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Pathways Recommended: Apoptosis
Targets Recommended: Apoptosis SNIPER

Results for "Apoptosis Modulators" in MCE Product Catalog:

1115

Inhibitors & Agonists

17

Screening Libraries

47

Peptides

1

Inhibitory Antibodies

351

Natural
Products

3

Recombinant Proteins

Cat. No. Product Name Target Research Areas
  • HY-15098
    Apoptozole

    Apoptosis Activator VII

    HSP Apoptosis Cancer
    Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with Kds of 0.21 and 0.14 μM, respectively, and can induce apoptosis.
  • HY-50900
    gamma-Secretase Modulators

    Amyloid-β production inhibitor; γ-Secretase Modulators

    Amyloid-β Neurological Disease
    gamma-Secretase Modulators (Amyloid-β production inhibitor) is a Amyloid-β production inhibitor. gamma-Secretase Modulators is useful for Alzheimer's disease.
  • HY-13757A
    Tamoxifen

    ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen (ICI 47699) is a selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen activates autophagy and induces apoptosis.
  • HY-13757
    Tamoxifen Citrate

    ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen Citrate (ICI 46474) is a selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate activates autophagy and induces apoptosis.
  • HY-133021
    Arazine

    N-Acetyl-S-farnesyl-L-cysteine

    Others Inflammation/Immunology
    Arazine (N-Acetyl-S-farnesyl-L-cysteine) is a cell-permeable modulator of G protein and G-protein coupled receptor signaling. Arazine can be a a substrate for isoprenylcysteine methyltransferase by competing with prenylated G protein or its receptors site.
  • 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-117959
    TAK-615

    LPL Receptor Inflammation/Immunology
    TAK-615 is a negative allosteric modulator (NAM) of the LPA1 receptor for the research of pulmonary fibrosis. TAK-615 binds the LPA1 receptor with high affinity (Kd high affinity of 1.7 nM and Kd low affinity of 14.5 nM).
  • HY-114348
    N,N'-Diacetyl-L-cystine

    DiNAC; (Ac-Cys-OH)2

    Others Cardiovascular Disease
    N,N'-diacetyl-L-cystine (DiNAC) is the disulphide dimer of N-acetylcysteine with immunomodulating properties. N,N'-diacetyl-L-cystine is a potent, orally active modulator of contact sensitivity/delayed type hypersensitivity reactions in rodents. N,N'-diacetyl-L-cystine also has antiatherosclerotic effects in Watanabe-heritable hyperlipidemic rabbit (WHHL) rabbits.
  • HY-19630
    ML289

    VU0463597

    mGluR Neurological Disease
    ML289 (VU0463597) is a potent, selective, and CNS-penetrant mGlu3 (IC50=0.66 μM) negative allosteric modulator. ML289 displays >15-fold selectivity over mGlu2 and is inactive against mGlu5.
  • HY-17609
    Difelikefalin

    CR-845; FE-202845

    Opioid Receptor Neurological Disease
    Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease.
  • 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-114372
    Lycopodine

    Lipoxygenase Caspase Apoptosis Cancer
    Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity. Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation.
  • HY-P1562
    PUMA BH3

    Bcl-2 Family Cancer
    PUMA BH3 is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
  • HY-124600
    NVR 3-778

    HBV Infection
    NVR 3-778 is a first-in-Class and oral bioavailable HBV CAM (capsid assembly modulator) belonging to the SBA (sulfamoylbenzamide) class, with anti-HBV activity.
  • HY-N6998
    Paederosidic acid

    Apoptosis Cancer
    Paederosidic acid is isolated from P. scandens with anticancer and anti‐inflammation activities. Paederosidic acid inhibits lung caner cells via inducing mitochondria-mediated apoptosis.
  • HY-N3415
    Kumatakenin

    Apoptosis Cancer
    Kumatakenin, a flavonoid that is isolated from cloves shows the effect of inducing apoptosis in ovarian cancer cells.
  • HY-100507
    Avadomide

    CC 122

    E1/E2/E3 Enzyme Apoptosis Cancer Inflammation/Immunology
    Avadomide (CC 122) is an orally active cereblon modulator. Avadomide modulates cereblon E3 ligase activity and induces apoptosis of diffuse large B-cell lymphoma (DLBCL) cell lines. Avadomide exhibits potent antitumor and immunomodulatory activities.
  • HY-113008A
    cis-Urocanic acid

    (Z)-Urocanic acid; cis-UCA

    5-HT Receptor Inflammation/Immunology
    cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.
  • 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-P1562A
    PUMA BH3 TFA

    Bcl-2 Family Cancer
    PUMA BH3 (TFA) is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
  • HY-116330A
    Hyperforin dicyclohexylammonium salt

    Hyperforin DCHA

    TRP Channel Calcium Channel Neurological Disease
    Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt shows antidepressant effect.
  • HY-13757AS
    Tamoxifen-​d5

    ICI 47699-​d5; (Z)-Tamoxifen-​d5; trans-Tamoxifen-​d5

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen-d5 (ICI 47699-d5) is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is a selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
  • HY-P0111
    Z-WEHD-FMK

    Caspase Cathepsin Cancer
    Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis.
  • HY-135276A
    Targaprimir-96 TFA

    MicroRNA Apoptosis Cancer
    Targaprimir-96 TFA is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 TFA selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 TFA binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 TFA directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells.
  • HY-13735A
    Quinacrine dihydrochloride

    Mepacrine dihydrochloride; SN-390 dihydrochloride

    Parasite Apoptosis Autophagy Mitophagy Cancer Infection
    Quinacrine dihydrochloride (Mepacrine dihydrochloride) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine dihydrochloride suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis.
  • HY-13735B
    Quinacrine hydrochloride hydrate

    Mepacrine hydrochloride hydrate; SN-390 hydrochloride hydrate

    Parasite Apoptosis Autophagy Mitophagy Cancer Infection
    Quinacrine hydrochloride hydrate (Mepacrine hydrochloride hydrate) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine hydrochloride hydrate suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis.
  • 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-N3308
    Medicarpin

    Apoptosis Cancer
    Medicarpin is a flavonoid isolated from Medicago sativa. Medicarpin induces apoptosis and overcome multidrug resistance in leukemia P388 cells by modulating P-gp-mediated efflux of drugs.
  • 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-12214A
    NVP-2

    CDK Apoptosis Cancer
    NVP-2 is a potent and selective ATP-competitive cyclin dependent kinase 9 (CDK9) probe, inhibits CDK9/CycT activity with an IC50 of 0.514 nM. NVP-2 displays inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases with IC50 values of 0.584 µM, 0.706 µM, and 0.605 µM, respectively. NVP-2 induces cell apoptosis.
  • HY-114245
    Se-Methylselenocysteine

    Methylselenocysteine; Se-Methylseleno-L-cysteine

    Apoptosis Cancer
    Se-Methylselenocysteine, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity. Se-Methylselenocysteine is orally bioavailable, and induces apoptosis.
  • HY-116896
    LY117018

    Estrogen Receptor/ERR Cancer
    LY117018, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 exerts antiproliferative effects on breast cancer cell lines.
  • HY-111052
    AZD7325

    GABA Receptor Cytochrome P450 Inflammation/Immunology Neurological Disease
    AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD7325 has the potential for the investigation of anxiety and dravet syndrome. PAM: positive allosteric modulator.
  • 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-14166
    MK-886

    L 663536

    FLAP Leukotriene Receptor PPAR Apoptosis Cancer
    MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis.
  • 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-N7000
    Perillyl alcohol

    Apoptosis Endogenous Metabolite Cancer
    Perillyl alcohol is a monoterpene isolated from the essential oils of lavendin, peppermint, spearmint, cherries, celery seeds, and several other plants. Perillyl alcohol is active in inducing apoptosis in tumor cells without affecting normal cells.
  • 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-123054
    BTSA1

    Bcl-2 Family Apoptosis Cancer
    BTSA1 is a potent, high affinity and orally active BAX activator with an IC50 of 250 nM and an EC50 of 144 nM. BTSA1 binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis.
  • 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-19696A
    Tauroursodeoxycholate Sodium

    Sodium tauroursodeoxycholate; Tauroursodeoxycholic acid sodium salt

    ERK Caspase Cancer
    Tauroursodeoxycholate Sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
  • HY-N7063
    Nerol

    Reactive Oxygen Species Fungal Mitochondrial Metabolism Apoptosis Endogenous Metabolite Infection
    Nerol is a constituent of neroli oil. Nerol Nerol triggers mitochondrial dysfunction and induces apoptosis via elevation of Ca 2+ and ROS. Antifungal activity.
  • HY-N2387
    Pinosylvin

    Bacterial Apoptosis Autophagy Cancer Infection
    Pinosylvin is a pre-infectious stilbenoid toxin isolated from the heartwood of Pinus spp, has anti-bacterial activities. Pinosylvin is a resveratrol analogue, can induce cell apoptosis and autophapy in leukemia cells.
  • HY-N1231
    Sophoraflavanone G

    Kushenol F

    Apoptosis Cancer
    Sophoraflavanone G (Kushenol F) is iaolated from Sophora flavescens and shows anti-tumor and anti-inflammatory properties.  Sophoraflavanone G (Kushenol F) induces MDA-MB-231 and HL-60 cells apoptosis through suppression of MAPK-related pathways.
  • HY-N0211
    Cyasterone

