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Pathways Recommended: Stem Cell/Wnt PI3K/Akt/mTOR Cell Cycle/DNA Damage
Targets Recommended: Akt Itk TOPK NAMPT PTEN SGK ATM/ATR SNIPER

Results for "293t cell and akt Inhibitors" in MCE Product Catalog:

9706

Inhibitors & Agonists

93

Screening Libraries

96

Dye Reagents

56

Biochemical Assay Reagents

485

Peptides

16

MCE Kits

19

Inhibitory Antibodies

1749

Natural
Products

57

Recombinant Proteins

Cat. No. Product Name Target Research Areas
  • HY-120210
    XY018

    ROR Cancer Inflammation/Immunology
    XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD).
  • HY-N0041
    Ginsenoside Rb3

    Gypenoside IV

    NF-κB COX NO Synthase Cancer Inflammation/Immunology
    Ginsenoside Rb3 is extracted from steamed Panax notoginseng. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
  • HY-101775A
    9-Hydroxyellipticine hydrochloride

    Topoisomerase Cancer Cardiovascular Disease
    9-Hydroxyellipticine hydrochloride is a inhibitor of Topo II and RyR. 9-Hydroxyellipticine hydrochloride exhibits antitumor, antioxidant and catecholamine-releasing activities. 9-Hydroxyellipticine hydrochloride exhibits IC50 values of 1.6 μM and 1.2μM in Hela S-3 and 293T cells, respectively.
  • HY-50862
    Akt1 and Akt2-IN-1

    Akt Cancer
    Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity.
  • HY-108317
    ABL127

    Others Cancer
    ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1) with IC50s of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively.
  • HY-122716
    PTGR2-IN-1

    Others Others
    PTGR2-IN-1 is a potent PTGR2 inhibitor with an IC50 of ~0.7 μM. PTGR2-IN-1 increases 15-keto-PGE2-dependent PPARγ transcriptional activity in PTGR2-transfected HEK293T cells.
  • HY-126257
    AKT-IN-3

    Akt Apoptosis Cancer
    AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells.
  • HY-112148
    AKT-IN-2

    Akt Cancer
    AKT-IN-2 is a potent, selective and orally bioavailable AKT inhibitor with an IC50 of 5 nM for AKT1.
  • HY-10355
    AKT inhibitor VIII

    akti-1/2

    Akt Apoptosis Cancer Metabolic Disease
    AKT inhibitor VIII (AKTi-1/2) is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity with IC50s of 58 nM, 210 nM, and 2119 nM, respectively.
  • HY-10249A
    AKT Kinase Inhibitor

    Akt Cancer
    AKT Kinase Inhibitor is an Akt kinase inhibitor with anti-tumor activity.
  • HY-18296
    AKT-IN-1

    Akt Cancer
    AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM.
  • HY-10721
    PF-AKT400

    akt protein kinase inhibitor

    Akt Cancer
    PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).
  • HY-P1432
    K-(D-1-Nal)-FwLL-NH2

    GHSR
    K-(D-1-Nal)-FwLL-NH2 is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-16558
    Butein

    2’,3,4,4’-tetrahydroxy Chalcone

    EGFR Autophagy Apoptosis Phosphodiesterase (PDE) Cancer
    Butein, isolated from Dalbergia odorifera T. Chen, 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-N3354
    Lupiwighteone

    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-130985
    9-Decyn-1-ol

    PROTAC Linker Cancer
    9-Decyn-1-ol is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs. 9-Decyn-1-ol can be used to conjugate GDC-0068 with Lenalidomide to generate INY-03-041. INY-03-041 is a potent, highly selective and PROTAC-based pan-Akt degrader. INY-03-041 inhibits Akt1, Akt2 and Akt3 with IC50s of 2.0 nM, 6.8 nM and 3.5 nM, respectively.
  • HY-N0314
    Pectolinarin

    Interleukin Related Prostaglandin Receptor NO Synthase Apoptosis Inflammation/Immunology
    Pectolinarin, isolated from Cirsium chanroenicum, possesses anti-inflammatory activity. Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin suppresses cell proliferation and inflammatory response and induces apoptosis via inactivation of the PI3K/Akt pathway.
  • HY-130988
    Ipatasertib-NH2

    GDC-0068-NH2; RG7440-NH2

    Ligand for Target Protein for PROTAC Cancer
    Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for target protein AKT for PROTAC, binds to lenalidomide, a ligand of ubiquitin E3 ligase cereblon (CRBN), via a ten-hydrocarbon linker to form INY-03-041 (HY-133120) to degrade AKT.
  • HY-10425
    A-443654

    Akt Cancer
    A-443654 is a pan-Akt inhibitor and has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM).
  • 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-N2232
    N-​Feruloyloctopamine

    Akt p38 MAPK Cancer
    N-Feruloyloctopamine, isolated from Garlic skin, is an antioxidant constituent. N-Feruloyloctopamine significantly decreases the phosphorylation levels of Akt and p38 MAPK.
  • 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-N2491
    Deoxyelephantopin

    NF-κB Cancer
    Deoxyelephantopin, a natural bioactive sesquiterpene lactone from Elephantopus scaber, has shown promising anticancer effects against a broad spectrum of cancers. Deoxyelephantopin inhibits NF-κB, MAPK, PI3K/Akt, and β-catenin signaling.
  • HY-P1115
    AKTide-2T

    Akt Others
    AKTide-2T is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position.
  • HY-P1115A
    AKTide-2T TFA

    Akt Others
    AKTide-2T TFA is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T TFA mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position.
  • HY-108232
    MK-2206

    Akt Autophagy Apoptosis Cancer
    MK-2206 is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206. Anticancer activities.
  • 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-123938
    CYH33

    PI3K Cancer
    CYH33 is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. CYH33 inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 has potent activity against solid tumors.
  • HY-19832
    SC66

    Akt Apoptosis Cancer
    SC66 is an Akt inhibitor, reduces cell viability in a dose- and time-dependent manner, inhibits colony formation and induces apoptosis in hepatocellular carcinoma (HCC) cells.
  • HY-100018
    BAY1125976

    Akt Cancer
    BAY1125976 is a selective allosteric Akt1/Akt2 inhibitor; inhibits Akt1 and Akt2 activity with IC50 values of 5.2 nM and 18 nM at 10 μM ATP, respectively.
  • HY-11005
    BX-912

    PDK-1 Apoptosis Cancer
    BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis.
  • HY-U00458
    K-80003

    TX-803

    Akt Cancer
    K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
  • HY-15965
    Uprosertib

    GSK2141795

    Akt Cancer
    Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.
  • HY-15965A
    Uprosertib hydrochloride

    GSK2141795 (hydrochloride)

    Akt Cancer
    Uprosertib hydrochloride (GSK2141795 hydrochloride) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.
  • HY-15431
    Capivasertib

    AZD5363

    Akt Autophagy Cancer
    Capivasertib (AZD5363) is an orally active and potent pan-AKT kinase inhibitor with IC50 of 3, 7 and 7 nM for Akt1,Akt2 and Akt3, respectively.
  • HY-110066
    (Z)-Guggulsterone

    Apoptosis VEGFR Akt Cancer
    Z-guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, inhibits the growth of human prostate cancer cells by causing apoptosis. Z-guggulsterone inhibits angiogenesis by suppressing the VEGF–VEGF-R2–Akt signaling axis.
  • HY-15727
    Afuresertib

    GSK2110183

    Akt PKC ROCK Cancer
    Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively.
  • HY-15727A
    Afuresertib hydrochloride

    GSK2110183 hydrochloride

    Akt PKC ROCK Cancer
    Afuresertib hydrochloride (GSK 2110183 hydrochloride) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively.
  • HY-50909
    Perifosine

    KRX-0401; NSC 639966; D21266

    Akt Autophagy Apoptosis Cancer
    Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
  • HY-18749
    SC79

    Akt Cancer Inflammation/Immunology Neurological Disease
    SC79, a unique specific and BBB permeable Akt activator, activates Akt in the cytosol and inhibits Akt membrane translocation. SC79 specifically binds to the PH domain of Akt.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-15369
    FPA-124

    Akt Apoptosis Cancer
    FPA-124, a cell-permeable copper complex, is a selective Akt inhibitor with an IC50 of 0.1 μM. FPA-124 interacts with both the pleckstrin homology (PH) and the kinase domains of Akt. FPA-124 induces apoptosis.
  • 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-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-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-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-16666
    3CAI

    Akt Cancer
    3CAI is a potent and specific AKT1 and AKT2 inhibitor.
  • HY-15186
    Ipatasertib

    GDC-0068; RG7440

    Akt Cancer
    Ipatasertib (GDC-0068) is a highly selective and ATP-competitive pan-Akt inhibitor with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively.
  • HY-15186A
    Ipatasertib dihydrochloride

    GDC-0068 dihydrochloride; RG-7440 dihydrochloride

    Akt Cancer
    Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive pan-Akt inhibitor with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively.
  • HY-12059A
    AT7867 dihydrochloride

    Akt PKA Ribosomal S6 Kinase (RSK) Cancer
    AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
  • HY-12059
    AT7867

    Akt PKA Ribosomal S6 Kinase (RSK) Cancer
    AT7867 is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
  • HY-19719A
    Miransertib hydrochloride

    ARQ-092 hydrochloride

    Akt Parasite Cancer Infection
    Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib hydrochloride is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research. Miransertib hydrochloride is effective against Leishmania.
  • HY-19719
    Miransertib

    ARQ-092

    Akt Parasite Cancer Infection
    Miransertib (ARQ-092) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research. Miransertib is effective against Leishmania.
  • 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-135297
    Mono-and diglycerides

    Others Others
    Mono-and diglycerides is formed by triglycerides being broken down by pancreatic lipase in the gastrointestinal lumen. Mono-and diglycerides is a food additive used as a nonionic emulsifier and mainly present in food fats.
  • HY-101625
    Recilisib

    Ex-RAD; ON 01210

    Akt PI3K Cancer
    Recilisib is a radioprotectant, which can activate AKT, PI3K activities in cells.
  • HY-130307
    Rubrofusarin

    Bacterial Cancer Inflammation/Immunology Neurological Disease
    Rubrofusarin is an orange polyketide pigment from Fusarium graminearum. Rubrofusarin is also an active ingredient of the Cassia species and ameliorates chronic restraint stress (CRS) -induced depressive symptoms through PI3K/Akt signaling. Rubrofusarin has anticancer, antibacterial, and antioxidant effects.
  • HY-120944
    BAY-7598

    MMP Inflammation/Immunology
    BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.
  • HY-10358
    MK-2206 dihydrochloride

    MK-2206 (2HCl)

    Akt Autophagy Apoptosis Cancer
    MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy.
  • HY-18676
    OSU-T315

    Integrin Autophagy Apoptosis Cancer
    OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner. OSU-T315 causes cell death through apoptosis and autophagy.
  • HY-112147
    IDO1 and HDAC1 Inhibitor

    Indoleamine 2,3-Dioxygenase (IDO) HDAC Cancer
    IDO1 and HDAC1 Inhibitor (Compound 10) is a dual IDO1 and HDAC1 inhibitor with IC50s of 69.0 nM and 66.5 nM, respectively.
  • 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-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-10249
    GSK-690693

    Akt AMPK Autophagy Cancer
    GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC50s of 2 nM, 13 nM, 9 nM for Akt1, Akt2 and Akt3, respectively. GSK-690693 is also an AMPK inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation.
  • HY-122913
    Borussertib

    Akt Cancer
    Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Akt wt.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-100894
    Biotin-VAD-FMK

    Caspase Cancer
    Biotin-VAD-FMK is a cell permeable, irreversible biotin-labeled caspase inhibitor, used to identify active caspases in cell lysates.
  • HY-110193
    SPP-86

    RET Cancer
    SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
  • HY-12063
    PHT-427

    Akt Apoptosis Cancer
    PHT-247 is an inhibitor of the pleckstrin homology (PH) domain of Akt, and it is also an inhibitor of PDPK1 with Kis of 2.7 µM and 5.2 µM and for Akt and PDPK1, respectively.
  • HY-124295
    MPT0E028

    HDAC Akt Apoptosis Cancer
    MPT0E028 is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. MPT0E028 reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. MPT0E028 has good anticancer activity.
  • HY-N0004
    Oridonin

    NSC-250682; Isodonol

    Akt Bacterial Cancer Infection Inflammation/Immunology
    Oridonin (NSC-250682), a diterpenoid isolated from Rabdosia rubescens, acts as an inhibitor of AKT, with IC50s of 8.4 and 8.9 μM for AKT1 and AKT2; Oridonin possesses anti-tumor, anti-bacterial and anti-inflammatory effects.
  • 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-N0551
    Wedelolactone

    Caspase Lipoxygenase Apoptosis Cancer Inflammation/Immunology
    Wedelolactone, a natural product from Ecliptae herba, suppresses LPS-induced caspase-11 expression by directly inhibiting the IKK Complex. Wedelolactone inhibits 5-lipoxygenase (5-Lox) (IC50~2.5 μM) activity by an oxygen radical scavenging mechanism. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells via downregulation of PKCε without inhibiting Akt. Anti-cancer, anti-inflammatory, and antioxidant activities.
  • HY-70027A
    p53 and MDM2 proteins-interaction-inhibitor dihydrochloride

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is an inhibitor of the interaction between p53 and MDM2 proteins.
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

    (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • 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-13254A
    A-674563 hydrochloride

    Akt Cancer
    A-674563 hydrochloride is a potent and selective Akt1 inhibitor with Ki of 11 nM.
  • HY-13254
    A-674563

    Akt Cancer
    A-674563 is a potent and selective Akt1 inhibitor with a Ki of 11 nM.
  • HY-16461
    Solenopsin

    Akt Cardiovascular Disease
    Solenopsin is an ATP-competitive AKT inhibitor with IC50 value of 10 μM .
  • 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-N7043
    Isosilybin A

    Apoptosis Cancer
    Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis.
  • HY-P2285
    AC 253

    Amyloid-β
    AC 253 is an Amylin (AMY3) receptor antagonist, inhibiting andrenomedulin-stimulated cAMP production. AC 253 protects against oligomeric Aβ-induced increase in intracellular Ca2+, activation of PKA, MAPK, Akt and cFOS and cell death in neuronal cell culture. AC 253 blocks electrophysiological effects of Aβ.
  • HY-19373
    RWJ-445167

    3DP-10017

    Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  • HY-100501
    M2698

    MSC2363318A

    Ribosomal S6 Kinase (RSK) Akt Cancer
    M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity.
  • HY-102080
    SAFit2

    FKBP Cancer
    SAFit2 is a highly potent, highly selective FK506-binding protein 51 (FKBP51) inhibitor with a Ki of 6 nM and also enhances AKT2-AS160 binding.
  • HY-70027
    p53 and MDM2 proteins-interaction-inhibitor (chiral)

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    p53 and MDM2 proteins-interaction-inhibitor (chiral) (Compound 32) is an inhibitor of the interaction between p53 and MDM2 proteins.
  • HY-70028
    p53 and MDM2 proteins-interaction-inhibitor (racemic)

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    p53 and MDM2 proteins-interaction-inhibitor (racemic) (Compound 2j) is an inhibitor of the interaction between p53 and MDM2 proteins.
  • HY-N0171A
    Beta-Sitosterol (purity>98%)

    β-Sitosterol (purity>98%); 22,23-Dihydrostigmasterol (purity>98%)

    Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Beta-Sitosterol (purity>98%) is a plant sterol. Beta-Sitosterol (purity>98%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
  • HY-N0107
    Cyclovirobuxine D

    Apoptosis Autophagy mTOR Akt Cardiovascular Disease
    Cyclovirobuxine D (CVB-D) is the main active component of the traditional Chinese medicine Buxus microphylla. Cyclovirobuxine D induces autophagy and attenuates the phosphorylation of Akt and mTOR. Cyclovirobuxine D inhibits cell proliferation of gastric cancer cells through suppression of cell cycle progression and inducement of mitochondria-mediated apoptosis. Cyclovirobuxine D is beneficial for heart failure induced by myocardial infarction.
  • HY-N2051
    Zeylenone

    Apoptosis Cancer
    Zeylenone, isolated from ethanol extract of the leaves of Uvaria grandiflora Roxb. Zeylenone, a naturally occurring cyclohexene oxide, inhibits proliferation and induces apoptosis in cervical carcinoma cells via PI3K/AKT/mTOR and MAPK/ERK pathways.
  • HY-76474
    BAY 61-3606

    Syk Apoptosis Cancer Inflammation/Immunology
    BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM. BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates. Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
  • HY-14985
    BAY 61-3606 dihydrochloride

    Syk Apoptosis Inflammation/Immunology Cancer
    BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM. BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
  • HY-107738
    Guggulsterone

    Z/E-Guggulsterone

    Apoptosis JNK Akt Caspase FXR Autophagy Cancer
    Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively.
  • HY-15615A
    TIC10

    ONC-201

    TNF Receptor Apoptosis Cancer
    TIC10 is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. TIC10 can cross the blood-brain barrier.
  • HY-N1505
    Loureirin A

    Akt Cardiovascular Disease
    Loureirin A is a flavonoid extracted from Dragon's Blood, can inhibit Akt phosphorylation, and has antiplatelet activity.
  • 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-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-107426
    Verrucarin A

    Muconomycin A

    Apoptosis Reactive Oxygen Species Cancer
    Verrucarin A (Muconomycin A), a Type D macrocyclic mycotoxin derived from the pathogen fungus Myrothecium verrucaria, is an inhibitor of protein synthesis. Verrucarin A inhibits growth of leukemia cell lines and activates caspases and apoptosis and inflammatory signaling in macrophages. Verrucarin A effectively increased the phosphorylation of p38 MAPK and diminished the phosphorylation of ERK/Akt. Verrucarin A caused cell cycle deregulation through the induction of p21 and p53.
  • HY-136583
    28-Epirapamycin

    Others Others
    28-Epirapamycin is an impurity of Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells.
  • 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-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>98%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
  • HY-P2498
    Cathepsin D and E FRET Substrate

    Cathepsin Others
    Cathepsin D and E FRET Substrate is a fluorogenic substrate for cathepsins D and E and not for B, H or L. The cleavage occurs at the Phe-Phe amide bond resul. Cathepsin D and E FRET Substrate is a valuable tool for routine assays and for mechanistic studies on cathepsins E and D.
  • 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-N2217
    Rotundic acid

    Akt mTOR p38 MAPK Apoptosis Inflammation/Immunology Cardiovascular Disease Cancer
    Rotundic acid, a triterpenoid obtained from I. rotunda, induces DNA damage and cell apoptosis in hepatocellular carcinoma through AKT/mTOR and MAPK Pathways. Rotundic acid possesses anti-inflammatory and cardio-protective abilities.
  • HY-N0712
    Typhaneoside

    Autophagy Inflammation/Immunology Cardiovascular Disease
    Typhaneoside, extracted from Typha angustifolia L., Typhaneoside can inhibit the excessive autophagy of hypoxia/reoxygenation cells and increase the phosphorylation of Akt and mTOR. Typhaneoside has certain effects on the cardiovascular system, including lowering blood lipid levels, promoting antiatherosclerosis activities, as well as improving immune and coagulation function.
  • 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-137497
    KRAS inhibitor-9

    Ras Apoptosis Cancer
    KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.
  • HY-136110
    2-Keto-D-galactose

    D-​Galactosone

    DNA/RNA Synthesis Cancer
    2-Keto-D-galactose (D-Galactosone) inhibits DNA synthesis, and inhibits proliferation of in vitro grown Ehrlich ascites tumor cells.
  • HY-N0678
    Icaritin

    Anhydroicaritin

    Autophagy Apoptosis Cancer
    Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium Genusis and potently inhibits proliferation of K562 cells (IC50 of 8 µM) and primary CML cells (IC50 of 13.4 µM for CML-CP and 18 µM for CML-BC). Icaritin can regulate MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis[3.
  • 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-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-15457
    Triciribine

    API-2; NSC 154020; TCN

    DNA/RNA Synthesis Akt HIV Cancer
    Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1/2 with IC50 of 130 nM, and 0.02-0.46 μM, respectively.
  • HY-136268
    AQX-435

    Phosphatase Apoptosis Inflammation/Immunology
    AQX-435 is a potent SHIP1 phosphatase activator. AQX-435 reduces PI3K activation downstream of the B-cell receptor (BCR) and induces apoptosis of malignant B cells, and reduces lymphoma growth.
  • 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-16071
    AT13148

    Akt PKA ROCK Ribosomal S6 Kinase (RSK) Cancer
    AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC50s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively.
  • HY-N2255
    Crebanine

    Akt Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Crebanine, an alkaloid from Stephania venosa, induces G1 arrest and apoptosis in human cancer cells. Crebanine exhibits anti-inflammatory activity via suppressing MAPKs and Akt signaling. Crebanine also possesses antiarrhythmic effect.
  • 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-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-N0103
    Sophocarpine

    Autophagy Apoptosis PI3K Akt Influenza Virus Cancer Infection Inflammation/Immunology
    Sophocarpine 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 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 has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
  • HY-P1887
    p5 Ligand for Dnak and DnaJ

    HSP Infection
    p5 Ligand for Dnak and DnaJ is a nonapeptide, which corresponds to the main binding site for the 23-residue part of the presequence of mitochondrial aspartate aminotransferase. p5 Ligand for Dnak and DnaJ is a high-affinity ligand for DnaK and DnaJ.
  • HY-N2283
    Deltonin

    ERK Akt Endogenous Metabolite Cancer
    Deltonin, a steroidal saponin, isolated from Dioscorea zingiberensis Wright, with antitumor activity; Deltonin inhibits ERK1/2 and AKT activation.
  • 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-N4058
    Helichrysetin

    Apoptosis Cancer
    Helichrysetin, isolated from the flowers of Helichrysum odoratissimum, is an ID2 (inhibitor of DNA binding 2) inhibitor, and suppresses DCIS (ductal carcinoma in situ) formation. Helichrysetin possess strong inhibitory effects on cell growth and is capable of inducing apoptosis in A549 cells.
  • HY-17561
    G-418 disulfate

    Geneticin sulfate; Antibiotic G-418 sulfate

    Bacterial Antibiotic Infection
    G-418 disulfate (Geneticin sulfate), is an aminoglycoside antibiotic, inhibits protein synthesis in eukaryotes and prokaryotes. G-418 disulfate is commonly used as a selective agent for eukaryotic cells.
  • HY-131344
    mTOR inhibitor-8

    mTOR Autophagy Cancer
    mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells.
  • 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-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-121222
    alpha-Bisabolol

    Apoptosis Cancer
    alpha-Bisabolol is a nontoxic sesquiterpene alcohol present in natural essential oil, with anticancer activity. alpha-Bisabolol exerts selective anticancer effect on A549 NSCLC cells (IC50=15 μM) via induction of cell cycle arrest, mitochondrial apoptosis and inhibition of PI3K/Akt signalling pathways. alpha-Bisabolol also strongly induces apoptosis in glioma 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-131140
    BD750

    JAK STAT Cancer Inflammation/Immunology
    BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively.
  • HY-15779
    K145

    SPHK Apoptosis Cancer
    K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity.
  • HY-15779A
    K145 hydrochloride

    SPHK Apoptosis Cancer
    K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity.
  • 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-15673
    KP372-1

    PI3K Akt Cancer
    KP372-1 is a PI3-K/Akt pathway inhibitor extracted from patent US7196083.
  • 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-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-N1255
    Scoulerine

    (-)-Scoulerine; Discretamine

    Microtubule/Tubulin Beta-secretase Apoptosis Cancer
    Scoulerine ((-)-Scoulerine), an isoquinoline alkaloid, is a potent antimitotic compound. Scoulerine is also an inhibitor of BACE1 (ß-site amyloid precursor protein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells.
  • HY-18728
    STF-31

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • 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-131061
    BET bromodomain inhibitor 1

    Epigenetic Reader Domain Cancer
    BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity.
  • 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-U00441
    DPBQ

    MDM-2/p53 Apoptosis Cancer
    DPBQ activates p53 and triggers apoptosis in a polyploid-specific manner, but does not inhibit topoisomerase or bind DNA. DPBQ elicits expression and phosphorylation of p53 and this effect is specific to tetraploid cells.
  • HY-18271
    CaMKII-IN-1

    CaMK Autophagy Inflammation/Immunology
    CaMKII-IN-1 is a potent and highly selective CaMKII inhibitor with IC50 of 63 nM; significantly high selectivity against CaMKIV, MLCK, p38a, Akt1, and PKC.
  • HY-17499
    EGFR-IN-12

    EGFR Apoptosis Cancer
    EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFR L858R and EGFR L861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity.
  • HY-135805
    JBJ-04-125-02

    EGFR Cancer
    JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR L858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities.
  • HY-136006
    (S,R,S)-AHPC-C6-NH2 dihydrochloride

    VH032-C6-NH2 dihydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer Inflammation/Immunology
    (S,R,S)-AHPC-C6-NH2 dihydrochloride (VH032-C6-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C6-NH2 dihydrochloride is XF038-161A, example 6, extracted from patent WO2019173516A1.
  • HY-133487B
    (S,R,S)-AHPC-C8-NH2

    VH032-C8-NH2

    E3 Ligase Ligand-Linker Conjugate Cancer Inflammation/Immunology
    (S,R,S)-AHPC-C8-NH2 (VH032-C8-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C8-NH2 is XF038-164A, example 8, extracted from patent WO2019173516A1.
  • HY-136006A
    (S,R,S)-AHPC-C6-NH2 hydrochloride

    VH032-C6-NH2 hydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer Inflammation/Immunology
    (S,R,S)-AHPC-C6-NH2 hydrochloride (VH032-C6-NH2 hydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C6-NH2 hydrochloride is XF038-161A, example 6, extracted from patent WO2019173516A1.
  • HY-133487
    (S,R,S)-AHPC-C8-NH2 dihydrochloride

    VH032-C8-NH2 dihydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer Inflammation/Immunology
    (S,R,S)-AHPC-C8-NH2 dihydrochloride (VH032-C8-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C8-NH2 is XF038-164A, example 8, extracted from patent WO2019173516A1.
  • HY-101255
    ODQ

    Guanylate Cyclase Apoptosis Cancer
    ODQ is a potent and selective soluble guanylyl cyclase (sGC, nitric oxide-activated enzyme) inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells.
  • HY-110086
    RWJ 50271

    Integrin Inflammation/Immunology
    RWJ 50271 is an selective and orally active inhibitor of lymphocyte function-associated antigen-1/intercellular adhesion molecule-1(LFA-1/ICAM-1) interaction with an IC50 of 5.0 μM (HL60 cells). RWJ 50271 inhibits LFA-1/ICAM-1-mediated cell adhesion.
  • HY-N3584
    Paris saponin VII

    Chonglou Saponin VII

    Akt p38 MAPK P-glycoprotein Bcl-2 Family Caspase PARP Autophagy Apoptosis Cancer
    Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii Maxim. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia.
  • HY-Y0520
    Itaconic acid

