam → 1′hydroxymidazolam, testosterone → 6β-hydroxytestosterone, and vincristine → vincristine M1 of 9, 4, and 38 nM, respectively. SR-9186 inhibits liver-stage development of P. falciparum to block ivermectin metabolism.
|
-
- HY-13675
-
ME-143
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-131710
-
PDE5-IN-3
|
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-108464A
-
Phenamil methanesulfonate
|
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.
|
-
- HY-119425
-
Razoxane
ICRF 159
|
Topoisomerase
|
Cancer
|
Razoxane (ICRF 159) is an antiangiogenic topoisomerase II inhibitor, can be used for the research of renal cell carcinoma (RCC).
|
-
- HY-N6577
-
-
- HY-113071
-
-
- HY-N0130
-
-
- HY-14664AS
-
-
- HY-B0141S2
-
Estradiol-d5
β-Estradiol-d5; 17β-Estradiol-d5; 17β-Oestradiol-d5
|
Estrogen Receptor/ERR
Endogenous Metabolite
|
Endocrinology
Cancer
|
Estradiol-d5 is deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
|
-
- HY-N7108
-
7-Hydroxyflavone
|
Others
|
Inflammation/Immunology
|
7-Hydroxyflavone is a flavonoid isolated from M. indica, with anti-inflammatory activity. 7-Hydroxyflavone protects renal cells from nicotine (NIC)-associated cytotoxicity via the ERK/Nrf2/HO-1 pathway.
|
-
- HY-N2375
-
L-Quebrachitol
|
Wnt
β-catenin
|
Metabolic Disease
|
L-Quebrachitol is a natural product isolated from many plants, promotes osteoblastogenesis by uppregulation of BMP-2, runt-related transcription factor-2 (Runx2), MAPK (ERK, JNK, p38α), and Wnt/β-catenin signaling pathway.
|
-
- HY-145373
-
BMS-986143
|
Btk
|
Inflammation/Immunology
|
BMS-986143 is an orally active, reversible BTK inhibitor with an IC50 of 0.26 nM. BMS-986143 also inhibits TEC, BLK, BMX, TXK FGR, YES1, ITK with IC50s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM,19 nM, 21 nM, respectively. BMS-986143 can be used for the research of autoimmune diseases.
|
-
- HY-12170
-
Prinomastat
AG3340; KB-R9896
|
MMP
Apoptosis
|
Cancer
|
Prinomastat (AG3340) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat crosses blood-brain barrier. Antitumor avtivity.
|
-
- HY-12170A
-
Prinomastat hydrochloride
AG3340 hydrochloride; KB-R9896 hydrochloride
|
MMP
Apoptosis
|
Cancer
|
Prinomastat hydrochloride (AG3340 hydrochloride) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat hydrochloride inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat hydrochloride can cross blood-brain barrier. Antitumor avtivity.
|
-
- HY-18728
-
-
- HY-100711
-
-
- HY-145953
-
VY-3-135
|
Others
|
Cancer
|
VY-3-135 is a potent, orally active, and stable ACSS2 inhibitor with an IC50 value of 44 nM. VY-3-135 is specific to ACSS2 among the AcCoA synthetase family of enzymes. VY-3-135 does not inhibit ACSS1 or ACSS3 enzymatic activity. VY-3-135 can be used for the research of breast cancer.
|
-
- HY-142680
-
EGFR-IN-23
|
EGFR
|
Cancer
|
EGFR-IN-23 is a potent EGFR TKI (tyrosine kinase inhibitor) with an IC50 of 8.05 nM for BaF3/EGFR-DEL19/T790M/C797S cell (WO2021244502A1, compound 8).
|
-
- HY-144102
-
HDAC-IN-29
|
HDAC
|
Cancer
|
HDAC-IN-29 (compound 13b) is a potent pan-HDAC inhibitor. HDAC-IN-29 shows antitumor activity.
|
-
- HY-N1231
-
Sophoraflavanone G
Kushenol F
|
Apoptosis
|
Cancer
|
Sophoraflavanone G (Kushenol F) is iaolated from Sophora flavescens and shows anti-tumor and anti-inflammatory properties. Sophoraflavanone G (Kushenol F) induces MDA-MB-231 and HL-60 cells apoptosis through suppression of MAPK-related pathways.
|
-
- HY-115768
-
Compound 48/80
Poly-p-methoxyphenethylmethylamine
|
Others
|
Cancer
Neurological Disease
|
Compound 48/80 (Poly-p-methoxyphenethylmethylamine) is widely used in animal and tissue models as a "selective" mast cell activator. Compound 48/80 acts at the mast cell membrane to stimulate trimeric G-proteins and induces degranulation via phospholipase C and D pathways.
|
-
- HY-113071A
-
-
- HY-119751
-
Hematein
|
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-N0158
-
Oxymatrine
|
TGF-beta/Smad
Influenza Virus
|
Cancer
Infection
Inflammation/Immunology
|
Oxymatrine, an alkaloid from the roots of Sophora species, 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-N1778
-
-
- HY-146047
-
Antibacterial agent 94
|
Bacterial
|
Infection
|
Antibacterial agent 94 (compound 5b) is a potent antibacterial agent. Antibacterial agent 94 show antibacterial activities and show the capability of eradicating MRSA persisters. Antibacterial agent 94 has an effect on bacterial membrane. Antibacterial agent 94 interferes in phosphatidylglycerol (PG) synthesis pathway.
|
-
- HY-B0141S6
-
-
- HY-N1778A
-
-
- HY-13676
-
Megestrol acetate
|
Progesterone Receptor
Autophagy
HIV
|
Endocrinology
Cancer
|
Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway.
|
-
- HY-147538
-
Antitumor agent-64
|
Apoptosis
|
Cancer
|
Antitumor agent-64 (Compound 8d) is a diosgenin derivative. Antitumor agent-64 exhibits potent cytotoxic activity against A549 cell line. Antitumor agent-64 induces A549 cells apoptosis via the mitochondria-related pathway.
|
-
- HY-N2110
-
Phellopterin
|
Others
|
Inflammation/Immunology
|
Phellopterin is a natural product isolated from P. trifoliata. 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-111364
-
Roy-Bz
|
PKC
|
Cancer
|
Roy-Bz is a selecive PKCδ activator. Roy-Bz potently inhibits the proliferation of colon cancer cells by inducing a PKCδ-dependent mitochondrial apoptotic pathway involving caspase-3 activation.
|
-
- HY-N0020
-
Echinacoside
|
Wnt
Reactive Oxygen Species
|
Neurological Disease
|
Echinacoside, one of the phenylethanoids isolated from the stems of Cistanche salsa, effectively inhibits Wnt/β-catenin signaling. Echinacoside elicits neuroprotection by activating Trk receptors and their downstream signal pathways. Antiosteoporotic activity.
|
-
- HY-N8102
-
-
- HY-15880
-
CCT007093
|
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-D0961
-
Gallocyanine chloride
|
Wnt
|
Neurological Disease
|
Gallocyanine chloride, a synthetic blue dyestuff, blocks DKK1 inhibitory activity by disrupting DKK1/LRP6 interaction. Its association with LRP6 is weak (IC50 of about 3 μM in the inhibition of DKK1 binding). Gallocyanine dye acts as a potential agent for the research of Alzheimer's disease and related neurodegenerative tauopathies.
|
-
- HY-115734
-
Phenylpyropene C
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-144706
-
Axl-IN-3
|
TAM Receptor
|
Cancer
|
Axl-IN-3 is a potent, selective and orally active AXL kinase inhibitor with an IC50 of 41.5 nM. Axl-IN-3 has lower inhibition of other kinases.
|
-
- HY-117102
-
ANI-7
|
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-N3316
-
Martynoside
|
Others
|
|
Martynoside protects ex vivo bone marrow cells from 5-fluorouracil (5-FU)-induced cell death and inflammation response by down-regulating the TNF signaling pathway.Martynoside is a potent antiestrogen in MCF-7 cells, increasing IGFBP3 levels
|
-
- HY-N2180
-
Pinoresinol dimethyl ether
(+)-Eudesmin
|
Others
|
Neurological Disease
|
Pinoresinol dimethyl ether ((+)-Eudesmin) is a non-phenolic furofuran lignan isolated from the stem bark of Magnolia kobus with neuritogenic activity. Pinoresinol dimethyl ether ((+)-Eudesmin) can induce neuritis outgrowth from PC12 cells by stimulating up-stream MAPK, PKC and PKA pathways.
|
-
- HY-120290
-
PU141
|
Histone Acetyltransferase
|
Cancer
|
PU141 is a selected pyridoisothiazolone HAT inhibitor. PU141 is selective toward CBP and p300. PU141 induces cellular histone hypoacetylation and inhibits growth of several neoplastic cell lines originating from different tissues. Anticancer activity.
|
-
- HY-100236
-
Madrasin
DDD00107587
|
Others
|
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
-
Demethyleneberberine
|
NF-κB
AMPK
|
Metabolic Disease
Inflammation/Immunology
|
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-117651
-
2-Fluoropalmitic acid
|
Acyltransferase
|
Cancer
|
2-Fluoropalmitic acid, an acyl-CoA synthetase inhibitor, acts as a candidate anti-glioma agent. 2-Fluoropalmitic acid suppresses the viability and stem-like phenotype of glioma stem cells (GSCs). 2-Fluoropalmitic acid also inhibits proliferation and invasion of glioma cell lines.
|
-
- HY-100711A
-
-
- HY-135808
-
BIZ 114
|
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-11006
-
KU-57788
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-N1486
-
-
- HY-142913
-
-
- HY-143899
-
FBA-IN-1
|
Fungal
|
Infection
|
FBA-IN-1 (compound 2a11) is a first-in-class, covalent and allosteric inhibitor of fructose-1,6-bisphosphate aldolase from Candida albicans (CaFBA). FBA-IN-1 inhibits the growth of Azole-resistant strains 103 with the MIC80 of 1 μg/mL.
|
-
- HY-A0256
-
Clavulanic acid
|
Antibiotic
Bacterial
|
Infection
Inflammation/Immunology
|
Clavulanic acid is a naturally occurring powerful bacterial β-lactamases inhibitor for research of infections caused by bacteria, including infections of the ears. Clavulanic acid is active against a wide spectrum of gram-positive and gram-negative bacterias.
|
-
- HY-125957
-
A-3 hydrochloride
|
PKA
Casein Kinase
CaMK
PKC
|
Others
|
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
|
-
- HY-N1193
-
Sulfuretin
|
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-147515
-
FGFR4-IN-11
|
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-111432
-
CCG-232601
|
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-115999
-
Carbonic anhydrase inhibitor 12
|
Carbonic Anhydrase
|
Cancer
|
Carbonic anhydrase inhibitor 12 is a potent CA II inhibitor, also has inhibitory activity in CA I (Kis of 1.72 and 271 nM in CA II and CA I, respectively). Carbonic anhydrase inhibitor 12 has potent anticancer activity against different cancer cell lines.
|
-
- HY-143483
-
NBTIs-IN-5
|
Bacterial
|
Infection
|
NBTIs-IN-5 (Compound 5r) is a NBTI (Novel Bacterial Topoisomerase Inhibitor) DNA gyrase inhibitor with an IC50 of 1.5 μM against Mycobacterium abscessus (Mabs) DNA gyrase. NBTIs-IN-5 inhibits Mabs bamboo bacterial growth with an MIC90 of 0.4 μM.
|
-
- HY-N6950
-
Hederacolchiside A1
|
PI3K
Akt
mTOR
Parasite
Apoptosis
|
Cancer
Infection
|
Hederacolchiside A1, isolated from Pulsatilla chinensis, suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K/Akt/mTOR signaling pathway. Hederacolchiside A1 has antischistosomal activity, affecting parasite viability both in vivo and in vitro.
|
-
- HY-B0141S3
-
Estradiol-d2
β-Estradiol-d2; 17β-Estradiol-d2; 17β-Oestradiol-d2
|
Estrogen Receptor/ERR
Endogenous Metabolite
|
Endocrinology
Cancer
|
Estradiol-d2 (β-Estradiol-d2) is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
|
-
- HY-B0141S1
-
Estradiol-d4
β-Estradiol-d4; 17β-Estradiol-d4; 17β-Oestradiol-d4
|
Estrogen Receptor/ERR
Endogenous Metabolite
|
Endocrinology
Cancer
|
Estradiol-D4 (β-Estradiol-D4) is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
|
-
- HY-123346
-
SW155246
|
DNA Methyltransferase
|
Cancer
|
SW155246 is a DNA methyltransferase (DNMT1) selective inhibitor with IC50s of 1.2 and 38 μM for hDNMT1 and mDNMT3A, respectively. SW155246 can be used for the research of cancer and other diseases.
|
-
- HY-N1333
-
Rubioncolin C
|
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-18777
-
KC7F2
|
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-139553
-
Zunsemetinib
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
-
Nigranoic acid
|
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-16724
-
Indoximod
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
(±)-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-113439S
-
12-HETE-d8
|
Apoptosis
|
Inflammation/Immunology
Cardiovascular Disease
|
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.12-HETE has both anti-thrombotic and pro-thrombotic effects. 12-HETE is a neuromodulator.
|
-
- HY-122575
-
Aurintricarboxylic acid
|
P2X Receptor
Influenza Virus
Topoisomerase
MicroRNA
Apoptosis
|
Infection
Inflammation/Immunology
Neurological Disease
|
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.
|
-
- HY-113126
-
-
- HY-N9814
-
Shanciol B
|
NO Synthase
|
Inflammation/Immunology
|
Shanciol B, isolated from the ethyl acetate extract of the air-dried whole plant of Pholidota imbricate Hook, inhibits nitric oxide (NO) production and 1,1-diphenyl-2-picrylhydrazil (DPPH) radical scavenging activity. Shanciol B is a microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor with anti-inflammatory activity.
|
-
- HY-147566
-
ATR-IN-14
|
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-146738
-
GSD-11
|
|
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.
|
-
- HY-N0781
-
Linderalactone
|
Apoptosis
|
Cancer
|
Linderalactone is an important sesquiterpene lactone isolated from Radix linderae. 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-145389
-
SZ-015268
|
CDK
|
Cancer
|
SZ-015268 is a CDK7 inhibitor with an IC50 of 23.56 nM. SZ-015268 has extremely significant anti-tumor advantages. SZ-015268 inhibits HCC70, OVCAR-3, HCT116 and HCC1806 cells proliferation with IC50s of 33, 80.56, 12.53, and 61.55 nM, respectively.
|
-
- HY-121750
-
CCG-222740
|
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-108543
-
NSC 95397
|
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.
|
-
- HY-143484
-
844-TFM
|
Bacterial
|
Infection
|
844-TFM is a NBTI (novel bacterial topoisomerase inhibitor) DNA gyrase inhibitor, with an IC50 of 1.5 μM. 844-TFM exhibits bactericidal properties against M. abscessus.
|
-
- HY-146275
-
LXRβ agonist-3
|
LXR
|
Cancer
|
LXRβ agonist-3 (compound 4-13) is a potent and selective LXRβ (liver X receptor β) agonist, with an EC50 of 0.095 μM. LXRβ agonist-3 efficiently inhibits U87EGFRvIII cell, with an IC50 of 3.75 μM. LXRβ agonist-3 shows antitumor activity, and can inhibit glioblastoma.