    EGFR Cancer
    Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors.
  • 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-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-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-120184
    VU0467485

    AZ13713945

    mAChR Neurological Disease
    VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity.
  • 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-13945
    NVP 231

    Apoptosis Cancer
    NVP 231 is a potent, specific, and reversible ceramide kinase (CerK) inhibitor(IC50=12 nM) that competitively inhibits binding of ceramide to CerK. NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage.
  • HY-19696
    Tauroursodeoxycholate

    TUDCA; UR 906; Taurolite

    ERK Caspase Endogenous Metabolite Cancer
    Tauroursodeoxycholate (TUDCA; UR 906; Taurolite) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
  • 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-133557
    XZ739

    PROTAC Bcl-2 Family Apoptosis Cancer
    XZ739, a CRBN-dependent PROTAC BCL-XL degrader with a DC50 value of 2.5 nM in MOLT-4 cells after 16 h treatment. XZ739 also induces cell death through caspase-mediated apoptosis.
  • HY-121149
    Droloxifene

    3-Hydroxytamoxifen

    Estrogen Receptor/ERR Cancer
    Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats .
  • 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-135671
    AhR modulator-1

    Aryl Hydrocarbon Receptor VEGFR Estrogen Receptor/ERR Cancer Endocrinology
    AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus.
  • 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-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-N6694
    4-​Bromo A23187

    Calcium Channel Bacterial Apoptosis Antibiotic Cancer Infection
    4-Bromo A23187 is a halogenated analog of the highly selective calcium ionophore A-23187. 4-Bromo A23187,a calcium modulator, induces apoptosis in different cells, including HL-60 cells.
  • HY-135748
    Polyinosinic-polycytidylic acid sodium

    Poly(I:C) sodium

    Toll-like Receptor (TLR) Apoptosis Cancer Inflammation/Immunology
    Polyinosinic-polycytidylic acid sodium (Poly(I:C) sodium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis.
  • HY-10018
    Toll-like receptor modulator

    Toll-like Receptor (TLR) Inflammation/Immunology
    Toll-like receptor modulator is a modulator of TLR7/8, which modulates immune function.
  • HY-19322
    PIM447

    LGH447

    Pim Apoptosis Cancer
    PIM447 (LGH447) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis.
  • HY-123979
    ζ-Stat

    NSC37044

    PKC Cancer
    ζ-Stat is a specific and atypical PKC-ζ inhibitor of, with an IC50 of 5 μM. ζ-Stat can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro.
  • HY-N0781
    Linderalactone

    Apoptosis Cancer
    Linderalactone is an important sesquiterpene lactone isolated from Radix linderae. Linderalactone inhibits cancer growth by modulating the expression of apoptosis-related proteins and inhibition of JAK/STAT signalling pathway. Linderalactone also inhibits the proliferation of the lung cancer A-549 cells with an IC50 of 15 µM.
  • HY-N0291
    (±)-Norcantharidin

    (±)-NCTD

    Apoptosis Cancer Inflammation/Immunology
    (±)-Norcantharidin ((±)-NCTD) is a compound possessing anti-angiogenetic activity with potential use in anti-cancertherapy. (±)-Norcantharidin could prevent tumorigenesis by inhibiting cell proliferation, inducing apoptosis and the cell cycle arrest, and anti-angiogenic effects.
  • HY-19696B
    Tauroursodeoxycholate dihydrate

    TUDCA dihydrate; UR 906 dihydrate; Taurolite dihydrate

    ERK Caspase Cancer
    Tauroursodeoxycholate dihydrate (TUDCA dihydrate; UR 906 dihydrate; Taurolite dihydrate) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
  • HY-117235
    Diallyl Trisulfide

    Reactive Oxygen Species Fungal Apoptosis Cancer Infection
    Diallyl Trisulfide is isolated from Garlic. Diallyl Trisulfide suppresses the growth of Penicillium expansum (MFC99 value: ≤ 90 μg/mL) and promotes apoptosis via production of reactive oxygen species (ROS) and disintegration of cellular ultrastructure. Anticancer effect.
  • HY-15618
    MK-7622

    M1 receptor modulator

    mAChR Neurological Disease
    MK-7622 (M1 receptor modulator) is a muscarinic M1 receptor positive allosteric modulator.
  • 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-136341
    7,8-Dihydroneopterin

    Apoptosis NO Synthase Endogenous Metabolite Inflammation/Immunology Neurological Disease
    7,8-Dihydroneopterin, an inflammation marker, induces cellular apoptosis in astrocytes and neurons via enhancement of nitric oxide synthase (iNOS) expression. 7,8-Dihydroneopterin can be used in the research of neurodegenerative diseases.
  • HY-108547
    Alexidine dihydrochloride

    Fungal Apoptosis Infection
    Alexidine dihydrochloride is an anticancer agent that targets a mitochondrial tyrosine phosphatase, PTPMT1, in mammalian cells and causes mitochondrial apoptosis. Alexidine dihydrochloride has antifungal and antibiofilm activity against a diverse range of fungal pathogens.
  • 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-135899
    SIRT7 inhibitor 97491

    Sirtuin Apoptosis Cancer
    SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway..
  • HY-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-50889
    gamma-secretase modulator 3

    γ-secretase Neurological Disease
    gamma-secretase modulator 3 is a gamma-secretase modulator.
  • HY-13629
    Etoposide

    VP-16; VP-16-213

    Topoisomerase Autophagy Mitophagy Bacterial Apoptosis Antibiotic Cancer Infection
    Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy.
  • HY-N7273
    Soyasaponin III

    Apoptosis Cancer
    Soyasaponin III, a monodesmodic oleanane triterpenoid, is one of the main potentially bioactive saponins found in soy (Glycine max) and related products. Soyasaponin III can induce apoptosis in Hep-G2 cells.
  • HY-100490
    Rilmenidine

    Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy 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 modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.
  • HY-N3085
    Phellamurin

    P-glycoprotein Apoptosis Cancer Metabolic Disease
    Phellamurin is a plant flavonone glycoside from the leaves of Phellodendron amurense and inhibits intestinal P-glycoprotein. Phellamurin also inhibits egg laying by Papilio protenor. Phellamurin induces cells apoptosis and has anti-tumor activity.
  • 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-N2009
    3-O-Methylgallic acid

    3,4-Dihydroxy-5-methoxybenzoic acid

    Apoptosis Cancer
    3-O-Methylgallic acid (3,4-Dihydroxy-5-methoxybenzoic acid) is an anthocyanin metabolite and has potent antioxidant capacity. 3-O-methylgallic acid inhibits Caco-2 cell proliferation with an IC50 value of 24.1 μM. 3-O-methylgallic acid also induces cell apoptosis and has anti-cancer effects.
  • HY-135419
    CB2 modulator 1

    Cannabinoid Receptor Inflammation/Immunology Neurological Disease
    CB2 modulator 1 (compound 130) is a potent CB2 modulator. CB2 modulator 1 has the potential for immunedisorders, inflammation, osteoporosis, renal ischemia.
  • HY-123604A
    TH1834 dihydrochloride

    Histone Acetyltransferase Apoptosis Cancer
    TH1834 dihydrochloride is a specific Tip60 (KAT5) histone acetyltransferase inhibitor. TH1834 dihydrochloride induces apoptosis and increases DNA damage in breast cancer. TH1834 dihydrochloride does not affect the activity of related histone acetyltransferase MOF. Anticancer activity.
  • HY-N1416
    Pogostone

    Bacterial Apoptosis Autophagy Infection Inflammation/Immunology
    Pogostone is isolated from patchouli with anti-bacterial and anti-cancer activities. Pogostone inhibits both gram negative and gram positive bacteria, also show inhibitory effect on corynebacterium xerosis with a MIC value of 0.098 µg/ml . Pogostone induces cell apoptosis and autophagy.
  • HY-123604
    TH1834

    Histone Acetyltransferase Apoptosis Cancer
    TH1834 is a specific Tip60 (KAT5) histone acetyltransferase (HAT) inhibitor. TH1834 induces apoptosis and increases DNA damage in breast cancer. TH1834 does not affect the activity of related histone acetyltransferase MOF. Anticancer activity.
  • HY-50162
    GPR120 modulator 1

    GPR120 Metabolic Disease
    GPR120 modulator 1 is useful for modulating G protein-coupled receptor 120 (GPR120).
  • HY-50172
    GPR120 modulator 2

    GPR120 Metabolic Disease
    GPR120 modulator 2 is useful for modulating G protein-coupled receptor 120 (GPR120).
  • HY-N6905
    Acetylarenobufagin

    HIF/HIF Prolyl-Hydroxylase Cancer
    Acetylarenobufagin is a steroidal hypoxia inducible factor-1 (HIF-I) modulator.
  • 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-12812
    Autotaxin modulator 1

    Phosphodiesterase (PDE) Others
    Autotaxin modulator 1 is a novel Autotaxin modulator extracted from Patent WO 2014018881 A1.
  • HY-113914
    9-ING-41

    GSK-3 Apoptosis Cancer
    9-ING-41 is a potent glycogen synthase kinase-3 (GSK-3) inhibitor. 9-ING-41 induces apoptosis and cell cycle arrest at prophase by targeting centrosomes and microtubule-bound GSK-3β. 9-ING-41 has anticancer activity.
  • 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-112154
    CXCR7 modulator 2