    Endogenous Metabolite Inflammation/Immunology
    Itaconic acid, a precursor of polymers, chemicals, and fuels, can be synthesized by many fungi. Itaconic acid also is a macrophage-specific metabolite. Itaconic acid mediates crosstalk between macrophage metabolism and peritoneal tumors.
  • HY-13072
    Cenisertib

    AS-703569; R-763

    Aurora Kinase Bcr-Abl Akt STAT FLT3 Cancer
    Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.
  • 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-119881
    Alafosfalin

    Bacterial Antibiotic Infection
    Alafosfalin is an inhibitor of cell wall biosynthesis. Alafosfalin is a phosphonodipeptide with antibacterial properties.
  • HY-N0774
    Isofraxidin

    COX MMP Toll-like Receptor (TLR) Inflammation/Immunology
    Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells. Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation.
  • HY-120504
    N-Acetyltyramine

    Bacterial Cancer Infection
    N-Acetyltyramine is a quorum-sensing inhibitor (QSI) compound produced by V. alginolyticus M3-10. N-Acetyltyramine is capable of inhibiting the QS of C. violaceum ATCC 12472. N-acetyltyramine reverses resistance in Doxorubicin-resistant leukemia P388 cells.
  • HY-N4182
    Licochalcone E

    Akt p38 MAPK Autophagy Inflammation/Immunology
    Licochalcone E, a flavonoid compound isolated from Glycyrrhiza inflate, inhibits NF-κB and AP-1 transcriptional activity through the inhibition of AKT and MAPK activation.
  • HY-13595
    Chrysophanol

    Chrysophanic acid

    EGFR Cancer
    Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of EGFR and suppresses activation of AKT and mTOR/p70S6K.
  • HY-16689
    VU 0240551

    Potassium Channel Others
    VU 0240551 is a potent neuronal K-Cl cotransporter KCC2 inhibitor (IC50=560 nM) and is selective versus NKCC1. VU 0240551 also inhibits hERG and L-type Ca 2+ channels. VU 0240551 attenuates GABA-induced hyperpolarization of P cells, produces a positive shift in the P cell GABA reversal potential and enhances P cell synaptic transmission.
  • 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-121629
    PS210

    PDK-1 Cancer
    PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K.
  • HY-N8441
    Neriifolin

    17β-Neriifolin

    Na+/K+ ATPase Apoptosis Cancer Inflammation/Immunology
    Neriifolin, a CNS-penetrating cardiac glycoside, is an inhibitor of the Na +, K +-ATPase. Neriifolin can target beclin 1, inhibits the formation of LC3-associated phagosomes and ameliorates experimental autoimmune encephalomyelitis (EAE) development. Neriifolin induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells[2.
  • HY-123390
    DB07107

    Bcr-Abl Akt Cancer
    DB07107 is a potent drug resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC50 value of 360 nM.
  • HY-135336A
    (S)-Verapamil hydrochloride

    (S)-(-)-Verapamil hydrochloride

    Leukotriene Receptor Calcium Channel Apoptosis Cancer
    (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells.
  • HY-122872
    MKK7-COV-9

    p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • 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-105019A
    Melflufen hydrochloride

    Melphalan flufenamide hydrochloride

    DNA Alkylator/Crosslinker Apoptosis Cancer
    Melflufen (Melphalan flufenamide) hydrochloride, a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen hydrochloride shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen hydrochloride induces irreversible DNA damage and cytotoxicity in MM cells.
  • HY-105019
    Melflufen

    Melphalan flufenamide

    DNA Alkylator/Crosslinker Apoptosis Cancer
    Melflufen (Melphalan flufenamide), a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells.
  • HY-N1435
    Oroxin B

    Apoptosis PI3K PTEN Autophagy Cancer
    Oroxin B (OB) is a flavonoid isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent. Oroxin B (OB) possesses obvious inhibitory effect and induces early apoptosis rather than late apoptosis on liver cancer cells through upregulation of PTEN, down regulation of COX-2, VEGF, PI3K, and p-AKT. Oroxin B (OB) selectively induces tumor-suppressive ER stress in malignant lymphoma cells.
  • HY-122295
    Dehydroleucodine

    Apoptosis Cancer Inflammation/Immunology
    Dehydroleucodine is a sesquiterpene lactone isolated from Gynoxys verrucosa. Dehydroleucodine is a mast cell stabilizer that inhibits tmast cell degranulation induced by compound 48/80. Dehydroleucodine inudces cells apoptosis, and has gastric ulcer inhibition and antileukemic effects.
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-N1403
    Tigogenin

    Others Metabolic Disease
    Tigogenin, one of steroidal sapogenins, is widely used for synthesizing steroid drugs. Tigogenin inhibits adipocytic differentiation and induces osteoblastic differentiation in mouse bone marrow stromal cells.
  • HY-N6017
    Bakkenolide A

    Others 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-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-122181A
    OTS186935 trihydrochloride

    Histone Methyltransferase Cancer
    OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells.
  • 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-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-101030
    MBM-17

    Apoptosis Cancer
    MBM-17 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM. It effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice.
  • 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-136123
    Tubulin inhibitor 8

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM.
  • HY-136122
    Tubulin inhibitor 7

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM.
  • HY-136121
    Tubulin inhibitor 6

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM.
  • HY-18621A
    OTS514 hydrochloride

    TOPK Apoptosis Cancer
    OTS514 hydrochloride is a highly potent TOPK inhibitor, which inhibits TOPK kinase activity with a median inhibitory concentration (IC50) value of 2.6 nM. OTS514 hydrochloride strongly suppresses the growth of TOPK-positive cancer cells. OTS514 hydrochloride induces cell cycle arrest and apoptosis.
  • HY-13685
    Miltefosine

    HePC; Hexadecyl phosphocholine

    Akt HIV Infection Cancer
    Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity. Miltefosine is an inhibitor of CTP-phosphocholine cytidyltransferase (CCT).
  • HY-N6927
    Isoforskolin

    Coleonol B

    TNF Receptor Interleukin Related Inflammation/Immunology
    Isoforskolin is the principle active component of C. forskohlii native to China. Isoforskolin reduces the secretion of lipopolysaccharide (LPS)-induced cytokines, namely TNF-α, IL-1β, IL-6 and IL-8, in human mononuclear leukocytes. Isoforskolin acts as an anti-inflammatory agent for the treatment of Lyme arthritis.
  • HY-N3415
    Kumatakenin

    Apoptosis Cancer
    Kumatakenin, a flavonoid that is isolated from cloves shows the effect of inducing apoptosis in ovarian cancer cells.
  • HY-13624A
    Epirubicin hydrochloride

    4'-Epidoxorubicin hydrochloride

    DNA/RNA Synthesis Topoisomerase Apoptosis Cancer
    Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride inhibits DNA and RNA synthesis. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
  • HY-13624
    Epirubicin

    4'-Epidoxorubicin

    DNA/RNA Synthesis Topoisomerase Apoptosis Cancer
    Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin inhibits DNA and RNA synthesis. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
  • 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-100579
    Ferrostatin-1

    Ferroptosis Fungal Cancer
    Ferrostatin-1, a potent and selective ferroptosis inhibitor, suppresses Erastin-induced ferroptosis in HT-1080 cells (EC50=60 nM). Ferrostatin-1, a synthetic antioxidant, acts via a reductive mechanism to prevent damage to membrane lipids and thereby inhibit cell death. Antifungal Activity.
  • HY-18621
    OTS514

    TOPK Apoptosis Cancer
    OTS514 is a highly potent TOPK inhibitor with an IC50 of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells. OTS514 induces cell cycle arrest and apoptosis.
  • HY-N2599
    Taraxerol acetate

    COX Apoptosis Cancer
    Taraxerol acetate is a COX-1 and COX-2 inhibitor with IC50 values of 116.3 μM and 94.7 μM, respectively. Taraxerol acetate the has the anticancer potential and induces cell apoptosis.
  • HY-100360
    MS049

    Histone Methyltransferase Cancer
    MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and do not affect the growth of HEK293 cells.
  • HY-100360A
    MS049 dihydrochloride

    Histone Methyltransferase Cancer
    MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and do not affect the growth of HEK293 cells.
  • HY-B0795
    MHY1485

    mTOR Autophagy Cancer
    MHY1485 is a potent cell-permeable mTOR activator that targets the ATP domain of mTOR. MHY1485 inhibits autophagy by suppression of fusion between autophagosomes and lysosomes.
  • 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-16981
    SB-332235

    CXCR Inflammation/Immunology
    SB-332235 is a potent, orally active nonpeptide CXCR2 antagonist, with an IC50 of 7.7 nM. SB-332235 displays 285-fold selectivity for CXCR2 over CXCR1. SB-332235 inhibits acute and chronic models of arthritis in the rabbit. SB-332235 inhibits viability of AML cells.
  • 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-124771
    RH01386

    Others Metabolic Disease
    RH01386 is a small molecule that can prevent ER stress-induced β cell dysfunction and death, and inhibits proapoptotic gene expression. RH01386 restores ER stress-impaired glucose-stimulated insulin secretion responses. RH01386 has the potential for type 2 diabetes treatment.
  • HY-103443
    HKI-357

    EGFR Cancer
    HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.
  • HY-P0315
    Crosstide

    Akt Others
    Crosstide is a peptide analog of glycogen synthase kinase α/β fusion protein sequence which is a substrate for Akt.
  • 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-14454
    TPh A

    Triphenyl Compound A

    Others Cancer
    TPh A (Triphenyl Compound A) is a potent inhibitor of the nuclear protein pirin and binds specifically to pirin with a Ki of 0.6 uM. TPh A disrupts the formation of the bcl3–pirin complex. TPh A can be used as a novel small molecule tool to regulate pirin in cells.
  • HY-N0104
    Curcumol

    (-)-Curcumol

    Apoptosis Cancer
    Curcumol ((-)-Curcumol), a bioactive sesquiterpenoid, possesses numerous pharmacological activities like anticancer, antimicrobial, antifungal, antiviral, and antiinflammatory. Curcumol is a potent inducer of apoptosis in numerous cancer cells via targeting key signaling pathways as MAPK/ERK, PI3K/Akt and NF-κB which are generally deregulated in several cancers.
  • 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-19992
    3-Bromopyruvic acid

    Bromopyruvic acid; Hexokinase II Inhibitor II, 3-BP

    Hexokinase Apoptosis Autophagy Cancer
    3-Bromopyruvate (Bromopyruvic acid) is an analogue of pyruvate and a potent hexokinase (HK)-II inhibitor with high tumor selectivity. 3-Bromopyruvate inhibits cell growth and induces apoptosis through interfering with glycolysis. 3-Bromopyruvate induces autophagy by stimulating ROS formation in breast cancer cells. Antimicrobial activities.
  • HY-101030A
    MBM-17S

    Apoptosis Cancer
    MBM-17S is a potent NIMA-related kinase 2 (Nek2) inhibitor, with an IC50 of 3 nM. MBM-17S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-17S shows antitumor activities, and no obvious toxicity to mice.
  • HY-122590
    Glabrescione B

    Gli Cancer
    Glabrescione B is the first compound that binds the Hedgehog (Hh) modulator Gli1. Glabrescione B impairs its activity by interfering with Gli1-DNA interaction. Glabrescione B inhibits the growth of Hedgehog-dependent tumor cells, the self-renewal ability, and clonogenicity of tumor-derived stem cells.
  • 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-13686
    PQ401

    IGF-1R Apoptosis Cancer
    PQ401 is a potent inhibitor of IGF-IR signaling. PQ401 inhibits IGF-I-stimulated IGF-IR autophosphorylation with an IC50 of 12.0 μM in a series of studies in MCF-7 cells. PQ401 is effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC50, 6 μM). PQ401 is a potential agent for breast and other IGF-I-sensitive cancers. PQ401 induces caspase-mediated apoptosis.
  • HY-13917A
    PND-1186 hydrochloride

    VS-4718 hydrochloride; SR-2516 hydrochloride

    FAK Apoptosis Cancer
    PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis.
  • HY-13917
    PND-1186

    VS-4718; SR-2516

    FAK Apoptosis Cancer
    PND-1186 (VS-4718) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis.
  • HY-135858
    SARS-CoV-IN-3

    SARS-CoV Parasite HIV Infection
    SARS-CoV-IN-3 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-3 shows anti-Coronavirus activity with an EC50 of 3.6 μM in Vero cells. SARS-CoV-IN-3 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 11.7 and 20.4 nM; and IC90s of 29.19 and 56 nM; respectively. SARS-CoV-IN-3 reduces HIV-1-induced cytopathic effect with an EC50 of 10 μM in MT-4 cells.
  • HY-P0023
    Cyclo(-RGDfK)

    Integrin Cancer
    Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
  • HY-138540
    1-Dodecylimidazole

    N-Dodecylimidazole

    Fungal Cancer
    1-Dodecylimidazole (N-Dodecylimidazole) is a lysosomotropic detergent and a cytotoxic agent. 1-Dodecylimidazole causes cell death by its acid-dependent accumulation in lysosomes, disruption of the lysosomal membrane, and releaseof cysteine proteases into the cytoplasm. 1-Dodecylimidazole has hypocholesterolaemic activity and broad-spectrum antifungal activity.
  • HY-135745
    Sulfentrazone

    Others Others
    Sulfentrazone is a phenyl triazolinone herbicide used for control of certain broadleaf and grass weed species. Sulfentrazone inhibits protoporphyrinogen oxidase, resulting in the disruption of lipid cell membranes.
  • HY-16062
    ARQ 621

    Kinesin Cancer
    ARQ 621 is an allosteric, potent and selective inhibitor of Eg5, a microtubule-based ATPase motor protein involved in cell division. Anti-tumor activity. ARQ 621 is a kinesin inhibitor.
  • HY-133511
    MLS000544460

    Phosphatase Cancer
    MLS000544460 is a highly selective and reversible Eya2 phosphatase inhibitor with a Kd of 2.0 μM and an IC50 of 4 μM. MLS000544460 inhibit Eya2 phosphatase mediated cell migration and has anti-cancer activity.
  • HY-18681
    Voxelotor

    GBT 440

    Others Cardiovascular Disease
    Voxelotor (GBT 440) is a potent inhibitor of haemoglobin S (HbS) polymerization. Voxelotor has the potential for sickle cell disease (SCD) treatment.
  • HY-114436
    MRTX-1257

    Ras Cancer
    MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells.
  • HY-P0023A
    Cyclo(-RGDfK) TFA

    Integrin Cancer
    Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
  • HY-109011
    Rosiptor

    AQX-1125

    Phosphatase Cancer
    Rosiptor (AQX-1125) is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects. Rosiptor (AQX-1125) inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro.
  • HY-B0789
    SU6656

    Src FAK Akt Cancer
    SU6656 is a Src family kinases inhibitor with IC50s of 280, 20, 130, 170 nM for Src, Yes, Lyn, and Fyn, respectively. SU6656 inhibits FAK phosphorylation at Y576/577, Y925, Y861 sites. SU6656 also inhibits p-AKT.
  • HY-A0133
    Chlorphenesin

    Bacterial Fungal Inflammation/Immunology
    Chlorphenesin is a reversible antigen-associated immunosuppressant. Chlorphenesin is an antibacterial and antifungal agent used in numerous eye care cosmetics.
  • HY-15477A
    YS-49 monohydrate

    Akt PI3K Angiotensin Receptor Adrenergic Receptor Cardiovascular Disease Endocrinology
    YS-49 (monohydrate) is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
  • HY-15477
    YS-49

    Akt PI3K Angiotensin Receptor Adrenergic Receptor Cardiovascular Disease Endocrinology
    YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
  • HY-N0732
    Jolkinolide B

    Apoptosis Cancer
    Jolkinolide B, a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud, is known to induce apoptosis in cancer cells.
  • HY-119339
    SX-682

    CXCR Cancer Inflammation/Immunology Endocrinology
    SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity.
  • HY-118355
    ALLM

    Calpain inhibitor II

    Proteasome Cathepsin Neurological Disease
    ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI).
  • HY-118630
    Vacuolin-1

    PIKfyve Autophagy Cancer
    Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor. Vacuolin-1 blocks the Ca 2+-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. vacuolin‐1 is a potent and selective PIKfyve inhibitor and inhibits late‐stage autophagy by impairing lysosomal maturation.
  • HY-108618
    BC11-38

    Phosphodiesterase (PDE) Endocrinology
    BC11-38 is a potent, selective, and biologically active PDE11 inhibitor, with IC50s of 0.28 µM and >100 µM for PDE11 and PDE1-10, respectively. BC11-38 elevates cAMP levels, PKA-mediated ATF-1 phosphorylation, and cortisol production in H295R cells.
  • HY-50896
    Erlotinib

    CP-358774; NSC 718781; OSI-774

    EGFR Autophagy Cancer
    Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer.
  • HY-N7006
    Timosaponin C

    Anemarsaponin C

    Others Inflammation/Immunology
    Timosaponin C is isolated from Rhizoma Anemarrhenae. Timosaponin C shows weaker NO inhibition in N9 microglial cells.
  • HY-15597
    Salinomycin

    Procoxacin

    Bacterial Wnt β-catenin Mitophagy Autophagy Apoptosis Antibiotic Cancer
    Salinomycin (Procoxacin), a polyether potassium ionophore antibiotic, selectively inhibits the growth of gram-positive bacteria. Salinomycin is a potent inhibitor of Wnt/β-catenin signaling, blocks Wnt-induced LRP6 phosphorylation. Salinomycin (Procoxacin) shows selective activity against human cancer stem cells.
  • HY-N5021
    Anhydrosafflor yellow B

    AHSYB

    Others Neurological Disease
    Anhydrosafflor yellow B (AHSYB) is a quinochalcone C-glycoside isolated from Carthamus tinctorius. Anhydrosafflor yellow B inhibits ADP-induced platelet aggregation, exhibits significant anti-oxidative effects in vitro, and possesses certain activity against H2O2-induced cytotoxicity in cultured PC12 cells and primary neuronal cells.
  • HY-B0517
    Mepivacaine

    Sodium Channel Neurological Disease
    Mepivacaine is an amide-type local anesthetic agent. Mepivacaine binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization.
  • HY-137471
    RBPJ Inhibitor-1

    RIN1

    Notch Cancer
    RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.
  • HY-135276
    Targaprimir-96

    MicroRNA Apoptosis Cancer
    Targaprimir-96 is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells.
  • HY-70002S
    Enzalutamide D3

    MDV3100 D3

    Androgen Receptor Autophagy Cancer
    Enzalutamide D3 is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.
  • 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-N6936
    Sennidin A

    HCV Akt GLUT Infection
    Sennidin A, isolated from the leaves of Cassia angustifolia, inhibits HCV NS3 helicase, with an IC50 of 0.8 μM. Sennidin A induces phosphorylation of Akt and glucose transporter 4 (GLUT4) translocation. Sennidin A stimulates the glucose incorporation.
  • HY-18959
    CWP232228

    β-catenin Wnt Cancer
    CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs).
  • HY-19747
    HPOB

    HDAC Apoptosis Cancer
    HPOB is a highly potent and selective inhibitor of HDAC6 with an IC50 of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6.
  • HY-14374
    GPP78

    CAY10618

    NAMPT Autophagy Cancer Inflammation/Immunology
    GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects.
  • HY-136312
    17-DMAP-GA

    Others Cancer
    17-DMAP-GA, a Geldanamycin (HY-15230) analogue, is an inhibitor of HSP90. 17-DMAP-GA causes cell cycle abnormalities.
  • 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-19826
    Isofistularin-3

    DNA Methyltransferase ADC Cytotoxin Autophagy Apoptosis Cancer
    Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM. Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin.
  • HY-12072
    Lck Inhibitor

    Src Inflammation/Immunology
    Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.
  • HY-W028690
    DNMDP

    Phosphodiesterase (PDE) Cancer
    DNMDP, a phosphodiesterase 3A (PDE3A) inhibitor, is a potent and selective cancer cell cytotoxic agent. DNMDP binding to PDE3A promotes an interaction between PDE3A and Schlafen 12 (SLFN12). DNMDP shows clear cell-selective cytotoxicity.
  • HY-124674A
    CCT365623 hydrochloride

    Monoamine Oxidase EGFR Akt TGF-beta/Smad Cancer
    CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor, with an IC50 of 0.89 μM. CCT365623 hydrochloride suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. CCT365623 hydrochloride is extremely well tolerated, and has good pharmacokinetic properties.
  • HY-13260
    CCT128930

    Akt Autophagy Cancer
    CCT128930 is a potent and selective inhibitor of Akt2 (IC50 6 nM) with 28-fold selectivity over the closely related PKA kinase (IC50 168 nM), as well as 20-fold selectivity over p70S6K (IC50 120 nM).
  • HY-13425
    Deguelin

    (-)-Deguelin; (-)-cis-Deguelin

    Akt Autophagy Apoptosis Cancer
    Deguelin, a naturally occurring rotenoid, acts as a chemopreventive agent by blocking multiple pathways like PI3K-Akt, IKK-NF-κB, and MAPK-mTOR-survivin-mediated apoptosis. Deguelin binding to Hsp90 leads to a decreased expression of numerous oncogenic proteins, including MEK1/2, Akt, HIF1α, COX-2, and NF-κB.
  • HY-135008
    J14

    Reactive Oxygen Species Cancer
    J14 is a reversible sulfiredoxin inhibitor with an IC50 of 8.1 μM. J14 induces oxidative stress (intracellular ROS accumulation) by inhibiting sulfiredoxin, leading to cytotoxicity and cancer cell death.
  • HY-129937A
    GNE-987

    PROTAC Epigenetic Reader Domain Cancer
    GNE-987 is a highly active chimeric BET degrader. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC).
  • HY-133570
    17-AEP-GA

    HSP ADC Cytotoxin Cancer
    17-AEP-GA, an HSP90 antagonist, is a potent inhibitor of glioblastoma cell proliferation, survival, migration and invasion. ADCs Toxin.
  • HY-131394
    5-Hydroxymethyl-2’-deoxycytidine

    5hmdC

    Others Cancer
    5-Hydroxymethyl-2’-deoxycytidine (5hmdC) is an oxidation derivative of 5-methyl-2'-deoxycytidine (5-mdC) in DNA. 5-Hydroxymethyl-2’-deoxycytidine may serve as a marker of irreversibly damaged cells.
  • 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-136528
    RA-9

    Deubiquitinase Apoptosis Cancer
    RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells.
  • HY-103349
    PETCM

    Caspase Apoptosis Cancer
    PETCM is an activator of caspase-3 and acts as an cytochrome c (cyto c)-dependent manner. PETCM promotes Apaf-1 oligomerization and induces cell apoptosis in HeLa cells.
  • HY-101519
    BETd-260

    ZBC 260

    PROTAC Epigenetic Reader Domain Apoptosis Cancer
    BETd-260 (ZBC 260) is a potent PROTAC BET degrader, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line. BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells.
  • HY-W011303
    Phytosphingosine

    Apoptosis Cancer
    Phytosphingosine is a phospholipid and has anti-cancer activities. Phytosphingosine induces cell apoptosis via caspase 8 activation and Bax translocation in cancer cells.
  • HY-N0671
    Rhapontin

    Rhaponiticin

    Apoptosis Cancer
    Rhapontin (Rhaponiticin), a component of rhubarb (Rheum officinale Baillon), induces apoptosis resulting in suppression of proliferation of human stomach cancer KATO III cells.
  • HY-10591
    Neuropathiazol

    Others Neurological Disease
    Neuropathiazol, a neuronal differentiation inducer, selectively induces neuronal differentiation of multipotent hippocampal neural progenitor cells.
  • HY-111360
    SPL-707

    γ-secretase Inflammation/Immunology
    SPL-707 is an orally active, selective signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 77 nM for hSPPL2a. SPL-707 inhibits γ-secretase (IC50=6.1 μM) and SPP (IC50=3.7 μM). SPL-707 has the potential for autoimmune diseases research by targeting B cells and dendritic cells.
  • HY-125729
    Ivermectin B1b

    Parasite SARS-CoV Infection
    Ivermectin B1b is the minor component of Ivermectin. Ivermectin, a potent anti-parasitic agent, inhibits the replication of SARS-CoV-2 in cell culture.
  • HY-107597
    SU3327

    JNK Metabolic Disease Inflammation/Immunology
    SU3327 is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. SU3327 also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. SU3327 shows less active against p38α and Akt kinase.
  • HY-14291
    Vildagliptin

    LAF237; NVP-LAF 237

    Dipeptidyl Peptidase Ferroptosis Apoptosis Metabolic Disease
    Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity.
  • HY-136453
    CR-1-31-B

    Eukaryotic Initiation Factor (eIF) Cancer
    CR-1-31-B is a potent eIF4A RNA helicase inhibitor. CR-1-31-B blocks MUC1-C translation in response to growth factor stimulation in breast cancer cells.
  • HY-134771
    YM-341619

    AS1617612

    STAT Inflammation/Immunology
    YM-341619 (AS1617612) is a potent and orally active STAT6 inhibitor with an IC50 of 0.70 nM. YM-341619 inhibits Th2 differentiation in mouse spleen T cells induced by IL-4 (IC50=0.28 nM) without affecting Th1 cell differentiation. YM-341619 is a promising compound for the the research of allergic diseases, such as allergic asthma.
  • HY-10253
    AG1024

    Tyrphostin AG 1024

    IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selective IGF-1R inhibitor with an IC50 of 7 μM. AG1024 inhibits phosphorylation of IR (IC50=57 μM). AG1024 induces apoptosis and has anti-cancer activity.
  • HY-15290
    AIM-100

    Ack1 Cancer
    AIM-100 is a potent and selective Ack1 inhibitor with an IC50 of 21.58 nM. AIM-100 also inhibits Tyr 267 phosphorylation. AIM-100 does not inhibits other kinases including PI3-kinase and AKT subfamily members. AIM-100 has an anticancer effect.
  • HY-N0003
    Honokiol

    NSC 293100

    Akt ERK Autophagy HCV Cancer
    Honokiol is a bioactive, biphenolic phytochemical that possesses potent antioxidative, anti-inflammatory, antiangiogenic, and anticancer activities by targeting a variety of signaling molecules. It inhibits the activation of Akt and enhances the phosphorylation of ERK1/ERK2. Honokiol can readily cross the blood brain barrier.
  • HY-100888
    Simurosertib

    TAK-931

    CDK Cancer
    Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM. Simurosertib has anti-cancer activity.
  • HY-111838A
    ZZW-115 hydrochloride

    Apoptosis Cancer
    ZZW-115 hydrochloride is a potent NUPR1 inhibitor, with a Kd of 2.1 μM. ZZW-115 hydrochloride induces tumor cell death by necroptosis and apoptosis. Anticancer activity.
  • HY-111838
    ZZW-115

    Apoptosis Cancer
    ZZW-115 is a potent NUPR1 inhibitor, with a Kd of 2.1 μM. ZZW-115 induces tumor cell death by necroptosis and apoptosis. Anticancer activity.
  • HY-101029
    MBM-55

    Apoptosis Cancer
    MBM-55 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice.
  • HY-N0361
    Dihydrocapsaicin