|
-
- HY-N0226
-
Epiberberine
|
AChE
Beta-secretase
|
Metabolic Disease
Neurological 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-N0226A
-
Epiberberine chloride
|
AChE
Beta-secretase
Reactive Oxygen Species
|
Metabolic Disease
Neurological Disease
|
Epiberberine chloride 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 chloride has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and may protect against Alzheimer disease. Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways. Epiberberine has the potential effect in the research of diabetic disease.
|
-
- HY-108617
-
YM976
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
YM976 is a phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.2 nM. YM976 shows the dissociation of anti-inflammatory activities from emetic effects and inhibits the antigen-induced airway responses.
|
-
- HY-N6674
-
Diazepinomicin
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-N6679A
-
10,11-Dehydrocurvularin
|
HSP
TGF-beta/Smad
|
Cancer
Infection
|
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-114395
-
NVS-ZP7-4
|
Others
|
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 druggable node in the Notch pathway.
|
-
- HY-145594
-
Safusidenib
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
Safusidenib is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma. Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively.
|
-
- HY-N7071A
-
Maduramicin ammonium
Maduramycin ammonium
|
Bacterial
Apoptosis
Antibiotic
|
Infection
|
Maduramicin ammonium (Maduramycin ammonium) is isolated from the actinomycete Actinomadura rubra. Maduramicin ammonium (Maduramycin ammonium) is an anticoccidial agent for the the treatment of Eimeria spp., E. adenoeides, E. gallopavonis, and E. dispersa infection. Maduramicin ammonium (Maduramycin ammonium) induces cell apoptosis in chicken myocardial cells via intrinsic and extrinsic pathways.
|
-
- HY-N5136
-
25(R,S)-Ruscogenin
|
PI3K
Akt
mTOR
|
Cancer
|
Ruscogenin suppresses HCC metastasis by reducing the expression of MMP-2, MMP-9, uPA, VEGF and HIF-1α via regulating the PI3K/Akt/mTOR signaling pathway. And Ruscogenin alleviates LPS-induced pulmonary endothelial cell apoptosis by su
|
-
- HY-N8211
-
Gypenoside L
|
p38 MAPK
ERK
NF-κB
|
Cancer
Inflammation/Immunology
|
Gypenoside L is a saponin that can be found in Gynostemma pentaphyllum. Gypenoside L increases the SA-β-galactosidase activity, promotes the production of senescence-associated secretory cytokines. Gypenoside L also can activate p38 and ERK MAPK pathways and NF-κB pathway to induce senescence. Gypenoside L exhibits anti-tumor and anti-inflammatory activities.
|
-
- HY-132601
-
Cobomarsen
MRG-106
|
Others
|
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-N1913
-
-
- HY-145155
-
Calpain-2-IN-1
|
Proteasome
|
Neurological Disease
|
Calpain-2-IN-1 (Formula 1A) is a isoform-specific calpain-2 inhibitor with Kis of 181 nM and 7.8 nM for calpain-1, and calpain-2, respectively. Calpain-2-IN-1 can be used for the research of neurodegenerative diseases and other diseases of synaptic function.
|
-
- HY-15583
-
-
- HY-122470
-
Stampidine
|
Reverse Transcriptase
HIV
|
Infection
|
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
|
-
- HY-124156A
-
KY-02327 acetate
|
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-N0072
-
Brazilin
|
Apoptosis
Autophagy
|
Cancer
Inflammation/Immunology
|
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-146058
-
NF-κB/PON1-IN-1
|
NF-κB
ROS
|
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-142924
-
ATR-IN-8
|
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-N4233
-
Bisabolangelone
|
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-124156
-
KY-02327
|
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-147694
-
-
- HY-16787
-
ICA-121431
|
Sodium Channel
|
Cardiovascular Disease
|
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
|
-
- HY-121993
-
Combretastatin A-1
|
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-125276
-
TH5487
|
Others
|
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-16125
-
Carboxyamidotriazole Orotate
L-651582 Orotate; CAI Orotate
|
Calcium Channel
|
Cancer
Inflammation/Immunology
|
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-101494
-
Temuterkib
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-144813
-
Gü2602
|
Cathepsin
|
Cancer
Inflammation/Immunology
|
Gü2602 is a potent, reversible cathepsin K (CatK) inhibitor with a Ki of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsin K zymogen.
|
-
- HY-113314
-
AFMK
|
Endogenous Metabolite
|
Cancer
|
AFMK, antioxidant metabolite of Melatonin, attenuates X-ray-induced oxidative damage to DNA, proteins and lipids in mice. AFMK is a poorer scavenger. The pKa of AFMK at physiological pH is 8.7. Antioxidant capacity. AFMK improves the anti-tumor effect of Gemcitabine in PANC-1 cells through the modulation of apoptotic pathway.
|
-
- HY-13676S
-
Megestrol acetate-d3
|
Progesterone Receptor
Autophagy
HIV
|
Endocrinology
Cancer
|
Megestrol acetate-d3 is the deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway.
|
-
- HY-N1967
-
Dihydrocurcumin
|
Fatty Acid Synthase (FASN)
|
Metabolic Disease
|
Dihydrocurcumin, a major metabolites of curcumin, reduces lipid accumulation and oxidative stress. Dihydrocurcumin regulates mRNA and protein expression levels of SREBP-1C, PNPLA3 and PPARα, increases protein expression levels of pAKT and PI3K, and reduced the levels of cellular NO and ROS via Nrf2 signaling pathways.
|
-
- HY-N2329
-
-
- HY-121246
-
Fluorofenidone
AKF-PD
|
Others
|
Inflammation/Immunology
|
Fluorofenidone (AKF-PD), an analogue of AMR69, shows equivalent antifibrotic activity, lower toxicity and longer half-life. Fluorofenidone (AKF-PD) attenuates the progression of renal interstitial fibrosis partly by suppressing NADPH oxidase and extracellular matrix (ECM) deposition via the PI3K/Akt signalling pathway.
|
-
- HY-N0408
-
Picroside II
|
NF-κB
Reactive Oxygen Species
Apoptosis
Influenza Virus
|
Cancer
Infection
Inflammation/Immunology
Neurological Disease
|
Picroside II, an iridoid compound extracted from Picrorhiza, exhibits anti-inflammatory and anti-apoptotic activities.
picroside II alleviates the inflammatory response in sepsis and enhances immune function by inhibiting the activation of NLRP3 inflammasome and NF-κB pathways.
Picroside II is an antioxidant, exhibits a significant neuroprotective effect through reducing ROS production and protects the blood-brain barrier (BBB) after cerebral ischemia-reperfusion (CI/R) injury. Picroside II has antioxidant, anti-inflammatory, immune regulatory, anti-virus and other pharmacological activities.
|
-
- HY-121725
-
MM-206
|
STAT
|
Cancer
|
MM-206, a STAT3 activity inhibitor, potently inhibits the STAT3 SH2 domain-phosphopeptide interaction with IC50 of 1.2 μM. MM-206 demonstrates dose-dependent induction of apoptosis in acute myeloid leukemia (AML) cell lines.
|
-
- HY-113509S
-
Lipoxin A4-d5
LXA4-d5
|
Interleukin Related
Endogenous Metabolite
|
Inflammation/Immunology
|
Lipoxin A4-d5 (LXA4-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. 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-144812
-
Gü1303
|
Cathepsin
|
Cancer
Inflammation/Immunology
|
Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a Ki of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen.
|
-
- HY-106011
-
SLX-4090
|
Others
|
Metabolic Disease
|
SLX-4090 is an orally active enterocytic-specific microsomal triglyceride transfer protein (MTP) inhibitor with an IC50 of 8.0 nM. SLX-4090 can be used for the research of dyslipidemia.
|
-
- HY-146105
-
Anticancer agent 65
|
Apoptosis
MDM-2/p53
ROS
MMP
Bcl-2 Family
|
Cancer
|
Anticancer agent 65 (compound 4c) shows excellent activity in cancer cell lines, especially A549 cells, with an IC50 of 1.07 μM. Anticancer agent 65 induces S-phase arrest in A549 cells and increases the expression level of p53 and p21. Anticancer agent 65 causes apoptosis, ROS generation and collapse of MMP in A549 cells.
|
-
- HY-N0628
-
-
- HY-B0667
-
-
- HY-B0667A
-
-
- HY-N6918
-
-
- HY-146504
-
Topoisomerase I/II inhibitor 3
|
Topoisomerase
PI3K
Apoptosis
ROS
|
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-33298
-
LM10
|
Others
|
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-146128
-
-
- HY-119390
-
AA-CW236
|
DNA Methyltransferase
|
Cancer
|
AA-CW236 is a MGMT (O6-methylguanine DNA methyltransferase) inhibitor. AA-CW236 targets MGMT active site Cys145 for covalent modification.
|
-
- HY-132993
-
Hcyb1
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
Hcyb1 is a highly selective, orally active PDE2 inhibitor. Hcyb1 has a highly selective inhibition of PDE2A (IC50=0.57 μM) and over 250-fold selectivity against other recombinant PDE family members. Hcyb1 produces neuroprotective and antidepressant‐like effects most likely mediated by cAMP/cGMP-CREB-BDNF signaling.
|
-
- HY-N0755
-
Rhoifolin
|
Insulin Receptor
GLUT
NF-κB
p38 MAPK
Autophagy
|
Metabolic Disease
Endocrinology
Cancer
|
Rhoifolin is a flavone glycoside isolated from Citrus grandis (L.) Osbeck leaves. Rhoifolin is beneficial for diabetic complications through enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and glucose transporter 4 (GLUT 4) translocation. Rhoifolin ameliorates titanium particle-stimulated osteolysis and attenuates osteoclastogenesis via RANKL-induced NF-κB and MAPK pathways.
|
-
- HY-13676S1
-
Megestrol acetate-d3-1
|
Progesterone Receptor
Autophagy
HIV
|
Endocrinology
Cancer
|
Megestrol acetate-d3-1 is deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway.
|
-
- HY-N6246
-
Asperulosidic Acid
|
NF-κB
ERK
|
Cancer
Inflammation/Immunology
|
Asperulosidic Acid (ASPA), a bioactive iridoid glycoside, is extracted from the herbs of Hedyotis diffusa Willd. Asperulosidic Acid (ASPA) has anti-tumor, anti-oxidant, and anti-inflammatory activities.
ASPA is related to the inhibition of inflammatory cytokines (TNF-α, IL-6) and mediators via suppression of the NF-κB and mitogen-activated protein kinase (MAPK) signaling pathways.
|
-
- HY-106420
-
-
- HY-116084
-
-
- HY-143656
-
SH379
|
Autophagy
|
Endocrinology
|
SH379 is the derivative of 2-methylpyrimidine-fused tricyclic diterpene. SH379 is a potent and orally active anti-late-onset hypogonadism agent. SH379 significantly promotes the expression of the key testosterone synthesis-related enzymes StAR and 3β-HSD. SH379 stimulates autophagy through regulating AMPK/mTOR signaling pathway.
|
-
- HY-146958
-
MAO-B-IN-8
|
Monoamine Oxidase
|
Neurological Disease
|
MAO-B-IN-8 is a potent reversible MAO-B inhibitor and an inhibitor of microglial production of neuroinflammatory mediator. MAO-B-IN-8 can be used for neurodegenerative disease research.
|
-
- HY-143873
-
Bcl-2-IN-5
|
Bcl-2 Family
|
Cancer
|
Bcl-2-IN-5 is a BCL-2 inhibitor with IC50s of 0.12 nM, 0.14 nM and 0.22 nM for Bcl-2 wild type, Bcl-2 D103Y and Bcl-2 G101V, respectively. Bcl-2-IN-5 inhibits the cell growth with IC50 values of 0.2 nM and 0.44 nM for Bcl 2-G101V knock-in RS4; 11 and RS4; 11 cells, respectively (WO2021208963A1; Example 155).
|
-
- HY-117724
-
AZ3976
|
PAI-1
|
Cardiovascular Disease
|
AZ3976 is a potent plasminogen activator inhibitor type 1 (PAI-1) inhibitor with an IC50 value of 26 μM in an enzymatic chromogenic assay. AZ3976 is active with an IC50 of 16 μM in a plasma clot lysis assay. AZ3976 does not bind to active PAI-1 but bound reversibly to latent PAI-1. AZ3976 inhibits PAI-1 by enhancing the latency transition of active PAI-1. AZ3976 displays profibrinolytic activities in a human plasma clot lysis assay.
|
-
- HY-16706A
-
Remodelin hydrobromide
|
Histone Acetyltransferase
|
Cancer
|
Remodelin, a specific inhibitor of N-acetyltransferase NAT10, can ameliorate Hutchinson-Gilford Progeria Syndrom (HGPS) cellular phenotypes. Remodelin acts in a progerin- and FTI-independent pathway, by targeting and inhibiting NAT10. NAT10 is a protein with histone acetylation activity and primarily identified to be involved in regulation of telomerase activity.
|
-
- HY-19356A
-
Didesmethylrocaglamide
|
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-146195
-
-
- HY-N0391
-
L-Citrulline
|
Endogenous Metabolite
|
Others
|
L-Citrulline is an amino acid derived from ornithine in the catabolism of proline or glutamine and glutamate, or from l-arginine via arginine-citrulline pathway.
|
-
- HY-B1898
-
Metadoxine
|
PKA
|
Metabolic Disease
|
Metadoxine blocks adipocyte differentiation in association with inhibition of the protein kinase A-cAMP response element binding protein (PKA-CREB) pathway.
|
-
- HY-17514
-
Itraconazole
R51211
|
Fungal
Hedgehog
Cytochrome P450
Autophagy
Antibiotic
|
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-11007
-
GNF-2
|
Bcr-Abl
SARS-CoV
|
Cancer
|
GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
|
-
- HY-146419
-
Anti-inflammatory agent 20
|
NF-κB
COX
TNF Receptor
|
Inflammation/Immunology
|
Anti-inflammatory agent 20 (compound 5a) is a potent inhibitor of NO activity. Anti-inflammatory agent 20 shows anti-inflammatory activity. Anti-inflammatory agent 20 suppresses LPS-induced inflammation via inhibiting the activation of NF-κB and MAPK signaling and thereby reducing IL-6, TNF-α, iNOS, and COX-2 upregulation.
|
-
- HY-117374
-
HDAC3-IN-1
|
HDAC
|
Cancer
|
HDAC3-IN-1 (compound 5) is a potent and selective HDAC3 inhibitor, with an IC50 of 5.96 nM.
|
-
- HY-144270
-
-
- HY-N2013
-
Aristolactam I
Aristololactam; Aristolactam
|
Caspase
Apoptosis
|
Inflammation/Immunology
|
Aristololactam I (AL-I), is the main metabolite of aristolochic acid I (AA-I), participates in the processes that lead to renal damage.