    CXCR Cardiovascular Disease Endocrinology
    CXCR7 modulator 2 is a modulator of C-X-C Chemokine Receptor Type 7 (CXCR7), with a Ki of 13 nM.
  • HY-50754
    gamma-secretase modulator 2

    γ-secretase Neurological Disease
    gamma-secretase modulator 2 is a potent and selective γ-secretase modulator for treatment of Alzheimer's disease.
  • HY-U00135
    Calcium channel-modulator-1

    Calcium Channel Cardiovascular Disease
    Calcium channel-modulator-1 is a calcium channel modulator; blocks aortic contraction with an IC50 of 0.8 μM.
  • HY-111996
    Kv3 modulator 1

    Potassium Channel Inflammation/Immunology
    Kv3 modulator 1 is a Kv3 voltage-gated potassium channel modulator extracted from patent WO2018020263A1, Compound X. Kv3 modulator 1 has the potential for inflammatory pain treatment.
  • HY-110201
    Estrogen receptor modulator 1

    Estrogen Receptor/ERR Cancer
    Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors.
  • HY-120079
    MSN-125

    Bcl-2 Family Cancer
    MSN-125 is a potent Bax and Bak oligomerization inhibitor. MSN-125 prevents mitochondrial outer membrane permeabilization (MOMP) with an IC50 of 4 μM. MSN-125 potently inhibits Bax/Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons, protects primary neurons against glutamate excitotoxicity.
  • 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-U00420
    Opioid receptor modulator 1

    Opioid Receptor Neurological Disease
    Opioid receptor modulator 1 is a opioid receptor modulator extracted from patent WO2014072809A2, Compound RA11 in EXAMPLE 7.
  • HY-U00429
    NOT Receptor Modulator 1

    Others Neurological Disease
    NOT Receptor Modulator 1 is a nuclear receptor NOT modulator extracted from patent WO 2008034974 A1, Example 39 in table1.
  • 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-101995
    Ridaifen-B

    RID-B

    Estrogen Receptor/ERR Cannabinoid Receptor Cancer Metabolic Disease Inflammation/Immunology
    Ridaifen-B (RID-B) is a potent antagonist of estrogen receptor α (ERα) with IC50 of 52.4 nM, a tamoxifen derivative. Ridaifen-B is a high affinity, selective, inverse agonist at CB2 receptor (Ki=43.7 nM) over 17 folds CB1 receptor (Ki=732 nM). Ridaifen-B modulates G-protein (IC50=300 nM) and adenylyl cyclase activity with potency values predicted by CB2 affinity (IC50=134 nM). Ridaifen-B has anti-inflammatory, anti-cancer, and anti-osteoclastogenic effects.
  • 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-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-107987
    CXCR7 modulator 1

    CXCR Endocrinology
    CXCR7 modulator 1 (compound 25) is a potent and orally bioavailable peptoid hybrid CXCR7 modulator, with a Ki of 9 nM.
  • HY-12203
    PFK-158

    Autophagy Apoptosis Cancer
    PFK-158 is a potent and selective PFKFB3 inhibitor with an IC50 value 137 nM. PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells. PFK-158 has broad anti-tumor activity. PFK-158 can also enhance Colistin's resistance to bacteria.
  • 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-N0492
    α-Lipoic Acid

    Thioctic acid; (±)-α-Lipoic acid; DL-α-Lipoic acid

    NF-κB HIV Mitochondrial Metabolism Endogenous Metabolite Apoptosis Cancer Infection Inflammation/Immunology
    α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells.
  • 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-124906
    JAMI1001A

    iGluR Neurological Disease
    JAMI1001A is a positive allosteric modulator of AMPA receptor. JAMI1001A efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms.
  • 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-13630
    Etoposide phosphate

    BMY-40481

    Topoisomerase Bacterial Autophagy Apoptosis Cancer Infection Neurological Disease
    Etoposide phosphate (BMY-40481) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate is the phosphate ester prodrug of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate induces cell cycle arrest, apoptosis, and autophagy.
  • 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-128153
    Thienopyridone

    Phosphatase Apoptosis Cancer
    Thienopyridone is a potent and selective phosphatase of regenerating liver (PRL) phosphatase inhibitor with IC50s of 173 nM, 277 nM and 128 nM for PRL-1, PRL-2, and PRL-3, respectively. Thienopyridone shows minimal effects on other phosphatases. Thienopyridone induces p130Cas cleavage and apoptosis and has anticancer effects.
  • HY-13724B
    Pipendoxifene hydrochloride

    Estrogen Receptor/ERR Cancer
    Pipendoxifene hydrochloride is a selective estrogen receptor modulators (SERMs).
  • HY-108584
    Flindokalner

    BMS-204352

    Potassium Channel Neurological Disease
    Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.
  • HY-105272A
    Loreclezole hydrochloride

    R 72063 hydrochloride

    GABA Receptor Neurological Disease
    Loreclezole hydrochloride, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
  • HY-105272
    Loreclezole

    R 72063

    GABA Receptor Neurological Disease
    Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
  • HY-112912
    P-gp modulator 1

    P-glycoprotein Cancer
    P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR).
  • HY-112699
    AMPA receptor modulator-1

    iGluR Neurological Disease
    AMPA receptor modulator-1 is a potent, orally active and selective AMPAR regulatory protein TARP γ-8 negative modulator with a pIC50 of 9.7, more selective over GluA1/γ-2 (pIC50=5).
  • HY-108937
    NSC 15364

    VDAC Apoptosis Neurological Disease Cardiovascular Disease
    NSC 15364 is an inhibitor of VDAC1 oligomerization and apoptosis.
  • HY-P1075
    CALP3

    Calcium Channel Cancer Neurological Disease
    CALP3, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.
  • HY-100430
    CCF642

    Others Cancer
    CCF642 is a potent protein disulfide isomerases (PDI) inhibitor with an IC50 of 2.9 μM. CCF642 causes acute endoplasmic reticulum (ER) stress in multiple myeloma cells accompanied by apoptosis-inducing calcium release. CCF642 has broad anti-multiple myeloma activity.
  • HY-119257
    ABT-100

    Farnesyl Transferase Cancer
    ABT-100 is a potent, highly selective and orally active farnesyltransferase inhibitor. ABT-100 inhibits cell proliferation (IC50s of 2.2 nM, 3.8 nM, 5.9 nM, 6.9 nM, 9.2 nM, 70 nM and 818 nM for EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells, respectively), increases apoptosis and decreases angiogenesis. ABT-100 possesses broad-spectrum antitumor activity.
  • HY-13630A
    Etoposide phosphate disodium

    BMY-40481 disodium

    Topoisomerase Autophagy Apoptosis Cancer Neurological Disease
    Etoposide phosphate disodium (BMY-40481 disodium) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate disodium is the phosphate ester prodrug of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate disodium induces cell cycle arrest, apoptosis, and autophagy.
  • 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-N0126
    Xanthone

    Bacterial Influenza Virus Fungal Apoptosis Cancer Infection Inflammation/Immunology
    Xanthone is isolated from Mangosteen and is known to control cell division and growth, apoptosis, inflammation, and metastasis in different stages of carcinogenesis. Xanthone has anti-oxidant, anti-tumor, anti-allergic, anti-inflammatory, anti-bacterial, anti-fungal, and anti-viral activities.
  • HY-108714
    NGP555

    γ-secretase Neurological Disease
    NGP555 is a γ-secretase modulator.
  • HY-N0292
    Oleuropein

    PPAR Apoptosis Aromatase Cancer Inflammation/Immunology Cardiovascular Disease
    Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity. Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase.
  • HY-123587
    PR-924

    Proteasome Apoptosis Cancer
    PR-924 is a selective tripeptide epoxyketone immunoproteasome subunit LMP-7 inhibitor with an IC50 of 22 nM. PR-924 covalently modifies proteasomal N-terminal threonine active sites. PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities.
  • 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-16350
    NKP-1339

    IT-139; KP-1339

    DNA/RNA Synthesis Apoptosis Cancer
    NKP-1339 (IT-139; KP-1339) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. NKP-1339 induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway. NKP-1339 has a high tumor targeting potential, strongly binds to serum proteins such as albumin and transferrin and activates in the reductive tumor milieu.
  • HY-120295
    A-192621

    Endothelin Receptor Apoptosis Endocrinology Cardiovascular Disease
    A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level.
  • HY-16734A
    Amiselimod hydrochloride

    MT-1303 hydrochloride

    LPL Receptor Cancer
    Amiselimod hydrochloride is a novel sphingosine 1-phosphate receptor-1 (S1P1) modulator, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators.
  • HY-19758A
    Sirtuin modulator 1

    Sirtuin Cancer
    Sirtuin modulator 1 is a modulator of SIRTl, a homolog of SIRT3, with EC1.5 of < 1 μM, extracted from patent WO 2010071853 A1, Compound No.4.
  • HY-W011391
    GPNA hydrochloride

    Apoptosis Cancer
    GPNA hydrochloride is a well known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride is a specific glutamine (Gln) transporter ASCT2 inhibitor. GPNA hydrochloride also inhibit Na +-dependent carriers, such as SNAT family (SNAT1/2/4/5), and the Na +-independent leucine transporters LAT1/2. GPNA reversibly induces apoptosis in A549 cells.
  • HY-103668A
    SSD114 hydrochloride

    GABA Receptor Neurological Disease
    SSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator.
  • HY-16950
    4-Hydroxytamoxifen