    TRP Channel Metabolic Disease
    Dihydrocapsaicin is a natural capsaicin, acts as a selective TRPV1 agonist, and also increases p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection.
  • HY-104047
    LM22B-10

    Trk Receptor Akt ERK Neurological Disease
    LM22B-10 is an activator of TrkB/TrkC neurotrophin receptor, and can induce TrkB, TrkC, AKT and ERK activation in vitro and in vivo.
  • HY-130122
    MG-277

    PROTAC Apoptosis Cancer
    MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor, GSPT1, with a DC50 of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity.
  • HY-N1039A
    Manool

    Others Cancer
    Manool is a diterpene from Salvia officinalis. Manool induces selective cytotoxicity in cancer cells. Manool arrests the cancer cells at the G(2)/M phase of the cell cycle.
  • HY-N7707
    Sandacanol

    Apoptosis Cancer
    Sandacanol is a specific agonist of olfactory receptor (OR10H1). Sandacanol induces cell cycle arrest and some apoptosis in bladder cancer cells.
  • HY-N2534
    Karanjin

    AMPK Apoptosis Cancer
    Karanjin is a major active furanoflavonol constituent of Fordia cauliflora. Karanjin induces GLUT4 translocation in skeletal muscle cells by increasing AMPK activity. Karanjin can induce cancer cell death through cell cycle arrest and enhance apoptosis.
  • HY-B0517A
    Mepivacaine hydrochloride

    Sodium Channel Neurological Disease
    Mepivacaine hydrochloride is an amide-type local anesthetic agent. Mepivacaine hydrochloride binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization.
  • HY-136895
    AZ12672857

    Prostaglandin Receptor Cancer
    AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM).
  • HY-14521
    Lometrexol

    DDATHF

    Antifolate Apoptosis Cancer
    Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
  • HY-14521B
    Lometrexol hydrate

    DDATHF hydrate

    Antifolate Apoptosis Cancer
    Lometrexol hydrate (DDATHF hydrate), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
  • 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-127170
    3-Hydroxycoumarin

    Others Others
    3-hydroxycoumarin is a potent and redox inhibitor of human 15-LOX-1. 3-hydroxycoumarin is recently demonstrated to protect sea urchin reproductive cells against ultraviolet B damage.
  • HY-14291A
    Vildagliptin dihydrate

    LAF237 dihydrate; NVP-LAF 237 dihydrate

    Dipeptidyl Peptidase Ferroptosis Apoptosis Metabolic Disease
    Vildagliptin dihydrate (LAF237 dihydrate) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin dihydrate possesses excellent oral bioavailability and potent antihyperglycemic activity.
  • HY-W013274
    CPTH2

    Histone Acetyltransferase Apoptosis Cancer
    CPTH2 is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B).
  • HY-15036
    Diclofenac

    COX Apoptosis Inflammation/Immunology
    Diclofenac is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
  • HY-15038
    Diclofenac potassium

    COX Apoptosis Inflammation/Immunology
    Diclofenac potassium is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac potassium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
  • HY-12892
    SKI-178

    SPHK Apoptosis Cancer
    SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both drug sensitive and multi-drug resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines.
  • 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-101867
    AU1235

    Bacterial Cancer Infection
    AU1235, an adamantyl urea, is a potent MmpL3 inhibitor. The Mycobacterium tuberculosis protein MmpL3 performs an essential role in cell wall synthesis, since it effects the transport of trehalose monomycolates across the inner membrane.
  • HY-135856
    SARS-CoV-IN-2

    SARS-CoV Parasite HIV Infection
    SARS-CoV-IN-2 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-2 shows anti-Coronavirus activity with an EC50 of 1.9 μM in Vero cells. SARS-CoV-IN-2 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 21.5 and 30 nM; and IC90s of 51.0 and 99.9 nM; respectively. SARS-CoV-IN-2 reduces HIV-1-induced cytopathic effect with an EC50 of 2.9 μM in MT-4 cells. Antimalarial and Antiviral Activities.
  • HY-14266
    Dapivirine

    TMC120; R147681

    HIV Reverse Transcriptase Apoptosis Autophagy Infection
    Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations.
  • 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-N3387
    Licoricidin

    Apoptosis NF-κB Akt MMP Cancer Inflammation/Immunology
    Licoricidin (LCD) is isolated from Glycyrrhiza uralensis Fisch, possesses anti-cancer activities. Licoricidin (LCD) inhibit SW480 cells (IC50=7.2 μM) by inducing cycle arrest, apoptosis and autophagy, and is a potential chemopreventive or chemotherapeutic agent against colorectal cancer. Licoricidin (LCD) inhibits Lung Metastasis by inhibition of tumor angiogenesis and lymphangiogenesis as well as changes in the local microenvironment of tumor tissues the anticarcinogenic effect. Licoricidin enhanced gemcitabine-induced cytotoxicity in Osteosarcoma (OS) cells by inactivation of the Akt and NF-κB pathways in vitro and in vivo. Licoricidin blocks UVA-induced photoaging via ROS scavenging, limits the activity of MMP-1, it can be considered as an active ingredient in new topically applied anti-ageing formulations.
  • HY-124675
    MYCMI-6

    NSC354961

    c-Myc Apoptosis Cancer
    MYCMI-6 (NSC354961) is a potent and selective endogenous MYC:MAX protein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with a Kd of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner (IC50<0.5 μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 induces apoptosis.
  • HY-131058
    Muscotoxin A

    ADC Cytotoxin Cancer
    Muscotoxin A is an ADC cytotoxin. Muscotoxin A is a cytotoxic lipopeptide that permeabilizes mammalian cell membranes and induces necrotic cell death.
  • HY-15036A
    Diclofenac diethylamine

    COX Apoptosis Inflammation/Immunology
    Diclofenac diethylamine is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac diethylamine induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
  • HY-15037
    Diclofenac Sodium

    GP 45840

    COX Apoptosis Inflammation/Immunology
    Diclofenac Sodium (GP 45840) is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac Sodium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
  • HY-121282A
    Mepazine hydrochloride

    Pecazine hydrochloride

    MALT1 Apoptosis Cancer
    Mepazine hydrochloride (Pecazine hydrochloride) is a potent and selective MALT1 protease inhibitor with IC50s of 0.83 and 0.42 μM for GSTMALT1 full length and GSTMALT1 325-760, respectively. Mepazine hydrochloride affects viability of ABC-DLBCL cells by enhancing apoptosis.
  • HY-D0226
    Quinizarin

    1,4-Dihydroxyanthraquinone

    DNA/RNA Synthesis Fungal Cancer Infection
    Quinizarin (1,4-Dihydroxyanthraquinone), a part of the anticancer agents such as Doxorubicin, Daunorubicin, and Adriamycin, interacts with DNA by intercalating mode (Kd=86.1 μM). Quinizarin is used as a fungicide and pesticide chemical and has shown the ability to inhibit tumor cell growth.
  • HY-121282
    Mepazine

    Pecazine

    MALT1 Apoptosis Cancer
    Mepazine (Pecazine) is a potent and selective MALT1 protease inhibitor with IC50s of 0.83 and 0.42 μM for GSTMALT1 full length and GSTMALT1 325-760, respectively. Mepazine affects viability of ABC-DLBCL cells by enhancing apoptosis.
  • HY-B0640A
    Epinastine hydrochloride

    WAL801 hydrochloride

    Histamine Receptor Endocrinology Inflammation/Immunology
    Epinastine hydrochloride (WAL801 hydrochloride) is an antihistamine and mast cell stabilizer. Epinastine hydrochloride is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine hydrochloride also inhibits IL-8 release and has an antiallergic action.
  • HY-100219
    CB1151

    VD/VDR Cancer
    CB1151 is a 20-epi analogue of 1,25 dihydroxyvitamin D3 (VD) with potent anti-tumor effects. CB1151 inhibits MCF-7 cell growth with an IC50 value of 0.82 nM.
  • HY-129388B
    CC-90011 benzenesulfonate

    LSD1-IN-7 benzenesulfonate

    Histone Demethylase Cancer
    CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
  • HY-100932
    ML-9

    Myosin Cancer
    ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
  • 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-N0128
    Sclareol

    Apoptosis Cancer
    Sclareol is isolated from Salvia sclarea with anticarcinogenic activity. Sclareol shows strong cytotoxic activity against mouse leukemia (P-388), human epidermal carcinoma (KB) cells and human leukemia cell lines. Sclareol induces cell apoptosis.
  • HY-101029A
    MBM-55S

    Ribosomal S6 Kinase (RSK) DYRK Apoptosis Cancer
    MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice.
  • 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-101058
    PD1-PDL1-IN 1

    PD-1/PD-L1 Inflammation/Immunology
    PD1-PDL1-IN 1 is a potent programmed cell death 1 (PD-1) inhibitor. PD1-PDL1-IN 1 is useful as immune modulator.
  • HY-B0640
    Epinastine

    WAL801

    Histamine Receptor Inflammation/Immunology Endocrinology
    Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action.
  • HY-101076
    L-690488

    Phosphatase Metabolic Disease
    L-690488 is a prodrug of L-690330 and is a selective inositol monophosphatase (IMPase) inhibitor. L-690488 has more effective cell penetration than L-690330.
  • HY-137295
    Ingenol 3,20-dibenzoate

    PKC Apoptosis Inflammation/Immunology
    Ingenol 3,20-dibenzoate is a potent protein kinase C (PKC) isoform-selective agonist. Ingenol 3,20-dibenzoate induces selective translocation of nPKC-delta, -epsilon, and -theta and PKC-mu from the cytosolic fraction to the particulate fraction and induces morphologically typical apoptosis through de novo synthesis of macromolecules. Ingenol 3,20-dibenzoate increases the IFN-γ production and degranulation by NK cells, especially when NK cells are stimulated by NSCLC cells.
  • HY-129388
    CC-90011 Methylbenzenesulfonate

    LSD1-IN-7 Methylbenzenesulfonate

    Histone Demethylase Cancer
    CC-90011 Methylbenzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 Methylbenzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 Methylbenzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
  • HY-70002
    Enzalutamide

    MDV3100

    Androgen Receptor Autophagy Cancer
    Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator.
  • HY-113914
    9-ING-41

    GSK-3 Apoptosis Autophagy Cancer
    9-ING-41 is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest, autophagy and apoptosis in cancer cells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic drugs.
  • HY-P1066
    Apelin-17(human, bovine)

    HIV Infection
    Apelin-17(human, bovine) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
  • HY-122181B
    OTS186935 hydrochloride

    Histone Methyltransferase Cancer
    OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells.
  • HY-136373
    Metazachlor

    Others Others
    Metazachlor is a herbicide of the chloroacetamide class. Metazachlor is an inhibitor of the synthesis of long chain fatty acids and has an effect on cell division or tissue differentiation in the germinating and emerging weed target species.
  • HY-120139
    KMH-233

    Others Cancer
    KMH-233, a potent, reversible and selective l-type amino acid transporter 1 (LAT1) inhibitor, inhibits the uptake of LAT1 substrate, l-leucin (IC50=18 μM) as well as cell growth. KMH-233 significantly potentiates the efficacy of Bestatin and Cisplatin even at low concentrations (25 μM).
  • HY-14674
    CP-724714

    EGFR Apoptosis Cancer
    CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC50 of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC50=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities.
  • HY-19617A
    EGFR-IN-1 hydrochloride

    EGFR Cancer
    EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-B2028
    Propargite

    Parasite Infection
    Propargite is a pesticide used to kill mites. Propargite induces β-cell necrosis preceded by DNA damage. Propargite induces MIN6 cell death with an IC50 of 1 μM.
  • HY-119906
    Conglobatin

    FW-04-806

    HSP Apoptosis Cancer
    Conglobatin (FW-04-806), a macrolide dilactone, is isolated from the culture of Streptomyces conglobatus. Conglobatin is an orally active Hsp90 inhibitor. Conglobatin can bind to the N-terminal domain of Hsp90 and disrupt Hsp90-Cdc37 complex formation. Conglobatin induces apoptosis in human breast cancer cells and esophageal squamous cell carcinoma cells, and exhibits antitumor activity in vivo.
  • HY-113204
    N-Oleoyl glycine

    Endogenous Metabolite Cannabinoid Receptor Akt Metabolic Disease
    N-Oleoyl glycine is a lipoamino acid, which stimulates adipogenesis associated with activation of CB1 receptor and Akt signaling pathway in 3T3-L1 adipocyte.
  • HY-N6935
    Sennidin B

    HCV Akt GLUT Infection Metabolic Disease
    Sennidin B, a stereoisomer isolated from the leaves of Cassia angustifolia, has lower activity than Sennidin A. Sennidin A inhibits HCV NS3 helicase, with an IC50 of 0.8 μM. Sennidin A induces phosphorylation of Akt and glucose transporter 4 (GLUT4) translocation. Sennidin A stimulates the glucose incorporation .
  • HY-108847
    Etanercept

    TNF Receptor Inflammation/Immunology
    Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis.
  • 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-121638
    CU-3

    Apoptosis Cancer Inflammation/Immunology
    CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.
  • HY-16196
    ENMD-1198

    IRC-110160

    Microtubule/Tubulin HIF/HIF Prolyl-Hydroxylase STAT Cancer
    ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
  • HY-19896
    COTI-2

    MDM-2/p53 Apoptosis Cancer
    COTI-2, an anti-cancer drug with low toxicity, is an orally available third generation activator of p53 mutant forms. COTI-2 acts both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation.
  • HY-15398A
    5,6-trans-Vitamin D3

    5,6-trans-Cholecalciferol; 5,6-trans-Colecalciferol

    VD/VDR Metabolic Disease
    5,6-trans-Vitamin D3 (5,6-trans-Cholecalciferol;5,6-trans-Colecalciferol) is a photoproduct of vitamin D3. Vitamin D3 is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.
  • HY-P1066A
    Apelin-17(human, bovine) TFA

    HIV Infection
    Apelin-17(human, bovine) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) TFA binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
  • 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-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-122181
    OTS186935

    Histone Methyltransferase Cancer
    OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells.
  • HY-108640
    HLI373

    MDM-2/p53 Parasite Apoptosis Cancer Infection
    HLI373 is an efficacious Hdm2 inhibitor. HLI373 inhibits the ubiquitin ligase activity of Hdm2. HLI373 is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents. Antimalarial activity.
  • HY-108640A
    HLI373 dihydrochloride

    MDM-2/p53 Parasite Apoptosis Cancer Infection
    HLI373 dihydrochloride is an efficacious Hdm2 inhibitor. HLI373 dihydrochloride inhibits the ubiquitin ligase activity of Hdm2. HLI373 dihydrochloride is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents. Antimalarial activity.
  • HY-125531
    Dactylorhin A

    Others Others
    Dactylorhin A, a succinate derivative ester, is isolated from rhizomes of Gymnadenia conopsea. Dactylorhin A exhibits moderate inhibitory effects on NO production effects in RAW 264.7 macrophage cells.
  • HY-19617B
    EGFR-IN-1 TFA

    EGFR Cancer
    EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-19617
    EGFR-IN-1

    EGFR Cancer
    EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-100932A
    ML-9 Free Base

    Myosin Cancer
    ML-9 (Free Base) is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 (Free Base) inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 (Free Base) induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
  • HY-15178
    Oglemilast

    GRC 3886

    Phosphodiesterase (PDE) Inflammation/Immunology
    Oglemilast (GRC 3886) is a potent and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 0.5 nM for PDE4D3. Oglemilast inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast has the potential for inflammatory airway diseases.
  • HY-103454
    MPP dihydrochloride

    Estrogen Receptor/ERR Cancer
    MPP dihydrochloride is a highly selective estrogen receptor alpha (ERα) antagonist. MPP dihydrochloride reduces the ratio of p-ERα/ERα.
  • HY-N4010
    Iriflophenone

    Others Cancer
    Iriflophenone, isolated from Aquilaria sinensis, stimulates MCF-7 and T-47D human breast cancer cells proliferation.
  • HY-125209A
    TH5427 hydrochloride

    DNA/RNA Synthesis Cancer
    TH5427 hydrochloride is a potent, selective NUDT5 inhibitor (IC50=29 nM). TH5427 hydrochloride shows an apparent 690-fold selectivity for NUDT5 over MTH1. TH5427 hydrochloride blocks progestin-dependent, PAR-derived nuclear ATP synthesis and subsequent chromatin remodeling, gene regulation and proliferation in breast cancer cells.
  • HY-N4114
    Picrocrocin

    Apoptosis Cancer
    Picrocrocin, an apocarotenoid found in the flowers of Cochliobolus sativus. Picrocrocin shows anticancer effect. Picrocrocin exhibits growth inhibitory effects against SKMEL-2 human malignant melanoma cells.
  • HY-N0069
    Solamargine

    Solamargin; δ-Solanigrine

    P-glycoprotein Apoptosis Cancer
    Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition. Solamargine significantly inhibits migration and invasion of HepG2 cells by down-regulating MMP-2 and MMP-9 expression and activity.
  • HY-102022
    α-Galactosylceramide

    α-GalCer; KRN7000

    Others Cancer Inflammation/Immunology
    α-Galactosylceramide (α-GalCer) is a synthetic glycolipid with antitumorial and immunostimulatory. α-Galactosylceramide is a very potent NKT cell agonist and binds effectively to CD1d. The complex of α-Galactosylceramide plus CD1d binds the NKT cell TCR (T cell antigen receptor).
  • HY-116304
    1G244

    Dipeptidyl Peptidase Apoptosis Cancer
    1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects.
  • HY-135855
    SARS-CoV-IN-1

    SARS-CoV Parasite Infection
    SARS-CoV-IN-1 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-1 shows anti-Coronavirus activity with an EC50 of 4.9 μM in Vero cells. SARS-CoV-IN-1 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 15.4 and 133.2 nM; and IC90s of 25.7 and 459.1 nM; respectively. Antimalarial and antiviral activities.
  • HY-10230
    Midostaurin

    PKC412; CGP 41251

    PKC Cancer
    Midostaurin (PKC412; CGP 41251) is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM.
  • HY-N7634
    Tectol

    Farnesyl Transferase Parasite Cancer Infection
    Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM. Tectol is a farnesyltransferase (FTase) inhibitor with IC50s of 2.09 and 1.73 μM for human and T. brucei FTase, respectively. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC50 of 3.44 μM.
  • HY-136594
    BODIPY aminoacetaldehyde

    BAAA

    Aldehyde Dehydrogenase (ALDH) Cancer
    BODIPY aminoacetaldehyde (BAAA) is a fluorescent substrate for both murine and human aldehyde dehydrogenase (ALDH). BODIPY aminoacetaldehyde consists of an aminoacetaldehyde moiety bonded to the BODIPY fluorochrome and can be used to label stem cells.
  • 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-104066
    Theliatinib

    HMPL-309

    EGFR Cancer
    Theliatinib (HMPL-309) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases. Anti-tumor activity.
  • HY-N2447
    Amarogentin

    AMPK Apoptosis Cancer Metabolic Disease
    Amarogentin is a secoiridoid glycoside that is mainly extracted from Swertia and Gentiana roots. Amarogentin exhibits many biological effects, including anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin exerts hepatoprotective and immunomodulatory effects. Amarogentin promotes apoptosis, arrests G2/M cell cycle and downregulates of PI3K/Akt/mTOR signalling pathways. Amarogentin exerts beneficial vasculo-metabolic effect by activating AMPK.
  • HY-110147A
    SSM3 tetraTFA

    Others Infection
    SSM3 tetraTFA is a potent synthetic furin inhibitor with an EC50 and a Ki of 54 nM and 12 nM, respectively. SSM3 tetraTFA is able to block furin-dependent cell surface processing of anthrax protective antigen-83 in vitro.
  • HY-126307
    Urolithin B

    NF-κB JNK ERK Akt AMPK Endogenous Metabolite Inflammation/Immunology
    Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.
  • 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-12830
    M-110

    Pim Cancer
    M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM.
  • HY-W011916
    Muramic acid

    Bacterial Others
    Muramic acid is a component in many Gram-positive bacterial cell walls, as marker for Gram-positive bacteria.
  • HY-18773
    Oct3/4-inducer-1

    Oct3/4 Inflammation/Immunology
    Oct3/4-inducer-1 (compound 2) is a potent Oct3/4 inducer. Oct3/4-inducer-1 promotes expression and stabilization of Oct3/4, and enhances its transcriptional activity in diverse human somatic cells.
  • HY-131042
    NNMTi

    Others Metabolic Disease
    NNMTi is a potent nicotinamide N-methyltransferase (NNMT) inhibitor (IC50=1.2 μM) and selectively binds to the NNMT substrate-binding site residues. NNMTi  promotes myoblast differentiation in vitro and enhances fusion and regenerative capacity of muscle stem cells (muSCs) in aged mice.
  • HY-112234
    L-Sepiapterin

    Sepiapterin

    Endogenous Metabolite Cancer
    L-Sepiapterin (Sepiapterin) is a precursor of the endothelial nitric oxide synthase (eNOS) cofactor tetrahydrobiopterin (BH4). L-Sepiapterin improves endothelial dysfunction in small mesenteric arteries from db/db mice, and induces angiogenesis. L-Sepiapterin inhibits cell proliferation and migration of ovarian cancer cells via down-regulation of p70 S6K-dependent VEGFR-2 expression.
  • HY-13603
    Crolibulin

    EPC2407

    Microtubule/Tubulin Apoptosis Cancer
    Crolibulin (EPC2407) is a tubulin polymerization inhibitor, with potent apoptosis induction and cell growth inhibition. Crolibulin has anti-tumor activity. Crolibulin also has cardiovascular toxicity and neurotoxicity.
  • HY-15244
    Alpelisib

    BYL-719

    PI3K Cancer
    Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity.
  • HY-12378
    BQ-123

    Endothelin Receptor Cardiovascular Disease
    BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.
  • HY-100746
    STF-62247

    Autophagy Cancer
    STF-62247 is an autophagy inducer that selectively cytotoxic to VHL-deficient renal cell carcinoma (IC50 of 0.625 μM and 16 μM in RCC4 and RCC4/VHL cells, respectively).
  • HY-125801
    3-Oxo-5β-cholanoic acid

    Dehydrolithocholic acid; 3-oxoLCA

    ROR Inflammation/Immunology
    3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid), a bile acid metabolite, inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd=1.13 μM).
  • HY-100608
    BMS453

    BMS-189453

    RAR/RXR Cancer
    BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.
  • HY-124652
    TBK1/IKKε-IN-4

    IKK Cancer
    TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR.
  • HY-15160A
    TAK-960 hydrochloride

    Polo-like Kinase (PLK) Cancer
    TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
  • HY-15160B
    TAK-960 dihydrochloride

    Polo-like Kinase (PLK) Cancer
    TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
  • HY-15160
    TAK-960

    Polo-like Kinase (PLK) Cancer
    TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
  • HY-11062
    Icilin

    AG-3-5

    TRP Channel Cancer Neurological Disease
    Icilin (AG-3-5) is an agonist of nonselective cation channel TRPM8, with antiproliferative activity. Icilin activates currents only in wild type TRPM8 and in the presence of Ca 2+. Icilin can induce G1 arrest in prostate cancer cells.
  • HY-12378A
    BQ-123 TFA

    Endothelin Receptor Cardiovascular Disease
    BQ-123 TFA is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 TFA inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.
  • HY-12646A
    Rhosin

    Ras Apoptosis Cancer
    Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis. Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability.
  • HY-12646
    Rhosin hydrochloride

    Ras Apoptosis Cancer
    Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis. Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability.
  • HY-103661
    BI-6C9

    Mitochondrial Metabolism Apoptosis Neurological Disease
    BI-6C9 is a highly specific BH3 interacting domain (Bid) inhibitor, which prevents mitochondrial outer membrane potential (MOMP) and mitochondrial fission, and protects the cells from mitochondrial apoptosis inducing factor (AIF) release and caspase-independent cell death in neurons.
  • HY-N8098
    Pulchinenoside E2

    Others Cancer
    Pulchinenoside E2 (Compound 8) is a triterpene saponin isolated from the roots of Pulsatilla chinensis. Pulchinenoside E2 shows cytotoxic to HL-60 cells with an IC50 value of 2.6 µg/mL.
  • HY-15160C
    TAK-960 monohydrochloride

    Polo-like Kinase (PLK) Cancer
    TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
  • HY-115452
    G5-7

    JAK Apoptosis Cancer
    G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr 1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study.
  • HY-112299
    TAS6417

    CLN-081

    EGFR Apoptosis Cancer
    TAS6417 (CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM.
  • HY-N0569
    Madecassic acid

    NO Synthase COX TNF Receptor Interleukin Related Inflammation/Immunology
    Madecassic acid is isolated from Centella asiatica (Umbelliferae). Madecassic acid has anti-inflammatory properties caused by iNOS, COX-2, TNF-alpha, IL-1beta, and IL-6 inhibition via the downregulation of NF-κB activation in RAW 264.7 macrophage cells.
  • HY-15346
    Copanlisib

    BAY 80-6946

    PI3K Apoptosis Cancer
    Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity.
  • HY-15346A
    Copanlisib dihydrochloride

    BAY 80-6946 dihydrochloride

    PI3K Apoptosis Cancer
    Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity.
  • HY-112764
    DMG-PEG 2000

    Others Metabolic Disease
    DMG-PEG 2000 is used for the preparation of liposome for siRNA delivery with improved transfection efficiency in vitro. DMG-PEG 2000 is also used for the lipid nanoparticle for an oral plasmid DNA delivery approach in vivo through a facile surface modification to improve the mucus permeability and delivery efficiency of the nanoparticles.
  • HY-15473A
    MLN120B dihydrochloride

    ML120B dihydrochloride

    IKK Cancer Inflammation/Immunology
    MLN120B dihydrochloride (ML120B dihydrochloride) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC50 of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis.
  • HY-N3446
    IVHD-valtrate

    Apoptosis Cancer
    IVHD-valtrate, an active Valeriana jatamansi derivative, is against human ovarian cancer cells in vitro and in vivo. IVHD-valtrate induces cancer cells apoptosis and arrests the ovarian cancer cells in the G2/M phase. IVHD-valtrate has the potential to be a novel chemotherapeutic agent for the human ovarian cancer research.
  • HY-135774
    6-Hydroxybenzbromarone

    Drug Metabolite Phosphatase Cardiovascular Disease
    6-Hydroxybenzbromarone is the major metabolite of Benzbromarone with a longer half-life and greater pharmacological potency than the parent compound. 6-Hydroxybenzbromarone is a protein Eyes Absent 3 (EYA3) inhibitor with an IC50 value of 21.5 μM. 6-Hydroxybenzbromarone is an angiogenic agent, has strong inhibitory effects on cell migration, tubulogenesis, and angiogenic sprouting.
  • HY-114356
    BPI-9016M

    c-Met/HGFR Cancer
    BPI-9016M is a potent, orally active, and selective dual c-Met and AXL tyrosine kinases inhibitor. BPI-9016M suppresses tumor cell growth, migration and invasion of lung adenocarcinoma.
  • HY-112608
    CHMFL-PI3KD-317

    PI3K Cancer
    CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells.
  • HY-119198
    NSC745885