Aristololactam I (AL-I) directly injures renal proximal tubule cells, the cytotoxic potency of AL-I is higher than that of AA-I and that the cytotoxic effects of these molecules are mediated through the induction of apoptosis in a caspase-3-dependent pathway.
|
-
- HY-14441
-
ML 10302
|
5-HT Receptor
|
Neurological Disease
|
ML 10302 is a potent agonist 5-HT4 receptor with Ki of 1.07 nM. 5-Hydroxytryptamine (5-HT4) receptor agonists stimulate gut motility through cholinergic pathways. ML10302 induces significant prokinesia both in the small bowel and colon through activation of cholinergic pathways. ML 10302 also has the potential for the research of neurology diseases.
|
-
- HY-B0141S4
-
Estradiol-13C6
β-Estradiol-13C6; E2-13C6; 17β-Estradiol-13C6; 17β-Oestradiol-13C6
|
Estrogen Receptor/ERR
Endogenous Metabolite
|
Endocrinology
Cancer
|
Estradiol-13C6 (β-Estradiol-13C6) is the 13C-labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
|
-
- HY-B0141S5
-
Estradiol-13C2
β-Estradiol-13C2; E2-13C2; 17β-Estradiol-13C2; 17β-Oestradiol-13C2
|
Estrogen Receptor/ERR
Endogenous Metabolite
|
Endocrinology
Cancer
|
Estradiol-13C2 (β-Estradiol-13C2) is the 13C-labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
|
-
- HY-N3426
-
Kazinol B
|
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
-
6-Hydroxyluteolin 7-glucoside
|
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-146549
-
RmlA-IN-1
|
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-15415
-
KB-R7943 mesylate
|
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-135825
-
TFEB activator 1
|
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-19528
-
SAH
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-N6636
-
Valencene
|
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-115928
-
M24
|
Bcl-2 Family
|
Cancer
|
M24 is a Mcl-1 selective inhibitor. M24 exhibits good binding affinity against Mcl-1 with Ki value of 0.33 μM. M24 exhibits good anti-proliferative activity and induce apoptosis in HepG2 cells.
|
-
- HY-113492
-
-
- HY-142517
-
EGFR-IN-25
|
EGFR
|
Cancer
|
EGFR-IN-25 is a potent EGFR inhibitor with IC50s of 9 nM and 60 nM for BaF3 cells (EGFR DEL19/T790M/C797S) and A431 cells (WT), respectively.
|
-
- HY-144266
-
-
- HY-19543
-
Brusatol
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-125817
-
BI-3406
|
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-108361
-
CCG-203971
|
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-15959
-
Savolitinib
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-131976
-
BVDV-IN-1
|
DNA/RNA Synthesis
|
Infection
|
BVDV-IN-1 is a non-nucleoside inhibitor (NNI) of bovine viral diarrhea virus (BVDV), with an EC50 of 1.8 μM. BVDV-IN-1 directly binds to a hydrophobic pocket of the BVDV RdRp. BVDV-IN-1 has antiviral activity against BVDV resistant to NNI thiosemicarbazone (TSC).
|
-
- HY-123037
-
Triadimefon
|
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-146551
-
RmlA-IN-2
|
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-135749
-
BN201
|
Others
|
Inflammation/Immunology
Neurological Disease
|
BN201 promotes neuronal differentiation, the differentiation of precursor cells to mature oligodendrocytes (EC50 of 6.3 μM) in vitro, and the myelination of new axons (EC50 of 16.6 μM). BN201 is able to cross the blood-brain barrier by active transport and activate pathways (IGF-1 pathway) associated with the response to stress and neuron survival. BN201 has potently neuroprotective effects.
|
-
- HY-N2312
-
Mogrol
|
ERK
STAT
|
Cancer
|
Mogrol is a biometabolite of mogrosides, and acts via inhibition of the ERK1/2 and STAT3 pathways, or reducing CREB activation and activating AMPK signaling.
|
-
- HY-100582
-
Ribitol
Adonitol; Adonite
|
Endogenous Metabolite
|
Others
|
Ribitol is a crystalline pentose alcohol formed by the reduction of ribose. Enhancing the flux of D-glucose to the pentose phosphate pathway in Saccharomyces cerevisiae for the production of D-ribose and ribitol.
|
-
- HY-W018004
-
-
- HY-113128
-
-
- HY-144321
-
Trk-IN-9
|
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-P1111
-
Lyn peptide inhibitor
|
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-119917
-
Gossypetin
|
p38 MAPK
MEK
Bacterial
|
Cancer
Infection
|
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-N0316
-
Mollugin
|
Others
|
Cancer
|
Mollugin is a major bioactive component isolated from Rubia cordifolia L.. Mollugin has an anti-cancer therapeutic effect by inhibiting TNF-α-induced NF-κB activation. Mollugin enhances the osteogenic action of BMP-2 via the p38-Smad signaling pathway .
|
-
- HY-N2112
-
Glaucocalyxin A
|
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-B0185A
-
Lidocaine hydrochloride
Lignocaine hydrochloride
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cancer
Cardiovascular Disease
|
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 drug to treat ventricular arrhythmia and an effective tumor-inhibitor.
|
-
- HY-138281
-
Complement factor D-IN-2
|
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-100036
-
MK-4101
|
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-131296
-
5-A-RU-PABC-Val-Cit-Fmoc
|
Others
|
Inflammation/Immunology
|
5-A-RU-PABC-Val-Cit-Fmoc is the prodrug of 5-A-RU. 5-A-RU, a precursor of bacterial Riboflavin, is a mucosal-associated invariant T (MAIT) cells activator. 5-A-RU forms potent MAIT-activating antigens via non-enzymatic reactions with small molecules, such as glyoxal and methylglyoxal, which are derived from other metabolic pathways.
|
-
- HY-144612
-
NS2B/NS3-IN-2
|
Virus Protease
|
Infection
|
NS2B/NS3-IN-2 is a potent dengue virus (DENV) NS2B/NS3 covalent inhibitor with an IC50 of 6.0 nM and Ki of 0.66 µM. NS2B/NS3-IN-2 shows no cytotoxicity and markedly increases the cell survival rate.
|
-
- HY-144689
-
BChE-IN-3
|
AChE
|
Neurological Disease
|
BChE-IN-3 (compound 45a) is a potent, selective, time-dependent and pseudoirreversible BChE inhibitor, with an IC50 of 56.9 nM. BChE-IN-3 also shows marginal and reversible (not time-dependent) inhibition of AChE.
|
-
- HY-10515
-
BX-320
|
PDK-1
|
Cancer
|
BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC50 of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect.
|
-
- HY-A0115
-
-
- HY-124379
-
TPCK
L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK
|
Ser/Thr Protease
|
Cancer
Inflammation/Immunology
|
TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is a potent serine protease inhibitor that reacts with the retinoblastoma protein (RB)-binding core of HPV-18 E7 protein and abolish its RB-binding capability. TPCK is able to modify E7 protein in live keratinocytes following its addition to the culture medium.
|
-
- HY-139690
-
CCG258747
|
Opioid Receptor
|
Cardiovascular Disease
|
CCG258747 is a selective GRK2 inhibitor (IC50=18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, >5500, and >550–fold, respectively).CCG258747 also blocks the internalization of the µ-opioid receptor. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure.
|
-
- HY-N10119
-
-
- HY-113128A
-
-
- HY-N6940
-
Prosapogenin A
Progenin III
|
Apoptosis
|
Cancer
|
Prosapogenin A, a natural product from Veratrum, induces apoptosis in human cancer cells in vitro via inhibition of the STAT3 signaling pathway and glycolysis.
|
-
- HY-113128B
-
-
- HY-114321
-
-
- HY-108647
-
EO 1428
|
p38 MAPK
|
Inflammation/Immunology
|
EO 1428 is a highly specific inhibitor of p38 of the aminobenzophenone class. EO 1428 (1 μM ) markedly attenuates LPS-induced tumor necrosis factor α-converting enzyme (TACE) activity up-regulation.
|
-
- HY-146383
-
H3R antagonist 2
|
Histamine Receptor
AChE
Monoamine Oxidase
|
Neurological Disease
|
H3R antagonist 2 (Compound 23) is a multitarget histamine H3 receptor (H3R) antagonist with a Ki of 170 nM for hH3R . H3R antagonist 2 shows inhibitory effects with IC50 values of 180, 880 and 775 nM for acetylcholinesterase, butyrylcholinesterase and human monoamine oxidase B (hMAO B), respectively. H3R antagonist 2 shows favorable anti-neuropathic pain and memory-enhancing effects. H3R can across BBB.
|
-
- HY-N2638
-
Ilexsaponin A
|
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-123503
-
Salicortin
|
JNK
NF-κB
|
Inflammation/Immunology
Neurological Disease
|
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-108473
-
TLR3-IN-1
|
Toll-like Receptor (TLR)
|
Cancer
|
TLR3-IN-1 is a potent, highly selective TLR3 signaling inhibitor. TLR3-IN-1 represses the expression of downstream signaling pathways mediated by the TLR3/dsRNA complex, including TNF-α and IL-1β.
|
-
- HY-18366A
-
RU-SKI 43 hydrochloride
|
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-18366
-
RU-SKI 43
|
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-132305
-
VEGFR-3-IN-1
|
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-114454
-
INH14
|
IKK
|
Cancer
Inflammation/Immunology
|
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-P1259
-
PR-39
|
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-N2787
-
8-Prenylnaringenin
|
Apoptosis
|
Cancer
|
8-prenylnaringenin is a prenylflavonoid isolated from hop cones (Humulus lupulus), with cytotoxicity. 8-prenylnaringenin has anti-proliferative activity against HCT-116 colon cancer cells via induction of intrinsic and extrinsic pathway-mediated apoptosis. 8-Prenylnaringenin also promotes recovery from immobilization-induced disuse muscle atrophy through activation of the Akt phosphorylation pathway in mice .
|
-
- HY-135483A
-
AR-R17779 hydrochloride
|
nAChR
|
Neurological Disease
|
AR-R17779 hydrochloride is a potent and selective full agonist of nAChR, with Kis of 92 and 16000 nM for α7 and α4β2 subtype, respectively. AR-R17779 hydrochloride can improve learning and memory in rats. AR-R17779 hydrochloride also has anxiolytic activity. AR-R17779 hydrochloride can reduce inflammation by activating antiinflammatory cholinergic (vagal) pathways.
|
-
- HY-130304
-
8-Isoprostaglandin E2
iPE2-III
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
8-Isoprostaglandin E2 (iPE2-III) is a member of the isoprostane class of prostanoids. 8-Isoprostaglandin E2 acts at the receptor for thromboxane A2 (the TP) in vivo to induce vasoconstriction and platelet aggregation. 8-Isoprostaglandin E2 enhances receptor-activated NFkappa B ligand (RANKL)-dependent osteoclastic potential of marrow hematopoietic precursors via the cAMP pathway.
|
-
- HY-115974
-
GRPR antagonist-1
|
Others
|
Cancer
|
GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis. Anticancer activity.
|
-
- HY-N10224
-
-
- HY-N2515
-
Ginsenoside Rk1
|
NF-κB
PI3K
JAK
Apoptosis
|
Cancer
Inflammation/Immunology
|
Ginsenoside Rk1 is a unique component created by processing the ginseng plant (mainly Sung Ginseng, SG) at high temperatures.
Ginsenoside Rk1 has anti-inflammatory effect, suppresses the activation of Jak2/Stat3 signaling pathway and NF-κB.
Ginsenoside Rk1 has anti-tumor effect, antiplatelet aggregation activities, anti-insulin resistance, nephroprotective effect, antimicrobial effect, cognitive function enhancement, lipid accumulation reduction and prevents osteoporosis.
Ginsenoside Rk1 induces cell apoptosis by triggering intracellular reactive oxygen species (ROS) generation and blocking PI3K/Akt pathway.
|
-
- HY-N1356
-
-
- HY-144254
-
PI3Kδ-IN-10
|
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-P1098
-
Ac2-26
|
NF-κB
|
Inflammation/Immunology
|
Ac2-26, an active N-terminal peptide of annexin A1 (AnxA1), attenuates ischemia-reperfusion-induced acute lung injury. Ac2-26 also decreases AnxA1 protein expression, inhibits the activation of NF-κB and MAPK pathways in the injured lung tissue.
|
-
- HY-B0094
-
Artemisinin
Qinghaosu; NSC 369397
|
HCV
Parasite
Akt
Ferroptosis
|
Cancer
Infection
Neurological Disease
|
Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial drug 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-B0252
-
Hydrochlorothiazide
HCTZ
|
TGF-beta/Smad
Potassium Channel
|
Metabolic Disease
Cardiovascular Disease
|
Hydrochlorothiazide (HCTZ), an orally active diuretic drug 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-142699
-
SSTR4 agonist 2
|
Others
|
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-W058849
-
MT 63-78
|
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-N1381
-
Periplocin
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
Periplocin is a cardiotonic steroid isolated from Periploca forrestii. 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-N4113
-
Glycycoumarin
|
Autophagy
|
Cancer
|
Glycycoumarin is a major bioactive coumarin of licorice. Glycycoumarin inhibits hepatocyte lipoapoptosis through activation of autophagy and inhibition of ER stress-mediated JNK and GSK-3-mediated mitochondrial pathway. Glycycoumarin exerts anti-liver cancer activity by directly targeting T-LAK cell-originated protein kinase .
|
-
- HY-16933
-
L-Alanosine
NSC-153353; SDX-102
|
Antibiotic
|
Cancer
Infection
|
L-Alanosine (NSC-153353), an antibiotic from Streptomyces alanosinicus, has antineoplastic activity. L-Alanosine (NSC-153353) inhibits adenylosuccinate synthetase, which converts inosine monophospate (IMP) into adenylosuccinate. L-Alanosine (NSC-153353) blocks the common de novo purine biosynthesis pathway and, thereby, inhibits tumor cells with MTAP deficiency.
|
-
- HY-113756A
-
Latanoprost acid
|
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-111557
-
YM-254890
|
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-113224
-
Desmosterol
|
Endogenous Metabolite
|
Metabolic Disease
|
Desmosterol is a molecule similar to cholesterol. Desmosterol is the immediate precursor of cholesterol in the Bloch pathway of cholesterol biosynthesis. Desmosterol, as an endogenous metabolite, used to study cholesterol metabolism.
|
-
- HY-B1328
-
-
- HY-115319
-
CP-24879 hydrochloride
|
Others
Ferroptosis
|
Inflammation/Immunology
|
CP-24879 (hydrochloride) is a potent, selective and combined delta5D/delta6D inhibitor. CP-24879 (hydrochloride) can significantly reduce intracellular lipid accumulation and inflammatory injury in hepatocytes. CP-24879 (hydrochloride) exhibits superior antisteatotic and anti-inflammatory actions in fat-1 and ω-3-treated hepatocytes, and can be used for non-alcoholic steatohepatitis research.
|
-
- HY-P1111A
-
Lyn peptide inhibitor TFA
|
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-142519
-
EGFR-IN-27
|
EGFR
|
Cancer
|
EGFR-IN-27 is a potent EGFR inhibitor with IC50s of <50 nM for EGFR Del, L858R, Del/T790M, L858R/T790M, Del/T790M/C797S, and L858R/T790M/C797S, respectively (WO2021249324A1, compound 511).
|
-
- HY-115904
-
FLT3/CDK4-IN-1
|
CDK
FLT3
|
Cancer
|
FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo.