    (Z)-4-Hydroxytamoxifen; trans-4-Hydroxytamoxifen

    Estrogen Receptor/ERR Cancer
    4-Hydroxytamoxifen is a selective estrogen receptor modulator (SERM).
  • HY-B0463
    Clomiphene citrate

    Clomifene citrate

    Estrogen Receptor/ERR Endocrinology
    Clomiphene citrate (Clomifene citrate) is a selective estrogen receptor modulator.
  • HY-101216
    Org-26576

    iGluR Neurological Disease
    Org-26576 is a AMPA receptor positive allosteric modulator.
  • HY-16423
    Rapacuronium bromide

    Org 9487

    mAChR Neurological Disease
    Rapacuronium bromide is an allosteric modulator of muscarinic acetylcholine receptor (mAChR).
  • HY-14612
    CPPHA

    mGluR Neurological Disease
    CPPHA is a selective positive allosteric modulator of mGluR5 receptor.
  • HY-112819
    Insulin levels modulator

    Insulin Receptor Metabolic Disease Endocrinology
    Insulin levels modulator could be used to treat diabetes.
  • HY-124745
    KY-05009

    MAP4K Wnt Apoptosis Cancer
    KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity.
  • HY-B1221
    Flufenamic acid

    COX AMPK Potassium Channel Chloride Channel Calcium Channel Parasite Inflammation/Immunology
    Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels.
  • HY-111763
    GPR40/FFAR1 modulator 1

    GPR40 Metabolic Disease
    GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1).
  • 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-N2587
    Irigenin

    Integrin Cancer
    Irigenin is a is a lead compound, and mediates its anti-metastatic effect by specifically and selectively blocking α9β1 and α4β1 integrins binding sites on C-C loop of Extra Domain A (EDA). Irigenin shows anti-cancer properties. It sensitizes TRAIL-induced apoptosis via enhancing pro-apoptotic molecules in gastric cancer cells.
  • HY-121618
    α-Thujone

    GABA Receptor Reactive Oxygen Species Parasite Apoptosis Autophagy Cancer Infection Neurological Disease
    α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and easily penetrates the blood-brain barrier.
  • HY-P1075A
    CALP3 TFA

    Calcium Channel Cancer Neurological Disease
    CALP3 TFA, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 TFA can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 TFA has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.
  • HY-130800
    Cereblon modulator 1

    Ligand for E3 Ligase Apoptosis Cancer Inflammation/Immunology
    Cereblon modulator 1 (compound F) is a cereblon (CRBN) E3 ligase modulator. Cereblon modulator 1 specifically binds to CRBN, thereby affecting the activity of the ubiquitin E3 ligase complex. This leads to the ubiquitination of certain substrate proteins and induces the proteasome-mediated degradation of certain transcription factors, including Ikaros (IKZF1) and Aiolos (IKZF3).
  • 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-114314
    BA-53038B

    HBV Infection
    BA-53038B is a HBV core protein allosteric modulator (CpAM), binding to the HAP pocket and modulating HBV capsid assembly in a distinct manner, with an EC50 value of 3.32 μM.
  • HY-15469
    GW791343 dihydrochloride

    P2X Receptor Neurological Disease
    GW791343 dihydrochloride is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2).
  • HY-128581
    γ-Secretase modulator 4

    γ-secretase Neurological Disease
    γ-Secretase modulator 4 is a potent γ-secretase modulator, reduces the Aβ42 level with IC50s of 0.014 μM and 0.017 μM in human and mouse, respectively.
  • 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.
  • 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.
  • HY-N6253
    Pinoresinol

    (+)-Pinoresinol

    Apoptosis Cancer
    Pinoresinol is a lignol of plant origin serving for defense in a caterpillar. Pinoresinol drastically sensitizes cancer cells against TNF-related apoptosis-inducing ligand (TRAIL) -induced apoptosis.
  • HY-111386
    E-7386

    Epigenetic Reader Domain Cancer
    E-7386 is an orally active CBP/beta-catenin modulator.
  • HY-19487
    Ribocil

    Bacterial Infection
    Ribocil is a highly selective chemical modulator of bacterial riboflavin riboswitches.
  • HY-16716
    Basmisanil

    RG1662; RO5186582

    GABA Receptor Neurological Disease
    Basmisanil is a highly selective GABAAα5 negative allosteric modulator.
  • HY-A0038
    Lasofoxifene Tartrate

    CP-336156

    Estrogen Receptor/ERR Endocrinology
    Lasofoxifene Tartrate is a non-steroidal selective estrogen receptor modulator (SERM).
  • HY-114530
    LY2452473

    Androgen Receptor Cancer Metabolic Disease
    LY2452473 is an orally bioavailable, selective androgen receptor modulator (SARM).
  • HY-13236
    LUF6000

    Adenosine Receptor Cardiovascular Disease
    LUF6000 is an allosteric modulator of the human A3 adenosine receptor (AR).
  • HY-100403
    Ro 67-7476

    mGluR Cancer
    Ro 67-7476 is a positive allosteric modulator of mGlu1 receptors.
  • HY-101858
    BQCA

    mAChR Neurological Disease
    BQCA a highly selective allosteric modulator of the M1 mAChR.
  • HY-117291A
    XMD-17-51 Trifluoroacetate

    Others Others
    XMD-17-51 Trifluoroacetate is a pyrimido-diazepinone compound that is able to modulate protein kinases.
  • HY-100186
    GSK-2881078

    Androgen Receptor Neurological Disease
    GSK 2881078 is a selective androgen receptor modulator potentially for the treatment of cachexia.
  • HY-18705
    Azoramide

    Apoptosis Endocrinology
    Azoramide is a small-molecule modulator of the unfolded protein response with antidiabetic activity.
  • HY-101845
    FITM

    mGluR Cancer
    FITM is a negative allosteric modulator of mGlu1 receptor with a Ki of 2.5 nM.
  • HY-109565
    ASTX660

    IAP Cancer
    ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
  • HY-128831
    Kv3 modulator 4

    Potassium Channel Inflammation/Immunology
    Kv3 modulator 4 is a Kv3.1 (pEC50=5.45) and Kv3.2 modulator extracted from patent WO2018020263A1, Cyclobutyl structure.
  • 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-16563
    Narciclasine

    Lycoricidinol

    ROCK Cancer
    Narciclasine is a plant growth modulator. Narciclasine modulates the Rho/Rho kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity as well as inducing actin stress fiber formation in a RhoA-dependent manner.
  • HY-15470
    GW791343 trihydrochloride

    P2X Receptor Neurological Disease
    GW791343 3Hcl is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2).
  • HY-128829
    Kv3 modulator 2

    Potassium Channel Inflammation/Immunology
    Kv3 modulator 2 (formula (I)) is a potent Kv3 channels modulator extracted from patent WO2018109484A1, compound formula (I) , has analgesic activity and is used in the prophylaxis or treatment of related disorders.
  • HY-N2184
    Furanodienone

    Apoptosis Cancer
    Furanodienone is one of the major bioactive constituents derived from Rhizoma Curcumae. Furanodienone induced apoptosis.
  • HY-N3032
    Xanthatin

    Apoptosis VEGFR Lipoxygenase Bacterial Cancer Infection Inflammation/Immunology
    Xanthatin is isolated from Xanthium strumarium leaves. Xanthatin exhibits strong antitumor activities against a variety of cancer cells through apoptosis persuasion and shows anti-inflammatory activities by inhibiting PGE2 synthesis and 5-lipoxygenase activity. Xanthatin is a potent and orally active inhibitor of VEGFR2 kinase activity with an IC50 of 3.8 μM and prominently blocks the phosphorylation of VEGFR2 at Tyr951 site. Xanthatin inhibits angiogenesis and has the potential for the investigation of breast cancer.
  • HY-110346
    AZD5582 dihydrochloride

    IAP Apoptosis Cancer
    AZD5582 dihydrochloride is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.
  • HY-12600
    AZD5582

    IAP Apoptosis Cancer
    AZD5582 is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.
  • HY-130680
    Syk-IN-3

    Syk Cancer
    Syk-IN-3, a potent spleen tyrosine kinase (Syk) inhibitor, extracted from patent WO2011075515A1, compound example 152, has an IC50 of 1 nM.
  • HY-106182
    TBC3711

    Endothelin Receptor Endocrinology
    TBC3711 is a endothelin receptor modulator, used for the research of endothelin-mediated disorders.
  • HY-12505
    CX546

    iGluR Autophagy Neurological Disease
    CX546 is a selective positive AMPAR modulator; the prototypical ampakine agent.
  • HY-N0273
    Brassinolide

    Brassin lactone

    Apoptosis Cancer
    Brassinolide is a predominant plant growth modulator that regulate plant cell elongation.
  • HY-N2371
    27-Hydroxycholesterol

    Estrogen Receptor/ERR LXR Endogenous Metabolite Cancer
    27-Hydroxycholesterol is a selective estrogen receptor modulator and an agonist of the liver X receptor.
  • HY-112788
    ONO-8590580

    GABA Receptor Neurological Disease
    ONO-8590580 is a GABAA α5 negative allosteric modulator.
  • 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-N6784
    Oligomycin B

    ATP Synthase Bacterial Apoptosis Neurological Disease
    Oligomycin B is an antibiotic isolated from marine Streptomyces, used as an eukaryotic ATP synthase inhibitor, induces apoptosis.
  • HY-N0428
    Obacunone