    Apoptosis Histone Methyltransferase Cancer
    NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers.
  • HY-19642
    Glesatinib

    MGCD265

    TAM Receptor c-Met/HGFR Cancer
    Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).
  • HY-19642A
    Glesatinib hydrochloride

    MGCD265 hydrochloride

    TAM Receptor c-Met/HGFR Cancer
    Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).
  • HY-110177
    SP-100030

    NF-κB Inflammation/Immunology
    SP-100030 is a potent NF-κB and activator protein-1 (AP-1) double inhibitor (IC50s=50 and 50 nM, respectively). SP-100030 inhibits IL-2, IL-8, and TNF-alpha production in Jurkat and other T cell lines. SP-100030 decreases murine collagen-induced arthritis (CIA).
  • HY-W011338
    Benzyl butyl phthalate

    Aryl Hydrocarbon Receptor Cancer
    Benzyl butyl phthalate, a member of phthalic acid esters (PAEs), can trigger the migration and invasion of hemangioma (HA) cells via upregulation of Zeb1. Benzyl butyl phthalate activates aryl hydrocarbon receptor (AhR) in breast cancer cells to stimulate SPHK1/S1P/S1PR3 signaling and enhances formation of metastasis-initiating breast cancer stem cells (BCSCs).
  • 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-128932
    Cefminox sodium

    MT-141

    Bacterial PPAR Prostaglandin Receptor Antibiotic Infection Cardiovascular Disease Endocrinology
    Cefminox sodium (MT-141) is a semisynthetic cephamycin, which exhibits a broad spectrum of antibacterial activity. Cefminox sodium (MT-141) also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ, upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium (MT-141) also prevents pulmonary arterial hypertension.
  • 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-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-18522
    AA26-9

    Phospholipase Metabolic Disease
    AA26-9 is a potent and broad spectrum serine hydrolase inhibitor. AA26-9 targets included serine peptidases, lipases, amidases, esterases, and thioesterases. AA26-9 shows inhibitory activity against approximately 1/3 of the 40+ serine hydrolases detected in immortalized T cell lines .
  • HY-113962
    7α,25-Dihydroxycholesterol

    7α,25-OHC

    EBI2/GPR183 Endogenous Metabolite Inflammation/Immunology
    7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells.
  • HY-136498
    T-705RMP

    Drug Metabolite Infection
    T-705RMP, a phosphorylated metabolite of T-705, exhibits a very weak inhibitory effect on the IMP dehydrogenase (IMPDH) activities of the host cells, with an IC50 of 601 μM.
  • 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-16399
    Pladienolide B

    Apoptosis Cancer
    Pladienolide B is a potent cancer cell growth inhibitor that targets the SF3B1 subunit of the spliceosome. Pladienolide B exerts antitumor activities mediated through the inhibition of pre-mRNA splicing. Pladienolide B induces apoptosis.
  • HY-103697
    Gardiquimod

    Toll-like Receptor (TLR) HIV Cancer Infection
    Gardiquimod, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 when used at concentrations below 10 μM.
  • HY-118341
    Clitocine

    Apoptosis Bcl-2 Family Cancer
    Clitocine, an adenosine nucleoside analog isolated from mushroom, is a potent and efficacious readthrough agent. Clitocine acts as a suppressor of nonsense mutations and can induce the production of p53 protein in cells harboring p53 nonsense-mutated alleles. Clitocine can induce apoptosis in multidrug-resistant human cancer cells by targeting Mcl-1. Anticancer activity.
  • HY-12319
    Cardiogenol C

    β-catenin Wnt Cancer
    Cardiogenol C is a potent cell-permeable pyrimidine inducer which prompts the differentiation of ESCs into cardiomyocytes (EC50=100 nM). Cardiogenol C also acts cardiomyogenic on already lineage-committed progenitor cell types with a limited degree of plasticity. Cardiogenol C is a useful cardiomyogenic agent and can be used as a tool to improve cardiac repair by cell transplantation therapy in animal models.
  • HY-12319A
    Cardiogenol C hydrochloride

    β-catenin Wnt Cardiovascular Disease
    Cardiogenol C hydrochloride is a potent cell-permeable pyrimidine inducer which prompts the differentiation of ESCs into cardiomyocytes (EC50=100 nM). Cardiogenol C hydrochloride also acts cardiomyogenic on already lineage-committed progenitor cell types with a limited degree of plasticity. Cardiogenol C hydrochloride is a useful cardiomyogenic agent and can be used as a tool to improve cardiac repair by cell transplantation therapy in animal models.
  • HY-130709
    PROTAC CDK2/9 Degrader-1

    PROTAC CDK Cancer
    PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with CRBN ligand.
  • HY-129099
    N-Desmethyltamoxifen

    PKC Estrogen Receptor/ERR Drug Metabolite Cancer
    N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
  • HY-129099A
    N-Desmethyltamoxifen hydrochloride

    PKC Estrogen Receptor/ERR Drug Metabolite Cancer
    N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
  • HY-N7262
    Hydroxyvalerenic acid

    Others Cancer
    Hydroxyvalerenic acid is isolated from Verbena officinalis, has a low toxicity with IC50 values of 123 and 165 μM against GLC4 and COLO 320 cells, respectively.
  • HY-15838
    ID-8

    DYRK Cancer
    ID-8 is an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase (DYRK). ID-8 sustains embryonic stem cell (ESC) self-renewal and pluripotency. ID-8 enhances Wnt-mediated hESC survival and proliferation via inhibition of DYRKs.
  • HY-13894
    Tyrphostin AG1296

    AG1296

    PDGFR c-Kit FLT3 Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range.
  • HY-N4000
    Digitonin

    Others Cancer
    Digitonin, a glycoside obtained from Digitalis purpurea, could increase cell permeability by binding to cholesterol molecules and reduce tumor growth. Digitonin is an natural detergent.
  • HY-10514
    BX795

    PDK-1 IKK Autophagy Cancer
    BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKɛ, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy.
  • HY-10230S
    Midostaurin-D5

    PKC412-D5; CGP 41251-D5

    Others Cancer
    Midostaurin-D5 (PKC412-D5) is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM.
  • HY-N0656A
    (+)-Usnic acid

    mTOR Bacterial Cancer
    (+)-Usnic acid is isolated from isolated from lichens, binds at the ATP-binding pocket of mTOR, and inhibits mTORC1/2 activity. (+)-Usnic acid inhibits the phosphorylation of mTOR downstream effectors: Akt (Ser473), 4EBP1, S6K, induces autophay, with anti-cancer activity. (+)-Usnic acid possesses antimicrobial activity against a number of planktonic gram-positive bacteria, including Staphylococcus aureus, Enterococcus faecalis, and Enterococcus faecium.
  • HY-N3119
    Paeoniflorigenone

    Apoptosis Cancer
    Paeoniflorigenone, isolated as an active ingredient from the root of moutan cortex, induces apoptosis selectively in the cancer cell lines and exhibits antiproliferative effect.
  • HY-133128
    FM26

    ROR Cancer
    FM26 (compound 25) is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 264 nM. FM26 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells.
  • HY-P1064
    Apelin-36(human)

    HIV Infection Metabolic Disease Cardiovascular Disease
    Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
  • HY-135680
    I-OMe-Tyrphostin AG 538

    I-OMe-AG 538

    IGF-1R Cancer Metabolic Disease
    I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50 of 1 µM.
  • HY-70068
    SB-408124

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    SB-408124 is a non-peptide OX1 receptor antagonist with Kis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 exhibits 50-fold selectivity over OX2 receptor.
  • HY-10251
    BMS-599626

    AC480

    EGFR Cancer
    BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.
  • HY-126666
    PNU-159682 carboxylic acid

    ADC Cytotoxin Cancer Inflammation/Immunology
    PNU-159682 carboxylic acid (compound 53) is a potent ADCs cytotoxin and encodes a member of the C-type lectin/C-type lectin-like domain (CTL/CTLD) superfamily. PNU-159682 carboxylic acid has protein fold and diverse functions, such as cell adhesion, cell-cell signalling, glycoprotein turnover, and roles in inflammation and immune response.
  • HY-13297
    PYZD-4409

    E1/E2/E3 Enzyme Cancer
    PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells.
  • HY-103697A
    Gardiquimod diTFA

    Toll-like Receptor (TLR) HIV Cancer Infection
    Gardiquimod diTFA, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod diTFA could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 when used at concentrations below 10 μM.
  • HY-B1057S2
    Nefopam D3

    Fenazoxine D3

    β-catenin Neurological Disease
    Nefopam D3 (Fenazoxine D3) is a deuterium labeled Nefopam (Fenazoxine). Nefopam is a centrally-acting but non-opioid analgesic drug, and Nefopam targets β-catenin protein level in mesenchymal cells.
  • HY-P1126
    Dolastatin 15

    DLS 15

    Microtubule/Tubulin ADC Cytotoxin Apoptosis Cancer
    Dolastatin 15 (DLS 15), a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the antitubulin agent Dolastatin 10. Dolastatin 15 induces cell cycle arrest and apoptosis in multiple myeloma cells. Dolastatin 15 can be used as an ADC cytotoxin.
  • HY-A0067
    Oxybenzone

    Benzophenone 3

    RAR/RXR Autophagy Apoptosis Neurological Disease
    Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells.
  • HY-B0902A
    Rufloxacin hydrochloride

    MF-934 hydrochloride

    Bacterial Infection
    Rufloxacin hydrochloride (MF-934 hydrochloride) is a fluoroquinolone antibacterial, inhibits B-cell differentiation in human mononuclear cells, inhibits Topo.
  • 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-101870B
    INCB053914 phosphate

    Pim Cancer
    INCB053914 phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. INCB053914 phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines.
  • HY-136057
    iFSP1

    Ferroptosis Cancer
    iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1) (AIFM2) with an EC50 of 103 nM. iFSP1 selectively induces ferroptosis in GPX4-knockout cells which overexpressed FSP1. iFSP1 is able to sensitize a variety of human cancer cell lines to the ferroptosis inducer, such as (1S,3R)-RSL3 (HY-100218A).
  • HY-16918
    Heptamidine

    SBi4211

    Others Cancer Inflammation/Immunology
    Heptamidine (SBi4211) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanoma cells with S100B over those without S100B. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM).
  • HY-102011
    BMS-1166

    PD-1/PD-L1 Cancer Inflammation/Immunology
    BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell 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-N6036
    Ganoderic acid F

    Others Cancer
    Ganoderic acid F is a ganoderic acid. Ganoderic acid F exhibits antitumor and antimetastatic activities through inhibition of angiogenesis and alteration of proteins involving cell proliferation and/or cell death, carcinogenesis, oxidative stress, calcium signaling, and endoplasmic reticulum stress.
  • HY-B0497B
    Niclosamide monohydrate

    BAY2353 monohydrate

    STAT Bacterial Antibiotic Infection
    Niclosamide monohydrate is an inhibitor of STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
  • HY-P1064A
    Apelin-36(human) TFA

    HIV Infection Metabolic Disease Cardiovascular Disease
    Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) TFA shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC550=8.61). Apelin-36(human) TFA has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
  • HY-13775
    XL019

    JAK Apoptosis Cancer
    XL019 is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.
  • HY-123076
    Pifithrin-α, p-Nitro, Cyclic

    PFN-α

    MDM-2/p53 Neurological Disease
    Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED50=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue.
  • HY-113846
    CMP-5 hydrochloride

    Histone Methyltransferase Cancer
    CMP-5 hydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 hydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 hydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected.
  • HY-113498
    Sphingomyelin

    Endogenous Metabolite Metabolic Disease Inflammation/Immunology Neurological Disease
    Sphingomyelin is a eukaryotic sphingolipid and one of the major constituents of cell membranes and particularly abundant in the myelin sheath that surrounds neuronal axons. Sphingomyelin plays an important role in cell processes, the regulation of inflammatory responses, and signal transduction. Sphingomyelin metabolism is associated with various central nervous system diseases and Niemann–Pick disease.
  • 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-128587
    Mevociclib

    SY-1365

    CDK Cancer
    Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors.
  • 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-16918A
    Heptamidine dimethanesulfonate

    SBi4211 dimethanesulfonate

    Others Cancer Inflammation/Immunology
    Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanoma cells with S100B over those without S100B. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM).
  • HY-13919
    Napabucasin

    STAT Cancer
    Napabucasin is a STAT3 inhibitor which blocks stem cell activity in cancer cells.
  • HY-B1776
    Spermidine

    Endogenous Metabolite Metabolic Disease
    Spermidine maintains cell membrane stability, increases antioxidant enzymes activities, improving photosystem II (PSII), and relevant gene expression. Spermidine significantly decreases the H2O2 and O2 .- contents.
  • HY-107846
    Xylan

    Others Others
    Xylan represents the main hemicellulose component in the secondary plant cell walls of flowering plants. Xylan is a polysaccharide made from units of xylose and contains predominantly β-D-xylose units linked as in cellulose.
  • HY-B1776A
    Spermidine trihydrochloride

    Others Metabolic Disease
    Spermidine trihydrochloride maintains cell membrane stability, increases antioxidant enzymes activities, improving photosystem II (PSII), and relevant gene expression. Spermidine trihydrochloride significantly decreases the H2O2 and O2 .- contents.
  • HY-120327
    KY-226

    Phosphatase Metabolic Disease Neurological Disease
    KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury.
  • HY-100734
    Histone Acetyltransferase Inhibitor II

    Histone Acetyltransferase Cancer
    Histone Acetyltransferase Inhibitor II (compound 2c) is a potent, selective and cell permeable p300 histone acetyltransferase inhibitor, with an IC50 of 5 µM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.
  • HY-19694
    BRD7552

    Others Endocrinology
    BRD7552, a potent PDX1 transcription factor inducer, upregulates PDX1 expression in both primary human islets and ductal cells, and induces epigenetic changes in the PDX1 promoter consistent with transcriptional activation. BRD7552 increases insulin expression. PDX1 is a key transcription factor involved in pancreas development and β cell function.
  • HY-10183
    Go6976

    PKC Infection
    Go6976 is a Protein Kinase C (PKC) inhibitor, with an IC50 of 20 nM.
  • HY-100237
    SZL P1-41

    E1/E2/E3 Enzyme Apoptosis Cancer
    SZL P1-41 is a specific Skp2 inhibitor, binds to the F-box domain of Skp2 to prevent Skp1 association and Skp2 SCF complex formation. SZL P1-41, like Skp2 deficiency, augments p27-mediated apoptosis/senescence, while it impairs Akt-driven glycolysis. Anti-tumor activities.
  • HY-133654
    2,3,3-Tribromopropenoic acid

    Others Others
    2,3,3-Tribromopropenoic acid is a 2,3,3-Tribromo product based on propenoic acid. 2,3,3-Tribromopropenoic acid is a polar aromatic brominated disinfection byproduct during chlorination in water and shows cytotoxic potency in mammalian cell chronic cytotoxicity experiments.
  • HY-75564
    Cyclo(Ala-Gly)

    Endogenous Metabolite Cancer
    Cyclo(Ala-Gly), a metabolite of a mangrove endophytic fungus, Penicillium thomi, exhibits cytotoxicity against A549, HepG2 and HT29 cells. The IC50 values range from 9.5 to 18.1 μM.
  • HY-12755
    ML141

    CID-2950007

    Ras Apoptosis Cancer
    ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines.
  • HY-120137
    CMP-5

    Histone Methyltransferase Cancer
    CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected.
  • HY-B0449
    Methacycline hydrochloride

    Bacterial Antibiotic Infection
    Methacycline hydrochloride is a tetracycline antibiotic and can inhibits bacterial protein synthesis. Methacycline hydrochloride is a potent epithelial-mesenchymal transition (EMT) inhibitor. Methacycline hydrochloride blocks EMT in vitro and fibrogenesis in vivo without directly affecting TGF-β1 Smad signaling. Methacycline hydrochloride is an antimicrobial and has the potential for pulmonary fibrosis.
  • HY-128206
    I3MT-3

    HMPSNE

    Hippo (MST) Metabolic Disease
    I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC50=2.7 μM). I3MT-3 is inactive for other H2S/sulfane sulfur-producing enzymes. I3MT-3 targets a persulfurated cysteine residue located in the active site of 3MST.
  • HY-108556
    RWJ-56110

    Protease-Activated Receptor (PAR) Apoptosis Cardiovascular Disease
    RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 inhibits angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 induces cell apoptosis.
  • HY-Y0248A
    Farnesol

    Endogenous Metabolite Bacterial Antibiotic Infection Cancer
    Farnesol is a sesquiterpene alcohol that modulates cell-to-cell communication in Candida albicans, and has the activity in inhibiting bacteria.
  • HY-121087
    BCI-215

    Phosphatase Cancer
    BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells.
  • HY-13440
    AMG 511

    PI3K Cancer
    AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model.
  • 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-114410
    CCI-006

    Mitochondrial Metabolism Cancer
    CCI-006 is a selective inhibitor and chemosensitizer of MLL-rearranged leukemia cells, by inhibits mitochondrial respiration resulting in insurmountable mitochondrial depolarization and a pro-apoptotic unfolded protein response (UPR) in a subset of MLL-r leukemia cells.
  • HY-134130
    Integrin modulator 1

    Integrin Inflammation/Immunology
    Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM.
  • HY-13306
    Pyrintegrin

    Integrin Metabolic Disease
    Pyrintegrin is an β1-integrin agonist and a 2,4-disubstituted pyrimidine that promotes embryonic stem cells survival. Pyrintegrin enhances cell-extracellular matrix (ECM) adhesion-mediated integrin signaling. Pyrintegrin can be used as a podocyte-protective agent and has robustly adipogenic.
  • HY-N7255
    Cycloartenol

    p38 MAPK Apoptosis Cancer
    Cycloartenol, a phytosterol compound, is one of the key precusor substances for biosynthesis of numerous sterol compounds. Cycloartenol inhibits the migration of glioma cells and suppresses the phosphorylation of the p38 MAP kinase. Cycloartenol has a variety of pharmacological activities such as anti-inflammatory, anti-tumor, antioxidant, antibiosis and anti-alzheimer's disease. Cycloartenol also plays an important role in the process of plant growth and development.
  • HY-19331
    WZB117

    GLUT Cancer
    WZB117 is a glucose transporter 1 (Glut1) inhibitor, which downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo.
  • HY-103637
    Vimirogant

    VTP-43742

    ROR Inflammation/Immunology
    Vimirogant (VTP-43742) is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant has the potential for autoimmune disorders research.
  • HY-103637A
    Vimirogant hydrochloride

    VTP-43742 hydrochloride

    ROR Inflammation/Immunology
    Vimirogant (VTP-43742) hydrochloride is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant hydrochloride exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant hydrochloride inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant hydrochloride has the potential for autoimmune disorders research.
  • HY-N1713
    29-Nor-20-oxolupeol

    Others Neurological Disease
    29-Nor-20-oxolupeol, extracted from Impatiens basamina, reduces NO levels in LPS-activated murine microglial cells with an IC50 of 44.21 µM.
  • HY-W015399
    4-Methylcinnamic acid

    Fungal Infection
    4-Methylcinnamic acid, a Cinnamic acid analog, can be used as a intervention catalyst for overcoming antifungal tolerance. 4-Methylcinnamic acid can improve the potency of cell wall-disrupting agents.
  • HY-N2028
    Demethylwedelolactone

    Others Cancer
    Demethylwedelolactone is a naturally occurring coumestan isolated from Eclipta alba. Demethylwedelolactone is a potent trypsin inhibitor with an IC50 of 3.0 μM. Demethylwedelolactone suppresses cell motility and cell invasion of breast cancer cell.
  • HY-W011404
    Tributyrin

    Glyceryl tributyrate

    Apoptosis Metabolic Disease
    Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed prodrug of Butyric Acid. Tributyrin diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into the cell in vivo. Tributyrin has potent antiproliferative, proapoptotic and differentiation-inducing effects.
  • 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-13915
    NSC348884

    Apoptosis Cancer
    NSC348884 is a nucleophosmin inhibitor disrupts oligomer formation and induces apoptosis, inhibits cell proliferation at an IC50 of 1.7-4.0 μM in distinct cancer cell lines.
  • HY-P1185
    Antagonist G

    Vasopressin Receptor Apoptosis Cancer
    Antagonist G is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy.
  • HY-123905
    LIN28 inhibitor LI71

    MicroRNA Others
    LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM. LIN28 inhibitor LI71 directly binds the cold shock domain (CSD) to suppress LIN28’s activity against let-7 in leukemia cells and embryonic stem cells.
  • HY-116894
    Rotundifuran

    Apoptosis Cancer
    Rotundifuran, a labdane type diterpene, is isolated from Vitex rotundifolia. Rotundifuran can inhibit the cell cycle progression and induce apoptosis in human myeloid leukaemia cells.
  • HY-117977
    FCPR03

    Phosphodiesterase (PDE) Inflammation/Immunology Neurological Disease
    FCPR03 is a potent and selective phosphodiesterase 4 (PDE4) inhibitor with IC50 values of 60 nM, 31 nM and 47 nM for PDE4 catalytic domain, PDE4B1 and PDE4D7, respectively. FCPR03 displays at least 2100-fold selectivity over other PDEs (PDE1-3 and PDE5-11). FCPR03 has anti-inflammatory, neuroprotective and antidepressant-like effects.
  • HY-19619
    m-3M3FBS

    Phospholipase Apoptosis Cancer
    m-3M3FBS is a potent phospholipase C (PLC) activator. m-3M3FBS stimulates superoxide generation in human neutrophils, upregulates intracellular calcium concentration, and stimulates inositol phosphate generation in various cell lines. m-3M3FBS induces monocytic leukemia cell apoptosis.
  • HY-P1185A
    Antagonist G TFA

    Vasopressin Receptor Apoptosis Cancer
    Antagonist G TFA is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy.
  • HY-10046
    Plerixafor

    AMD 3100; JM3100; SID791

    CXCR HIV Virus Protease Cancer Infection Endocrinology Inflammation/Immunology
    Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM.
  • HY-50908
    Ridaforolimus

    MK-8669; Deforolimus; AP23573

    mTOR Autophagy Cancer
    Ridaforolimus (MK-8669) is a potent and selective mTOR inhibitor; inhibits ribosomal protein S6 phosphorylation with an IC50 of 0.2 nM in HT-1080 cells.
  • HY-12624
    ON123300

    CDK AMPK Cancer
    ON123300, a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent ON123300 causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors. ON123300 inhibits CDK6 with an IC50 of 9.82 nM.
  • HY-N7019
    19-Hydroxybufalin

    Others Cancer
    19-Hydroxybufalin is a bufadienolide, inhibits epithelial-mesenchymal transition and attenuates the migration and invasion of PC3 cells.
  • HY-125965
    BioA-IN-13

    Bacterial Infection
    BioA-IN-13 is a potent, cell permeable and whole-cell active inhibitor of Mycobacterium tuberculosis BioA enzyme.
  • HY-B0862
    Pendimethalin

    Others Others
    Pendimethalin is an herbicide that controls annual grasses and certain broadleaf weeds. Pendimethalin inhibits cell division and cell elongation.
  • HY-N1992
    Theaflavin 3,3'-digallate

    TF-3; ZP10

    Virus Protease HSV HIV Cancer Infection
    Theaflavin 3,3'-digallate (TF-3) is a potent Zika virus (ZIKV) protease inhibitor with an IC50 of 2.3 μM. Theaflavin 3,3'-digallat directly binds to ZIKVpro (Kd=8.86 µM) and inhibits ZIKV replication. Theaflavin 3,3'-digallat inhibits the activity of gp41 and NS2B-3 protease and has antiviral activity against HSV and HIV-1. Theaflavin 3,3'-digallate, the typical pigment in black tea, is a potent antitumor agent.
  • HY-W013699
    Chlorhexidine diacetate

    Bacterial Antibiotic Infection
    Chlorhexidine diacetate is a biguanide disinfectant with rapid bactericidal activity against both Gram-positive and Gram-negative organism. The antibacterial effect of chlorhexidine diacetate is related to its action on the bacterial cell membrane and to precipitation of intracellular contents.
  • HY-B0986
    Hexylresorcinol

    4-Hexylresorcinol

    Parasite Bacterial Apoptosis Glucosidase Cancer Infection Metabolic Disease
    Hexylresorcinol (4-Hexylresorcinol) is a natural compound found in plants with antimicrobial, anthelmintic, antiseptic and antitumor activities. Hexylresorcinol can induce apoptosis in squamous carcinoma cells. Hexylresorcinol is a reversible and noncompetitive inhibitor of α-glucosidase. Hexylresorcinol has protective effects against oxidative DNA damage.
  • HY-P1201
    Cyclosomatostatin

    Somatostatin Receptor Cancer
    Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
  • HY-136648A
    2'-Deoxyadenosine-5'-triphosphate trisodium

    dATP trisodium

    Endogenous Metabolite Others
    2'-Deoxyadenosine-5'-triphosphate trisodium (dATP trisodium) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
  • HY-113950
    Dichlorophenyl-ABA

    Others Neurological Disease
    Dichlorophenyl-ABA is an inhibitor of transthyretin (TTR) amyloid fibril formation, inhibiting aggregate formation in more than 80% in TTR L55P-expressing cells.
  • HY-15518
    LCL161

    IAP Cancer
    LCL161 is a IAP inhibitor which inhibits XIAP in HEK293 cell and cIAP1 in MDA-MB-231 cell with IC50s of 35 and 0.4 nM, respectively.
  • HY-17362
    Vancomycin hydrochloride

    Bacterial Autophagy Antibiotic Infection Cancer
    Vancomycin hydrochloride is an antibiotic for the treatment of bacterial infections. It acts by inhibiting the second stage of cell wall synthesis of susceptible bacteria. Vancomycin also alters the permeability of the cell membrane and selectively inhibits ribonucleic acid synthesis.
  • HY-100395
    F16

    Apoptosis Cancer
    F16 is a potent growth inhibitor of the neu-overexpressing cells and also selectively inhibits proliferation of mammary epithelial as well as a variety of mouse mammary tumor and human breast cancer cell lines.
  • HY-10583
    Y-27632 dihydrochloride

    ROCK Apoptosis Cancer
    Y-27632 dihydrochloride is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 dihydrochloride induces apoptosis. Y-27632 dihydrochloride primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.
  • HY-108556A
    RWJ-56110 dihydrochloride

    Protease-Activated Receptor (PAR) Apoptosis Cardiovascular Disease
    RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.
  • HY-123952
    RTC-5

    TRC-382

    EGFR Cancer
    RTC-5 (TRC-382) is an optimized phenothiazine with anti-cancer potency. RTC-5 demonstrates efficacy against a xenograft model of an EGFR driven cancer, its effects is attributed to concomitant negative regulation of PI3K-AKT and RAS-ERK signaling.
  • HY-W008344
    2-Chloroadenosine

    Others Others
    2-Chloroadenosine, a stable adenosine analogue, protects against long term development of ischaemic cell loss in the rat hippocampus. 2-Chloroadenosine is an apparent competitive inhibitor of uridine influx (apparent Ki=33 μM) and high-affinity nitrobenzylthioinosine binding (apparent Ki=0.18 mM). 2-Chloroadenosine is a transported permeant for the nucleoside transporter in human erythrocytes.
  • HY-109566
    AZD1390