|
-
- HY-B1640
-
Ethacrynic acid
Etacrynic acid
|
Gutathione S-transferase
NF-κB
Calcium Channel
|
Cancer
Inflammation/Immunology
|
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-P1259A
-
PR-39 TFA
|
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-116084S
-
-
- HY-N4126
-
6-Demethoxytangeretin
|
ALK
|
Cancer
Inflammation/Immunology
Neurological Disease
|
6-Demethoxytangeretin is a citrus flavonoid isolated from Citrus depressa. 6-Demethoxytangeretin exerts anti-inflammatory activity and anti-allergic activity, suppresses production and gene expression of interleukin-6 in human mast cell-1 via anaplastic lymphoma kinase (ALK) and mitogen-activated protein kinase (MAPK) pathways. 6-Demethoxytangeretin facilitates the CRE-mediated transcription associated with learning and memory in cultured hippocampal neurons.
|
-
- HY-145303
-
-
- HY-N1798
-
-
- HY-142963
-
-
- HY-75342
-
-
- HY-139621
-
-
- HY-133068
-
5-Hydroxyferulic acid
|
COMT
|
Others
|
5-Hydroxyferulic acid is a hydroxycinnamic acid and is a metabolite of the phenylpropanoid pathway. 5-Hydroxyferulic acid is a precursor in the biosynthesis of sinapic acid and is also a COMT non-esterifed substrate.
|
-
- HY-112331
-
SJ000291942
|
TGF-β Receptor
|
Cancer
|
SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway. BMPs are members of the transforming growth factor beta (TGFβ) family of secreted signaling molecules.
|
-
- HY-142512
-
EGFR-IN-24
|
EGFR
|
Cancer
|
EGFR-IN-24, a potent EGFR inhibitor, shows inhibition against EGFR(del19/T790M/C797S) and EGFR(L858R/T790M/C797S), respectively.
|
-
- HY-147671
-
-
- HY-13065
-
Isobavachalcone
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.
|
-
- HY-P1036
-
Compstatin
|
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-18285
-
Longdaysin
|
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-144369
-
Proteasome-IN-4
|
Proteasome
|
Cancer
|
Proteasome-IN-4 is an excellent and non-covalent proteasome inhibitor (IC50=8.39 nM). Proteasome-IN-4 has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines. Proteasome-IN-4 can be used for cancer research.
|
-
- HY-107553
-
Chetomin
|
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-133556
-
IQZ23
|
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-122534
-
Mensacarcin
|
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-N0284
-
Esculetin
|
PI3K
Akt
|
Cancer
Inflammation/Immunology
|
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-13968
-
JW 55
|
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-P1098A
-
Ac2-26 TFA
|
NF-κB
|
Inflammation/Immunology
|
Ac2-26 TFA, an active N-terminal peptide of annexin A1 (AnxA1), attenuates ischemia-reperfusion-induced acute lung injury. Ac2-26 also decreases AnxA1 protein expression, inhibits the activation of NF-κB and MAPK pathways in the injured lung tissue.
|
-
- HY-N0047
-
Polyphyllin I
|
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-147770
-
NF-κB-IN-6
|
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-125035
-
LCH-7749944
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.
|
-
- HY-19893
-
Antroquinonol
(+)-Antroquinonol
|
Keap1-Nrf2
|
Cancer
Inflammation/Immunology
|
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.
|
-
- HY-127105A
-
-
- HY-108538
-
Ethacrynic acid D5
|
Gutathione 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
-
ERK1/2 inhibitor 3
|
ERK
|
Cancer
Inflammation/Immunology
|
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-145026
-
ERK1/2 inhibitor 4
|
ERK
|
Cancer
Inflammation/Immunology
|
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-124858
-
SC99
|
STAT
JAK
Apoptosis
|
Cancer
Cardiovascular Disease
|
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-145027
-
ERK1/2 inhibitor 5
|
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-145028
-
ERK1/2 inhibitor 6
|
ERK
|
Cancer
Inflammation/Immunology
|
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-B0667S1
-
-
- HY-103252
-
-
- HY-N2991
-
Dehydropachymic acid
|
Autophagy
|
Neurological Disease
|
Dehydropachymic acid is one of the major triterpenes isolated from Poria cocos. Dehydropachymic acid is more effective in autophagy-lysosome pathway (ALP) impaired cells rather than normal cells.
|
-
- HY-102028
-
KY1220
|
Wnt
β-catenin
|
Cancer
|
KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway; with an IC50 of 2.1 μM in HEK293 reporter cells.
|
-
- HY-132971
-
Thalidomide-piperazine hydrochloride
|
Others
|
Cancer
|
Thalidomide-piperazine hydrochloride has the potential for the research of leprosy and multiple myeloma. Thalidomide-piperazine hydrochloride used as a tool in developmental biology leads to important discoveries in the biochemical pathways of limb development.
|
-
- HY-103640
-
Amifostine thiol dihydrochloride
WR-1065 dihydrochloride
|
MDM-2/p53
|
Cancer
|
Amifostine thiol (WR-1065) dihydrochloride can protect normal tissues from the toxic effects of certain cancer drugs and activate p53 through a JNK-dependent signaling pathway.
|
-
- HY-13540
-
E7016
GPI 21016
|
PARP
|
Cancer
|
E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent.
|
-
- HY-19986
-
AAL993
|
VEGFR
|
Cancer
Cardiovascular Disease
|
IC50s of 130 nM, 23 nM, and 18 nM for VEGFR1, VEGFR2, and VEGFR3, respectively. AAL993 shows less potently inhibits other tyrosine kinases. AAL993 possesses potent antiangiogenic and antitumor properties.
|
-
- HY-120371
-
-
- HY-B0185AS1
-
Lidocaine-d6 hydrochloride
Lignocaine-d6 hydrochloride
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cancer
Cardiovascular Disease
|
Lidocaine-d6 (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). 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 drug to treat ventricular arrhythmia and an effective tumor-inhibitor.
|
-
- HY-12037A
-
Rigosertib
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-B0097
-
Floxuridine
5-Fluorouracil 2'-deoxyriboside
|
Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
Bacterial
CMV
HSV
Apoptosis
|
Cancer
Infection
|
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-16146
-
Combretastatin A-1 phosphate tetrasodium
OXi-4503 tetrasodium
|
Microtubule/Tubulin
|
Cancer
|
Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a prodrug 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-17508
-
Clarithromycin
|
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-147674
-
-
- HY-147672
-
-
- HY-W015913
-
-
- HY-W017389
-
-
- HY-N4176
-
Ginkgolide K
|
Autophagy
|
Neurological Disease
|
Ginkgolide K, isolated from Ginkgo biloba, induces protective autophagy through the AMPK/mTOR/ULK1 signaling pathway. Ginkgolide K possesses neuroprotective activity.
|
-
- HY-145721
-
Mongersen
GED-0301
|
TGF-beta/Smad
|
Inflammation/Immunology
|
Mongersen is a 21-mer phosphorothioate antisense oligonucleotide targeting the mRNA of the Smad7 protein, thus leading to suppression of TGF-β1 pathways and remission of Crohn's disease.
|
-
- HY-113204
-
-
- HY-10971A
-
Alisertib sodium
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-126248
-
Tankyrase-IN-2
|
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-124418
-
SBI-477
|
Others
|
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
|
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). CC-99677 is extracted from patent WO2020236636, compound 1.
|
-
- HY-145686
-
ANKRD22-IN-1
|
Others
|
Inflammation/Immunology
|
ANKRD22-IN-1 is a potent inhibitor of ANKRD22. ANKRD22-IN-1 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-N0076
-
Bilobalide
(-)-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-B0185
-
Lidocaine
Lignocaine
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cancer
Cardiovascular Disease
|
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-112801
-
F-1
|
ALK
ROS
|
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-114491A
-
Rineterkib hydrochloride
|
Raf
ERK
|
Cancer
|
Rineterkib hydrochloride (compound B) is an orally active RAF and ERK1/2 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.
|
-
- HY-114491
-
Rineterkib
|
Raf
ERK
|
Cancer
|
Rineterkib (compound B) is an orally active RAF and ERK1/2 inhibitor in the study 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.
|
-
- HY-N6704
-
Enniatin A1
|
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-128891
-
Eperisone
|
Others
|
Neurological Disease
|
Eperisone 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 is a centrally acting muscle relaxant inhibiting the pain reflex pathway, having a vasodilator effect[2 .
|
-
- HY-113965
-
CUR61414
|
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-114395A
-
(R)-NVS-ZP7-4
|
Others
|
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 druggable node in the Notch pathway.
|
-
- HY-143400
-
HSP70-IN-3
|
HSP
|
Cancer
|
HSP70-IN-3 is a potent HSP70 inhibitor (IC50s of 1.1 and 1.9 μM in ASZ001 and C3H10T1/2, respectively). HSP70-IN-3 has anti-Hh (Hedgehog signaling) activity and anti-proliferative activity and reduces expression of the oncogenic transcription factor GLI1.
|
-
- HY-100368
-
MELK-8a
NVS-MELK8a
|
MELK
|
Cancer
|
MELK-8a (NVS-MELK8a) is a highly potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor with IC50 of 2 nM. MELK-8a also inhibits Flt3 (ITD), Haspin, PDGFRα with IC50s of 0.18, 0.19, and 0.42 μM, respectively. MELK plays an essential role in regulating cell mitosis in a subset of cancer cells.
|
-
- HY-100386
-
Ticlopidine
PCR 5332
|
Cytochrome P450
|
Cardiovascular Disease
|
Ticlopidine (PCR 5332), an antithrombotic prodrug, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 µM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 µM and 149 µM for NTPDase2 and NTPDase3, respectively. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively.
|
-
- HY-126077
-
MTI-31
|
mTOR
|
Cancer
Inflammation/Immunology
|
MTI-31 is a potent, orally active and highly selective inhibitor of mTORC1 and mTORC2. MTI-31 is selective for mTOR (Kd: 0.20 nM) versus PIK3CA, PIK3CB and PIK3G with >5,000 fold selectivity in mTOR binding assays. MTI-31 shows an IC50 of 39 nM for mTOR in LANCE assay of mTOR substrate phosphorylation with 100 μM ATP. MTI-31 can be used for the research of breast cancer.
|
-
- HY-14664CS1
-
(3S,5R)-Fluvastatin-d7 sodium
(3S,5R)-XU 62-320-d7 sodium
|
HMG-CoA Reductase (HMGCR)
|
Cancer
Cardiovascular Disease
|
(3S,5R)-Fluvastatin-d7 sodium ((3S,5R)-XU 62-320-d7 sodium) is the deuterium labeled (3S,5R)-Fluvastatin sodium. (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-W008820
-
Glutaric acid
|
Endogenous Metabolite
|
Metabolic Disease
|
Glutaric acid, C5 dicarboxylic acid, is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I.
|
-
- HY-101085
-
SKL2001
|
Wnt
β-catenin
|
Cancer
|
SKL2001 is an agonist of the Wnt/β-catenin pathway, with anti-cancer activity. SKL2001 stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction.
|
-
- HY-122816
-
HLY78
|
Wnt
|
Cancer
Neurological Disease
|
HLY78 is an activator of the Wnt/β-catenin signaling pathway, which targets the DIX domain of Axin and potentiates the Axin-LRP6 association to promote Wnt signaling transduction.
|
-
- HY-B0835S
-
Fenobucarb-d3
|
Apoptosis
|
Neurological Disease
|
Fenobucarb-d3 is the deuterium labeled Fenobucarb. Fenobucarb is a carbamate insecticide. Fenobucarb induces zebrafish developmental neurotoxicity through pathways involved in inflammation, oxidative stress, degeneration and apoptosis.
|
-
- HY-P1036A
-
Compstatin TFA
|
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-12037
-
Rigosertib sodium
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-144614
-
JH-XVII-10
|
DYRK
Apoptosis
|
Cancer
Neurological Disease
|
JH-XVII-10 is a potent, selective and orally active DYRK1A and DYRK1B inhibitor with IC50s of 3 nM and 5 nM for DYRK1A and DYRK1B, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines.
|
-
- HY-146261
-
HI5
|
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-116425
-
N-1-Naphthylphthalamic acid
Alanap 1
|
Others
|
Others
|
N-1-Naphthylphthalamic acid is a polar auxin transport inhibitor. N-1-Naphthylphthalamic acid disrupts leaf initiation, KNOX protein regulation, and formation of leaf margins in maize.
|
-
- HY-N4314
-
Scutellarein tetramethyl ether
4',5,6,7-Tetramethoxyflavone
|
Bacterial
|
Infection
Inflammation/Immunology
|
Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is a bioactive component of Siam weed extract. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) exhibits anti-inflammatory activity through NF-κB pathway. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) modulats of bacterial drug resistance via efflux pump inhibition. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) can enhance blood coagulation.
|
-
- HY-121140
-
AZ1729
|
Others
|
Metabolic Disease
|
AZ1729 is a potent free fatty acid 2 receptor (FFA2) activator, acting as a direct allosteric agonist and as a positive allosteric modulator. AZ1729 increases the activity of the endogenously produced short chain fatty acid propionate in Gi-mediated pathways, but not at those transduced by Gq/G11. AZ1729 induces inhibition of isoproterenol-induced lipolysis in mouse adipocytes. AZ1729 also can Induce migration of human neutrophils. AZ1729 can be used for researching the signaling pathways of the physiological roles of FFA2.
|
-
- HY-N0632
-
Esculentoside A
|
COX
NF-κB
|
Inflammation/Immunology
|
Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta.
Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models, has selective inhibitory activity towards cyclooxygenase-2 (COX-2).
Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways.
|
-
- HY-B1901
-
Eperisone hydrochloride
(±)-Eperisone hydrochloride
|
Others
|
Neurological Disease
|
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[2 .
|
-
- HY-137092
-
IACS-13909
|
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-N0292
-
Oleuropein
|
PPAR
Apoptosis
Aromatase
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
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-142686
-
SGK1-IN-3
|
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-N7110
-
6-Hydroxyflavone
|
Others
|
Inflammation/Immunology
|
6-Hydroxyflavone is a naturally occurring flavone, with anti-inflammatory activity. 6-Hydroxyflavone exhibits inhibitory effect towards bovine hemoglobin (BHb) glycation. 6-Hydroxyflavone can activate AKT, ERK 1/2, and JNK signaling pathways to effectively promote osteoblastic differentiation. 6-Hydroxyflavone inhibits the LPS-induced NO production .
|
-
- HY-117857
-
-
- HY-10971
-
Alisertib
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-N6896
-
Isoviolanthin
|
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-N2535
-
Coniferaldehyde
Ferulaldehyde
|
Apoptosis
|
Inflammation/Immunology
|
Coniferaldehyde (Ferulaldehyde) is an effective inducer of heme oxygenase-1 (HO-1). Coniferaldehyde exerts anti-inflammatory properties in response to LPS. Coniferaldehyde inhibits LPS-induced apoptosis through the PKCα/β II/Nrf-2/HO-1 dependent pathway in RAW264.7 macrophage cells.
|
-
- HY-15114
-
S 17092
S 17092-1
|
Others
|
Neurological Disease
|
S 17092 (S 17092-1) is a potent cerebral prolyl-endopeptidase (PEP) inhibitor with an IC50 of 1.2 nM. S 17092 can be used for the research of memory impairment and cognitive disorders associated with cerebral aging.
|
-
- HY-143402
-
Topoisomerase I/II inhibitor 2
|
Topoisomerase
|
Cancer
|
Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in treating liver cancer.
|
-
- HY-110354
-
UCM05
G28UCM
|
Fatty Acid Synthase (FASN)
Bacterial
Antibiotic
|
Cancer
Infection
|
UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) shows activity against HER2+ breast cancer xenografts and is active in anti-HER2 drug-resistant cell lines. UCM05 is a Filamentous temperature-sensitive protein Z (FtsZ) inhibitor and inhibits the growth of the Gram-positive bacterium B. subtilis with MIC values of 100 μM but lack activity on the Gram-negative bacterium E. coli.
|
-
- HY-145428
-
BT-GSI
|
Notch
γ-secretase
|
Cancer
|
BT-GSI is a γ-secretase inhibitor (GSI) and a bone-targeted Notch inhibitor. BT-GSI has dual anti-myeloma and anti-resorptive properties, which can be used for the research of multiple myeloma and associated bone disease. BT-GSI inhibits tumor growth and osteolytic disease progression.
|
-
- HY-N9521
-
-
- HY-N1420
-
Rhamnose
L-Rhamnose
|
Endogenous Metabolite
|
Cancer
|
Rhamnose (L-Rhamnose) is a monosaccharide found in plants and bacteria. Rhamnose-conjugated immunogens is used in immunotherapies. Rhamnose crosses the epithelia via the transcellular pathway and acts as a marker of intestinal absorption.
|
-
- HY-113013
-
Hydroxypyruvic acid
β-Hydroxypyruvic acid; 3-Hydroxypyruvic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
Hydroxypyruvic acid (β-Hydroxypyruvic acid) is an intermediate in the metabolism of glycine, serine and threonine. Hydroxypyruvic acid is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase. Hydroxypyruvic acid is involved in the metabolic disorder which is the dimethylglycine dehydrogenase deficiency pathway.
|
-
- HY-101017
-
-
- HY-144776
-
NAT
|
Others
|
Neurological Disease
|
NAT is an initial hit of NAMPT activator. NAMPT is the rate-limiting enzyme in the NAD salvage pathway, which makes it an attractive target for the research of many diseases associated with NAD exhaustion such as neurodegenerative diseases.
|
-
- HY-N0391S4
-
L-Citrulline-d4
|
Endogenous Metabolite
|
Others
|
L-Citrulline-d4 is the deuterium labeled L-Citrulline. L-Citrulline is an amino acid derived from ornithine in the catabolism of proline or glutamine and glutamate, or from l-arginine via arginine-citrulline pathway.
|
-
- HY-N7697
-
Chitotetraose tetrahydrochloride
|
Others
|
Others
|
Chitotetraose tetrahydrochloride is an arbuscular mycorrhizal (AM) fungal short-chain chitin oligomer. Chitotetraose tetrahydrochloride activates the AM fungal-dependent conserved symbiosis signaling pathway (CSSP) in actinorhizal plant species.
|
-
- HY-136901
-
-
- HY-N0391S5
-
L-Citrulline-d7
|
Endogenous Metabolite
|
Others
|
L-Citrulline-d7 is the deuterium labeled L-Citrulline. L-Citrulline is an amino acid derived from ornithine in the catabolism of proline or glutamine and glutamate, or from l-arginine via arginine-citrulline pathway.
|
-
- HY-W009371A
-
D-Ribose 5-phosphate
|
Endogenous Metabolite
|
Metabolic Disease
|
D-Ribose 5-phosphate is an intermediate of the oxidative branch of the pentose phosphate pathway (PPP) and an end product of the nonoxidative branch of the PPP. D-Ribose 5-phosphate is used in the synthesis of nucleotides and nucleic acids.
|
-
- HY-136512
-
Streptazolin
|
Antibiotic
|
Infection
Inflammation/Immunology
|
Streptazolin is an antibiotic. Streptazolin increases bacterial killing and elaboration of immunostimulatory cytokines by macrophages in vitro. Streptazolin stimulates the macrophage NF-κB pathway via PI3K signaling.
|
-
- HY-N0391S2
-
L-Citrulline-d6
|
Endogenous Metabolite
|
Others
|
L-Citrulline-d6 is the deuterium labeled L-Citrulline. L-Citrulline is an amino acid derived from ornithine in the catabolism of proline or glutamine and glutamate, or from l-arginine via arginine-citrulline pathway.
|
-
- HY-146445
-
-
- HY-17473
-
Embelin
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-17514S
-
Itraconazole-d5
|
Fungal
Hedgehog
Cytochrome P450
Autophagy
Antibiotic
|
Infection
Cancer
|
Itraconazole-d5 (R51211-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.
|
-
- HY-16558
-
Butein
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-144761
-
TOPK-p38/JNK-IN-1
|
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-N2217
-
-
- HY-N1420A
-
Rhamnose monohydrate
L-Rhamnose monohydrate
|
Others
|
Cancer
|
Rhamnose monohydrate (L-Rhamnose monohydrate) is a monosaccharide found in plants and bacteria. Rhamnose monohydrate-conjugated immunogens is used in immunotherapies. Rhamnose monohydrate crosses the epithelia via the transcellular pathway and acts as a marker of intestinal absorption.
|
-
- HY-N2490
-
-
- HY-B0835
-
Fenobucarb
|
Apoptosis
|
Neurological Disease
Cardiovascular Disease
|
Fenobucarb is a carbamate insecticide. Fenobucarb induces zebrafish developmental neurotoxicity through pathways involved in inflammation, oxidative stress, degeneration and apoptosis. Fenobucarb is a possible risk factor to cardiovascular and cerebrovascular systems in animals.
|
-
- HY-113108
-
(R)-3-Hydroxyisobutyric acid
|
Endogenous Metabolite
|
Metabolic Disease
|
(R)-3-Hydroxyisobutyric acid is an intermediate in the pathways of l-valine and thymine and plays an important role in the diagnosis of the very rare inherited metabolic diseases 3-hydroxyisobutyric aciduria and methylmalonic semialdehyde dehydrogenase deficiency.
|
-
- HY-144267
-
Glucosylceramide synthase-IN-2
|
Others
|
Metabolic Disease
Neurological Disease
|
Glucosylceramide synthase-IN-2 (compound T-690) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 15 nM and 190 nM for human GCS and mouse GCS, respectively.Glucosylceramide synthase-IN-2 exhibits noncompetitive type inhibition with C8-ceramide and UDP-glucose.Glucosylceramide synthase-IN-2 can be used for Gaucher's disease research.
|
-
- HY-147613
-
PI3K/mTOR Inhibitor-6
|
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-145963
-
DRB18
|
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-115620
-
AQX-016A
|
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-N1356S
-
-
- HY-P9931
-
Guselkumab
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-19528S
-
SAH-d4
SAH (S-Adenosylhomocysteine)-d4
|
Endogenous Metabolite
|
Metabolic Disease
|
SAH-d4 (SAH (S-Adenosylhomocysteine)-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. SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 µM.
|
-
- HY-103164
-
-
- HY-12383
-
Pelubiprofen
|
COX
|
Inflammation/Immunology
Neurological Disease
|
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.
|
-
- HY-114413
-
YZ129
|
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-122198
-
ML367
|
Others
|
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-N1445
-
Isoquercetin
Quercetin 3-glucoside
|
NF-κB
NO Synthase
|
Inflammation/Immunology
Cancer
|
Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway. Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies.
|
-
- HY-144332
-
PHD2/HDACs-IN-1
|
HDAC
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
PHD2/HDACs-IN-1 is a potent PHD2/HDACs hybrid inhibitor (IC50s of 1.15 μM, 19.75 μM, 26.60 μM and 15.98 μM for PHD2, HDAC1, HDAC2 and HDAC6, respectively). PHD2/HDACs-IN-1 is a low-toxicity renoprotective agent for research of cisplatin-induced acute kidney injury (AKI).
|
-
- HY-143881
-
FGFR4-IN-6
|
FGFR
|
Cancer
|
FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC50 value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity.
|
-
- HY-145951
-
Amidate-VC-PAB-MMAF
|
Drug-Linker Conjugates for ADC
|
Cancer
|
Amidate-VC-PAB-MMAF consists a cleavable ADC linker (Amidate-VC-PAB) and a potent tubulin polymerization inhibitor (MMAF). Amidate-VC-PAB-MMAF can be used in the synthesis of antibody-drug conjugates (ADCs). Amidate-VC-PAB-MMAF reduces off-target cytotoxicity of ADCs.
|
-
- HY-W018004S
-
L-Homocitrulline-d3
|
Endogenous Metabolite
|
Metabolic Disease
|
L-Homocitrulline-d3 is the deuterium labeled L-Homocitrulline. L-Homocitrulline is metabolized to homoarginine through homoargininosuccinate via the urea cycle pathway and its metabolic abnormality could lead to Lysinuric Protein Intolerance (LPI).
|
-
- HY-N2477
-
Taraxerol
|
Apoptosis
NF-κB
|
Cancer
Inflammation/Immunology
|
Taraxerol is isolated from Abroma augusta L, and has anti-inflammtory and anti-cancer effects. Taraxerol attenuates acute inlammation through inhibition of NF-κB signaling pathway. Taraxerol induces cell apoptosis.
|
-
- HY-111876
-
SNIPER(TACC3)-1
|
SNIPERs
|
Cancer
|
SNIPER(TACC3)-1 targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway based on IAP ligand. SNIPER(TACC3)-1 induces cancer cell death.
|
-
- HY-N0682
-
-
- HY-117089
-
Tetraconazole
|
Fungal
|
Infection
|
Tetraconazole, a chiral triazole fungicide, is widely used for the prevention of plant disease in wheat fields. Tetraconazole alters the methionine and ergosterol biosynthesis pathways in Saccharomyces yeasts promoting changes on volatile derived compounds.
|
-
- HY-111877
-
SNIPER(TACC3)-2
|
SNIPERs
|
Cancer
|
SNIPER(TACC3)-2 targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway based on IAP ligand. SNIPER(TACC3)-2 induces cancer cell death.
|
-
- HY-W009371
-
D-Ribose 5-phosphate disodium
|
DNA/RNA Synthesis
|
Metabolic Disease
|
D-Ribose 5-phosphate disodium is an intermediate of the oxidative branch of the pentose phosphate pathway (PPP) and an end product of the nonoxidative branch of the PPP. D-Ribose 5-phosphate disodium is used in the synthesis of nucleotides and nucleic acids.
|
-
- HY-W009371C
-
-
- HY-113224S
-
Desmosterol-d6
|
Endogenous Metabolite
|
Metabolic Disease
|
Desmosterol-d6 is the deuterium labeled Desmosterol. Desmosterol is a molecule similar to cholesterol. Desmosterol is the immediate precursor of cholesterol in the Bloch pathway of cholesterol biosynthesis. Desmosterol, as an endogenous metabolite, used to study cholesterol metabolism.
|
-
- HY-N2357
-
-
- HY-N8498
-
GKK1032B
|
Apoptosis
|
Cancer
|
GKK1032B is an alkaloid compound that can be found in endophytic fungus Penicillium sp. GKK1032B can induce the apoptosis of human osteosarcoma MG63 cells through caspase pathway activation.
|
-
- HY-110133
-
JTE-607
|
Interleukin Related
|
Inflammation/Immunology
|
JTE-607, a highly selective inflammatory cytokine synthesis inhibitor, protects from endotoxin shock in mice. JTE-607 inhibits inflammatory cytokine production, including TNF-α, IL-1β, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC50s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively. Cleavage and Polyadenylation Specificity Factor 3 (CPSF3) is the target of JTE-607.
|
-
- HY-B0094S1
-
Artemisinin-d4
Qinghaosu-d4; NSC 369397-d4
|
HCV
Parasite
Akt
Ferroptosis
|
Cancer
Infection
Neurological Disease
|
Artemisinin-d4 (Qinghaosu-d4) is the deuterium labeled Artemisinin. Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial drug 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-128872
-
-
- HY-115888
-
MIF2-IN-1
|
Others
|
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-146287
-
Zn(BQTC)
|
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-130723
-
AMPK activator 2
|
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-146743
-
Antitumor agent-53
|
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-111875
-
SNIPER(BRD)-1
|
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-B0252S
-
Hydrochlorothiazid-d2
HCTZ-d2
|
TGF-beta/Smad
Potassium Channel
|
Metabolic Disease
Cardiovascular Disease
|
Hydrochlorothiazid-d2 (HCTZ-d2) is the deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic drug 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-B0185S1
-
Lidocaine-d10
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cancer
Cardiovascular Disease
|
Lidocaine-d10 is the deuterium labeled Lidocaine. 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-N2259
-
Curcumenol
(+)-Curcumenol
|
Cytochrome P450
|
Cancer
Inflammation/Immunology
Neurological Disease
|
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-100487
-
TAK-243
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-P1791
-
Lactoferrin (17-41)
Lactoferricin B; Lfcin B
|
Bacterial
Fungal
Apoptosis
|
Cancer
Infection
|
Lactoferrin 17-41 (Lactoferricin B), a peptide corresponding to residues 17-41 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms, including Gram-positive and Gramnegative bacteria, viruses, protozoa, and fungi. Lactoferrin 17-41 has antitumor activities.
|
-
- HY-P1791B
-
Lactoferrin (17-41) (acetate)
Lactoferricin B acetate; Lfcin B acetate
|
Bacterial
Fungal
Apoptosis
|
Cancer
Infection
|
Lactoferrin 17-41 (Lactoferricin B) acetate, a peptide corresponding to residues 17-41 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms, including Gram-positive and Gramnegative bacteria, viruses, protozoa, and fungi. Lactoferrin 17-41 acetate has antitumor activities.
|
-
- HY-16563
-
Narciclasine
Lycoricidinol
|
ROCK
|
Cancer
|
Narciclasine is a plant growth modulator. Narciclasine modulates the Rho/Rho kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity as well as inducing actin stress fiber formation in a RhoA-dependent manner.
|
-
- HY-12848
-
SAG
|
Smo
|
Cancer
|
SAG is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo.
|
-
- HY-108439
-
Neurodazine
|
Wnt
Hedgehog
|
Neurological Disease
|
Neurodazine is an imidazole-based small molecule, serve as a promoter of neurogenesisin pluripotent cells. Neurodazine promotes neurogenesis by activating Wnt and Shh signaling pathways. Neurodazine selectively suppresses astrocyte differentiation of P19 cells.
|
-
- HY-113131
-
Dihydroxyacetone phosphate
|
Endogenous Metabolite
|
Metabolic Disease
|
Dihydroxyacetone phosphate is an important intermediate in lipid biosynthesis and in glycolysis. It is a biochemical compound involved in many metabolic pathways, including the Calvin cycle in plants and glycolysis. Dihydroxyacetone phosphate is found to be associated with transaldolase deficiency, which is an inborn error of metabolism.
|
-
- HY-12848B
-
SAG hydrochloride
|
Smo
|
Cancer
|
SAG hydrochloride is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG hydrochloride activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo.
|
-
- HY-17363S
-
Dimethyl fumarate-d6
|
Keap1-Nrf2
|
Inflammation/Immunology
|
Dimethyl fumarate D6 is a deuterium labeled Dimethyl fumarate. Dimethyl fumarate is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator and induces upregulation of antioxidant gene expression.