    Apoptosis Cancer
    Obacunone, isolated from seeds of Marsh White grapefruit, exhibits anti-tumor activity by the induction of apoptosis.
  • HY-122760
    Bax activator-1

    Bcl-2 Family Apoptosis Cancer
    Bax activator-1 (compound 106) is a Bax activator that induces Bax-dependent tumor cell apoptosis.
  • HY-103661
    BI-6C9

    Mitochondrial Metabolism 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-15598
    20-HETE

    20-hydroxy Arachidonic Acid

    Potassium Channel NF-κB NO Synthase Reactive Oxygen Species NADPH Oxidase Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease
    20-HETE (20-hydroxy Arachidonic Acid) is a CYP450 metabolite and a potent vasoconstrictor. 20-HETE is an endogenous inhibitor of the large-conductance Ca 2+-activated K + channel in renal arterioles. 20-HETE constricts smooth muscles, stimulates smooth muscle proliferation and migration. 20-HETE increases NADPH oxidase, ROS, and NF-κB activity. 20-HETE also inhibits endothelial NO synthase and inhibits apoptosis of pulmonary artery smooth muscle cells.
  • HY-113952
    Actinonin

    (-)-Actinonin

    Aminopeptidase Bacterial MMP Apoptosis Antibiotic Cancer Infection
    Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities.
  • 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-14383
    RAD140

    Androgen Receptor Endocrinology Cancer
    RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM).
  • HY-111453
    AZD7594

    AZ13189620

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    AZD7594 is a potent selective nonsteroidal glucocorticoid receptor modulator, with an IC50 of 0.9 nM.
  • HY-101488
    CC-885

    Ligand for E3 Ligase Cancer
    CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity.
  • HY-U00178
    Idoxifene

    CB7432

    Estrogen Receptor/ERR Cancer
    Idoxifene (CB7432) is a novel tissue-specific selective estrogen receptor modulator (SERM).
  • HY-B1405
    Dehydroisoandrosterone 3-acetate

    Dehydroepiandrosterone 3-acetate; DHEA acetate

    Androgen Receptor Endocrinology Cancer
    Dehydroepiandrosterone 3-acetate is a testosterone/estrogen precursor and known modulator of vertebrate aggression.
  • HY-17614
    Ezutromid

    SMT C1100; BMN 195; VOX-C1100

    Others Cancer
    Ezutromid is a novel Small utrophin's translation modulator with EC50 of 0.4 uM .
  • HY-U00339
    H3 receptor-MO-1

    Histamine Receptor Endocrinology
    H3 receptor-MO-1 is a modulator of histamine H3 receptor.
  • HY-119037
    UK-101

    Proteasome Apoptosis Cancer
    UK-101 is a potent and selective immunoproteasome β1i (LMP2) inhibitor with an IC50 value of 104 nM, displays 144- and 10-fold selectivity over β1c (IC50=15 μM) and β5 subunit (IC50=1 μM), respectivey. UK-101 induces cell apoptosis and can be used for the study of prostate cancer.
  • HY-123056
    EAD1

    Autophagy Apoptosis Cancer
    EAD1 is a potent autophagy inhibitor with antiproliferative activity in lung and pancreatic cancer cells. EAD1 also induces apoptosis.
  • HY-107457
    AZD-8529

    mGluR Neurological Disease
    AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
  • HY-101093
    PD-1-IN-1

    PD-1/PD-L1 Inflammation/Immunology
    PD-1-IN-1 is an inhibitor of programmed cell dealth-1 (PD-1) extracted from patent WO2015033299A1, compound example 4. PD-1-IN-1 can be used as immune modulator.
  • HY-100550
    MSDC 0160

    Mitoglitazone; CAY10415

    Insulin Receptor Mitochondrial Metabolism Neurological Disease Endocrinology
    MSDC 0160 (Mitoglitazone) is a mitochondrial target of thiazolidinediones (mTOT)-modulating insulin sensitizer and a modulator of mitochondrial pyruvate carrier (MPC). MSDC 0160 is a thiazolidinedione (TZD) with antidiabetic and neuroprotective activities. MSDC 0160 has the potential for Alzheimer′s disease.
  • HY-P0079
    Neuromedin N

    Neuromedin N (rat, mouse, porcine, canine)

    Dopamine Receptor Neurological Disease
    Neuromedin N is a potent modulator of dopamine D2 receptor agonist binding in rat neostriatal membranes.
  • HY-N1368B
    (-)-Borneol

    L-Borneol

    GABA Receptor Neurological Disease
    (-)-Borneol has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM.
  • HY-10937
    Farampator

    CX-691; Org24448

    iGluR Neurological Disease
    Farampator (CX-691;Org24448) is an AMPA receptor positive modulator.
  • HY-109073
    Rovazolac

    LXR Inflammation/Immunology
    Rovazolac is a liver x receptor (LXR) modulator extracted from patent WO2013130892A1.
  • HY-112564
    JNJ-632

    HBV Infection
    JNJ-632 is a hepatitis B virus (HBV) capsid assembly modulator (CAM).
  • HY-15476
    VU 0364439

    mGluR Neurological Disease
    VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.
  • HY-P1010A
    Z-LEHD-FMK TFA

    Caspase Cancer Inflammation/Immunology
    Z-LEHD-FMK TFA is an irreversible caspase-9 inhibitor, protects against lethal reperfusion injury and attenuate apoptosis.
  • HY-15608
    MPTP hydrochloride

    Dopamine Receptor Apoptosis Neurological Disease Cancer
    MPTP hydrochloride is a brain penetrant dopamine neurotoxin, inducing Parkinson’s Disease. MPTP hydrochloride, a precusor of MPP +, induces apoptosis.
  • HY-136621
    5-HT1A modulator 2 hydrochloride

    5-HT Receptor Neurological Disease
    5-HT1A modulator 2 hydrochloride, a derivative of 8-OH-DPAT (HY-112061), is a modulator of 5-HT1A with a Ki of 53 nM for 5-HT1A binding.
  • HY-116624
    MAZ51

    VEGFR Apoptosis Cancer
    MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity.
  • HY-N2389
    Formosanin C

    Apoptosis Cancer
    Formosanin C is a diosgenin saponin isolated from Paris formosana Hayata and an immunomodulator with antitumor activity. Formosanin C induces apoptosis.
  • HY-N0580
    Fraxetin

    Apoptosis
    Fraxetin is isolated from Cortex Fraxini. Fraxetin has antitumor, anti-oxidation effects and anti-inflammory effects. Fraxetin induces apoptosis.
  • HY-128777
    WEHI-9625

    VDAC Cancer
    WEHI-9625 is a tricyclic sulfone small molecule inhibitor of apoptosis with an EC50 of 69 nM. WEHI-9625 binds to VDAC2 and promotes its ability to inhibit apoptosis driven by mouse BAK, but is completely inactive against both human BAK and the closely related apoptosis effector BAX.
  • HY-107457A
    AZD-8529 mesylate

    mGluR Neurological Disease
    AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
  • HY-18102A
    GLPG0492 R enantiomer

    Androgen Receptor Neurological Disease
    GLPG0492 R enantiomer is the R enantiomer of GLPG-0492, which is a novel selective androgen receptor modulator.
  • HY-19559
    JNJ-46778212

    VU 0409551

    mGluR Neurological Disease
    JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC50 of 260 nM.
  • HY-13262
    Lumacaftor

    VX-809; VRT 826809

    CFTR Autophagy Inflammation/Immunology
    Lumacaftor (VX-809; VRT 826809) is a CFTR modulator that corrects the folding and trafficking of CFTR protein.
  • HY-107651
    VU 0365114

    mAChR Others
    VU 0365114 is a mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM.
  • HY-U00282
    Chymase-IN-2

    Others Inflammation/Immunology
    Chymase-IN-2 is a chymase modulator which is useful in the treatment of inflammatory and serine protease mediated disorders.
  • 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-11027
    MK-0773

    PF-05314882

    Androgen Receptor Endocrinology
    MK-0773 is a selective androgen receptor modulators (SARMs) that binds to AR with an IC50 of 6.6 nM.
  • HY-10932
    Aniracetam

    Ro 13-5057

    nAChR iGluR Neurological Disease
    Aniracetam(Ro 13-5057) is a nootropics and neuroprotective drug, which is selectively modulates the AMPA receptor and nAChR.
  • HY-114775
    RCGD423

    Interleukin Related Inflammation/Immunology Neurological Disease
    RCGD423 is a gp130 modulator, which prevents articular cartilage degeneration and promotes repair.
  • HY-12023
    Andarine

    GTx-007; S-4

    Androgen Receptor Cancer
    Andarine (S-4) is an investigational selective androgen receptor modulator (SARM) and an active partial agonist.
  • HY-N6721
    T-​2 Tetraol

    Others Infection
    T-​2 Tetraol is a metabolite of T-2 toxin, and also a trichothecene mycotoxin, with less toxicity and is unable to induce apoptosis.
  • HY-128830
    Kv3 modulator 3

    Potassium Channel Inflammation/Immunology
    Kv3 modulator 3 (Compound 4) is a selective modulator of Kv3.1 and/or Kv3.2 and/or Kv3.3 channels extracted from patent WO2017098254A1, compound 4, has analgesic activity for use in the prophylaxis o or treatment of pain.
  • HY-136650
    Fludarabine triphosphate