    ATM/ATR Cancer Inflammation/Immunology
    AZD1390 is a potent, highly selective, orally bioavailable, brain-penetrant ATM inhibitor with an IC50 of 0.78 nM in cell.
  • HY-N0438
    Pimpinellin

    Apoptosis Cancer
    Pimpinellin is a constituent of Cyrtomium fortumei (J.). Pimpinellin inhibits the growth of tumor cells via the induction of tumor cell apoptosis.
  • HY-114313
    Microtubule inhibitor 1

    Microtubule/Tubulin Cancer
    Microtubule inhibitor 1 is an antitumor agent with microtubule polymerization inhibitory activity, with an IC50 value of 9-16 nM in cancer cells.
  • 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-100195
    SAR-020106

    Checkpoint Kinase (Chk) Cancer
    SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer drugs.
  • HY-P1065
    Apelin-36(rat, mouse)

    HIV Infection Metabolic Disease Cardiovascular Disease
    Apelin-36(rat, mouse) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.
  • HY-P1201A
    Cyclosomatostatin TFA

    Somatostatin Receptor Cancer
    Cyclosomatostatin TFA is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin TFA can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
  • HY-W019870A
    Glufosinate

    Others Neurological Disease
    Glufosinate, a phosphinic acid analogue of glutamic acid, is a herbicide which is converted by plant cells into PT (L-phosphinothricin). Glufosinate exerts neurotoxic activity.
  • HY-17600S
    Acalabrutinib D4

    ACP-196 D4

    Btk Cancer
    Acalabrutinib D4 (ACP-196 D4) is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor.
  • HY-112314
    AZD0424

    Src Bcr-Abl Apoptosis Cancer
    AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells.
  • HY-138537
    NF-κB-IN-1

    IKK Cancer
    NF-κB-IN-1, a 4-arylidene crucumin analogue, is a potent NF-κB signaling pathway inhibitor. NF-κB-IN-1 directly inhibits IKK to block NF-κB activation. NF-κB-IN-1 effectively inhibits the viability of lung cancer cells and attenuates the clonogenic activity of A549 cells.
  • HY-122502
    Pyrazofurin

    DNA/RNA Synthesis Cancer
    Pyrazofurin, a pyrimidine nucleoside analogue with antineoplastic activity, inhibits cell proliferation and DNA synthesis in cells by inhibiting uridine 5'-phosphate (UMP) synthase. Pyrazofurin is an active, sensitive orotate-phosphoribosyltransferase inhibitor with IC50s between 0.06-0.37 µM in the three squamous cell carcinoma (SCC) cell lines Hep-2, HNSCC-14B and HNSCC-14C.
  • HY-15978
    P7C3-A20

    Others Neurological Disease
    P7C3-A20 is a derivative of P7C3 with potent proneurogenic and neuroprotective activity. P7C3-A20 exerts an antidepressant-like effect. P7C3-A20 can cross the blood-brain barrier and therefore has the potential for brain injury treatment.
  • HY-108307
    Micronomicin sulfate

    Gentamicin C2b sulfate; Antibiotic XK-62-2 sulfate; Sagamicin sulfate

    Antibiotic Bacterial Infection
    Micronomicin sulfate (Gentamicin C2b sulfate) is an aminoglycoside antibiotic isolated from Micromonospora. Micronomicin sulfate is a broad-spectrum antibiotic close to the gentamicin-type antibiotics, exhibits a high activity against Pseudomonas, Proteus, Klebsiella pneumoniae, Serratia, etc (MIC=0.001-8.3 μg/ml).
  • HY-131448
    A3334

    Others Metabolic Disease
    A3051 is a potent and orally active inhibtor of CXXC5-DVL extracted from patent WO2020079569, has an IC50 of 63.06 nM. A3334 can be used for the research of high fat diet (HFD)-induced and methionine-choline deficient diet (MCD)-induced phenotypes such as obesity, diabetes, and NASH.
  • HY-121018
    Daltroban

    BM-13505; SKF 96148

    Prostaglandin Receptor Cardiovascular Disease
    Daltroban (BM-13505) is a selective and specific thromboxane A2 (TXA2) receptor antagonist. Daltroban increase intracellular calcium in vascular smooth muscle cells. Daltroban shows protective effect in reperfusion injury.
  • HY-15826
    SGC-CBP30

    Epigenetic Reader Domain Histone Acetyltransferase Cancer Inflammation/Immunology
    SGC-CBP30 is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects.
  • HY-12826
    IMB-XH1

    Bcl-2 Family Bacterial Cancer
    IMB-XH1 is an inhibitor of myeloid cell factor 1 (Mcl-1). IMB-XH1 is a non-competitive Delhi metallo-β-lactamase (NDM-1) inhibitor. The IC50s of IMB-XH1 against metallo-β-lactamases NDM-1, IMP-4, ImiS and L1 are 0.4637 μM, 3.980 μM, 0.2287 μM and 1.158 μM, respectively.
  • HY-135784
    OSMI-2

    Acyltransferase Metabolic Disease
    OSMI-2 (Compound 1b) is a cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-2 increases detained intron splicing in cells.
  • HY-U00177
    GDP366

    Survivin Cancer
    GDP366, a dual inhibitor of survivin and Op18, induces cell growth inhibition, cellular senescence and mitotic catastrophe in human cancer cells.
  • HY-15184
    Elaiophylin

    Azalomycin B; Gopalamicin; Efomycin E

    Autophagy Cancer
    Elaiophylin (Azalomycin B; Gopalamicin; Efomycin E) is an autophagy inhibitor, exerts antitumor activity as a single agent in ovarian cancer cells.
  • HY-114926
    KT185

    MAGL Neurological Disease
    KT185 is an orally-bioavailable, brain-penetrant and selective ABHD6 inhibitor, with an IC50 0.21 nM in Neuro2A cells.
  • HY-112716
    N-alpha-Tosyl-L-lysine chloromethyl ketone hydrochloride

    Others Cancer
    N-alpha-Tosyl-L-lysine chloromethyl ketone (TLCK), a trypsin like protease inhibitor, sensitizes HeLa cells to Fas-mediated cell death.
  • HY-19637
    SW044248

    Topoisomerase Cancer
    SW044248 is a non-canonical topoisomerase I inhibitor, and selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines.
  • HY-114170
    ML604440

    Proteasome Inflammation/Immunology
    ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor. ML604440 impairs MHC class I cell surface expression, IL-6 secretion and differentiation of naïve T helper cells to T helper 17 cells. ML604440 strongly ameliorates disease in experimental colitis and EAE.
  • HY-136383
    AZA1

    Rac1/Cdc42-IN-1

    Ras Apoptosis Cancer
    AZA1 is a potent dual inhibitor of Rac1 and Cdc42. AZA1 induces prostate cancer cells apoptosis and inhibits prostate cancer cells proliferation, migration and invasion.
  • HY-136427
    KRM-III

    Others Inflammation/Immunology
    KRM-III is a potent and orally active T-cell antigen receptor (TCR) inhibitor. KRM-III inhibits TCR- and phorbol myristate acetate/ionomycin-induced activation of nuclear factor of activated T cells (NFAT) and T-cell proliferation with an IC50 of ~5 μM. Anti-inflammatory activity.
  • HY-15771A
    Tirabrutinib hydrochloride

    ONO-4059 hydrochloride; GS-4059 hydrochloride

    Btk Cancer
    Tirabrutinib (ONO-4059) hydrochloride is a selective and novel inhibitor of BTK with IC50 2.2 nm, Tirabrutinib binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development.
  • HY-10126
    Barasertib-HQPA

    AZD2811; INH-34; AZD1152-HQPA

    Aurora Kinase Apoptosis Cancer
    Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib-HQPA (AZD2811) induces growth arrest and apoptosis in cancer cells.
  • HY-109520
    Glatiramer acetate

    Others Inflammation/Immunology
    Glatiramer acetate, a synthetic analogue of myelin basic protein and an immunomodulating agent, can be used for the research of multiple sclerosis. Glatiramer acetate exhibits strong and promiscuous binding to MHC molecules and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression.
  • 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-129055
    Isoeleutherin

    Fungal Inflammation/Immunology
    Isoeleutherin is a naphthopyran derivative isolated from E. americana Merr. Et Heyne with anti-fungal, anti-viral, and anti-tumor activities. Isoeleutherin plays an important role in selective modulation of T helper cell-mediated immune responses.
  • HY-W008661
    Deoxyguanosine triphosphate trisodium salt

    dGTP trisodium salt; 2'-Deoxyguanosine-5'-triphosphate trisodium salt

    DNA/RNA Synthesis Others
    Deoxyguanosine triphosphate (dGTP) trisodium salt is a nucleotide precursor in cells for DNA synthesis. Deoxyguanosine triphosphate trisodium salt is used in reverse transcription-polymerase chain reaction (RT-PCR) for DNA amplification.
  • HY-15861
    Targapremir-210

    TGP-210

    MicroRNA Apoptosis Cancer
    Targapremir-210 (TGP-210) is a potent and selective miR-210 inhibitor. Targapremir-210 inhibits pre-miR-210 processing with high binding affinity (Kd~200 nM).
  • HY-16697
    CID 16020046

    GPR55 Cancer
    CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca 2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function.
  • HY-N0728
    α-Linolenic acid

    PI3K Akt Cancer Cardiovascular Disease
    α-Linolenic acid, isolated from seed oils, is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer.
  • 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-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 P13K/AKT/GSK-3β signaling pathways. Isolongifolene has antioxidant, anti-inflammatory, anticancer and neuroprotective properties.
  • HY-21141
    Cysteine protease inhibitor-2

    Cathepsin Cancer
    Cysteine protease inhibitor-2 is a cysteine protease inhibitor extracted from patent US20070032499A1, compound 12. Cysteine protease inhibitor-2 inhibits the cells growth of DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.
  • HY-15648F
    GSK-J4 hydrochloride

    Histone Demethylase Cancer
    GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable prodrug of GSK-J1.
  • HY-112062
    POL1-IN-1

    DNA/RNA Synthesis Cancer
    POL1-IN-1 is a RNA polymerase 1 (POL1, also known as Pol I) inhibitor with an IC50 of less than 0.5 uM. POL1-IN-1 inhibits ribosome biogenesis by inhibiting POL1 transcription.
  • HY-12743A
    K-7174 dihydrochloride

    Others Inflammation/Immunology
    K-7174 dihydrochloride is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.
  • HY-12743
    K-7174

    Others Inflammation/Immunology
    K-7174 is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.
  • HY-W019870
    Glufosinate ammonium

    Others Neurological Disease
    Glufosinate ammonium, a phosphinic acid analogue of glutamic acid, is an herbicide which is converted by plant cells into PT (L-phosphinothricin). Glufosinate ammonium exerts neurotoxic activity.
  • HY-114503
    NSAH

    DNA/RNA Synthesis Cancer
    NSAH is a reversible and competitive nonnucleoside ribonucleotide reductase (RR) inhibitor, with cell-free IC50 of 32 μM and cell-based IC50 of ~250 nM, respectively.
  • HY-101055
    Kinetin riboside

    N6-Furfuryladenosine

    Apoptosis Cancer
    Kinetin riboside, a cytokinin analog, can induce apoptosis in cancer cells. It inhibits the proliferation of HCT-15 cells with an IC50 of 2.5 μM.
  • HY-101524
    TC13172

    Mixed Lineage Kinase Cancer
    TC13172 is a mixed lineage kinase domain-like protein (MLKL) inhibitor with an EC50 value of 2 nM for HT-29 cells.
  • HY-15405
    Teriflunomide

    A77 1726

    Others Inflammation/Immunology
    Teriflunomide is the active metabolite of leflunomide, an approved therapy for rheumatoid arthritis. It inhibits pyrimidine synthesis and therefore potently decreases T cell and B cell proliferation.
  • HY-P1065A
    Apelin-36(rat, mouse) TFA

    HIV Infection Metabolic Disease Cardiovascular Disease
    Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) TFA binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) TFA blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.
  • HY-15295
    Vonoprazan Fumarate

    TAK-438

    Proton Pump Metabolic Disease
    Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
  • 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-108716
    CBS9106

    SL-801

    CRM1 Apoptosis Cancer
    CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities. CBS9106, inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells.
  • HY-103489
    PI-273

    PI4K Apoptosis Cancer
    PI-273 is a first reversibly and specific phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC50 of 0.47 μM. PI-273 can inhibit breast cancer cell proliferation, block the cell cycle and induce cell apoptosis.
  • HY-100007
    Vonoprazan

    TAK-438 free base

    Proton Pump Endocrinology
    Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
  • HY-15304
    Dynasore

    Dynamin Autophagy Virus Protease Metabolic Disease
    Dynasore is a cell-permeable dynamin inhibitor with an IC50 of 15 μM.
  • HY-P0151
    SN50

    NF-κB Inflammation/Immunology
    SN50 is a cell permeable inhibitor of NF-κB translocation.
  • HY-12797
    GF 15

    Others Cancer
    GF 15 is a potent inhibitor of centrosomal clustering in tumor cells.
  • HY-103359
    Ceranib1

    Others Cancer
    Ceranib1 is a ceramidase inhibitor. Ceranib1 inhibits ceramidase activity toward an exogenous ceramide analog, induces the accumulation of multiple ceramide species, decreases levels of sphingosine and S1P. Ceranib1 inhibits the proliferation of ovarian cancer cells.
  • HY-N4171
    Dihydrocucurbitacin B

    Others Inflammation/Immunology
    Dihydrocucurbitacin B, a triterpene isolated from Cayaponia tayuya roots, inhibits nuclear factor of activated T cells (NFAT), induces cell cycle arrested in the G0 phase, and inhibits delayed type hypersensitivity.
  • HY-10127
    Barasertib

    AZD1152

    Aurora Kinase Apoptosis Cancer
    Barasertib (AZD1152), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib (AZD1152) induces growth arrest and apoptosis in cancer cells.
  • HY-15694
    SMIP004

    E1/E2/E3 Enzyme Apoptosis Cancer
    SMIP004 is a SKP2 E3 ligase inhibitor, which downregulates SKP2 and to stabilise p27. SMIP004 is a cancer cell selective apoptosis inducer of human prostate cancer cells.
  • HY-112914
    mTOR inhibitor-1

    mTOR Autophagy Cancer
    mTOR inhibitor-1 is a novel mTOR pathway inhibitor which can suppress cells proliferation and inducing autophagy.
  • HY-135785
    OSMI-3

    Acyltransferase Metabolic Disease
    OSMI-3 (Compound 2b) is a potent, long-lasting, and cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-3 increases detained intron splicing in cells.
  • HY-15004
    AUZ 454

    K03861

    CDK Cancer
    AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins.
  • HY-118224
    BPH-715

    Parasite Infection
    BPH-715 is a bisphosphonate, inhibits Plasmodium liver-stage growth, with an IC50 of 10 μM for Plasmodium exoerythrocytic forms in HepG2 cells.
  • HY-114322
    VZ185

    PROTAC Epigenetic Reader Domain Cancer
    VZ185 is a potent, fast, and selective VHL based dual degrader probe of BRD9 and BRD7 with DC50s of 4.5 and 1.8 nM, respectively. VZ185 is cytotoxic in EOL-1 and A-402 cells, with EC50s of 3 nM and 40 nM, respectively.
  • HY-N2292
    Kinsenoside

    Keap1-Nrf2 Apoptosis Inflammation/Immunology
    Kinsenoside is a main active component isolated from plants of the genus Anoectochilus, and exhibits many biological activities and pharmacological effects. Kinsenoside rescues the nucleus pulposus cells (NPCs) viability under oxidative stress and protects against apoptosis, senescence and mitochondrial dysfunction in a Nrf2-dependent way.
  • HY-Y0445A
    Sodium dichloroacetate

    PDHK Reactive Oxygen Species NKCC Apoptosis Cancer
    Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor.
  • HY-10846
    Delamanid

    OPC-67683

    Bacterial Antibiotic Cancer
    Delamanid, a newer mycobacterial cell wall synthesis inhibitor, inhibits the synthesisi of mucolic acids.
  • HY-15700
    PluriSIn 1

    NSC 14613

    Stearoyl-CoA Desaturase (SCD) Apoptosis Cancer
    PluriSIn 1 (NSC 14613) is an inhibitor of stearoyl-coA desaturase (SCD), and is a pluripotent cell-specific inhibitor.
  • HY-16662
    Oncrasin-1

    Ras Apoptosis Cancer
    Oncrasin-1 is a potent and effective anticancer inhibitor that kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations; also led to abnormal aggregation of PKCι in nucleus of sensitive cells but not in resistant cells.
  • HY-17511
    Potassium oxonate

    Potassium azaorotate; Potassium otastat

    Others Metabolic Disease
    Potassium oxonate is an inhibitor of uricase, inhibits the phosphorylation of 5-FU to 5-fluorouridine-5'-monophosphate catalyzed by pyrimidine phosphoribosyl-transferase in a different manner from allopurinol in cell-free extracts and intact cells in vitro.
  • HY-N6745
    Citreoviridin

    Na+/K+ ATPase Apoptosis Infection Cardiovascular Disease
    Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na +/K +-ATPase whereas in microsomes, both Na +/K +-ATPase and Mg 2+-ATPase activities are significantly stimulated in a dose-dependent manner. Citreoviridin inhibits cell proliferation and enhances apoptosis of human umbilical vein endothelial cells.
  • HY-119738
    OSMI-1

    Acyltransferase Metabolic Disease
    OSMI-1 is a cell-permeable O-GlcNAc transferase (OGT) inhibitor with an IC50 value of 2.7 μM. OSMI-1 inhibits protein O-linked N-acetylglucosamine (O-GlcNAcylation) in several mammalian cell lines without qualitatively altering cell surface N- or O-linked glycans.
  • HY-12458
    Pyrindamycin A

    DNA/RNA Synthesis Cancer Infection
    Pyrindamycin A is an antibiotic that inhibits DNA synthesis. Pyrindamycin A shows antitumor activities against murine leukemia, exhibits stronger cytotoxic activities towards murine and human tumor cell lines and especially towards doxorubicin-resistant cells, inhibits P388 and P388/ADR cells with the same IC50 of 3.9 μg/ml.
  • 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-110115
    TC-Mps1-12

    Mps1 Cancer
    TC-Mps1-12 is a potent and selective monopolar spindle 1 (Mps1) inhibitor, with an IC50 of 6.4 nM.
  • HY-N0162
    Luteolin

    Luteoline; Luteolol; Digitoflavone

    Keap1-Nrf2 Apoptosis Autophagy Endogenous Metabolite Cancer Inflammation/Immunology
    Luteolin (Luteoline), a flavanoid compound, is a potent Nrf2 inhibitor. Luteolin has anti-inflammatory, anti-cancer properties, including the induction of apoptosis and cell cycle arrest, and the inhibition of metastasis and angiogenesis, in several cancer cell lines, including human non-small lung cancer cells.
  • HY-N1931
    Epifriedelanol

    Others Cancer
    Epifriedelanol is a triterpenoid isolated from the root bark of Ulmus davidiana, with antitumor activity. Epifriedelanol inhibits cellular senescence in human primary cells.
  • HY-124632
    WJ460

    Others Cancer
    WJ460 is a potent myoferlin (MYOF) inhibitor, which interacts directly with MYOF and exerts anti-metastatic activity in the nanomolar range in breast cancer cells.
  • HY-N6602
    α-Solanine

    Apoptosis Cancer
    α-solanine, a bioactive component and one of the major steroidal glycoalkaloids in potatoes, has been observed to inhibit growth and induce apoptosis in cancer cells.
  • HY-A0068
    Aurothioglucose

    Gold thioglucose

    Others Cancer
    Aurothioglucose (Gold thioglucose) is a well known active-site inhibitor of TrxR1, inhibited TrxR1 activity in HeLa cell cytosol but had no effect on the viability of the cells.
  • HY-N6862
    Lucideric acid A

    MMP Cancer
    Lucideric acid A is a natural compound isolated from Ganoderma lucidum, inhibits PMA-induced MMP-9 activity, with anti-invasive effect on hepatoma cells.
  • HY-13668
    Lomeguatrib

    PaTrin-2

    DNA Methyltransferase Cancer
    Lomeguatrib is a O 6-methylguanine-DNA methyltransferase (MGMT) inhibitor, with IC50s of 9 nM in cell-free assay and ∼6 nM in MCF-7 cells.
  • 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-N6727
    Gliotoxin

    Aspergillin

    Apoptosis PKA NF-κB Bacterial Fungal Antibiotic Infection Inflammation/Immunology
    Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis. Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells.
  • HY-N0504
    Lovastatin

    Mevinolin

    HMG-CoA Reductase (HMGCR) Autophagy Ferroptosis Cardiovascular Disease Cancer
    Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.
  • HY-10222
    Ixabepilone

    BMS-247550; Aza-epothilone B

    Microtubule/Tubulin Apoptosis Cancer
    Ixabepilone (BMS-247550) is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis.
  • HY-135383B
    (Z)-Pitavastatin calcium

    Others Metabolic Disease
    (Z)-Pitavastatin calcium is the Z-Isomer of Pitavastatin hemicacium. Pitavastatin calcium is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin calcium inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells.
  • HY-N6782
    Oligomycin

    ATP Synthase Fungal Antibiotic Cancer Infection
    Oligomycin, an antifungal antibiotic, is an inhibitor of H +-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells.
  • HY-10498
    Lexibulin

    CYT-997

    Microtubule/Tubulin Reactive Oxygen Species Apoptosis Cancer
    Lexibulin (CYT-997) is a potent and orally active tubulin polymerisation inhibitor with IC50s of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Lexibulin induces cell apoptosis and induces mitochondrial ROS generation in GC cells.
  • HY-10498A
    Lexibulin dihydrochloride

    CYT-997 dihydrochloride

    Microtubule/Tubulin Reactive Oxygen Species Apoptosis Cancer
    Lexibulin dihydrochloride (CYT-997 dihydrochloride) is a potent and orally active tubulin polymerisation inhibitor with IC50s of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Lexibulin dihydrochloride induces cell apoptosis and induces mitochondrial ROS generation in GC cells.
  • HY-18679
    TC-N 22A

    mGluR Neurological Disease
    TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo.
  • HY-B1596
    Ceftizoxime

    Bacterial Antibiotic Infection
    Ceftizoxime is a bacterial inhibitor which acts by interfering with bacterial cell wall synthesis and inhibiting cross-linking of the peptidoglycan.
  • HY-18965
    TAS-301

    PKC Cardiovascular Disease
    TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF.
  • HY-100498
    GSK2256098

    FAK Apoptosis Cancer
    GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.
  • HY-138239
    WEE1-IN-3

    Wee1 Cancer
    WEE1-IN-3 is a potent Wee1 kinase inhibitor with an IC50 of <10 nM. WEE1-IN-3 has anticancer activities.
  • HY-121497
    3-Methoxybenzamide

    3-MBA

    PARP Bacterial Cancer
    3-Methoxybenzamide (3-MBA), an inhibitor of ADP-ribosyltransferase (ADPRTs) and PARP, inhibits cell division in Bacillus subtilis, leading to filamentation and eventually lysis of cells. 3-Methoxybenzamide (3-MBA) enhances in vitro plant growth, microtuberization, and transformation efficiency of blue potato (Solanum tuberosum L. subsp. andigenum).
  • HY-17371
    Oxaliplatin

    DNA Alkylator/Crosslinker DNA/RNA Synthesis Autophagy Cancer
    Oxaliplatin is a DNA synthesis inhibitor. Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and causes cell death. Oxaliplatin time-dependently inhibits human melanoma cell lines C32 and G361 with IC50 values of 0.98 μM and 0.14 μM, respectively. Oxaliplatin induces cell autophagy.
  • HY-121802
    Dynarrestin

    Hedgehog Cancer
    Dynarrestin is a aminothiazole inhibitor of cytoplasmic dyneins 1 and 2. Dynarrestin rapidly and reversibly inhibits dynein 1-driven microtubule gliding in vitro plus a range of dynein 1- and 2-dependent processes in cells without affecting ATP hydrolysis and interfering with ciliogenesis. Dynarrestin suppresses hedgehog (Hh)-dependent proliferation of neuronal precursors and tumor cells.
  • HY-13721
    Phenoxodiol

    Idronoxil; Dehydroequol; Haginin E

    Caspase Apoptosis Topoisomerase Cancer
    Phenoxodiol, a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. This agent also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21 WAF1 via a p53 independent manner.
  • HY-16658B
    Z-VAD-FMK

    Z-VAD(OH)-FMK

    Caspase Cancer
    Z-VAD-FMK (Z-VAD(OH)-FMK) is a well-know pan caspase inhibitor, which does not inhibit ubiquitin carboxy-terminal hydrolase L1 (UCHL1) activity even at concentrations as high as 440 μM.
  • HY-N6744
    Chaetoglobosin A

    Apoptosis Cancer Infection
    Chaetoglobosin A, the active principle within the extract of Penicillium aquamarinium, is a member of the cytochalasan family. Chaetoglobosin A preferentially induces apoptosis. Chaetoglobosin A targets filamentous actin in CLL cells and thereby induces cell-cycle arrest and inhibits membrane ruffling and cell migration.
  • HY-77813
    Benzyl isothiocyanate

    Bacterial Apoptosis Antibiotic Cancer Endocrinology
    Benzyl isothiocyanate is a member of natural isothiocyanates with antimicrobial activity. Benzyl isothiocyanate potent inhibits cell mobility, migration and invasion nature and matrix metalloproteinase-2 (MMP-2) activity of murine melanoma cells.
  • HY-111425
    SSE15206

    Microtubule/Tubulin Apoptosis Cancer
    SSE15206 is a microtubule polymerization inhibitor (GI50 = 197 nM in HCT116 cells) that overcomes multidrug resistance. Causes aberrant mitosis resulting in G2/M arrest due to incomplete spindle formation in cancer cells.
  • HY-120215
    KT203

    MAGL Metabolic Disease
    KT203 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.31 nM in Neuro2A cells.
  • HY-N6860
    Lucidenic acid C

    MMP Cancer
    Lucidenic acid C is a natural compound isolated from Ganoderma lucidum, inhibits PMA-induced MMP-9 activity, with anti-invasive effect on hepatoma cells.
  • HY-100636
    Gefitinib N-oxide

    EGFR Cancer
    Gefitinib N-oxide is the N-oxide derivative of Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.
  • HY-120177
    KT182

    MAGL Others
    KT182 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.24 nM in Neuro2A cells.
  • HY-12873
    RBC8

    Ras Cancer
    RBC8 is a novel small molecule inhibitor of Ral GTPase; has IC50 of 3.5 μM in H2122 cell and 3.4 μM in H358 cell.
  • HY-B0497
    Niclosamide

    BAY2353

    STAT Parasite Antibiotic Infection Cancer
    Niclosamide (BAY2353) is an orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Niclosamide (BAY2353) inhibits STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
  • HY-127002A
    Squarunkin A hydrochloride