|
-
- HY-N0608
-
Myrislignan
|
NF-κB
|
Inflammation/Immunology
|
Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation.
|
-
- HY-12754
-
ML228
CID-46742353
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
ML228 (CID-46742353) is a potent the Hypoxia Inducible Factor (HIF) pathway activator with EC50 of 1 μM. ML228 potently activates HIF in vitro as well as its downstream target VEGF.
|
-
- HY-113206
-
-
- HY-N0391S3
-
L-Citrulline-13C
|
Endogenous Metabolite
|
Others
|
L-Citrulline-13C is the 13C-labeled L-Citrulline. L-Citrulline is an amino acid derived from ornithine in the catabolism of proline or glutamine and glutamate, or from l-arginine via arginine-citrulline pathway.
|
-
- HY-116015
-
-
- HY-129098
-
DMHCA
|
LXR
|
Metabolic Disease
|
DMHCA, a potent and selective LXR agonist, specifically activates the cholesterol efflux arm of the LXR pathway without stimulating triglyceride synthesis. DMHCA has anti-inflammatory effects and can be used for the research of cholesterol homeostasis diabetes.
|
-
- HY-144707
-
AK-778-XXMU
|
Apoptosis
|
Cancer
|
AK-778-XXMU is a potent inhibitor of DNA Binding 2 (ID2) antagonist with a KD of 129 nM. AK-778-XXMU can inhibit cell migration and invasion of glioma cell lines, induce apoptosis, and more importantly, slow down the tumor growth.
|
-
- HY-122214
-
AC-73
|
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 drug and an inducer of autophagy in leukemic cells.
|
-
- HY-N1372A
-
Fangchinoline
|
HIV
FAK
Apoptosis
Autophagy
|
Cancer
Infection
|
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-13811
-
NSC697923
|
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-121537
-
CAY10404
|
COX
Akt
Apoptosis
|
Cancer
Inflammation/Immunology
Neurological Disease
|
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-144765
-
NF-κB-IN-4
|
NF-κB
Apoptosis
|
Inflammation/Immunology
Neurological Disease
|
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-107024
-
Osteogenic Growth Peptide (10-14)
OGP(10-14); Historphin
|
Src
|
Others
|
Osteogenic Growth Peptide (10-14) (OGP(10-14)), the C-terminal truncated pentapeptide of osteogenic growth peptide (OGP), retains the full OGP-like activity. Osteogenic Growth Peptide (10-14) is responsible for the binding to the OGP receptor and activates an intracellular Gi-protein-MAP kinase signaling pathway. Osteogenic Growth Peptide (10-14) is a potent mitogen and stimulator of osteogenesis and hematopoiesis. Osteogenic Growth Peptide (10-14) acts as a Src inhibitor.
|
-
- HY-120419
-
PF9601N
|
Monoamine Oxidase
|
Neurological Disease
|
PF9601N, an monoamine oxidase B (MAO-B) inhibitor, possesses neuroprotective properties in several in vitro and in vivo models of Parkinson's disease (PD). PF9601N can be used for the research of neurodegenerative diseases mediated by excitotoxicity.
|
-
- HY-128861A
-
ACT001
|
PAI-1
STAT
PI3K
Akt
Apoptosis
|
Cancer
Inflammation/Immunology
|
ACT001 is an orally active PAI-1 inhibitor by inhibiting the phosphorylation of PI3K and AKT. ACT001 inhibits the phosphorylation of STAT3 and PD-L1 expression by directly binding to STAT3. ACT001, a fumarate salt form of DMAMCL (a prodrug of Micheliolide), can cross the blood-brain barrier. ACT001 exerts synergistic effects in combination with Cisplatin (HY-17394) by inhibiting PI3K/AKT pathway in glioma. ACT001 has potent anti-glioblastoma (GBM) activity and immunomodulatory effects.
|
-
- HY-113013A
-
Hydroxypyruvic acid lithium hydrate
β-Hydroxypyruvic acid lithium hydrate; 3-Hydroxypyruvic acid lithium hydrate
|
Endogenous Metabolite
|
Metabolic Disease
|
Hydroxypyruvic acid lithium hydrate (β-Hydroxypyruvic acid lithium hydrate) is an intermediate in the metabolism of glycine, serine and threonine. Hydroxypyruvic acid lithium hydrate is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase. Hydroxypyruvic acid lithium hydrate is involved in the metabolic disorder which is the dimethylglycine dehydrogenase deficiency pathway.
|
-
- HY-101981
-
Uridine 5'-monophosphate
5'-Uridylic acid
|
Endogenous Metabolite
|
Others
|
Uridine 5'-monophosphate (5'-Uridylic acid), a monophosphate form of UTP, can be acquired either from a de novo pathway or degradation products of nucleotides and nucleic acids in vivo and is a major nucleotide analogue in mammalian milk.
|
-
- HY-N0427
-
Phellodendrine
|
Akt
NF-κB
|
Inflammation/Immunology
|
Phellodendrine, a isoquinoline alkaloid, is one of important characteristic ingredients in the Phellodendri chinensis cortex. phellodendrine is against AAPH-induced oxidative stress through regulating the AKT/NF-κB pathway. Phellodendrine has good antioxidant, and anti-inflammatory effect .
|
-
- HY-N4253
-
Kudinoside D
|
Others
|
Metabolic Disease
|
Kudinoside D is a main natural component of triterpenoid saponin derived from Ilex kudingcha. Kudinoside D suppresses adipogenesis through modulation of the AMPK pathway in 3T3-L1 adipocytes.
|
-
- HY-136433
-
N,N'-Dinitrosopiperazine
1,4-Dinitrosopiperazine; DNP
|
Others
|
Cancer
|
N,N'-Dinitrosopiperazine (1,4-Dinitrosopiperazine; DNP) is a carcinogen with specificity for nasopharyngeal epithelium and facilitates NPC metastasis. N,N'-Dinitrosopiperazine regulates multiple signaling pathways through protein phosphorylation, including LYRIC at serine 568.
|
-
- HY-107091
-
Aspartyl-alanyl-diketopiperazine
DA-DKP
|
Others
|
Inflammation/Immunology
|
Aspartyl-alanyl-diketopiperazine (DA-DKP) is an immunomodulatory molecule generated by cleavage and cyclization from the N-terminus of human albumin and can modulate the inflammatory immune response through a molecular pathway implicated in T- lymphocyte anergy.
|
-
- HY-N5106
-
(E)-Flavokawain A
|
Apoptosis
|
Cancer
|
(E)-Flavokawain A, a chalcone extracted from Kava, has anticarcinogenic effect. (E)-Flavokawain A induces apoptosis in bladder cancer cells by involvement of bax protein-dependent and mitochondria-dependent apoptotic pathway and suppresses tumor growth in mice.
|
-
- HY-N6076
-
Tenuifoliside A
|
ERK
|
Neurological Disease
|
Tenuifoliside A is isolated from Polygala tenuifolia, has anti-apoptotic and antidepressant-like effects. Tenuifoliside A exhibits its neneurotrophic effects and promotes cell proliferation through the ERK/CREB/BDNF signal pathway in C6 cells.
|
-
- HY-100807
-
-
- HY-W008820S
-
Glutaric acid-d6
|
Endogenous Metabolite
|
Metabolic Disease
|
Glutaric acid-d6 is the deuterium labeled Glutaric acid. Glutaric acid is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I.
|
-
- HY-W011417
-
Cinnabarinic acid
|
mGluR
Apoptosis
|
Others
|
Cinnabarinic acid is a specific orthosteric agonist of mGlu4 by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis.
|
-
- HY-N8107
-
Matairesinol monoglucoside
|
Others
|
Others
|
Matairesinol monoglucoside, a lignan compound, exhibits low activity on IFN-γ/STAT1 and IL-6/STAT3 signaling pathways with inhibition ratio of 5.8% and 7.0%, respectively.
|
-
- HY-124151
-
Adenosine-2'-monophosphate
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
-
Lidocaine-d10 N-Oxide
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cancer
Cardiovascular Disease
|
Lidocaine-d10 N-Oxide is the deuterium labeled Lidocaine. 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-N0631
-
Cornuside
|
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-B0965A
-
Thioridazine
|
Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Neurological Disease
|
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-133033
-
COQ7-IN-1
|
Others
|
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-N2996
-
Ganodermanondiol
|
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-B0252S1
-
Hydrochlorothiazid-13C,d2
HCTZ-13C,d2
|
TGF-beta/Smad
Potassium Channel
|
Metabolic Disease
Cardiovascular Disease
|
Hydrochlorothiazid-13C,d2 is the 13C- and deuterium labeled. Hydrochlorothiazide (HCTZ), an orally active diuretic drug 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-147614
-
PI3K/mTOR Inhibitor-7
|
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-144739
-
-
- HY-144741
-
-
- HY-N2420
-
Flavokawain A
|
Apoptosis
|
Cancer
|
Flavokawain A, a proming anticarcinogenic agent, is a chalcone from kava extract with anti-tumor activity. Flavokawain A induces cell apoptosis by involvement of Bax protein-dependent and mitochondria-dependent apoptotic pathway. Flavokawain A has the potential for the study of bladder cancer.
|
-
- HY-N0171A
-
-
- HY-113131A
-
Dihydroxyacetone phosphate hemimagnesium hydrate
|
Endogenous Metabolite
|
Metabolic Disease
|
Dihydroxyacetone phosphate hemimagnesium hydrate is an important intermediate in lipid biosynthesis and in glycolysis. It is a biochemical compound involved in many metabolic pathways, including the Calvin cycle in plants and glycolysis. Dihydroxyacetone phosphate hemimagnesium hydrate is found to be associated with transaldolase deficiency, which is an inborn error of metabolism.
|
-
- HY-103252S1
-
-
- HY-116506
-
Bigelovin
|
RAR/RXR
Reactive Oxygen Species
Apoptosis
Autophagy
|
Cancer
|
Bigelovin, a sesquiterpene lactone isolated from Inula helianthus-aquatica, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.
|
-
- HY-108417
-
Debio 0617B
|
STAT
JAK
Bcr-Abl
|
Cancer
|
Debio 0617B, a multi-kinase inhibitor, reduces maintenance and self-renewal of primary human AML CD34 + stem/progenitor cells. Debio 0617B has a unique profile targeting key kinases upstream of STAT3/STAT5 signaling such as JAK, SRC, ABL, and class III/V receptor tyrosine kinases (TKs). Debio 0617B has documented efficacy in STAT3-driven solid tumors.
|
-
- HY-N0373
-
Licochalcone B
|
Amyloid-β
Apoptosis
NOD-like Receptor (NLR)
|
Neurological Disease
|
Licochalcone B is an extract from the root of Glycyrrhiza inflate. 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-14117
-
-
- HY-146680
-
FLT3/ITD-IN-4
|
FLT3
RET
CDK
MAP4K
|
Cancer
|
FLT3/ITD-IN-4 (Compound 16) is a selective FMS-like tyrosine kinase 3 internal tandem duplications (FLT3-ITD) inhibitor with an IC50 of 2.3 nM. FLT3/ITD-IN-4 can be used for acute myeloid leukemia research.
|
-
- HY-125197
-
BRD5631
|
Autophagy
|
Inflammation/Immunology
|
BRD5631 is an autophagy enhancer, enhances autophagy through an mTOR-independent pathway. BRD5631 affects several cellular disease phenotypes previously linked to autophagy, including protein aggregation, cell survival, bacterial replication, and inflammatory cytokine production.
|
-
- HY-N0608A
-
(Rac)-Myrislignan
|
NF-κB
|
Inflammation/Immunology
|
(Rac)-Myrislignan is the racemate of Myrislignan. Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation.
|
-
- HY-N2993
-
Polyporenic acid C
|
Apoptosis
|
Cancer
|
Polyporenic acid C is a lanostane-type triterpenoid isolated from P. cocos. Polyporenic acid C induces cell apoptosis through the death receptor-mediated apoptotic pathway without the involvement of the mitochondria. Polyporenic acid C is promising agent for lung cancer therapy.
|
-
- HY-N3376
-
Liriodenine
Spermatheridine; VLT045
|
Apoptosis
|
Cancer
|
Liriodenine (Spermatheridine; VLT045) is an aporphine alkaloid isolated from the plant Mitrephora sirikitiae and has anti-cancer activities. Liriodenine induces cell apoptosis, activates the intrinsic pathway by induction of caspase-3 and caspase-9.
|
-
- HY-100490B
-
Rilmenidine phosphate
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cancer
Cardiovascular Disease
|
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-B0185AS
-
Lidocaine-d10 hydrochloride
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cancer
Cardiovascular Disease
|
Lidocaine-d10 (Lignocaine-d10) hydrochloride is the deuterium labeled Lidocaine hydrochloride. 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, an amide derivative, has the potential for the research of the ventricular arrhythmia.
|
-
- HY-B0965
-
-
- HY-100490
-
Rilmenidine
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cancer
Cardiovascular Disease
|
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.
|
-
- HY-N6064
-
Polygalacin D
|
Apoptosis
IAP
|
Cancer
|
Polygalacin D (PGD) is a bioactive compound isolated from Platycodon grandiflorum (Jacq.) 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-146971
-
Nrf2/HO-1-IN-1
|
NO Synthase
ROS
|
Inflammation/Immunology
|
Nrf2/HO-1-IN-1 is a potent Nrf2/HO-1 pathway inhibitor, with an IC50 value of 0.38 μM for NO. Nrf2/HO-1-IN-1 can significantly reduce the level of ROS in cells. Nrf2/HO-1-IN-1 can be used for researching anti-inflammatory.
|
-
- HY-146884
-
MET kinase-IN-3
|
c-Met/HGFR
VEGFR
|
Cancer
|
MET kinase-IN-3 (compound 8) is an orally active and potent MET inhibitor, with an IC50 of 9.8 nM. MET kinase-IN-3 shows good and broad-spectrum antiproliferative activity against cancer cell lines.
|
-
- HY-N9480
-
Vinaxanthone
SM-345431
|
Phospholipase
|
Cancer
|
Vinaxanthone (SM-345431) is a potent and selective semaphorin3A inhibitor. Vinaxanthone exhibits semaphorin3A inhibiting activity with an IC50 of 0.1-0.2 μM. Vinaxanthone shows selective inhibitory activity against phospholipase C (PLC) from rat brain, mutine colon 26 Adenocarcinoma and murine fibroblasts NIH3T3 with IC50s being 5.4, 9.3 and 44 μM, respectively.
|
-
- HY-120793
-
CMC2.24
TRB-N0224
|
Ras
Apoptosis
MMP
|
Cancer
Inflammation/Immunology
|
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-144450
-
PI3K-IN-29
|
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-147691
-
MPO-IN-5
|
Glutathione Peroxidase
Potassium Channel
|
Inflammation/Immunology
|
MPO-IN-5 (compound 1) is a potent, irreversible MPO (myeloperoxidase) inhibitor. MPO-IN-5 inhibits MPO peroxidation and hERG binding, with IC50 values of 0.22 and 2.8 μM, respectively. MPO-IN-5 shows rapid kinetics of inhibition, with enzyme inactivation rate (kinact/Ki) of 23000 M −1s −1.