    F-ara-ATP

    Nucleoside Antimetabolite/Analog Drug Metabolite DNA/RNA Synthesis Apoptosis Cancer
    Fludarabine triphosphate (F-ara-ATP), the cytotoxic metabolite of Fludarabine phosphate (HY-B0028), inhibits ribonucleotide reductase and DNA polymerase and ultimately leads to cellular apoptosis.
  • 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-A0031
    Bazedoxifene

    TSE-424

    Estrogen Receptor/ERR Cancer
    Bazedoxifene (TSE-424) is a selective estrogen receptor modulator (SERM) currently in development for osteoporosis prevention and treatment.
  • HY-13058B
    (R)-ADX-47273

    mGluR Neurological Disease
    (R)-ADX-47273 is a potent mGluR5 positive allosteric modulator, with an EC50 of 168 nM for potentiation .
  • HY-101291
    Iberdomide

    CC-220

    Ligand for E3 Ligase Apoptosis Inflammation/Immunology Cancer
    Iberdomide (CC-220) is a cereblon (CRBN) modulator with an IC50 value of 60 nM.
  • HY-15255
    Zosuquidar

    LY335979

    P-glycoprotein Cancer
    Zosuquidar (LY335979) is a potent negative modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM.
  • HY-109037
    Mavacamten

    MYK461; SAR439152

    Myosin Cardiovascular Disease
    Mavacamten is a modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
  • HY-18162
    JNJ-42153605

    mGluR Neurological Disease
    JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with an EC50 of 17 nM.
  • HY-19720
    Emixustat

    ACU-4429

    Others Metabolic Disease
    Emixustat, a novel visual cycle modulator, is an inhibitor of the visual cycle isomerase with an IC50 value of 4.4 nM in vitro.
  • HY-16998
    SR2211

    ROR Inflammation/Immunology
    SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM.
  • HY-N5014
    Liensinine perchlorate

    Apoptosis Cancer Inflammation/Immunology
    Liensinine Perchlorate is a constituent of Nelumbo nucifera Gaertn, with ani-hypertension and anti-cancer activities. Liensinine Perchlorate induces colorectal cancer (CRC) cell apoptosis.
  • 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-B0691A
    Ecabet sodium

    TA-2711

    Reactive Oxygen Species Bacterial Infection
    Ecabet sodium (TA-2711) is currently applied to some gastrointestinal disease by inhibiting the ROS production and improving Helicobacter pylori eradication. Ecabet sodium reduces apoptosis.
  • 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-13251
    Silvestrol

    (-)-Silvestrol

    Eukaryotic Initiation Factor (eIF) Apoptosis Autophagy Cancer
    Silvestrol is a eukaryotic translation initiation factor 4A (eIF4A) inhibitor isolated from the fruits and twigs of Aglaia foveolata. Silvestrol induces autophagy and caspase-mediated apoptosis.
  • HY-N2334A
    Glycochenodeoxycholic acid sodium salt

    Chenodeoxycholylglycine sodium salt; Sodium glycochenodeoxycholate

    Endogenous Metabolite Apoptosis Cancer
    Glycochenodeoxycholic acid sodium salt (Chenodeoxycholylglycine sodium salt) is a bile acid formed in the liver from chenodeoxycholate and glycine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. Glycochenodeoxycholic acid sodium salt (Chenodeoxycholylglycine sodium salt) induces hepatocyte apoptosis.
  • HY-N3619
    Conophylline

    Apoptosis Endocrinology Neurological Disease
    Conophylline is a vinca alkaloid extracted from leaves of a tropical plant Ervatamia microphylla. Conophylline is a differentiation inducer of for pancreatic cells. Conophylline suppresses HSC and induces apoptosis.
  • HY-N7070
    Geranyl acetate

    Apoptosis Cancer
    Geranyl acetate, an acyclic monoterpene ester derived from geraniol, is widely used in the cosmetics industry due to its pleasant scent. Geranyl acetate can induces cell apoptosis.
  • HY-N1455
    Falcarinol

    Panaxynol; Carotatoxin

    HSP Cancer
    Falcarinol (Panaxynol) is a natural, orally active Hsp90 inhibitor targeting both the N-terminal and C-terminal of Hsp90 with limited toxicities. Falcarinol (Panaxynol) induces apoptosis.
  • HY-N2334
    Glycochenodeoxycholic acid

    Chenodeoxycholylglycine

    Endogenous Metabolite Apoptosis Cancer
    Glycochenodeoxycholic acid (Chenodeoxycholylglycine) is a bile acid formed in the liver from chenodeoxycholate and glycine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. Glycochenodeoxycholic acid (Chenodeoxycholylglycine) induces hepatocyte apoptosis.
  • HY-111343
    ONC212

    Apoptosis Cancer Endocrinology
    ONC212, a fluorinated-ONC201 analogue, is a promising anti-cancer agent and also a selective agonist of GPR132. ONC212 also induces apoptosis.
  • HY-W011522
    Taurolidine

    Bacterial Apoptosis Antibiotic Cancer Infection
    Taurolidine is a broad-spectrum antimicrobial for the prevention of central venous catheter-related infections. Taurolidine has a direct and selective antineoplastic effect on brain tumor cells by the induction of apoptosis.
  • 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-B0005A
    Toremifene

    GTx 006; Z-Toremifene

    Estrogen Receptor/ERR Cancer
    Toremifene (NK 622; FC 1157a) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis.
  • HY-14774
    Monepantel

    AAD1566

    nAChR Cancer
    Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
  • HY-109046
    Tulrampator

    CX-1632

    iGluR Neurological Disease
    Tulrampator (CX-1632) is an orally bioavailable positive AMPAR (allosteric modulator of AMPA receptor). Antidepressant.
  • HY-101746
    GSK376501A

    PPAR Metabolic Disease
    GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus.
  • HY-101583
    NEO 376

    SPI-376

    5-HT Receptor GABA Receptor Dopamine Receptor Neurological Disease
    NEO 376 is a selective modulator of 5-HT1 receptor, GABA receptor and dopamine receptor, with anti-psychotic actively.
  • HY-15393
    VU 0357121

    mGluR Neurological Disease
    VU0357121 is a novel positive and highly selective allosteric modulator (PAM) of mGlu5R with EC50 of 33 nM.
  • HY-18340
    (R)​-​CR8

    CR8, (R)-Isomer

    CDK Apoptosis Cancer Neurological Disease
    (R)​-​CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)​-​CR8 inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)​-​CR8 induces apoptosis and has neuroprotective effect. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K.
  • HY-18340A
    (R)​-​CR8 trihydrochloride

    CR8, (R)-Isomer trihydrochloride

    CDK Apoptosis Cancer Neurological Disease
    (R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect. (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K.
  • HY-107661
    Arundic Acid

    ONO-2506; (R)-2-Propyloctanoic acid

    Others Neurological Disease
    Arundic acid (ONO-2506) is an astrocyte-modulating agent, which delays the expansion of cerebral infarcts by modulating the activation of astrocytes through inhibition of S-100β synthesis. Arundic acid (ONO-2506) has been developed as a therapeutic agent for stroke and Alzheimer’s disease.
  • HY-16940
    24(S)-Hydroxycholesterol

    24S-OHC; 24S-HC; Cerebrosterol

    LXR iGluR Endogenous Metabolite Metabolic Disease
    24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators.
  • HY-100558
    Bafilomycin A1

    (-)-Bafilomycin A1

    Proton Pump Bacterial Autophagy Apoptosis Antibiotic Cancer Infection
    Bafilomycin A1, a macrolide antibiotic isolated from the Streptomyces species, is a specific inhibitor of vacuolar-type H + ATPase (V-ATPase). Bafilomycin A1 inhibits autophagy and induces apoptosis.
  • HY-113953
    Z-Asp-CH2-DCB

    Caspase Inflammation/Immunology
    Z-Asp-CH2-DCB is an irreversible broad spectrum caspase inhibitor. Z-Asp-CH2-DCB also inhibits proteases with caspase-like activity. Z-D-CH2-DCB blocks the production of IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B (SEB)-stimulated peripheral blood mononuclear cells (PBMC), and reduces SEB-1-stimulated T-cell proliferation in a dose-dependent manner. Z-Asp-CH2-DCB prevents SU5416-induced septal cell apoptosis and emphysema development.
  • HY-108511A
    PB28

    Sigma Receptor Apoptosis SARS-CoV Cancer Infection
    PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity.
  • HY-16766
    Decoglurant

    RO4995819

    mGluR Neurological Disease
    Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant.
  • HY-18292
    ARN2966

    Amyloid-β Neurological Disease
    ARN2966 is a potent post-transcriptional modulator of APP expression; reduces expression of APP with resultant lower production of Aβ.
  • HY-100728
    BMT-145027

    mGluR Neurological Disease
    BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM.
  • HY-100298
    Caldaret

    MCC-135

    Na+/Ca2+ Exchanger Cardiovascular Disease
    Caldaret is an intracellular Ca 2+ handling modulator that acts through reverse mode Na +/Ca 2+ exchanger inhibition.
  • HY-17590
    Radafaxine hydrochloride

    GW-353162A; BW-306U

    Monoamine Transporter Neurological Disease
    Radafaxine hydrochloride (GW-353162A) is a DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator.
  • HY-17030
    Acamprosate calcium

    Calcium N-acetylhomotaurinate

    GABA Receptor Neurological Disease
    Acamprosate calcium(Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems; reduces alcohol consumption in animal models of alcohol addiction.
  • HY-16950B
    (E)-4-Hydroxytamoxifen