    Src Cancer
    Squarunkin A hydrochloride is a potent and selective UNC119-cargo interaction inhibitor (IC50 of 10 nM for inhibiting the UNC119A-myristoylated Src N-terminal peptide interaction). Squarunkin A hydrochloride interferes with the activation of Src kinase in cells.
  • 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-126679
    Apoptolidin

    ATP Synthase Apoptosis Cancer
    Apoptolidin is a polyketide isolated from Nocardiopsis bacteria. Apoptolidin is a selective mitochondrial F1FO ATPase inhibitor. Apoptolidin is an apoptosis inducer and induces apoptotic cell death in cells transformed with the adenovirus type 12 oncogenes including ElA (IC50=10-17 ng/ml) but not in normal cells.
  • HY-134582
    dCBP-1

    PROTAC Epigenetic Reader Domain Cancer
    dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on PROTAC. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression.
  • HY-106420
    16,16-Dimethyl prostaglandin E2

    16,16-dimethyl PGE2

    Prostaglandin Receptor Inflammation/Immunology
    16,16-Dimethyl prostaglandin E2 (16,16-dimethyl PGE2) is an orally active vertebrate Hematopoietic stem cells (HSCs) homeostasis critical regulator. 16,16-Dimethyl prostaglandin E2 can act through EP2/EP4 and has an interaction with the Wnt pathway.
  • HY-P1629
    Temporin A

    Bacterial Fungal Antibiotic Infection
    Temporin A is a short alpha-helical antimicrobial peptide isolated from the skin of the frog Rana temporaria. Temporin A is effective against a broad spectrum of Gram-positive bacteria. Temporin A interacts directly with the cell membrane of the microorganism and it is non-toxic to erythrocytes at concentrations that are antimicrobial. Temporin A also has antifungal activities (against yeast-like Candida albicans).
  • HY-P0069A
    L-JNKI-1

    JNK Neurological Disease
    L-JNKI-1 is a cell-permeable peptide inhibitor specific for JNK.
  • HY-P1286
    PKC β pseudosubstrate

    PKC Neurological Disease
    PKC β pseudosubstrate is a selective cell-permeable inhibitor of PKC.
  • HY-B0313
    Hydroxyurea

    Hydroxycarbamide

    DNA/RNA Synthesis Autophagy Apoptosis HIV Cancer
    Hydroxyurea is a cell apoptosis inducer that inhibit DNA synthesis through inhibition of ribonucleotide reductase.
  • HY-B1300
    Cefonicid sodium

    Bacterial Antibiotic Infection
    Cefonicid sodium is a broadspectrum cephalosporin antibiotic which inhibits the formation of the bacterial cell wall.
  • HY-21972
    BCI-121

    Histone Methyltransferase Cancer
    BCI-121 is a SMYD3 inhibitor that impairs the proliferation of cancer cell.
  • HY-18632A
    GSK2879552 dihydrochloride

    Histone Demethylase Cancer
    GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.
  • HY-15648B
    GSK-J4

    Histone Demethylase Apoptosis Cancer
    GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable prodrug of GSK-J1. GSK-J4 induces endoplasmic reticulum stress-related apoptosis.
  • HY-N1506
    Ganodermanontriol

    Others Cancer
    Ganodermanontriol, a sterol isolated from Ganoderma lucidum, induces anti-inflammatory activity in tert-butyl hydroperoxide (t-BHP)-damaged hepatic cells through the expression of HO-1. Ganodermanontriol exhibits hepatoprotective activity.
  • HY-B0790
    TAI-1

    Apoptosis Cancer
    TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI50 of 13.48 nM in K562 cells.
  • HY-N2486
    Desoxyrhaponticin

    Fatty Acid Synthase (FASN) Apoptosis Cancer
    Desoxyrhaponticin is a stilbene glycoside from the Tibetan nutritional food Rheum tanguticum Maxim. Desoxyrhaponticin is a Fatty acid synthase (FASN) inhibitor, and has apoptotic effect on human cancer cells.
  • HY-118660
    Anhydrotetracycline hydrochloride

    Antibiotic Bacterial Infection
    Anhydrotetracycline hydrochloride, a tetracycline biosynthetic precursor, is a potent competitive broad-spectrum tetracycline destructase enzymes inhibitor. Anhydrotetracycline hydrochloride is an effector for tetracycline controlled gene expression systems in eukaryotic cells.
  • HY-12425
    DGAT1-IN-1

    Acyltransferase Metabolic Disease
    DGAT1-IN-1 is a potent DGAT1 inhibitor with IC50 of < 10 nM(cell lysate from Hep3B cells overexpressing human DGAT1).
  • HY-N3558
    Ceanothic acid

    Emmolic acid

    Others Cancer
    Ceanothic acid (Emmolic acid) is a ring-A homologue of betulinic acid. Ceanothic acid inhibits OVCAR-3, HeLa, and FS-5 cells with the cell survival of 68%, 65%, and 81%, respectively.
  • HY-12842
    UC-112

    IAP Apoptosis Cancer
    UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor; potently inhibit cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines(IC50=0.7-3.4 uM).
  • 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-136351
    THZ-P1-2

    Autophagy Cancer
    THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines.
  • HY-N4053
    Heraclenin

    Others Inflammation/Immunology
    Heraclenin, a natural furanocoumarin, isolated from the root parts of the plant Prangos pabularia. Heraclenin significantly inhibits T cell receptor-mediated proliferation in human primary T cells in a concentration-dependent manner by targeting nuclear factor of activated T-cells (NFAT).
  • HY-120836
    AOH1160

    DNA/RNA Synthesis Apoptosis Cancer
    AOH1160 is a potent, first-in-class, orally available small molecule proliferating cell nuclear antigen (PCNA) inhibitor, interferes with DNA replication, blocks homologous recombination-mediated DNA repair, causes cell-cycle arrest and induces apoptosis. AOH1160 selectively kills many types of cancer cells (mean GI50=330 nM) without causing significant toxicity to a broad range of nonmalignant cells.
  • HY-15609
    AZD-3463

    ALK/IGF1R inhibitor

    ALK IGF-1R Autophagy Apoptosis Cancer Endocrinology
    AZD-3463 (ALK/IGF1R inhibitor) is an orally active ALK/IGF1R inhibitor, with a Ki of 0.75 nM for ALK. AZD3463 induces apoptosis and autophagy in neuroblastoma cells.
  • HY-117650A
    RG7834

    RO 7020322

    HBV Infection
    RG7834 (RO 7020322) is a highly selective and orally bioavailable HBV inhibitor, potently inhibits HBV antigens (both HBsAg and HBeAg) and HBV DNA, with IC50s of 2.8, 2.6, and 3.2 nM, respectively, in dHepaRG Cells.
  • HY-106101
    Echinomycin

    Quinomycin A; NSC-13502

    HIF/HIF Prolyl-Hydroxylase Cancer
    Echinomycin (Quinomycin A) is potent small-molecule and cell-permeable inhibitor of hypoxia-inducible factor-1 (HIF-1) DNA-binding activity. Echinomycin selectively inhibits the cancer stem cells (CSCs) with an IC50 of 29.4 pM.
  • 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-120548
    KBU2046

    Others Cancer
    KBU2046 is an oral, highly selective inhibitor of cell motility and cell invasion in vitro. KBU2046 binds chaperone heterocomplexes, selectively alters binding of client proteins that regulate motility, and lacks all of the hallmarks of classical HSP90 inhibitors. KBU2046 inhibits cancer metastasis and prolongs life.
  • HY-129492
    GNF4877

    DYRK GSK-3 Metabolic Disease
    GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells).
  • HY-12462
    WS3

    Others Inflammation/Immunology
    WS3 is a novel proliferative molecule that promotes pancreatic β cell proliferation in rodent and human primary islets. WS3 can be used for the research of type 1 diabetes.
  • HY-126378
    LSP-249

    Others Inflammation/Immunology
    LSP-249 (example 35), extracted from patent WO2016011209A1, is a plasma kallikrein inhibitor under the study for angioedema, with an EC50 less than 100 nM in cell.
  • HY-N4219
    Saikosaponin B3

    Others Metabolic Disease Neurological Disease
    Saikosaponin B3 is a saikosaponin isolated from the roots of Bupleurum falcatum L., with analgesic effect. Saikosaponin B3 inhibits ACTH-induced lipolysis in the fat cells.
  • HY-15894
    BQ-788 sodium salt

    Endothelin Receptor Cardiovascular Disease Endocrinology Cancer
    BQ-788 sodium salt is a potent and selective ETB receptor antagonist, inhibiting ET-1 binding to ETB receptors with an IC50 of 1.2 nM in human Girrardi heart cells.
  • HY-N1516
    Ganoderenic acid D

    Apoptosis Cancer
    Ganoderenic acid D is a triterpene identified from the effective compounds of Ganoderma lucidum extract (GLE). Ganoderenic acid D inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.
  • 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-A0098
    Tunicamycin

    Bacterial Fungal Influenza Virus Antibiotic Cancer Infection Inflammation/Immunology
    Tunicamycin is a mixture of homologous nucleoside antibiotic that inhibits N-linked glycosylation and blocks GlcNAc phosphotransferase (GPT). Tunicamycin causes accumulation of unfolded proteins in cell endoplasmic reticulum (ER) and induces ER stress, and causes blocking of DNA synthesis and cell cycle arrest in G1 phase. Tunicamycin inhibits gram-positive bacteria, yeasts, fungi, and viruses and has anti-cancer activity.Tunicamycin increases exosome release in cervical cancer cells.
  • HY-101567
    BMS-986158

    Epigenetic Reader Domain Cancer
    BMS-986158 is a potent BET inhibitor with IC50s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively.
  • HY-103002
    SU5408

    VEGFR2 Kinase Inhibitor I

    VEGFR Cardiovascular Disease
    SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and cell-permeable inhibitor of VEGFR2 kinase with an IC50 of 70 nM.
  • 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-B0496
    PMSF

    Phenylmethylsulfonyl fluoride; Benzylsulfonyl fluoride

    Cathepsin Others
    PMSF is an irreversible serine/cysteine protease inhibitor commonly used in the preparation of cell lysates.
  • HY-13307
    JK184

    Hedgehog Cancer
    JK184 is a potent Hedgehog (Hh) pathway inhibitor with IC50 of 30 nM in mammalian cells.
  • HY-16695
    MIM1

    Inhibitor of Mcl-1

    Bcl-2 Family Cancer
    MIM-1 is an inhibitor of myeloid cell factor 1 (Mcl-1).
  • HY-100755
    KR-33493

    Others Neurological Disease
    KR-33493 is a potent inhibitor of Fas-mediated cell death (FAF1).
  • HY-P1286A
    PKC β pseudosubstrate TFA

    PKC Neurological Disease
    PKC β pseudosubstrate TFA is a selective cell-permeable inhibitor of PKC.
  • HY-129337
    Reveromycin A

    Antibiotic Fungal Apoptosis Cancer Infection
    Reveromycin A, a benzoquinoid antibiotic isolated from the genus Streptomyces, is a selective inhibitor of protein synthesis in eukaryotic cells. Reveromycin A inhibits bone resorption by inducing apoptosis specifically in osteoclasts. Reveromycin A has antiproliferative activity against tumor cell lines and antifungal activity.
  • HY-108900
    Leu-AMS

    Aminoacyl-tRNA Synthetase Bacterial Cancer Infection
    Leu-AMS (compound 6), a leucine analogue, is a potent inhibitor of leucyl-tRNA synthetase (LRS) with an IC50 of 22.34 nM, which inhibits the catalytic activity of LRS but did not affect the leucine-induced mTORC1 activation. Leu-AMS shows cytotoxicity in cancer cells and normal cells, and inhibits the growth of bacteria.
  • HY-32340
    Lexacalcitol

    KH1060

    VD/VDR Cancer Inflammation/Immunology
    Lexacalcitol (KH1060), a vitamin D analog, is potent regulators of cell growth and immune responses. Lexacalcitol can be used for the research of graft rejection, psoriasis, cancer and auto-immune diseases.
  • HY-14590
    Kaempferol

    Kempferol; Robigenin

    Estrogen Receptor/ERR Autophagy Mitophagy Apoptosis HIV Parasite Endogenous Metabolite Cancer
    Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK. Kaempferol can be uesd for the research of breast cancer.
  • HY-50895S
    Gefitinib D8

    ZD1839 D8

    EGFR Autophagy Cancer
    Gefitinib D8 (ZD1839 D8) is a deuterium labeled Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.
  • HY-101413
    Iberin

    NSC 321801

    Apoptosis Endogenous Metabolite Bacterial Cancer
    Iberin (NSC 321801), a sulfoxide analogue of sulforaphane, is a naturally occurring member of isothiocyanate family. Iberin inhibits cell survival with an IC50 of 2.3 μM in HL60 cell. Iberin induces apoptosis.
  • HY-128522
    ARS-1323-alkyne

    Ras Cancer
    ARS-1323-alkyne, a switch-II pocket (S-IIP) inhibitor, is a conformational specific chemical reporter of KRAS G12C nucleotide state in living cells.
  • HY-N6626
    Pyraclostrobin

    Fungal Bacterial Infection Metabolic Disease
    Pyraclostrobin is a strobilurin fungicide that inhibits mitochondrial complex III of fungal and mammalian cells. Pyraclostrobin induces triglyceride accumulation and triglyceride accumulation in 3T3-L1 cells.
  • HY-N0726
    Dracorhodin perchlorate

    Dracohodin perochlorate

    Apoptosis Cancer
    Dracorhodin perchlorate (Dracohodin perochlorate) is a natural product extracted from a natural medicine Dragon's blood. Dracorhodin perchlorate inhibits cell proliferation and induces cell cycle arrest and apoptosis.
  • HY-N4285
    Negletein

    5,6-Dihydroxy-7-methoxyflavone

    TNF Receptor Interleukin Related Inflammation/Immunology Neurological Disease
    Negletein is a neuroprotectant enhances the action of nerve growth factor and induces neurite outgrowth in PC12 cells. Negletein shows promising anti-inflammatory activity via inhibition of TNF-α and IL-1β with IC50 values of 16.4 and 10.8 μM, respectively.
  • HY-112055
    DIM-C-pPhOH

    Apoptosis Cancer
    DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively.
  • HY-131183
    PROTAC PD-1/PD-L1 degrader-1

    PROTAC PD-1/PD-L1 Inflammation/Immunology
    PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 degrader, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner.
  • HY-137658
    Purine riboside triphosphate

    PTP

    Nucleoside Antimetabolite/Analog Others
    Purine riboside triphosphate is a triphosphate derivative of purine riboside. Purine riboside is a naturally occurring base analog which closely resembles adenosine. Purine riboside inhibits carcinogenic growth. Purine riboside strongly inhibits RNA and DNA synthesis in different cancer ascites cells.
  • HY-N6734
    K-252b

    PKC Infection
    K-252b, an indolocarbazole isolated from the actinomycete Nocardiopsis, is a PKC inhibitor. K-252b can be used to inhibit extracellular kinases of cells in culture because it can’t pass through cell membrane freely .
  • HY-129065
    Nourseothricin sulfate

    Streptothricin sulfate

    Fungal Bacterial Antibiotic Infection
    Nourseothricin sulfate (Streptothricin sulfate) is a broad-spectrum antibiotic that destroys the outer membrane of Gram-negative bacteria and is a dominant selective marker for Fonsecaea pedrosoi. Nourseothricin sulfate inhibits protein biosynthesis in prokaryotic cells and strongly inhibits the growth of eukaryotes like fungi and can also be used as a elective marker for a wide range of organisms including bacteria, yeast, filamentous fungi, and plant cells.
  • HY-12726A
    Liproxstatin-1 hydrochloride

    Ferroptosis Cancer
    Liproxstatin-1 hydrochloride is a potent ferroptosis inhibitor and inhibits ferroptotic cell death (IC50=22 nM).
  • HY-111446
    EPAC 5376753

    Others Cancer Metabolic Disease Cardiovascular Disease
    EPAC 5376753 is an allosterically inhibitor of Epac which inhibits Epac1 with an IC50 of 4 µM in Swiss 3T3 cells.
  • HY-12726
    Liproxstatin-1

    Ferroptosis Cancer
    Liproxstatin-1 is a potent ferroptosis inhibitor and inhibits ferroptotic cell death (IC50=22 nM).
  • HY-N7654
    (-)-Epipodophyllotoxin

    Apoptosis Cancer
    (-)-Epipodophyllotoxin (2) is an antiproliferative agent against cancer cells isolated from American mayapple Podophyllum peltatum, with GI50s of 0.36 and 0.24 μM in HeLa cells and MCF-7 cells, respectively. (-)-Epipodophyllotoxin can inhibit mitotic spindle assembly in vitro.
  • HY-B2145
    Ilaprazole sodium

    IY-81149 sodium

    Proton Pump TOPK Cancer Inflammation/Immunology
    Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
  • HY-116282D
    Dextran sulfate sodium salt (MW 450000-550000)

    Apoptosis HIV Inflammation/Immunology
    Dextran sulfate sodium salt (MW 450000-550000) is a is a polymer of anhydroglucose with the molecular weight range of 450000-550000. Dextran sulfate sodium salt inhibits the replication of the human immunodeficiency virus by preventing the adsorption of the virus into host cells.
  • HY-116282C
    Dextran sulfate sodium salt (MW 35000-45000)

    Apoptosis HIV Inflammation/Immunology
    Dextran sulfate sodium salt (MW 35000-45000) is a is a polymer of anhydroglucose with the molecular weight range of 35000-45000. Dextran sulfate sodium salt inhibits the replication of the human immunodeficiency virus by preventing the adsorption of the virus into host cells.
  • HY-116282A
    Dextran sulfate sodium salt (MW 4500-5500)

    Apoptosis HIV Inflammation/Immunology
    Dextran sulfate sodium salt (MW 4500-5500) is a is a polymer of anhydroglucose with the molecular weight range of 4500-5500. Dextran sulfate sodium salt inhibits the replication of the human immunodeficiency virus by preventing the adsorption of the virus into host cells.
  • HY-N6644
    Crocin III

    Others Cancer Inflammation/Immunology
    Crocin III is a crocetin from saffron (Crocus sutivus L.). Crocetins inhibit cell growth of tumor cells and has anti-inflammatory activity. Crocins serve as spices and coloring agents.
  • HY-116282B
    Dextran sulfate sodium salt (MW 16000-24000)

    Apoptosis HIV Inflammation/Immunology
    Dextran sulfate sodium salt (MW 16000-24000) is a is a polymer of anhydroglucose with the molecular weight range of 16000-24000. Dextran sulfate sodium salt inhibits the replication of the human immunodeficiency virus by preventing the adsorption of the virus into host cells.
  • HY-19095
    TNP-351

    Antifolate Cancer
    TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo.
  • HY-120635
    BMS-1001 hydrochloride

    PD-1/PD-L1 Cancer Inflammation/Immunology
    BMS-1001 hydrochloride is an orally active human PD-L1/PD-1 immune checkpoint inhibitor. BMS-1001 hydrochloride exhibits low-toxicity in cells.
  • HY-131036
    MAO-IN-M30 dihydrochloride

    Monoamine Oxidase Neurological Disease
    MAO-IN-M30 dihydrochloride is an orally active, brain-permeable, and brain selective irreversible MAO-A (IC50=37 nM) and MAO-B (IC50=57 nM) inhibitor. MAO-IN-M30 dihydrochloride is a potent iron chelator and radical scavenger. MAO-IN-M30 dihydrochloride has a neuroprotective effect against Dexamethasone-induced brain cell apoptosis. MAO-IN-M30 dihydrochloride also exhibits neurorestorative activity in post MPTP and lactacystin models of Parkinson's disease.
  • HY-115537
    NAE-IN-M22

    Apoptosis Cancer
    NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo.
  • HY-10585A
    Valproic acid sodium salt

    Sodium Valproate

    HDAC Autophagy Mitophagy HIV Notch Cancer
    Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
  • HY-100415
    UKI-1

    UKI-1C

    PAI-1 Ser/Thr Protease Infection Cancer
    UKI-1 (UKI-1C) is a potent urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 0.41 μM. UKI-1 is also a low molecular weight serine protease inhibitor. UKI-1 is a potent antimetastatic agent and inhibits the invasive capacity of carcinoma cells.
  • HY-N2567
    (±)-Decursinol

    Bacterial Cancer
    (±)-Decursinol is a potent FtsZ inhibitor. (±)-Decursinol inhibits B. anthracis FtsZ polymerization with an IC50 of 102 μM.
  • HY-19324
    EPZ031686

    Histone Methyltransferase Cancer
    EPZ031686 is an orally available SMYD3 inhibitor with an IC50 of 3 nM in cell-free assay.
  • HY-19563
    A-893

    Histone Methyltransferase Cancer
    A-893 is a cell-active inhibitor of Methyltransferase SMYD2, with an IC50 of 2.8 nM.
  • HY-12053A
    Vinorelbine ditartrate

    KW-2307; Nor-5'-anhydrovinblastine ditartrate

    Microtubule/Tubulin Autophagy Cancer
    Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
  • HY-D0850
    Tartaric acid disodium dihydrate

    Sodium tartrate dibasic dihydrate; Sodium tartrate dihydrate

    Phosphatase Cancer
    Tartaric acid disodium dihydrate is a Acid phosphatase inhibitor, is a sodium salt used in buffers for molecular biology and cell culture applications.
  • HY-13541
    ADH-1

    Others Cancer
    ADH-1, an N-cadherin antagonist, inhibits N-cadherin mediated cell adhesion.
  • HY-B0535
    Ethambutol

    Emb

    Bacterial Antibiotic Infection
    Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.
  • HY-B0312
    Dipyridamole

    Phosphodiesterase (PDE) Cardiovascular Disease
    Dipyridamole (Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.
  • HY-15723
    NSC 23766

    Ras Cancer
    NSC 23766 is a cell-permeable, reversible and specific inhibitor of Rac GTPase, used for cancer treatment.
  • HY-12053
    Vinorelbine

    KW-2307 base

    Microtubule/Tubulin Autophagy Cancer
    Vinorelbine is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
  • HY-16268
    Kartogenin

    KGN

    TGF-beta/Smad Inflammation/Immunology
    Kartogenin (KGN) is an inducer of differentiation of human mesenchymal stem cells into chondrocytes, with an EC50 of 100 nM. Kartogenin binds filamin A, disrupts its interaction with the transcription factor core-binding factor β subunit (CBFβ), and induces chondrogenesis by regulating the CBFβ-RUNX1 transcriptional program. Kartogenin can be used for the research of osteoarthritis (OA).
  • HY-17406
    Tolcapone

    Ro 40-7592

    COMT Amyloid-β Neurological Disease
    Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.
  • HY-100544
    FLLL32

    STAT JAK Apoptosis Cancer
    FLLL32, a synthetic analog of curcumina, is a JAK2/STAT3 dual inhibitor with anti-tumor activity. FLLL32 can inhibit the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.
  • 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-122571
    Retro-2

    Filovirus Parasite Autophagy Cancer Infection
    Retro-2 is a selective inhibitor of retrograde protein trafficking at the endosome-trans-Golgi network interface. Retro-2 is an ebolavirus (EBOV) infection inhibitor with an EC50 of 12.2 µM in HeLa cells. Retro-2 induces cell autophagy.
  • HY-17372
    Rofecoxib

    MK 966

    COX Inflammation/Immunology Cancer
    Rofecoxib is a potent, specific and orally active COX-2 inhibitor, with IC50s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over human COX-1 (IC50 > 50 μM in U937 cells and > 15 μM in Chinese hamster ovary cells).
  • HY-N1990
    Gypenoside XLIX

    PPAR Inflammation/Immunology Cardiovascular Disease
    Gypenoside XLIX, a dammarane-type glycoside, is a prominent component of G. pentaphyllum. Gypenoside XLIX is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator and inhibits cytokine-induced vascular cell adhesion molecule-1 (VCAM-1) overexpression and hyperactivity in human endothelial cells.
  • HY-126324
    IV-23

    Apoptosis Cancer
    IV-23 (Compound 20) is a potent Noxa mediated apoptosis inducer, and it is a promising anticancer agent with potential. IV-23 inhibits cell growths in vitro and in vivo, reduces colony formation, arrests cell cycle at M phase, and induces esophageal squamous cell carcinoma (ESCC).
  • HY-W011434
    Triglycidyl isocyanurate

    TGIC; Teroxirone

    MDM-2/p53 Apoptosis Cancer Inflammation/Immunology
    Triglycidyl isocyanurate (TGIC; Teroxirone) is a triazene triepoxide with antiangiogenic and antineoplastic activities. Triglycidyl isocyanurate inhibits the growth of non-small-cell-lung cancer cells via p53 activation. Triglycidyl isocyanurate induces cell apoptosis. Triglycidyl isocyanurate can be used for cancer research.
  • HY-15894A
    BQ-788

    Endothelin Receptor Cardiovascular Disease Endocrinology
    BQ-788 is a potent, selective ETB receptor antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, poorly inhibiting the binding to ETA receptors in human neuroblastoma cell line SK-N-MC cells with IC50 of 1300 nM.
  • HY-W009749
    L-Cystathionine

    Endogenous Metabolite Apoptosis Cardiovascular Disease
    L-Cystathionine is a nonprotein thioether and is a key amino acid associated with the metabolic state of sulfur-containing amino acids. L-Cystathionine protects against Homocysteine-induced mitochondria-dependent apoptosis of vascular endothelial cells (HUVECs). L-Cystathionine plays an important role in cardiovascular protection.
  • HY-106934
    Peldesine

    BCX 34

    Nucleoside Antimetabolite/Analog HIV Cancer Infection Inflammation/Immunology
    Peldesine (BCX 34) is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research.
  • HY-106934A
    Peldesine dihydrochloride

    BCX 34 dihydrochloride

    Nucleoside Antimetabolite/Analog HIV Cancer Infection Inflammation/Immunology
    Peldesine (BCX 34) dihydrochloride is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine dihydrochloride is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine dihydrochloride has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research.
  • HY-W008947
    SEW​2871

    LPL Receptor Inflammation/Immunology Neurological Disease
    SEW2871 is a highly selective, orally active S1P1 agonist with an EC50 of 13.8 nM. SEW2871 activates ERK, Akt, and Rac signaling pathways and induces S1P1 internalization and recycling. SEW2871 reduces lymphocyte numbers in blood and has therapeutic implications in contexts of diabetes, Alzheimer’s disease, liver fibrosis, and inflammatory responses.
  • HY-100303A
    FR194738

    Others Metabolic Disease
    FR194738 is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM.
  • HY-16904
    RI-2

    RAD51 Cancer
    RI-2 is a reversible RAD51 inhibitor, with an IC50 of 44.17 μM, and specifically inhibits homologous recombination repair in human cells.
  • HY-13813
    Blebbistatin

    Myosin Others
    Blebbistatin is a selective non-muscle myosin II (NMII) inhibitor, promotes directional migration of corneal endothelial cells (CECs) and accelerates wound healing, and better preserves cell junctional integrity and barrier function.
  • HY-100004
    Fumarate hydratase-IN-1