|
-
- HY-19961
-
KIN1408
|
HCV
Influenza Virus
|
Infection
|
KIN1408 is an agonist of the RIG-1-like receptor (RLR) pathway and exhibits a broad-spectrum antiviral activity. KIN1408 exhibits activity against HCV, influenza A, dengue virus 2, Ebola, Nipah, and Lassa viruses.
|
-
- HY-119500
-
-
- HY-W008820S1
-
Glutaric acid-d4
|
Endogenous Metabolite
|
Metabolic Disease
|
Glutaric acid-d4 is the deuterium labeled Glutaric acid. Glutaric acid, C5 dicarboxylic acid, is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I.
|
-
- HY-142693
-
-
- HY-W008820S2
-
Glutaric acid-d2
|
Endogenous Metabolite
|
Metabolic Disease
|
Glutaric acid-d2 is the deuterium labeled Glutaric acid. Glutaric acid, C5 dicarboxylic acid, is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I.
|
-
- HY-113573
-
Protosappanin A
PTA
|
JAK
STAT
|
Inflammation/Immunology
|
Protosappanin A (PTA), an immunosuppressive ingredient and major biphenyl compound isolated from Caesalpinia sappan L, suppresses JAK2/STAT3-dependent inflammation pathway through down-regulating the phosphorylation of JAK2 and STAT3.
|
-
- HY-145848
-
-
- HY-143434
-
FLT3/D835Y-IN-1
|
FLT3
|
Cancer
|
FLT3/D835Y-IN-1 (compound 13a) is a orally active, potent and selective FLT3 and FLT3/D835Y inhibitor, with IC50 values of 0.26 nM and 0.18 nM, respectively. FLT3/D835Y-IN-1 also blocks tumor growth, has anticancer efficacy, and can be used to research for AML (acute myeloid leukemia).
|
-
- HY-143718
-
JAK3/BTK-IN-3
|
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-146033
-
HPV18-IN-1
|
Others
|
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-112671
-
CDDO-dhTFEA
RTA dh404
|
Keap1-Nrf2
NF-κB
|
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.
|
-
- HY-100490A
-
Rilmenidine hemifumarate
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cancer
Cardiovascular Disease
|
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
-
JAK3/BTK-IN-2
|
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-19528S1
-
SAH-13C5
SAH (S-Adenosylhomocysteine)-13C5
|
Endogenous Metabolite
|
Metabolic Disease
|
SAH-13C5 (SAH (S-Adenosylhomocysteine)-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. SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 µM.
|
-
- HY-143720
-
JAK3/BTK-IN-5
|
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, compound 35)
|
-
- HY-143719
-
JAK3/BTK-IN-4
|
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
-
Scutellarin
|
STAT
Akt
HIV
|
Cancer
Infection
|
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-143716
-
JAK3/BTK-IN-1
|
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-117983
-
RU-505
|
Amyloid-β
|
Neurological Disease
|
RU-505 is an effective β-amyloid (Aβ)-fibrinogen interaction inhibitor with IC50s of 5.00 and 2.72 μM in fluorescence polarization (FP) and AlphaLISA assays, respectively. RU-505 is highly permeable to the BBB. RU-505 reduces cerebral amyloid angiopathy (CAA). RU-505 can be used for the research of Alzheimer’s disease (AD).
|
-
- HY-N7496
-
Odoroside A
|
Apoptosis
|
Cancer
|
Odoroside A is an active ingredient extracted from the leaves of Nerium oleander Linn. Odoroside A has anti-cancer activity. Odoroside A could induce apoptosis and cell cycle arrest through ROS/p53 signaling pathway, leading to the tumor cell death.
|
-
- HY-W008956
-
Myoseverin
|
Microtubule/Tubulin
|
Inflammation/Immunology
|
Myoseverina, a microtubule-binding molecule, induces the reversible fission of multinucleated myotubes into mononucleated fragments. Myoseverina affects the expression of a variety of growth factor, immunomodulatory, extracellular matrix-remodeling, and stress response genes, consistent with the activation of pathways involved in wound healing and tissue regeneration.
|
-
- HY-N6872
-
Actein
|
JNK
Akt
Apoptosis
Autophagy
|
Cancer
|
Actein is a triterpene glycoside isolated from the rhizomes of Cimicifuga foetida. Actein suppresses cell proliferation, induces autophagy and apoptosis through promoting ROS/JNK activation, and blunting AKT pathway in human bladder cancer. Actein has little toxicity in vivo.
|
-
- HY-147656
-
NAMPT degrader-1
|
NAMPT
Autophagy
|
Cancer
|
NAMPT degrader-1 (Compound A3) is an nicotinamide phosphoribosyltransferase (NAMPT) degrader with an IC50 of 0.023 μM. NAMPT degrader-1 significantly induces the degradation of NAMPT through the autophagy-lysosomal pathway and shows excellent cellular antitumor potency.
|
-
- HY-N0119
-
Naringin Dihydrochalcone
Naringin DC
|
NF-κB
|
Cancer
|
Naringin Dihydrochalcone is an artificial sweetener derived from naringin. Naringin is a major flavanone glycoside obtained from tomatoes, grapefruits, and many other citrus fruits. Naringin exhibits biological properties such as antioxidant, anti-inflammatory, and antiapoptotic activities. Naringin suppresses NF-κB signaling pathway.
|
-
- HY-B1899A
-
Taurodeoxycholic acid sodium hydrate
Sodium taurodeoxycholate monohydrate
|
Caspase
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
|
Taurodeoxycholic acid sodium hydrate (Sodium taurodeoxycholate monohydrate) prevents apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid sodium hydrate is investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.
|
-
- HY-12316
-
20(S)-Hydroxycholesterol
20α-Hydroxycholesterol
|
Smo
Endogenous Metabolite
|
Cancer
|
20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells.
|
-
- HY-146351
-
HDAC-IN-38
|
HDAC
|
Neurological Disease
|
HDAC-IN-38 (compound 13) is a potent HDAC inhibitor. HDAC-IN-38 shows similar micro-molar inhibitory activity toward HDAC1, 2, 3, 5, 6, and 8. HDAC-IN-38 increases cerebral blood flow (CBF), attenuates cognitive impairment, and improves hippocampal atrophy. HDAC-IN-38 also increases the level of histone acetylation (H3K14 or H4K5).
|
-
- HY-147695
-
c-Met-IN-12
|
c-Met/HGFR
|
Cancer
|
c-Met-IN-12 (compound 4r) is an orally active, potent and selective type II c-Met kinase inhibitor, with an IC50 of 10.6 nM. c-Met-IN-12 displays high inhibitory effects (inhibition rate > 80% in 1 μM) against AXL, Mer and TYRO3 kinases. c-Met-IN-12 can be used a scaffold for further kinase selectivity enhancement. c-Met-IN-12 shows antitumor efficacy.
|
-
- HY-146323
-
Antitumor agent-58
|
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-135699
-
TD52
|
Apoptosis
Phosphatase
Akt
|
Cancer
|
TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity.
|
-
- HY-138188
-
KRA-533
|
Ras
|
Cancer
|
KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells.
|
-
- HY-N0496
-
Ruscogenin
|
NOD-like Receptor (NLR)
|
Cardiovascular Disease
|
Ruscogenin, an important steroid sapogenin derived from Ophiopogon japonicus, attenuates cerebral ischemia-induced blood-brain barrier dysfunction by suppressing TXNIP/NLRP3 inflammasome activation and the MAPK pathway and exerts significant anti-inflammatory and anti-thrombotic activities.
|
-
- HY-13755A
-
(R)-Sulforaphane
L-Sulforaphane
|
Others
|
Cancer
|
(R)-Sulforaphane (L-Sulforaphane) is a highly potent inducer of the Keap1/Nrf2/ARE pathway. (R)-Sulforaphane is a far more potent inducer of the carcinogen-detoxifying enzyme systems in rat liver and lung than the S-isomer.
|
-
- HY-N0682S1
-
Pyridoxine-d2 hydrochloride
Pyridoxol-d2 hydrochloride; Vitamin B6-d2 hydrochloride
|
Endogenous Metabolite
Keap1-Nrf2
|
Neurological Disease
|
Pyridoxine-d2 (Pyridoxol-d2) hydrochloride is the deuterium labeled Pyridoxine hydrochloride. Pyridoxine hydrochloride is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
|
-
- HY-N3796
-
Echinulin
Echinuline
|
NF-κB
|
Inflammation/Immunology
|
Echinulin (Echinuline) is a cyclic dipeptide carrying a triprenylated indole moiety. Echinulin contributes to the activation of T cell subsets, which leads to NF-κB activation.Echinulin exerts its immune roles by the NF-κB pathway.Echinulin has the potential to serve as a immunotherapeutic agent.
|
-
- HY-107855
-
DL-Mevalonolactone
(±)-Mevalonolactone; Mevalolactone
|
Endogenous Metabolite
|
Metabolic Disease
|
DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential (∆Ψm), NAD(P)H content and the capacity to retain Ca 2+ in the brain, besides inducing mitochondrial swelling.
|
-
- HY-125355
-
SEC
|
Apoptosis
|
Cancer
|
SEC induces activation of ANXA7 GTPase via the AMPK/mTORC1/STAT3 signaling pathway. SEC selectively promotes apoptosis in cancer cells, expressing a high level of ITGB4 by inducing ITGB4 nuclear translocation.
|
-
- HY-118783
-
2-Hexyl-4-pentynoic acid
(±)-2-Hexyl-4-pentynoic acid
|
HDAC
HSP
|
Neurological Disease
|
2-Hexyl-4-pentynoic acid ((±)-2-Hexyl-4-pentynoic acid), valproic acid (VPA) derivative, exhibits potential roles of HDAC inhibition (IC50=13 µM) and HSP70 induction. Potent neuroprotective effects. 2-Hexyl-4-pentynoic acid causes histone hyperacetylation and protect against glutamate-induced excitotoxicity in cultured neurons.
|
-
- HY-115975
-
GRPR antagonist-2
|
Others
|
Cancer
|
GRPR antagonist-2 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 0.77 and 2.5 μM in HGC-27 and Pan02 cells, respectively). Anticancer activity.
|
-
- HY-112823A
-
Almonertinib mesylate
HS-10296 mesylate
|
EGFR
|
Cancer
|
Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer.
|
-
- HY-10182B
-
Laduviglusib trihydrochloride
CHIR-99021 trihydrochloride; CT99021 trihydrochloride
|
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-131972
-
PF-06843195
|
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-50907
-
ABT-737
|
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-10182
-
Laduviglusib
CHIR-99021; CT99021
|
GSK-3
Wnt
β-catenin
Autophagy
|
Cancer
|
Laduviglusib (CHIR-99021) is a potent and selective 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-100490S
-
Rilmenidine-d4
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cancer
Cardiovascular Disease
|
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.
|
-
- HY-146725
-
FBPase-IN-1
|
Others
|
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-12383S
-
Pelubiprofen-13C,d3
|
COX
|
Inflammation/Immunology
Neurological Disease
|
Pelubiprofen-13C,d3 is the 13C- and deuterium labeled. 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.
|
-
- HY-B0965AS
-
Thioridazine-d3 hydrochloride
|
Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Neurological Disease
|
Thioridazine-d3 hydrochloride is the deuterium labeled Thioridazine. 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-107944
-
Chlorphenesin carbamate
Maolate; U 19646
|
Others
|
Neurological Disease
|
Chlorphenesin carbamate is a centrally acting skeletal muscle relaxant. Chlorphenesin carbamate can be used for the research of pain and discomfort related to skeletal muscle trauma and inflammation. Chlorphenesin carbamate is a selective blocker of polysynaptic pathways at the spinal and supra-spinal levels. Antinociceptive effect.
|
-
- HY-130116A
-
IACS-8779 disodium
|
STING
|
Cancer
|
IACS-8779 disodium is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy. IACS-8779 disodium shows robust activation of the STING pathway in vitro and a superior systemic anti-tumor response in the B16 murine model of melanoma.
|
-
- HY-128790S1
-
4-Methoxyestrone-13C6
|
Endogenous Metabolite
|
Metabolic Disease
|
4-Methoxyestrone-13C6 is a 13C-labeled 5'-Guanylic acid. 5'-Guanylic acid (5'-GMP) is involved in several metabolic disorders, including the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and
|
-
- HY-124136
-
WYC-209
|
RAR/RXR
Apoptosis
Autophagy
|
Cancer
|
WYC-209, a synthetic retinoid, is a retinoic acid receptor (RAR) agonist. WYC-209 induces apoptosis primarily via the caspase 3 pathway (IC50=0.19 μM for inmalignant murine melanoma TRCs), and has long-term effects with little toxicity.
|
-
- HY-137662
-
5'-Phosphoguanylyl-(3',5')-guanosine
pGpG
|
Others
|
Metabolic Disease
|
5'-Phosphoguanylyl-(3',5')-guanosine (pGpG) is an intermediate molecule produced by the pathway for enzymatic cyclic diguanylate (c-di-GMP) degradation. 5'-Phosphoguanylyl-(3',5')-guanosine can be used to detect the metabolism of nucleic acids.
|
-
- HY-19744
-
T6167923
|
MyD88
|
Inflammation/Immunology
|
T6167923 is a potent and 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 an 50 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.
|
-
- HY-112371
-
(S)-CR8
|
CDK
|
Cancer
|
(S)-CR8 is the S-isomer of CR8. (S)-CR8 is a potent and selective CDK inhibitor with IC50s of 0.060, 0.080, 0.11, 0.12, and 0.15 μM for CDK2/cyclin E, CDK2/cyclin A, CDK9/cyclin T, CDK5/p25, and CDK1/cyclin B, respectively. (S)-CR8 reduces SH-SY5Y cells survival (IC50 0.40 μM).
|
-
- HY-129566
-
-
- HY-110302
-
6'-GNTI dihydrochloride
|
Opioid Receptor
|
Neurological Disease
|
6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons.
|
-
- HY-Y1250S5
-
Fmoc-Gly-OH-13C2
|
Endogenous Metabolite
|
Inflammation/Immunology
|
Fmoc-Gly-OH-13C2 is a 13C-labeled Xanthine. Xanthine, a plant alkaloid found in tea, coffee, and cocoa, is a mild stimulant of the central nervous system. Xanthine also acts as an intermediate product on the pathway of purine degradation[1][2][3].
|
-
- HY-15129
-
O-Phospho-L-serine
L-Serine O-phosphate; L-SOP
|
mGluR
Endogenous Metabolite
|
Neurological Disease
|
O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2.
|
-
- HY-N2485
-
4'-Methoxyresveratrol
4'-O-Methylresveratrol
|
Others
|
Inflammation/Immunology
|
4'-Methoxyresveratrol (4'-O-Methylresveratrol) is a polyphenol derived from Dipterocarpaceae, with antiandrogenic, antifungal and anti-inflammatory activities. 4'-Methoxyresveratrol alleviates AGE-induced inflammation through suppressing RAGE-mediated MAPK/NF-κB signaling pathway and NLRP3 inflammasome activation.