    Estrogen Receptor/ERR Cancer
    (E)-4-Hydroxytamoxifen, the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.
  • HY-B0005
    Toremifene Citrate

    FC 1157a; NK 622

    Estrogen Receptor/ERR Apoptosis Cancer
    Toremifene Citrate(NK 622; FC 1157a) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis.
  • HY-112282
    BI-1408

    γ-secretase Neurological Disease
    BI-1408 is a potent γ secretase modulator with an IC50 of 0.04 μM for 42.
  • HY-111498
    RGX-104

    LXR Cancer Inflammation/Immunology
    RGX-104 is a small-molecule LXR agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
  • HY-19872
    AZD-6280

    GABA Receptor Neurological Disease
    AZD-6280 is a selective GABAA(α2/3) receptor modulator, used for treatment of generalized anxiety disorder.
  • HY-14419
    TCN238

    mGluR Neurological Disease
    TCN238 is an orally bioavailable mGlu4 receptor positive allosteric modulator (PAM) with an EC50 of 1 μM.
  • 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-122751
    (R)-DNMDP

    Phosphodiesterase (PDE) Cancer
    (R)-DNMDP is a potent and selective cancer cell cytotoxic agent. (R)-DNMDP, the R-form of DNMDP, binds PDE3A directly. DNMDP binding to PDE3A promotes an interaction between PDE3A and Schlafen 12 (SLFN12).
  • HY-10999
    Trametinib

    GSK1120212; JTP-74057

    MEK Autophagy Apoptosis Cancer
    Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.
  • HY-N0052A
    Sanguinarine chloride

    Pseudochelerythrine chloride; Sanguinarium chloride

    Apoptosis Autophagy Bacterial Parasite Cancer
    Sanguinarine chloride, a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.
  • HY-N0052
    Sanguinarine

    Pseudochelerythrine; Sanguinarin

    Apoptosis Autophagy Cancer
    Sanguinarine, a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.
  • HY-N2303
    Eriocalyxin B

    Apoptosis Cancer Inflammation/Immunology
    Eriocalyxin B is an ent-Kaurene diterpenoid isolated from Chinese herb Isodon eriocalyx. Eriocalyxin B has anti-cancer and anti-infammatory activities. Eriocalyxin B induces cell apoptosis.
  • HY-123611
    Supinoxin

    RX-5902

    DNA/RNA Synthesis Apoptosis Cancer
    Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM.
  • HY-12040
    Elesclomol

    STA-4783

    Apoptosis Cancer
    Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis.
  • HY-N0780
    Isoalantolactone

    (+)-Isoalantolactone; Isohelenin

    Apoptosis Autophagy Bacterial Endogenous Metabolite Cancer
    Isoalantolactone is an apoptosis inducer, which also acts as an alkylating agent.
  • HY-12949
    ML204

    TRP Channel Neurological Disease
    ML204 is a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels.
  • HY-B2121
    6-Methoxy-2-naphthoic acid

    Naproxen impurity O

    iGluR Neurological Disease
    6-Methoxy-2-naphthoic acid is an NMDA receptor modulator extracted from patent WO 2012019106 A2.
  • HY-13058
    ADX-47273

    mGluR Neurological Disease
    ADX-47273 is a positive allosteric modulator selective for the metabotropic glutamate receptor subtype mGluR5(EC50=170 nM).
  • HY-16728
    Rapastinel

    GLYX-13

    iGluR Neurological Disease
    Rapastinel (GLYX-13) is an N-methyl-D-aspartate receptor (NMDAR) modulator that has characteristics of a glycine site partial agonist.
  • HY-W001692
    Ocinaplon

    DOV 273547

    GABA Receptor Neurological Disease
    Ocinaplon (DOV 273547) is a partial GABAA receptor positive allosteric modulator with relatively high efficacy at the α1 subunit.
  • HY-111536
    Mitochonic acid 5

    MA-5

    Mitochondrial Metabolism Cardiovascular Disease
    Mitochonic acid 5 binds mitochondria and ameliorates renal tubular and cardiac myocyte damage. Mitochonic acid 5 modulates mitochondrial ATP synthesis.
  • HY-125880
    SBI-553

    Neurotensin Receptor Endocrinology Neurological Disease
    SBI-553 is a potent and brain penetrant NTR1 allosteric modulator, with an EC50 of 0.34 μM.
  • HY-112426
    LAU159

    GABA Receptor Neurological Disease
    LAU159 is a functionally selective positive modulator of α1β3 GABA(A) receptor with an EC50 of 2.2 μM.
  • HY-18654
    ADX88178

    mGluR Neurological Disease
    ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4.
  • HY-119941
    VU0652835

    mGluR Neurological Disease
    VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC50 of 81 nM.
  • HY-101855
    Anle138b

    Others Neurological Disease
    Anle138b is an oligomeric aggregation inhibitor. Anle138b is an oligomer modulator for neurodegenerative diseases such Parkinson's disease.
  • HY-Y0272
    Saccharin

    Bacterial Inflammation/Immunology
    Saccharin is an orally active, non-caloric artificial sweeteners (NAS). Saccharin has bacteriostatic and microbiome-modulating properties.
  • HY-N1963
    Curzerene

    Gutathione S-transferase Cancer
    Curzerene is a sesquiterpene is isolated from the rhizome of Curculigo orchioides Gaertn with anti-cancer activity. Curzerene inhibits glutathione S-transferase A1 (GSTA1) mRNA and protein expression. Curzerene induces cell apoptosis.
  • HY-112607
    Tubulin inhibitor 1

    Microtubule/Tubulin Apoptosis Cancer
    Tubulin inhibitor 1 is a tubulin inhibitor, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis.
  • HY-N2477
    Taraxerol

    Apoptosis NF-κB Cancer Inflammation/Immunology
    Taraxerol is isolated from Abroma augusta L, and has anti-inflammtory and anti-cancer effects. Taraxerol attenuates acute inlammation through inhibition of NF-κB signaling pathway. Taraxerol induces cell apoptosis.
  • HY-16138
    CG-200745

    HDAC Autophagy Apoptosis Cancer
    CG-200745 is a potent HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. CG200745 inhibits deacetylation of histone H3 and tubulin. CG200745 induces apoptosis.
  • HY-N6882
    Genistein 8-c-glucoside

    G8CG

    Mitochondrial Metabolism Apoptosis Cancer
    Genistein 8-c-glucoside (G8CG) is a natural glucoside isolated from flowers of Lupinus luteus L. Genistein 8-c-glucoside induces mitochondrial membrane depolarization and induces apoptosis.
  • HY-12025
    Serdemetan

    JNJ-26854165

    MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    Serdemetan(JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53.
  • HY-112633
    SMN-C3

    DNA/RNA Synthesis Others
    SMN-C3 is an orally active SMN2 splicing modulator and has the potential to treat spinal muscular atrophy (SMA).
  • HY-12509
    PEPA

    iGluR Neurological Disease
    PEPA is an allosteric modulator of AMPA receptors; binds to the GluA2o and GluA3o LBDs and can be utilized as an indicator of AMPA receptor heterogeneity.
  • HY-100084
    Methyl-3β-hydroxycholenate

    ROR Inflammation/Immunology
    Methyl-3β-hydroxycholenate is a ROR gamma modulator extracted from patent US20110263046 A1, in figure 2.
  • HY-15446
    Basimglurant

    RG7090; CTEP Derivative

    mGluR Neurological Disease
    Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM.
  • HY-107456
    E6130

    Others Inflammation/Immunology Endocrinology
    E6130 is an orally active and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bowel disease.
  • HY-12152
    PNU-120596

    NSC 216666

    nAChR Neurological Disease
    PNU-120596 (NSC 216666 ) is a potent and selective positive allosteric α7 nAChR modulator with an EC50 of 0.2 μM.
  • HY-14609A
    MPEP

    mGluR Neurological Disease
    MPEP is a potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors.
  • HY-12157
    VU 0238429

    mAChR Others
    VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
  • HY-U00013
    Nitroflurbiprofen

    HCT 1206; NO-flurbiprofen; Nitroxybutyl flurbiprofen

    COX Cardiovascular Disease
    Nitroflurbiprofen is a cyclooxygenase (COX) inhibitor with nitric oxide (NO)-donating properties, modulates the increased intrahepatic vascular tone in portal hypertensive cirrhotic rats.
  • HY-B1494
    Picrotoxinin

    Chloride Channel GABA Receptor Neurological Disease
    Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors.
  • HY-13574A
    Biricodar

    VX-710

    P-glycoprotein Cancer
    Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
  • 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-N2566
    Euscaphic acid

    DNA/RNA Synthesis PI3K Apoptosis Cancer
    Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC50 values of 61 and 108 μM. Euscaphic acid induces apoptosis.
  • HY-P1687
    Siomycin A

    Bacterial Apoptosis Cancer
    Siomycin A is a thiopeptide antibiotic and is a Forkhead box M1(FOXM1) selective inhibitor without affecting other members of the Forkhead box family. Siomycin A has anti-tumor and promotes apoptosis.
  • HY-124958
    NDMC101

    NF-κB Dipeptidyl Peptidase Metabolic Disease Inflammation/Immunology
    NDMC101 is a potent osteoclastogenesis inhibitor and inhibits osteoclast differentiation via down-regulation of NFATc1-modulated gene express. NDMC101 is similar to the DPP4 substrate and is a significant inhibitor of early T-cell activation via DPP4 inhibition. NDMC101can be used for study of bone disorders, such as rheumatoid arthritis, and synovial inflammation et al.
  • HY-110339
    RKI 1447 dihydrochloride