    Mitochondrial Metabolism Cancer
    Fumarate hydratase-IN-1 (compound 2) is a cell-permeable fumarate hydratase inhibitor. Fumarate hydratase-IN-1 has antiproliferative activity against several cancer cell lines with a mean IC50 of 2.2 μM.
  • HY-114305
    A1874

    PROTAC Epigenetic Reader Domain Cancer
    A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation.
  • HY-109049
    Adavivint

    SM04690; Lorecivivint

    Wnt Inflammation/Immunology Cancer
    Adavivint (SM04690; Lorecivivint) is a potent and selective inhibitor of canonical Wnt signaling, with an EC50 of 19.5 nM via a high-throughput TCF/LEF-reporter assay in SW480 colon cancer cells.
  • HY-16191
    ELR510444

    Microtubule/Tubulin Apoptosis Cancer
    ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.
  • HY-13057
    O6BTG-octylglucoside

    Glucose-conjugated MGMT inhibitor

    DNA Methyltransferase Cancer
    O6BTG-octylglucoside is a potent O 6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells.
  • HY-12521
    GSK-5498A

    CRAC Channel Inflammation/Immunology
    GSK-5498A is a selective small molecule blocker of CARC (IC50, 1 μM); inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.
  • HY-101664
    Ilaprazole

    IY-81149

    Proton Pump TOPK Cancer Inflammation/Immunology
    Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
  • HY-135396
    (1S,2S)-Bortezomib

    Proteasome Apoptosis Cancer
    (1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans.
  • HY-136833
    X5050

    Others Neurological Disease
    X5050 is a REST inhibitor, with an EC50 of 2.1 μM.
  • HY-115686
    8-Azaadenosine

    Adenosine Deaminase Cancer Inflammation/Immunology
    8-Azaadenosine is a potent ADAR1 (adenosine deaminases acting on double-stranded RNA) inhibitor. 8-Azaadenosine reduces A-to-I editing activity in a leukemia cell line, restores let-7 and inhibits leukemia stem cells self-renewal in vitro.
  • HY-130254
    Src Inhibitor 3

    Src Cancer Inflammation/Immunology
    Src Inhibitor 3 is a potent, orally active c-terminal Src kinase (CSK) with IC50 values below 3 nM and 4 nM in CSK HTRF and Caliper assay, respectively. Src Inhibitor 3 shows the ability to increase T cell proliferation induced by T cell receptor signaling.
  • HY-15355
    Loviride

    R 89439

    Reverse Transcriptase HIV Infection
    Loviride (R 89439) is a non-nucleoside reverse transcriptase inhibitor (NNRTI), with an IC50 of 0.3 µM for reverse transcriptase from HIV-1. Loviride (R 89439) inhibits HIV-1, HIV-2 and SIV replication in MT-4 cells.
  • HY-B0228
    Adenosine

    Adenine riboside; D-Adenosine

    Nucleoside Antimetabolite/Analog Autophagy Apoptosis Endogenous Metabolite Cancer Metabolic Disease
    Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation.
  • HY-129189
    RAS GTPase inhibitor 1

    Ras Cancer
    RAS GTPase inhibitor 1 (example 51) is a RAS GTPase inhibitor with anti-tumor activity, extracted from patent WO2018212774A1. RAS GTPase inhibitor 1 (example 51) exhibits an EC50 less than 1 μM for at least one nucleotide exchange and an IC50 less than 1 μM in H727 cells.
  • HY-10225
    Belinostat

    PXD101; PX105684

    HDAC Autophagy Cancer
    Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.
  • HY-100693
    SYP-5

    HIF/HIF Prolyl-Hydroxylase Cancer
    SYP-5 is a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis.
  • HY-13541A
    ADH-1 trifluoroacetate

    Others Cancer
    ADH-1 trifluoroacetate is an N-cadherin antagonist, which inhibits N-cadherin mediated cell adhesion.
  • HY-101071A
    Monastrol

    (±)-Monastrol

    Kinesin Apoptosis Cancer
    Monastrol is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5 with an IC50 value of 14 μM.
  • HY-18664
    PFI-4

    Epigenetic Reader Domain Cancer
    PFI-4 is a potent and selective and cell permeable BRPF1 bromodomain inhibitor (IC50 = 80 nM).
  • HY-B0535A
    Ethambutol dihydrochloride

    Emb dihydrochloride

    Bacterial Antibiotic Infection
    Ethambutol dihydrochloride (Emb dihydrochloride) is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.
  • HY-19971
    ML239

    Others Cancer
    ML239 is a potent and selective inhibitor of breast cancer stem cells, with an IC50 of 1.16 μM.
  • HY-12762
    QS11

    Others Cancer
    QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 µM. QS11 modulates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells.
  • HY-10218
    Everolimus

    RAD001; SDZ-RAD

    mTOR FKBP Autophagy Apoptosis Cancer
    Everolimus (RAD001) is a Rapamycin derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities.
  • HY-15003
    ATH686

    FLT3 Apoptosis Cancer
    ATH686 is a potent, selective and ATP-competitive FLT3 inhibitor. ATH686 target mutant FLT3 protein kinase activity and inhibit the proliferation of cells harboring FLT3 mutants via induction of apoptosis and cell cycle inhibition. ATH686 has antileukemic effects.
  • HY-100853
    IWP-O1

    Porcupine Wnt Cancer
    IWP-O1 is a highly potent Porcupine (Porcn) inhibitor, with an EC50 of 80 pM in L-Wnt-STF cells. IWP-O1 prevents the secretion of Wnt proteins. IWP-O1 suppresses the phosphorylation of Dvl2/3 and LRP6 in HeLa cells.
  • HY-N3023
    3,4-Dihydroxybenzylamine hydrobromide

    NSC 263475 hydrobromide

    DNA/RNA Synthesis Cancer
    3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) is an improved dopamine analog cytotoxic and inhibits DNA polymerase activity in melanoma cells. 3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) displays growth inhibitory activity in melanoma cell lines with varying degrees of tyrosinase activity.
  • HY-107856
    5-Fluorouridine

    Others Cancer
    5-Fluorouridine is a metabolite of 5-fluorouracil with anticancer activity. 5-fluorouridine inhibits rRNA synthesis of human colon carcinoma cells. 5-Fluorouridine exhibits cytotoxic effect on growth of L1210 cells with an IC50 of 2 nM.
  • HY-124617A
    AMXT-1501 tetrahydrochloride

    Apoptosis Cancer Inflammation/Immunology
    AMXT-1501 tetrahydrochloride is an orally active polyamine transport inhibitor. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells. Combination of DFMO and AMXT‐1501 induces caspase‐3 mediated apoptosis in NB cell lines.
  • HY-117819
    TMP920

    ROR Inflammation/Immunology
    TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM.
  • HY-102064
    SR 57227A

    5-HT Receptor Neurological Disease
    SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.
  • HY-P1454
    Fz7-21

    Ac-LPSDDLEFWCHVMY-NH2

    Wnt Cancer
    Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2), a peptide antagonist of Frizzled 7 (FZD 7) receptors, selectively binds to FZD7 CRD subclass. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC50=100 nM) or transfected with a construct expressing WNT3A or WNT1. Fz7-21 also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells (IC50=50 nM).
  • HY-N1150
    Thymidine

    DThyd; NSC 21548

    DNA/RNA Synthesis Endogenous Metabolite Others
    Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.
  • HY-128607
    Mcl1-IN-9

    Bcl-2 Family Cancer
    Mcl1-IN-9 is a potent myeloid cell leukemia-1 (Mcl-1) Inhibitor with an IC50 of 446 nM in reengineered BCR-ABL+ B-ALL cells and a Ki of 0.03 nM.
  • HY-N6601
    Pomolic acid

    Randialic acid A

    Apoptosis Cancer
    Randialic acid A (Pomolic acid) is a pentacyclic triterpene isolated from Euscaphis japonica (Tunb.). Randialic acid A (Pomolic acid) inhibits tumor cells growth and induces cell apoptosis. Randialic acid A (Pomolic acid) has a potential for the treatment of prostate cancer (PC).
  • HY-P1103
    CTCE-9908

    CXCR Cancer
    CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells.
  • HY-100321
    MCHR1 antagonist 2

    MCHR1 (GPR24) Potassium Channel Metabolic Disease Endocrinology
    MCHR1 antagonist 2 is an antagonist of melanin concentrating hormone receptor 1, with an IC50 of 65 nM; MCHR1 antagonist 2 also inhibits hERG, with an IC50 of 4.0 nM in IMR-32 cells.
  • HY-19553
    LP99

    Epigenetic Reader Domain Inflammation/Immunology
    LP99, an epigenetic probe, is a potent and selective inhibitor of the BRD7 and BRD9 bromodomains with a Kd of 99 nM against BRD9. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells.
  • HY-128595
    MT-4

    Others Cancer
    MT-4 blocks the TG2/FN complex at the interface between cancer cells and the tumor niche. MT-4 inhibits the adhesion of ovarian cancer (OC) cells to the peritoneum.
  • HY-126075A
    WS-383

    E1/E2/E3 Enzyme Cancer
    WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
  • HY-N2403
    Dihydrolycorine

    Others Neurological Disease
    Dihydrolycorine, isolated from Lycoris radiate Herb, is an inhibitor of protein synthesis in eukarytic cells by inhibiting the peptide bone formation step.
  • HY-12682
    Glutaminase C-IN-1

    Compound 968

    Glutaminase Cancer
    Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts.
  • HY-100541
    INH6

    Apoptosis Cancer
    INH6 is a potent Nek2/Hec1 inhibitor; inhibits the growth of HeLa cells with an IC50 of 2.4 μM.
  • HY-19352
    T56-LIMKi

    T5601640

    LIM Kinase (LIMK) Cancer
    T56-LIMKi is a selective inhibitor of LIMK2; inhibits the growth of Panc-1 cells with an IC50 of 35.2 μM.
  • HY-13062
    Daunorubicin hydrochloride

    Daunomycin hydrochloride; RP 13057 hydrochloride; Rubidomycin hydrochloride

    Topoisomerase DNA/RNA Synthesis ADC Cytotoxin Bacterial Autophagy Apoptosis Antibiotic Cancer Infection
    Daunorubicin (Daunomycin) hydrochloride is a topoisomerase II inhibitor with potent antineoplastic activities. Daunorubicin hydrochloride inhibits DNA and RNA synthesis in sensitive and resistant Ehrlich ascites tumor cells.
  • HY-N7452
    Coumermycin A1

    JAK Bacterial Metabolic Disease
    Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria.
  • HY-N0779A
    Silybin

    Apoptosis Cancer Inflammation/Immunology
    Silybin is a flavonolignan isolated from milk thistle (Silybum marianum) seeds. Silybin induces apoptosis and exhibits hepatoprotective, antioxidant, anti-inflammatory, anti-cancer activity.
  • HY-101849
    Fasentin

    GLUT Cancer Cardiovascular Disease
    Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity.
  • HY-126585
    SAICAR

    Endogenous Metabolite Cancer
    SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC50 of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions.
  • HY-108476
    INDY

    DYRK Cancer
    INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells.
  • HY-13018
    MRT67307

    IKK ULK Autophagy Cancer Inflammation/Immunology
    MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 also blocks autophagy in cells.
  • HY-103397
    Nanaomycin A

    DNA Methyltransferase Parasite Cancer Infection
    Nanaomycin A is the first selective DNMT3B inhibitor with an IC50 of 500 nM. Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells. Nanaomycin A inhibits in vitro growth of the human malaria parasite Plasmodium falciparum with an IC80 value of 33.1 nM.
  • HY-13018A
    MRT67307 hydrochloride

    IKK ULK Autophagy Cancer Inflammation/Immunology
    MRT67307 hydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 hydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 hydrochloride also blocks autophagy in cells.
  • HY-125840
    Belzutifan

    PT2977; MK-6482

    HIF/HIF Prolyl-Hydroxylase Cancer
    Belzutifan (PT2977) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. Belzutifan, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. Belzutifan is a potential treatment for clear cell renal cell carcinoma (ccRCC).
  • HY-P1318
    Ac-RYYRIK-NH2

    Opioid Receptor Neurological Disease
    Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
  • HY-16673
    PSN632408

    GPR119 Metabolic Disease
    PSN632408, a selective, orally active GPR119 agonist, shows similar potency to OEA at both recombinant mouse and human GPR119 receptors (EC50=5.6 and 7.9 uM, respectively). PSN632408 can stimulate β-cell replication and improve islet graft function. PSN632408 has the potential for the research of obesity and related metabolic disorders.
  • HY-12810
    EHop-016

    Ras Cancer
    EHop-016 is a potent and selective Rac GTPase Rac1 and Rac3 inhibitor. EHop-016 inhibits Rac1 activity with an IC50 of 1.1 μM in MDA-MB-435 cells. EHop-016 inhibits Vav2 interaction with Rac, Rac-activated PAK1, lamellipodia formation, and cell migration.
  • HY-10585
    Valproic acid

    VPA; 2-Propylpentanoic Acid

    HDAC Autophagy Mitophagy HIV Notch Cancer
    Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
  • HY-131904
    POMHEX

    Enolase Apoptosis Cancer Metabolic Disease
    POMHEX, a racemic mixture and a cell-permeable pivaloyloxymethyl (POM) prodrug of HEX, is a potent, ENO2-specific inhibitor of enolase. POMHEX exhibits low-nanomolar potency against ENO1-deleted cells in vitro and is capable of eradicating ENO1-deleted xenografted tumours in vivo. POMHEX is a potent glycolysis inhibitor.
  • HY-17600
    Acalabrutinib

    ACP-196

    Btk Cancer
    Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
  • HY-W016099
    3-Methyl-2-quinoxalinecarboxylic acid

    MQCA

    Others Cancer
    3-Methyl-2-quinoxalinecarboxylic acid (MQCA), an important N-oxide reductive metabolite of Quinocetone or Olaquindox, potently inhibits the growth of Chang liver cells through S phase arrest of the cell cycle.
  • HY-110182
    SP-141

    MDM-2/p53 Cancer
    SP-141 is a specific inhibitor of MDM2. SP-141 promotes MDM2 auto-ubiquitination and degradation. SP-141 might be used for the research of pancreatic cancer and breast cancer cells.
  • HY-136195
    TL13-110

    ALK Cancer
    TL13-110 is a negative control for TL13-112 (HY-123919) and a potent ALK inhibitor with an IC50 of 0.34 nM. TL13-110 does not degrade ALK in cells.
  • HY-136194
    TL13-22

    ALK Cancer
    TL13-22 is a negative control for TL13-12 (HY-122582) and a potent ALK inhibitor with an IC50 of 0.54 nM. TL13-22 does not degrade ALK in cells.
  • HY-130608
    Mutated EGFR-IN-3

    EGFR Cancer
    Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively.
  • HY-P1454A
    Fz7-21 TFA

    Ac-LPSDDLEFWCHVMY-NH2 TFA

    Wnt Cancer
    Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) TFA , a peptide antagonist of Frizzled 7 (FZD 7) receptors, selectively binds to FZD7 CRD subclass. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC50=100 nM) or transfected with a construct expressing WNT3A or WNT1. Fz7-21 also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells (IC50=50 nM).
  • HY-101597
    NVX-207

    Apoptosis Cancer
    NVX-207, a Betulinic acid-derived anti-cancer compound, shows anti-tumor activity (mean IC50=3.5 μM) against various human and canine cell lines. NVX-207-induced apoptosis is associated with activation of the intrinsic apoptotic pathway via cleavage of caspases -9, -3, -7 and of PARP.
  • HY-117388
    THI0019

    Integrin Inflammation/Immunology
    THI0019 is a potent integrin α4β1 (VLA-4) agonist with an EC50 range of 1-2 μM. THI0019 induces stem/progenitor cells adhesion. THI0019 also regulates adhesion mediated by α4β7, α5β1 and αLβ2.
  • HY-N6693
    Valinomycin

    NSC 122023

    Bacterial Apoptosis Antibiotic Autophagy Infection
    Valinomycin (NSC 122023) is a cyclic depsipeptide antibiotic first isolated from Streptomyces fulvissimus, act as a potassium selective ionophore. Valinomycin (NSC 122023) inhibits lymphocyte proliferation by its effects on the cell membrane, and induces apoptosis in CHO cells. Valinomycin induces activation of PINK1 leading to Parkin Ser65 phosphorylation.
  • HY-P0069
    D-JNKI-1

    AM-111; XG-102

    JNK Others
    D-JNKI-1 (AM-111) is a highly potent and cell-permeable peptide inhibitor of JNK.
  • HY-114361
    OSMI-4

    Others Metabolic Disease
    OSMI-4 is a low nanomolar O-GlcNAc transferase (OGT) inhibitor, with an EC50 of 3 μM in cells.
  • HY-101073
    Salermide

    Sirtuin Apoptosis Cancer
    Salermide is an inhibitor of Sirt1 and Sirt2; can cause strong cancer-specific apoptotic cell death.
  • HY-135846
    PDD00031705

    Others Cancer
    PDD00031705 is a benzimidazolone core cell-inactive inhibitor of Poly (ADP-ribose) glycohydrolase (PARG).
  • HY-16691
    AK-7

    Sirtuin Neurological Disease
    AK-7 is a selective cell- and brain-permeable SIRT2 inhibitor, with an IC50 of 15.5 μM.
  • HY-12409
    PFI-3

    Epigenetic Reader Domain Cancer
    PFI-3 is a selective, potent and cell-permeable SMARCA2/4 bromodomain inhibitor with a Kd of 89 nM.
  • HY-15773
    PF-4708671

    Ribosomal S6 Kinase (RSK) Autophagy Cancer
    PF-4708671 is a potent cell-permeable S6K1 inhibitor with a Ki of 20 nM and IC50 of 160 nM.
  • HY-101465
    AK-1

    Sirtuin Neurological Disease
    AK-1 is a potent, specific and cell-permeable SIRT2 inhibitor, with an IC50 of 12.5 μM.
  • HY-50895
    Gefitinib

    ZD1839

    EGFR Autophagy Cancer
    Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
  • HY-B0240
    Disulfiram

    Tetraethylthiuram disulfide; TETD

    Aldehyde Dehydrogenase (ALDH) Interleukin Related Pyroptosis Metabolic Disease Cancer
    Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells[1-4].
  • HY-50895A
    Gefitinib hydrochloride

    ZD-1839 hydrochloride

    EGFR Cancer
    Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity.
  • HY-18666
    D77

    HIV Infection
    D77 is anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75. D77 inhibits HIV-1(IIIB) replication by EC50 value of 23.8 μg/ml in MT-4 cell (5.03 μg/ml for C8166 cells).
  • 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-12204
    PFK-015

    Autophagy Cancer
    PFK-015 is an effective inhibitor of PFKFB3 with IC50 of 110 nM (recombinant PFKFB3) and inhibits PFKFB3 activity in cancer cells with IC50 of 20 nM.
  • HY-12622
    HSP70-IN-1

    HSP Cancer
    HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.
  • HY-12444
    Y15

    FAK Inhibitor 14

    FAK Cancer
    Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.
  • HY-112445
    SGC3027

    Histone Methyltransferase Cancer
    SGC3027 is a histone methyltransferase inhibitor. SGC3027 is the first potent, selective and cell active chemical probe for PRMT7.
  • HY-100303
    FR194738 free base

    Others Metabolic Disease
    FR194738 free base is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM.
  • HY-135318
    NBDHEX

    Glutathione Peroxidase Apoptosis Autophagy Cancer
    NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.
  • HY-129168
    USP7-IN-5

    Deubiquitinase Cancer
    USP7-IN-5 is a potent ubiquitin specific protease 7 (USP7) inhibitor extracted from patent WO2017212012A1, example 40, has an IC50 of 49.9 nM.
  • HY-129169
    USP7-IN-6

    Deubiquitinase Cancer
    USP7-IN-6 is a potent ubiquitin specific protease 7 (USP7) inhibitor, extracted from patent WO2017212010A1, example 25, has an IC50 of 6.8 nM.
  • HY-P1318A
    Ac-RYYRIK-NH2 TFA

    Opioid Receptor Neurological Disease
    Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
  • HY-N4201
    β-Hydroxyisovalerylshikonin

    EGFR Src Cancer
    Beta-hydroxyisovalerylshikonin is a natural product isolated from Lithospermium radix, acts as a potent inhibitor of protein tyrosine kinases (PTK), with IC50s of 0.7μM and 1μM for EGFR and v-Src receptor, respectively. Beta-hydroxyisovalerylshikonin is effective against a wide variety of tumor cell lines, and most efficiently induces cell-death in NCI-H522 and DMS114 cells.
  • HY-112823
    Almonertinib

    HS-10296

    EGFR Cancer
    Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib 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 is used for the research of the non-small cell lung cancer.
  • HY-112823B
    Almonertinib hydrochloride

    HS-10296 hydrochloride

    EGFR Cancer
    Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride 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 hydrochloride is used for the research of the non-small cell lung cancer.
  • HY-12757
    YHO-13177

    BCRP Cancer
    YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells.
  • HY-117421A
    CM-579 trihydrochloride

    Histone Methyltransferase DNA Methyltransferase Cancer
    CM-579 trihydrochloride is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells.
  • HY-117421
    CM-579

    Histone Methyltransferase DNA Methyltransferase Cancer
    CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells.
  • HY-B0392
    (S)-(+)-Rolipram

    (+)-Rolipram; (S)-Rolipram

    Phosphodiesterase (PDE) Apoptosis Inflammation/Immunology Cancer
    (S)-(+)-Rolipram ((+)-Rolipram) is a cyclic AMP(cAMP)-specific phosphodiesterase (PDE) inhibitor, with an IC50 of 1100 nM. (S)-(+)-Rolipram can suppresse tumor necrosis factor-alpha (TNFα) production by human mononuclear cells.
  • HY-16657
    TAPI-1

    MMP Cancer Inflammation/Immunology
    TAPI-1 is a TACE (ADAM17) inhibitor and blocks the shedding of several cell surface proteins. TAPI-1 is also a metalloproteinase (MMP) inhibitor.
  • HY-119808
    Terrein

    Melanocortin Receptor Apoptosis Antibiotic Cancer
    Terrein is a melanogenesis inhibitor. Terrein induces apoptosis in breast cancer cell lines . Terrein is an inhibitor of quorum sensing and c-di-GMP in Pseudomonas aeruginosa.
  • HY-126075
    WS-383 free base

    E1/E2/E3 Enzyme Cancer
    WS-383 free base is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 free base inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
  • HY-100012
    CBR-5884

    Others Cancer
    CBR-5884 is an active, selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with an IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis.
  • HY-N6733
    Aphidicolin

    DNA/RNA Synthesis HSV Apoptosis Antibiotic Infection Inflammation/Immunology
    Aphidicolin is an inhibitor of DNA polymerase α and δ, prevents mitotic cell division by interfering with the activity of DNA polymerase. Aphidicolin is an antibiotic produced by the mold Cephalosporium aphidicola. Aphidicolin is a potent inhibitor of cellular deoxyribonucleic acid synthesis and inhibits the growth of herpes simplex virus. Aphidicolin potentiates apoptosis induced by arabinosyl nucleosides in a human promyelocytic leukemia cell line.
  • HY-133016
    M8891

    Others Cancer Cardiovascular Disease
    M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 54 nM and a Ki of 4.33 nM. M8891 does not inhibit MetAP-1 (IC50>10 µM). M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity.
  • HY-101297
    Z-IETD-FMK

    Z-IE(OMe)TD(OMe)-FMK

    Caspase Cancer
    Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a selective and cell permeable caspase-8 inhibitor. Z-IETD-FMK is also a granzyme B inhibitor.
  • HY-N6791
    KT5823

    PKA PKC Bacterial Apoptosis Antibiotic Infection Inflammation/Immunology
    KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 is a staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na +/I - symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation.
  • HY-N6682
    Cytochalasin D

    Zygosporin A; NSC 209835

    Arp2/3 Complex Bacterial Antibiotic YAP Infection
    Cytochalasin D (Zygosporin A; NSC 209835) is a potent and cell-permeable inhibitor of actin polymerization derived from fungus, inhibits the G-actin–cofilin interaction by binding to G-actin. Cytochalasin D (Zygosporin A; NSC 209835) also inhibits the binding of cofilin to F-actin and decreases the rate of both actin polymerization and depolymerization in living cells.Cytochalasin D can reduce exosome release, in turn reducing the amount of survivin present in the tumour environment. Cytochalasin D induces phosphorylation and cytoplasmic retention of YAP.
  • HY-N2415
    Podophyllotoxone

    Microtubule/Tubulin Cancer
    Podophyllotoxone is isolated from the roots of Dysosma versipellis and has anti-cancer activities.Podophyllotoxone is able to inhibit the tubulin polymerization.
  • HY-16214
    FX-11

    LDHA Inhibitor FX11

    Lactate Dehydrogenase Apoptosis Cancer
    FX-11 (LDHA Inhibitor FX11) is a potent lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 23.3 μM for HeLa cell and a Ki value of 8 μM.
  • HY-13229
    BOC-D-FMK

    Caspase Apoptosis Cancer
    Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor. Boc-D-FMK inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM.
  • HY-12688
    Succinyl phosphonate

    Endogenous Metabolite Reactive Oxygen Species Neurological Disease
    Succinyl phosphonate is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
  • HY-13744
    Rubitecan

    RFS 2000; 9-Nitrocamptothecin

    Topoisomerase Cancer
    Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells.
  • HY-N6932
    Voacamine

    Cannabinoid Receptor P-glycoprotein Cancer Metabolic Disease
    Voacamine, an indole alkaloid, isolated from Voacanga Africana, exhibits potent cannabinoid CB1 receptor antagonistic activity. Voacamine also inhibits P-glycoprotein (P-gp) action in multidrug-resistant tumor cells.
  • HY-111588
    Xanthoangelol

    Apoptosis Monoamine Oxidase Bacterial AMPK Cancer Infection Inflammation/Immunology
    Xanthoangelol, extracted from Angelica keiskei, suppresses obesity-induced inflammatory responses. Xanthoangelol possesses antibacterial activity. Xanthoangelol inhibits monoamine oxidases. Xanthoangelol induces apoptosis in neuroblastoma and leukemia cells.
  • HY-B1700A
    Mivacurium dichloride

    nAChR Neurological Disease
    Mivacurium dichloride is a benzylisoquinoline derivative and is a short-acting non-depolarizing neuromuscular blocking agent and skeletal muscle relaxant. Mivacurium dichloride couples with the nAChR to reduce or inhibit the depolarizing effect of acetylcholine on the terminal disc of the muscle cell.
  • HY-12681
    CCT251545

    Wnt Cancer
    CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with an IC50 of 5 nM in 7dF3 cells. CCT251545 is a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
  • HY-16172
    DMAPT

    Dimethylamino Parthenolide

    NF-κB Cancer
    DMAPT (Dimethylamino Parthenolide), a water soluble analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect.
  • HY-13326
    ASP3026

    ALK Apoptosis Cancer
    ASP3026 is a potent, selective and orally active inhibitor of anaplastic lymphoma kinase (ALK). ASP3026 induces apoptosis of tumor cells. ASP3026 can be used for the research of non-small cell lung cancer (NSCLC).
  • HY-108701
    Nampt-IN-3