|
-
- HY-100807S
-
-
- HY-114858
-
Epiblastin A
|
Casein Kinase
|
Cancer
|
Epiblastin A is an ATP competitive casein kinase 1 (CK1) inhibitor with IC50s of 8.9, 0.5, and 4.7 µM for CK1α, CK1δ, and CK1 ɛ, respectively. Epiblastin A induces reprogramming of epiblast stem cells into embryonic stem cells by inhibition of CK1.
|
-
- HY-79128S
-
-
- HY-119272
-
EF24
|
ERK
Caspase
|
Cancer
|
EF24 is a curcumin analogue with greater anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK.
|
-
- HY-N6973
-
Boldine
|
Others
|
Inflammation/Immunology
|
Boldine is an aporphine isoquinoline alkaloid extracted from the root of Litsea cubeba and also possesses these properties, including antioxidant, anti-inflammatory and cytoprotective effects. Boldine suppresses osteoclastogenesis, improves bone destruction by down-regulating the OPG/RANKL/RANK signal pathway and may be a potential therapeutic agent for rheumatoid arthritis.
|
-
- HY-N0682S
-
Pyridoxine-d3 hydrochloride
Pyridoxol-d3 hydrochloride; Vitamin B6-d3 hydrochloride
|
Endogenous Metabolite
Keap1-Nrf2
|
Neurological Disease
|
Pyridoxine-d3 (Pyridoxol-d3) hydrochloride is the deuterium labeled Pyridoxine hydrochloride. Pyridoxine hydrochloride (Pyridoxol; Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
|
-
- HY-117937
-
BC-1215
|
Ligands for E3 Ligase
|
Inflammation/Immunology
|
BC-1215 is an inhibitor of F-box protein 3 (FBXO3, a ubiquitin E3 ligase component, IC50=0.9 μg/mL for IL-1β release). BC-1215 decreases Fbxo3-Fbxl2 interaction and prevents SCF Fbxo3 catalyzed Fbxl2 ubiquitination. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1–TRAF6. BC-1215, interacts with ApaG to profoundly inhibit secretion of a broad spectrum of TH1 panel cytokines from human PBMC.
|
-
- HY-109041
-
Razuprotafib
AKB-9778
|
Phosphatase
|
Inflammation/Immunology
|
Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM).
|
-
- HY-136065
-
bpV(phen)
|
PTEN
Phosphatase
Parasite
Apoptosis
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
|
bpV(phen), a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
|
-
- HY-B1521
-
Aluminum Hydroxide
|
Others
|
Inflammation/Immunology
|
Aluminum Hydroxide is an orally active main form of aluminum used as adjuvant. Aluminum hydroxide-based adjuvant researches include the repository effect, pro-phagocytic effect, and activation of the pro-inflammatory NLRP3 pathway. Aluminum Hydroxide also acts as adjuvant to compensate low inherent immunogenicity of subunit vaccines.
|
-
- HY-N2438
-
Methylophiopogonanone B
|
Ras
|
Others
|
Methylophiopogonanone B, homoisoflavonoid, is extracted from the root of Ophiopogon japonicas, shows high antioxidant ability. Methylophiopogonanone B increases GTP-Rho and acts via the Rho signaling pathway, inducing cell morphological change via actin cytoskeletal reorganization, including dendrite retraction and stress fiber formation.
|
-
- HY-N0171B
-
Beta-Sitosterol (purity>75%)
β-Sitosterol (purity>75%); 22,23-Dihydrostigmasterol (purity>75%)
|
Apoptosis
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
Beta-Sitosterol (purity>75%) includes 75% β-sitosterol and 10% campesterol. Beta-Sitosterol is a plant sterol. Beta-Sitosterol (purity>75%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
|
-
- HY-N6901
-
Luteolin 7-sulfate
|
Others
|
Metabolic Disease
|
Luteolin 7-sulfate is isolated from Phyllospadix iwatensis Makino, a marine plant. Luteolin 7-sulfate attenuates TYR gene expression through the intervention of a cAMP-responsive element binding protein (CREB)- and microphthalmia-associated transcription factor (MITF)-mediated signaling pathway, leading to the decreased melanin synthesis.
|
-
- HY-N5112B
-
β,β-Dimethylacrylshikonin
Isoarnebin I
|
Others
|
Cancer
|
β,β-Dimethylacrylshikonin (Isoarnebin I) is a naphthoquinone derivative isolated from Arnebia nobilis, promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway.β,β-Dimethylacrylshikonin has anti-tumor activity.
|
-
- HY-17363
-
-
- HY-117066
-
CL075
3M002
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
CL075 (3M002) is a selective TLR8 agonist with immunomodulating properties. CL075 triggers a MyD88-dependent signaling pathway to elicit production of inflammatory cytokines and type I interferons (IFNs) via activation of NF-κB and IRF7, respectively.
|
-
- HY-146093
-
Antitumor agent-62
|
Apoptosis
|
Cancer
|
Antitumor agent-62 (Compound 47) is a NO-releasing antitumor agent. Antitumor agent-62 shows antiproliferative activity against four cancer cell lines. Antitumor agent-62 activates mitochondrial apoptosis pathway and arrests cell cycle at G2/M phase.
|
-
- HY-B0965S
-
Thioridazine-d3 2-Sulfone
|
Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Cancer
Infection
Neurological Disease
|
Thioridazine-d3 2-Sulfone is the deuterium labeled Thioridazine hydrochloride. 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).
|
-
- HY-10182A
-
Laduviglusib monohydrochloride
CHIR-99021 monohydrochloride; CT99021 monohydrochloride
|
GSK-3
Wnt
β-catenin
Autophagy
|
Cancer
|
Laduviglusib (CHIR-99021) monohydrochloride is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib monohydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib monohydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib monohydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib monohydrochloride induces autophagy.
|
-
- HY-142949
-
ALK5-IN-7
|
ALK
|
Cancer
Inflammation/Immunology
|
ALK5-IN-7 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-7 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 4).
|
-
- HY-N0261
-
Aurantio-obtusin
|
Others
|
Inflammation/Immunology
Cardiovascular Disease
|
Aurantio-obtusin is an anthraquinone isolated from Semen Cassiae, with anti-Inflammatory, anti-oxidative, anti-coagulating and anti-hypertension activities. Aurantio-obtusin relaxes systemic arteries through endothelial PI3K/AKT/eNOS-dependent signaling pathway in rats, thus acts as a new potential vasodilator. Aurantio-obtusin inhibits allergic responses in IgE-mediated mast cells and anaphylactic models and is potential for treatment for allergy-related diseases.
|
-
- HY-N6257
-
Cafestol
|
ERK
PGE synthase
COX
NF-κB
|
Cancer
Inflammation/Immunology
|
Cafestol, one of the major components of coffee, is a coffee-specific diterpene from. Cafestol is a ERK inhibitor for AP-1-targeted activity against PGE2 production and the mRNA expression of cyclooxygenase (COX)-2 in LPS-activated RAW264.7 cells. Cafestol has strong inhibitory activity on PGE2 production by suppressing the NF-kB activation pathway. Cafestol contributes to its beneficial effects through various biological activities such as chemopreventive, antitumorigenic, hepatoprotective, antioxidative and antiinflammatory effects.
|
-
- HY-16705
-
BRD4770
|
Histone Methyltransferase
|
Cancer
|
BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC50 of 5 µM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence.
|
-
- HY-142950
-
ALK5-IN-6
|
ALK
|
Cancer
Inflammation/Immunology
|
ALK5-IN-6 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-6 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 1).
|
-
- HY-44062
-
G9a-IN-1
|
Histone Methyltransferase
|
Inflammation/Immunology
Cancer
|
G9a-IN-1 (Compound 113) is a G9a protein inhibitor. G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes histone H3 lysine 9 dimethylation (H3K9me2), which is a reversible modification generally associated with transcriptional gene silencing. G9a-IN-1 can be used for the research of autoimmune disorders or cancer.
|
-
- HY-N0941
-
beta-Mangostin
β-Mangostin
|
Bacterial
Parasite
Apoptosis
|
Cancer
Infection
|
beta-Mangostin (β-Mangostin) is a xanthone compound present in Cratoxylum arborescens, with antibacterial and antimalarial activities. beta-Mangostin exhibits antimycobacterial activity against Mycobacterium tuberculosis with an MIC of 6.25 μg/mL. beta-Mangostin possesses in vitro antimalarial activity against Plasmodium falciparum, with an IC50 of 3.00 μg/mL. beta-Mangostin has potent anticancer activity against various cancers (such as hepatocellular carcinoma, leukaemic).
|
-
- HY-113629
-
2-Keto-D-Glucose
D-Glucosone; D-Arabino-hexos-2-ulose
|
Others
|
Infection
|
2-Keto-D-Glucose (D-Glucosone) is a key intermediate in a secondary metabolic pathway leading to the antibiotic Cortalcerone. 2-Keto-D-Glucose is also an intermediate in the conversion of D-glucose into D-fructose. 2-Keto-D-Glucose is found in various natural sources, including fungi, algae, and shellfish.
|
-
- HY-135897
-
-
- HY-N2026A
-
Propylparaben sodium
Propyl parahydroxybenzoate sodium; Propyl 4-hydroxybenzoate sodium
|
Endogenous Metabolite
Bacterial
Apoptosis
|
Infection
|
Propylparaben sodium (Propyl parahydroxybenzoate) is an antimicrobial preservative which can be produced naturally by plants and bacteria. Propylparaben sodium is prevalently used in cosmetics, pharmaceuticals, and foods. Propylparaben sodium disrupts antral follicle growth and steroidogenic function by altering the cell-cycle, apoptosis, and steroidogenesis pathways. Propylparaben sodium also decreases sperm number and motile activity in rats.
|
-
- HY-N0392
-
Polygalasaponin F
|
Toll-like Receptor (TLR)
PI3K
Akt
NF-κB
|
Inflammation/Immunology
|
Polygalasaponin F, an oleanane-type triterpenoid saponin extracted from Polygala japonica, decreases the release of the inflammatory cytokine tumor necrosis factor a (TNFa). Polygalasaponin F reduces neuroinflammatory cytokine secretion through the regulation of the TLR4-PI3K/AKT-NF-kB signaling pathway .
|
-
- HY-117433
-
-
- HY-N0171
-
Beta-Sitosterol (purity>80%)
β-Sitosterol (purity>80%); 22,23-Dihydrostigmasterol (purity>80%)
|
Endogenous Metabolite
Apoptosis
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
Beta-Sitosterol (purity>80%) includes β-sitosterol (≥80%), stigmasterol, campesterol and brassicasterol mainly. Beta-Sitosterol is a plant sterol. Beta-Sitosterol (purity>80%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
|
-
- HY-N2026
-
Propylparaben
Propyl parahydroxybenzoate; Propyl 4-hydroxybenzoate
|
Endogenous Metabolite
Bacterial
Apoptosis
|
Infection
|
Propylparaben (Propyl parahydroxybenzoate) is an antimicrobial preservative which can be produced naturally by plants and bacteria. Propylparaben is prevalently used in cosmetics, pharmaceuticals, and foods. Propylparaben disrupts antral follicle growth and steroidogenic function by altering the cell-cycle, apoptosis, and steroidogenesis pathways. Propylparaben also decreases sperm number and motile activity in rats.
|
-
- HY-N0527
-
Pentagalloylglucose
Penta-O-galloyl-β-D-glucose; 1,2,3,4,6-Pentagalloyl glucose
|
Others
|
Infection
|
Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) is a gallotannin isolated from various plants. It suppressed interleukin (IL)-4 induced signal pathway in B cell, and inhibited IgE production partially caused by increasing a population of Treg cells in conjunction with Treg-inducing factors. Pentagalloylglucose possesses significant anti-rabies virus (RABV) activity.
|
-
- HY-N7363
-
Isolongifolene
(-)-Isolongifolene
|
Apoptosis
|
Cancer
Inflammation/Immunology
Neurological Disease
|
Isolongifolene ((-)-Isolongifolene) is a tricyclic sesquiterpene isolated from Murraya koenigii. Isolongifolene attenuates Rotenone-induced oxidative stress, mitochondrial dysfunction and apoptosis through the regulation of PI3K/AKT/GSK-3β signaling pathways. Isolongifolene has antioxidant, anti-inflammatory, anticancer and neuroprotective properties.
|
-
- HY-122818
-
bpV(phen) trihydrate
|
PTEN
Phosphatase
Parasite
Apoptosis
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
|
bpV(phen) trihydrate, a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) trihydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) trihydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) trihydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
|
-
- HY-N0617
-
Sanggenon C
|
NF-κB
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
Sanggenon C is a flavanone Diels-Alder adduct compound, which is isolated from the root bark of Morus cathayana. Sanggenon C exerts protective effects against cardiac hypertrophy and fibrosis via suppression of the calcineurin/NFAT2 pathway. Sanggenon C inhibits inducible nitric oxide synthase expression in RAW264.7 cells, and tumor necrosis factor-α-stimulated cell adhesion and vascular cell adhesion molecule-1 expression, by suppressing NF-κB activity. Sanggenon C possesses antioxidant, anti-inflammatory activities and inhibits Pancreatic lipase (PL) with the an IC50 of 3.00 μM.
|
-
- HY-144041
-
CSF1R-IN-5
|
c-Fms
|
Cancer
|
CSF1R-IN-5 is a potent inhibitor of CSF1R. CSF-1R is expressed in macrophages, and the survival and differentiation of macrophages depends on the CSF-1/CSF-1R signaling pathway. CSF1R-IN-5 affects the exchange of inflammatory factors between TAMs and glioma cells. CSF1R-IN-5 has the potential for the research of cancer disease (extracted from patent WO2021197276A1, compound 11).
|
-
- HY-N0103A
-
Sophocarpine monohydrate
|
Autophagy
Apoptosis
PI3K
Akt
Influenza Virus
|
Cancer
Infection
Inflammation/Immunology
|
Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine (monohydrate) significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine (monohydrate) has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
|
-
- HY-144040
-
CSF1R-IN-4
|
c-Fms
|
Cancer
|
CSF1R-IN-4 is a potent inhibitor of CSF1R. CSF-1R is expressed in macrophages, and the survival and differentiation of macrophages depends on the CSF-1/CSF-1R signaling pathway. CSF1R-IN-4 affects the exchange of inflammatory factors between TAMs and glioma cells. CSF1R-IN-4 has the potential for the research of cancer disease (extracted from patent WO2021197276A1, compound 104).
|
-
- HY-N6588
-
3,4,5-Tricaffeoylquinic acid
3,4,5-triCQA
|
Akt
NF-κB
|
Inflammation/Immunology
|
3,4,5-Tricaffeoylquinic acid (3,4,5-triCQA) inhibits tumor necrosis factor-α-stimulated production of inflammatory mediators in keratinocytes via suppression of Akt- and NF-κB-pathways. 3,4,5-Tricaffeoylquinic acid induces cell cycle arrest at G0/G1, actin cytoskeleton organization, chromatin remodeling, neuronal differentiation, and bone morphogenetic protein signaling in human neural stem cells. 3,4,5-Tricaffeoylquinic acid has the potential for the research of aging-associated diseases.
|
-
- HY-N7676
-
Marein
|
AMPK
HDAC
|
Metabolic Disease
Neurological Disease
Cardiovascular Disease
|
Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC50 of 100 µM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects.
|
-
- HY-N0103
-