    NAMPT HDAC Autophagy Apoptosis Cancer
    Nampt-IN-3 (Compound 35) simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC with IC50s of 31 nM and 55 nM, respectively. Nampt-IN-3 effectively induces cell apoptosis and autophagy and ultimately leads to cell death.
  • HY-15465A
    KN-93 hydrochloride

    CaMK Autophagy Cancer
    KN-93 hydrochloride is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.
  • HY-P0121
    ReACp53

    MDM-2/p53 Cancer
    ReACp53 could inhibit p53 amyloid formation and rescue p53 function in cancer cell lines.
  • HY-17353
    BIBR 1532

    Telomerase Apoptosis Cancer
    BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay.
  • HY-13506
    M344

    D 237; MS 344

    HDAC Cancer
    M344 (D 237) is an inhibitor of histone deacetylase (IC50=100 nM) and an inducer of terminal cell fifferentiation.
  • HY-16107
    BMS-303141

    ATP Citrate Lyase Metabolic Disease
    BMS-303141 is a potent, cell-permeable ATP-citrate lyase (ACL) inhibitor with an IC50 of 0.13 μM.
  • HY-19725
    A-1155463

    Bcl-2 Family Cancer
    A-1155463 is a highly potent and selective BCL-XL inhibitor with an EC50 of 70 nM in Molt-4 cell.
  • HY-13623A
    Entecavir monohydrate

    BMS200475 monohydrate; SQ34676 monohydrate

    HBV Infection
    Entecavir monohydrate (BMS200475 monohydrate; SQ34676 monohydrate) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.
  • HY-15465
    KN-93

    CaMK Autophagy Cancer
    KN-93 is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.
  • HY-P1009
    Z-YVAD-FMK

    Caspase Cancer
    AA-Z-YVAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor with anti-inflammatory and anti-tumor activities.
  • HY-13623
    Entecavir

    BMS200475; SQ34676

    HBV Infection
    Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.
  • HY-P9902
    Pembrolizumab

    MK-3475; Lambrolizumab

    PD-1/PD-L1 Cancer
    Pembrolizumab is a humanized antibody inhibiting the programmed cell death 1 (PD-1) receptor, used in cancer immunotherapy.
  • HY-108248
    KU-32

    HSP Metabolic Disease Neurological Disease Cardiovascular Disease
    KU-32 is a novel, novobiocin-based Hsp90 inhibitor that can protect against neuronal cell death.
  • HY-100861
    C-11

    ADC Cytotoxin Cancer
    C-11 is a tubulin inhibitor and acts as a ADC cytotoxin, displays cytotoxicity for carcinoma cell lines.
  • HY-17024
    Cyclopamine

    11-Deoxojervine

    Hedgehog Smo Endogenous Metabolite Cancer
    Cyclopamine is a Hedgehog (Hh) pathway antagonist with an IC50 of 46 nM in the Hh cell assay. Cyclopamine is also a selective Smo inhibitor.
  • HY-100269
    Chymase-IN-1

    Others Inflammation/Immunology
    Chymase-IN-1 is a potent, selective, orally active, nonpeptide inhibitor of human mast cell chymase with an IC50 of 29 nM.
  • HY-12454
    DM4

    Microtubule/Tubulin Cancer
    DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody drug conjugate.
  • HY-10455
    Carfilzomib

    PR-171

    Proteasome Autophagy Apoptosis Cancer
    Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
  • HY-116147
    Ceranib-2

    LPL Receptor Apoptosis Cancer
    Ceranib-2 is a potent and nonlipid ceramidase inhibitor that inhibits cellular ceramidase activity with an IC50 of 28 μM in SKOV3 cells. Ceranib-2 induces the accumulation of multiple ceramide species, decreases levels of sphingosine and sphingosine-1-phosphate (S1P), and induces cell apoptosis. Anticancer activity.
  • HY-118482
    Sauristolactam

    Saurolactam

    Others Neurological Disease
    Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus chinensis, has significant neuroprotective activity against glutamate-induced toxicity in primary cultured rat cortical cells. Sauristolactam also inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation.
  • HY-125911
    Gossypin

    NF-κB Cancer Inflammation/Immunology Cardiovascular Disease
    Gossypin is a flavone isolated from Hibiscus vitifolius and has antioxidant, antiinflammatory, anticancer, anticataract, antidiabetic, analgesic and hepatoprotective activities. Gossypin inhibits NF-κB and NF-κB-regulated gene expression. Gossypin inhibits RANKL-induced osteoclastogenesis both in mouse primary bone marrow cells and RAW 264.7 cells in vitro.
  • HY-136555
    GSK717

    NOD-like Receptor (NLR) Inflammation/Immunology
    GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells.
  • HY-117383
    NGI-1

    ML414

    Virus Protease Cancer
    NGI-1 (ML414) is a potent oligosaccharyltransferase (OST) inhibitor, directly targeting and blocking the function of the OST catalytic subunits STT3A and STT3B. NGI-1 is a cell permeable inhibitor and can effectively reduce virus infectivity without affecting cell viability.
  • HY-N0293
    Paeoniflorin

    Peoniflorin

    HSP Neurological Disease
    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.
  • HY-12326A
    c-di-AMP sodium

    Cyclic diadenylate sodium; Cyclic-di-AMP sodium

    STING Bacterial Endogenous Metabolite Inflammation/Immunology
    c-di-AMP (Cyclic diadenylate) sodium is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP sodium is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP sodium acts as a potent mucosal adjuvant stimulating both humoral and cellular responses.
  • HY-122815
    Fusicoccin

    Fusicoccin A

    Apoptosis Cancer
    Fusicoccin (Fusicoccin A), a fungal pytotoxin, is a stabilizer of specific 14-3-3 protein-protein interactions. Fusicoccin sabilizes H +-ATPase/14-3-3 cmplex in pants, maintaining the enzyme in activated state. Fusicoccin also stabilizes 14-3-3 protein interactions with binding partners containing a C-terminal 14-3-3 recognition motif (a mode 3 motif), such as ERα, GPIbα, TASK3, CTFR, and p53. Fusicoccin induces apoptosis in cancer cells and has anticancer activity.
  • HY-111640
    3'-Azido-3'-deoxy-5-methylcytidine

    HIV Reverse Transcriptase Infection
    3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells.
  • HY-107407
    SB-218078

    Checkpoint Kinase (Chk) CDK PKC Apoptosis Cancer
    SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest.
  • HY-129767
    CMLD012612

    Eukaryotic Initiation Factor (eIF) Cancer
    CMLD012612 is an amidino-rocaglate containing a hydroxamate group and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012612 inhibits cell translation and is cytotoxic to NIH/3T3 cells with an IC50 value of 2 nM. CMLD012612 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A) and possesses potent anti-neoplastic activity.
  • HY-119016A
    SK1-​I hydrochloride

    BML-258 hydrochloride

    SPHK Cancer
    SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM. SK1-I hydrochloride (BML-258 hydrochloride) has good water solubility. SK1-I hydrochloride (BML-258 hydrochloride) shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I hydrochloride (BML-258 hydrochloride) enhances autophagy and has antitumor activity.
  • HY-119016
    SK1-I

    BML-258

    SPHK Cancer
    SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM. SK1-I (BML-258) has good water solubility. SK1-I (BML-258) shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I (BML-258) enhances autophagy and has antitumor activity.
  • HY-N2600
    Kuwanon H

    Bombesin Receptor Cancer
    Kuwanon H is a flavonoid isolated from Morus bombycis, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a Ki value of 290 nM in cells.
  • HY-128605
    PD-1-IN-22

    PD-1/PD-L1 Cancer
    PD-1-IN-22 is a potent programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction inhibitor with an IC50 of 92.3 nM.
  • HY-124653
    HSP27 inhibitor J2

    J2

    HSP Cancer
    HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition.
  • HY-100111
    GLX351322

    NADPH Oxidase Metabolic Disease
    GLX351322 is an inhibitor of NADPH oxidase 4 (Nox4), and inhibits hydrogen peroxide production from NOX4-overexpressing cells with an IC50 of 5 μM.
  • HY-W011044
    CID 5951923

    KLF Cancer
    CID 5951923 is a potent inhibitor of Krüppel-like factor 5 (KLF5), with an IC50 of 603 nM. CID 5951923 can inhibit proliferation of cancer cells in vitro.
  • HY-13991
    CCG-1423

    Ras Cancer
    CCG-1423 is a novel inhibitor of RhoA/C-mediated gene transcription that is capable of inhibiting invasion of PC-3 prostate cancer cells in a Matrigel model of metastasis.
  • HY-16667
    HLM006474

    Others Cancer
    HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells.
  • HY-100223
    Calpeptin

    Cathepsin Proteasome Apoptosis Inflammation/Immunology
    Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets. Calpeptin is also an inhibitor of cathepsin K.
  • HY-115570
    GW406108X

    GW108X

    Kinesin ULK Autophagy Cancer
    GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK.
  • HY-115510
    SPR inhibitor 3

    SPRi3

    Others Inflammation/Immunology
    SPR inhibitor 3 (SPRi3) is a potent sepiapterin reductase (SPR) inhibitor. SPR inhibitor 3 (SPRi3) displays high binding affinity to human SPR in a cell-free assay (IC50=74 nM) and efficiently reduces biopterin levels in a cell-based assay (IC50=5.2 μM). SPR inhibitor 3 (SPRi3) reduces neuropathic and inflammatory pain through a reduction of BH4 levels.
  • HY-12688A
    Succinyl phosphonate trisodium salt

    Endogenous Metabolite Reactive Oxygen Species Cancer Metabolic Disease Neurological Disease
    Succinyl phosphonate trisodium salt is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
  • HY-122615
    SPOP-IN-6b

    Others Cancer
    SPOP-IN-6b is a speckle-type POZ protein (SPOP) inhibitor extracted from patent CN 107141287, SPOP-B-88.
  • HY-111418
    EBI-2511

    Histone Methyltransferase Cancer
    EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC50 of 6 nM in Pfeffiera cell lines, respectively.
  • HY-12808
    STF-118804

    NAMPT Apoptosis Cancer
    STF-118804 is a highly specific NAMPT inhibitor; reduces the viability of most B-ALL cell lines with IC50 <10 nM.
  • HY-18665
    GSK-5959

    Epigenetic Reader Domain Cancer
    GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with an IC50 of ~ 80 nM.
  • HY-17602
    Amcasertib

    BBI503

    Others Cancer
    Amcasertib is an orally administered investigational agent designed to inhibit cancer stem cell pathways, including Nanog, by targeting stemness kinases.
  • HY-14394
    TBB

    NSC 231634; Casein Kinase II Inhibitor I

    Casein Kinase Cancer
    TBB is a cell-permeable and ATP-competitive CK2 inhibitor with an IC50 of 0.15 μM for rat liver CK2.
  • HY-13257
    Thiazovivin

    ROCK Cancer
    Thiazovivin is a potent ROCK inhibitor, which can protect human embryonic stem cells. Thiazovivin improves the efficiency of iPSC generation.
  • HY-101405
    Gestrinone

    R 2323

    Estrogen Receptor/ERR Inflammation/Immunology
    Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.
  • HY-13867
    Bisindolylmaleimide I

    GF109203X; Go 6850

    PKC Metabolic Disease Cancer
    Bisindolylmaleimide I (GF109203X) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor with a Ki of 14 nM.
  • HY-112125A
    KRN2 bromide

    Others Inflammation/Immunology
    KRN2 (bromide) is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 0.1 μM.
  • HY-N0125
    Diosmetin

    Cytochrome P450 Cancer
    Diosmetin is a natural flavonoid which inhibits human CYP1A enzyme activity with an IC50 of 40 μM in HepG2 cell.
  • HY-17567B
    Heparin Lithium salt

    Autophagy Others
    Heparin Lithium salt is an anticoagulant which binds reversibly to antithrombin III (ATIII). Heparin Lithium salt significantly inhibits exosome-cell interactions.
  • HY-101523
    Cdc7-IN-1

    CDK Cancer
    Cdc7-IN-1 (Compound 13) is a highly potent, selective and ATP competitive inhibitor of Cdc7 kinase, with an IC50 value of 0.6 nM at 1 mM ATP and with slow off-rate characteristics. Cdc7-IN-1 potently inhibits Cdc7 activity in cancer cells, and effectively induces cell death.
  • HY-14904A
    Umifenovir hydrochloride

    Influenza Virus SARS-CoV Infection
    Umifenovir hydrochloride is a potent, orally active broad-spectrum antiviral with activity against a number of enveloped and non-enveloped viruses. Umifenovir hydrochloride is used as an anti-influenza virus agent. Umifenovir hydrochloride could effectively inhibit the fusion of virus with host cells. Umifenovir hydrochloride is an efficient inhibitor of SARS-CoV-2 in vitro. Anti-inflammatory activity.
  • HY-17406S
    Tolcapone D7

    Ro 40-7592 D7

    COMT Amyloid-β Neurological Disease
    Tolcapone D7 (Ro 40-7592 D7) is a deuterium labeled Tolcapone. Tolcapone is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.
  • HY-N4100
    Trilobatin

    HIV SGLT Infection
    Trilobatin, a natural sweetener derived from Lithocarpus polystachyus Rehd, Trilobatin is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope. Neuroprotective effects. Trilobatin is also a SGLT1/2 inhibitor that selectively induces the proliferation of human hepatoblastoma cells.
  • HY-112257
    S-23

    Androgen Receptor Metabolic Disease
    S-23 is an orally active selective androgen receptor modulator (SARM) with a Ki of 1.7 nM. S-23 induces androgen receptor (AR)-mediated transcriptional activation in CV-1 cells. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats.
  • HY-137498
    EBOV/MARV-IN-1

    Others Infection
    EBOV/MARV-IN-1 is a potent inhibitor of Ebola virus (EBOV) and Marburg virus (MARV), with broad-spectrum activity (EC50=0.31, and 0.82 µM, respectively) and low cytotoxicity (SI>100) in HeLa cells.
  • HY-77293
    (E)-[6]-Dehydroparadol

    Apoptosis Keap1-Nrf2 Cancer
    (E)-[6]-Dehydroparadol, an oxidative metabolite of [6]-Shogaol (HY-14616), is a potent Nrf2 activator. (E)-[6]-Dehydroparadol can inhibit the growth and induce the apoptosis of human cancer cells.
  • HY-119402
    BCL6-IN-8c

    Bcl-2 Family Cancer
    BCL6-IN-8c is a potent and orally active B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor with an IC50 of 0.10 µM in cell-free enzyme-linked immunosorbent assay.
  • HY-B0990
    Thiostrepton

    Bacterial Antibiotic Infection
    Thiostrepton is a thiazole antibiotic which selectively inhibits FOXM1. FOXM1 binds to YAP/TEAD complex. YAP/TEAD/FOXM1 complex binding at regulatory regions of genes governing cell cycle may impact cell proliferation.
  • HY-N2557
    Euphorbia Factor L1

    Apoptosis Cancer Cardiovascular Disease
    Euphorbia Factor L1 is a diterpenoid from Euphorbia lathyris L., reduces the expression of Bcl-2, PI3K, AKT and mTOR protein and mRNA, upregulates cleaved caspase-9 and caspase-3 levels, buts shows no effect on pro-caspase-9 and pro-caspase-3. Euphorbia Factor L1 induces apoptosis, has anticancer, antiadipogenesis, antiosteoclastogenesis and multidrug resistance-modulating effect.
  • HY-112615
    NAMPT inhibitor-linker 1

    NAMPT Drug-Linker Conjugates for ADC Cancer
    NAMPT inhibitor-linker 1 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.
  • HY-18643
    TZ9

    E1/E2/E3 Enzyme Cancer
    TZ9 is a novel inhibitor of Rad6 ubiquitin conjugating enzyme(E2 enzyme); inhibits MDA-MB-231 cell proliferation with IC50 of ~6 uM.
  • HY-134665
    NITD-2

    DNA/RNA Synthesis Infection
    NITD-2, a dengue virus (DENV) polymerase inhibitor, inhibits the DENV RdRp-mediated RNA elongation. NITD-2 penetrates cell membrane poorly.
  • HY-114166
    2-D08

    E1/E2/E3 Enzyme TAM Receptor Cancer
    2-D08 is a cell permeable, mechanistically unique inhibitor of protein SUMOylation. 2-D08 also inhibits Axl with an IC50 of 0.49 nM.
  • HY-138203
    Z-LE(OMe)TD(OMe)-FMK

    Caspase Apoptosis Cancer
    Z-LE(OMe)TD(OMe)-FMK is a selective caspase-8 inhibitor. Z-LE(OMe)TD(OMe)-FMK can inhibit cell apoptosis.
  • HY-128726
    ITK inhibitor 2

    Itk Inflammation/Immunology
    ITK inhibitor 2 is a interleukin-2-inducible T-cell kinase (ITK) inhibitor extracted from patent WO2011065402A1, compound 4, with an IC50 of 2 nM.
  • HY-114317
    MARK4 inhibitor 1

    Apoptosis Cancer
    MARK4 inhibitor 1 is a potent microtubule affinity-regulating kinase 4 (MARK4) inhibitor, with an IC50 of 1.54 μM. MARK4 inhibitor 1 inhibits cancer cell proliferation, metastasis and induces apoptosis.
  • HY-W009731
    Dibenzoylmethane

    Keap1-Nrf2 Cancer Metabolic Disease
    Dibenzoylmethane, a minor ingredient in licorice, activates Nrf2 and prevents various cancers and oxidative damage. Dibenzoylmethane, an analog of curcumin, results in dissociation from Keap1 and nuclear translocation of Nrf2.
  • HY-N0322
    Cholesterol

    Estrogen Receptor/ERR Endogenous Metabolite Metabolic Disease
    Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.
  • HY-N2346
    Tubulysin E

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin E is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin E is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • HY-N7049
    Tubulysin F

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin F is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin F is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • HY-N7052
    Tubulysin I

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin I is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin I is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • HY-N7050
    Tubulysin G

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin G is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin G is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • HY-N2347
    Tubulysin C

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin C is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin C is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • HY-133011
    nAChR agonist 1

    nAChR Neurological Disease
    nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca 2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease.
  • HY-N6842
    ArnicolideC

    Others Cancer Infection
    ArnicolideC is a sesquiterpene lactone isolated Centipeda minima. ArnicolideC exertes a cytotoxic effect on the panel of Nasopharyngeal carcinoma (NPC) cells, significantly inhibiting cell growth in a dose- and time- dependent manner. ArnicolideC also exhibits inhibitory effects on NPC proliferation.
  • HY-111756
    BLM-IN-1

    Apoptosis Cancer
    BLM-IN-1 (compound 29) is an effective Bloom syndrome protein (BLM) inhibitor, with a strong BLM binding KD of 1.81 μM and an IC50 of 0.95 μM for BLM. Induces DNA damage response, as well as apoptosis and proliferation arrest in cancer cells.
  • HY-101130
    PNU-74654

    Wnt β-catenin Apoptosis Cancer
    PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC50 of 129.8 μM in NCI-H295 cell.
  • HY-13551
    Amsacrine

    m-AMSA; acridinyl anisidide

    Topoisomerase Autophagy Cancer
    Amsacrine (m-AMSA; acridinyl anisidide) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
  • HY-17427
    Emtricitabine

    BW1592

    HIV Reverse Transcriptase Infection
    Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 µM in PBMC cell. It is an antiviral drug for the treatment of HIV infection.
  • HY-N0083
    Betulin

    Trochol

    Fatty Acid Synthase (FASN) Apoptosis Endogenous Metabolite Cancer
    Betulin (Trochol), is a sterol regulatory element-binding protein (SREBP) inhibitor with an IC50 of 14.5 μM in K562 cell line.
  • HY-13749B
    Sitagliptin phosphate monohydrate

    MK-0431 phosphate monohydrate

    Dipeptidyl Peptidase Autophagy Metabolic Disease
    Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
  • HY-100244
    NS1652

    Chloride Channel Neurological Disease
    NS1652 is a reversible anion conductance inhibitor, blocks chloride channel, with an IC50 of 1.6 μM in human and mouse red blood cells.
  • HY-P1261
    Parstatin(mouse)

    Protease-Activated Receptor (PAR) Inflammation/Immunology Cardiovascular Disease
    Parstatin(mouse), a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis.
  • HY-13551A
    Amsacrine hydrochloride

    m-AMSA hydrochloride; acridinyl anisidide hydrochloride

    Topoisomerase Autophagy Cancer
    Amsacrine hydrochloride (m-AMSA hydrochloride; acridinyl anisidide hydrochloride) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
  • HY-13749
    Sitagliptin

    MK-0431

    Dipeptidyl Peptidase Autophagy Metabolic Disease
    Sitagliptin (MK-0431) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
  • HY-P1262
    Parstatin(human)

    Protease-Activated Receptor (PAR) Inflammation/Immunology Cardiovascular Disease
    Parstatin(human), a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis.
  • HY-13749A
    Sitagliptin phosphate

    MK-0431 phosphate

    Dipeptidyl Peptidase Autophagy Metabolic Disease
    Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
  • HY-W008638
    2'-Deoxyinosine

    Endogenous Metabolite Cancer Metabolic Disease
    2’-deoxyadenosine inhibits the growth of human colon-carcinoma cell lines and is found to be associated with purine nucleoside phosphorylase (PNP) deficiency.
  • HY-13413
    Tofogliflozin (hydrate)

    CSG-452 hydrate

    SGLT Reactive Oxygen Species Metabolic Disease
    Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2 (SGLT2) inhibitor with an IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2. Tofogliflozin partially inhibits high glucose-induced reactive oxyen species (ROS) generation in tubular cells.
  • HY-130240
    GCN2-IN-6

    Eukaryotic Initiation Factor (eIF) Cancer
    GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells).
  • HY-19805
    STO-609

    CaMK AMPK Autophagy Metabolic Disease
    STO-609 is a selective and cell-permeable inhibitor of the Ca 2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC50 ~0.02 g/ml.
  • HY-133779
    Gefitinib impurity 5

    Others Others
    Gefitinib impurity 5 is the impurity of Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
  • HY-131257
    Gefitinib impurity 1

    Others Others
    Gefitinib impurity 1 is the impurity of Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
  • HY-126246
    CDC25B-IN-1

    Phosphatase Cancer
    CDC25B-IN-1 (compound 4a) is a potent inhibitor of cell division cycle 25B (CDC25B) phosphatase, with a Ki of 8.5 μM. CDC25B-IN-1 potently inhibits cell proliferation and colony formation, causes an increase of the G2/M phase.
  • HY-16200
    Ethynylcytidine

    ECyD; TAS-106; 3'-C-Ethynylcytidine

    DNA/RNA Synthesis Nucleoside Antimetabolite/Analog Cancer
    Ethynylcytidine (ECyD), a nucleoside analog and a potent inhibitor of RNA synthesis, inhibits RNA polymerases I, II and II. Ethynylcytidine has robust antitumor activity in a wide range of models of cancer.
  • HY-124761
    Poloppin

    Polo-like Kinase (PLK) Autophagy Cancer
    Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC50=26.9 μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (Kd= 29.5 μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis. Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors.
  • HY-50751
    Linifanib

    ABT-869; AL-39324

    PDGFR VEGFR FLT3 c-Fms c-Kit Autophagy Apoptosis Cancer
    Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis.
  • HY-13555
    β-Lapachone

    ARQ-501; NSC-26326

    Topoisomerase Autophagy Apoptosis Cancer
    β-Lapachone (ARQ-501;NSC-26326) is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.
  • HY-17393
    Carboplatin

    NSC 241240

    DNA Alkylator/Crosslinker Autophagy DNA/RNA Synthesis Cancer
    Carboplatin (NSC 241240) is a DNA synthesis inhibitor which binds to DNA, inhibits replication and transcription and induces cell death. Carboplatin (NSC 241240) is a derivative of CDDP and a potent anti-cancer agent.
  • HY-13605
    Cytarabine

    Cytosine β-D-arabinofuranoside; Cytosine Arabinoside; Ara-C

    DNA/RNA Synthesis Nucleoside Antimetabolite/Analog HSV Autophagy Endogenous Metabolite Apoptosis Cancer Infection
    Cytarabine, a nucleoside analog, causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC50 of 16 nM. Cytarabine has antiviral effects against HSV.
  • HY-13605A
    Cytarabine hydrochloride

    Cytosine β-D-arabinofuranoside hydrochloride; Cytosine Arabinoside hydrochloride; Ara-C hydrochloride

    DNA/RNA Synthesis Nucleoside Antimetabolite/Analog HSV Autophagy Cancer Infection
    Cytarabine hydrochloride, a nucleoside analog, causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC50 of 16 nM. Cytarabine hydrochloride has antiviral effects against HSV.
  • HY-103028A
    GSK963

    RIP kinase Others
    GSK963 is a chiral, highly potent and selective inhibitor of RIP1 kinase, with an IC50 of 29 nM. GSK963 is a selective and potent inhibitor of necroptosis in murine and human cells in vitro.
  • HY-12964
    SGI-7079

    TAM Receptor Cancer
    SGI-7079 is a potent and ATP-competitive Axl inhibitor, significantly inhibits the proliferation of SUM149 or KPL-4 cells with an IC50 of 0.43 or 0.16 μM, respectively.
  • HY-103693
    NAZ2329

    Phosphatase Cancer
    NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties.
  • HY-124131
    DS-437

    Histone Methyltransferase Cancer Inflammation/Immunology
    DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC50s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3.
  • HY-136241
    OT-82

    NAMPT Cancer
    OT-82 is a potent, selective and orally active inhibitor of NAMPT. OT-82 is selectively toxic to cells of hematopoietic origin and induces cell death in a NAD + dependent manner. OT-82 is a promising antineoplastic agent for the study of hematological malignancies.
  • HY-123159
    AKI603

    Aurora Kinase Cancer
    AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells.
  • HY-103061
    Dehydro-ZINC39395747

    Others Cardiovascular Disease
    Dehydro-ZINC39395747 is a derivative of ZINC39395747. ZINC39395747 is a potent cytochrome b5 reductase 3 (CYB5R3) inhibitor with an IC50 of 9.14 μM and a Kd of 1.11 μM. ZINC39395747 can increase NO bioavailability in vascular cells.
  • HY-135773
    CRTh2 antagonist 3

    Prostaglandin Receptor PDK-1 Inflammation/Immunology Cardiovascular Disease
    CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist. CRTh2 antagonist 3 enhances the activity of PDK1 toward a short peptide substrate, with an EC50 of 2 μM and a Kd of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation.
  • HY-100218A
    RSL3

    (1S,3R)-RSL3

    Glutathione Peroxidase Ferroptosis Cancer
    RSL3 ((1S,3R)-RSL3) is an inhibitor of glutathione peroxidase 4 (GPX4) (ferroptosis activator), reduces the expression of GPX4 protein, and induces ferroptotic death of head and neck cancer cell. RSL3 increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells.
  • HY-N7053
    Tubulysin M

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin M is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin M is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • HY-N7051
    Tubulysin H

    Microtubule/Tubulin<