    ROCK Apoptosis Cancer
    RKI 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC50s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively. RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis.
  • HY-100016
    AZD0156

    ATM/ATR Apoptosis Cancer
    AZD0156 is a potent, selective and orally active ATM inhibitor with an IC50 of 0.58 nM. AZD0156 inhibits the ATM-mediated signaling, prevents DNA damage checkpoint activation, disrupts DNA damage repair, and induces tumor cell apoptosis.
  • HY-13288
    Org 27569

    Cannabinoid Receptor Neurological Disease
    Org 27569 is a potent CB1 receptor allosteric modulator, which increases agonist binding, yet blocks agonist-induced CB1 signaling.
  • HY-15748
    JNJ-40411813

    ADX-71149

    mGluR Neurological Disease
    JNJ-40411813 (ADX-71149) is a novel positive allosteric modulator of the metabotropic Glutamate 2 receptor (mGlu2R) with EC50 of 147 nM.
  • HY-100366
    Lu AF21934

    mGluR Neurological Disease
    Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC50 of 500 nM for mGlu4 receptor.
  • HY-U00366
    S1PR1-MO-1

    LPL Receptor Inflammation/Immunology
    S1PR-MO-1 is the modulator of sphingosine-1-phosphate receptor, used for research of hyperproliferative, inflammatory diseases.
  • HY-15204
    Tonabersat

    SB-220453

    Gap Junction Protein Inflammation/Immunology Neurological Disease
    Tonabersat (SB-220453) is a gap-junction modulator. Tonabersat prevents inflammatory damage in the central nervous system.
  • HY-16728B
    Rapastinel Trifluoroacetate

    GLYX-13 Trifluoroacetate

    iGluR Neurological Disease
    Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with glycine-site partial agonist properties. Rapastinel Trifluoroacetate has the potential for major depressive disorder treatment.
  • HY-U00068
    PPARα-MO-1

    PPAR Metabolic Disease
    PPARα-MO-1 is a potent PPARα modulator extracted from patent WO/2004/110982A1, formula I.
  • HY-13277
    IRAK inhibitor 3

    IRAK Inflammation/Immunology
    IRAK inhibitor 3 is an interleukin-1 (IL-I) receptor-associated kinase (IRAK) kinase modulator extracted from patent WO2008030579 A2.
  • HY-124622
    NNC-0640

    Glucagon Receptor Metabolic Disease
    NNC-0640 is a potent human G-protein-coupled glucagon receptor (GCGR) negative allosteric modulator (NAM) with an IC50 of 69.2 nM.
  • HY-116463
    E1R

    Sigma Receptor Neurological Disease
    E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity.
  • HY-A0036
    Bazedoxifene acetate

    TSE-424 acetate

    Estrogen Receptor/ERR Cancer
    Bazedoxifene acetate (TSE-424 acetate) is a third generation selective estrogen receptor modulator (SERM) with IC50s of 26 and 99 nM for ERα and ERβ, respectively.
  • HY-112920
    TM-25659

    Others Metabolic Disease
    TM-25659 is a transcriptional co-activator with PDZ-binding motif (TAZ) modulator. Anti-osteoporotic and anti-obesity activities.
  • HY-N0852
    Benzoylpaeoniflorin

    Others Cardiovascular Disease
    Benzoylpaeoniflorin is a natural product; may treat coronary heart disease by decreasing apoptosis.
  • HY-16701
    BV6

    IAP Cancer
    BV6 is an antagonist of cIAP1 and XIAP, members of the inhibitors of apoptosis (IAP) family.
  • HY-108540
    LAT1-IN-1

    BCH

    Apoptosis Cancer
    LAT1-IN-1 (BCH) is a selective and competitive inhibitor of large neutral amino acid transporter 1 (LAT1) significantly inhibit cellular uptake of amino acids and mTOR phosphorylation, which induces the suppression of cancer growth and apoptosis.
  • HY-N6016
    Bacopaside II

    Apoptosis Cancer
    Bacopaside II, an extract from the medicinal herb Bacopa monnieri, blocks the Aquaporin-1 (AQP1) water channel and impairs migration of cells that express AQP1. Bacopaside II induces cell cycle arrest and apoptosis.
  • HY-15695
    Puromycin aminonucleoside

    NSC 3056

    Bacterial Apoptosis Dipeptidyl Peptidase Aminopeptidase Antibiotic Cancer
    Puromycin aminonucleoside (NSC 3056) is the aminonucleoside portion of the antibiotic puromycin, and used in nephrosis animal models. Puromycin aminonucleoside induces apoptosis. Puromycin aminonucleoside is a reversible inhibitor of dipeptidyl peptidase II and cytosol alanyl aminopeptidase.
  • HY-119687
    Bifenazate

    GABA Receptor Infection
    Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm. Bifenazate is a positive allosteric modulator of GABA receptor.
  • HY-114269
    (-)-(S)-B-973B

    nAChR Neurological Disease
    (-)-(S)-B-973B is a potent allosteric agonist and positive allosteric modulator of α7 nAChR, with antinociceptive activity.
  • HY-111098
    GSK1702934A

    TRP Channel Cardiovascular Disease
    GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3.
  • HY-10043
    gamma-secretase modulator 1

    γ-secretase Neurological Disease
    γ-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.
  • HY-19371
    Lorediplon

    GABA Receptor Neurological Disease
    Lorediplon is a novel non-benzodiazepine, hypnotic drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.
  • HY-16951
    VU-1545

    mGluR Neurological Disease
    VU-1545 is a metabotropic glutamate receptor 5 positive allosteric modulator (mGluR5 PAM) with a Ki of 156 nM and an EC50 of 9.6 nM.
  • HY-18102
    GLPG0492

    Androgen Receptor Others
    GLPG0492 is a novel selective androgen receptor modulator; exhibited anabolic activity on muscle, strongly dissociated from the androgenic activity on prostate after oral dosing.
  • HY-112814
    VU6001376

    mGluR Neurological Disease
    VU6001376 is a potent and selective positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4 PAM) with an EC50 of 50.1 nM.
  • HY-119810
    Seletracetam

    Ucb 44212

    Others Neurological Disease
    Seletracetam (Ucb 44212) is an analog of the antiepileptic agent Levetiracetam. Seletracetam is a small molecule SV2A modulator for the research of epilepsy.
  • HY-114381
    GT 949

    EAAT2 Neurological Disease
    GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM.
  • HY-10454
    Delanzomib

    CEP-18770

    Proteasome Cancer
    Delanzomib(CEP-18770) is a novel orally-active inhibitor of the chymotrypsin-like activity of the proteasome that down-modulates the nuclear factor-kappaB (NF-kappaB) activity.
  • HY-100409
    PHCCC

    mGluR Cancer
    PHCCC is a Group I mGluR antagonist with an IC50 of 3 μM. PHCCC is a selective positive modulator of mGlu4 receptor. Antiparkinsonian effect.
  • HY-N3755
    Dihydroresveratrol

    Estrogen Receptor/ERR Cancer
    Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations.
  • HY-124909
    (6R)-FR054

    Apoptosis Cancer
    (6R)-FR054 is an active isomer of FR054. FR054 is an inhibitor of the HBP enzyme PGM3, with a remarkable anti-breast cancer effect. FR054induces endoplasmic reticulum (ER) stress and a ROS-dependent apoptosis.
  • HY-N0816
    Polyphyllin VI

    Apoptosis Cancer
    Polyphyllin VI, an active saponin mainly isolated from traditional medicinal plant Paris polyphylla, possess anti-cancer activities. Polyphyllin VI induces G2/M cell cycle arrest and triggers apoptosis.
  • HY-P1176
    NTR 368

    Apoptosis Neurological Disease
    NTR 368 is a peptide derived from p75 neurotrophin receptor (p75NTR) corresponding to residues 368-381 of the human receptor. NTR 368 has helix forming propensity in the presence of micellar lipid. NTR 368 is a potent inducer of neural apoptosis.
  • 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-18950
    GSK2795039

    NADPH Oxidase Reactive Oxygen Species Cancer
    GSK2795039 is a NADPH oxidase 2 (NOX2) inhibitor with a mean pIC50 of 6 in different cell-free assays. GSK2795039 inhibits reactive oxygen species (ROS) production and NADPH consumption. GSK2795039 reduces apoptosis.
  • 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-N0036
    Costunolide

    (+)-Costunolide; Costus lactone

    Apoptosis Endogenous Metabolite Cancer
    Costunolide, a sesquiterpene lactone, exhibits anti-inflammatory and anti-oxidant properties and mediates apoptosis.
  • HY-N0532
    Morroniside

    MMP Metabolic Disease Neurological Disease
    Morroniside has neuroprotective effect by inhibiting neuron apoptosis and MMP2/9 expression.
  • HY-15584A
    Taltobulin trifluoroacetate

    HTI-286 trifluoroacetate; SPA-110 trifluoroacetate

    Microtubule/Tubulin ADC Cytotoxin Apoptosis Cancer
    Taltobulin trifluoroacetate (HTI-286 trifluoroacetate), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin trifluoroacetate inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
  • HY-130117
    AlbA-DCA

    Reactive Oxygen Species Apoptosis Cancer
    AlbA-DCA is a conjugate formed by the attachment of Albiziabioside A (AlbA) to a dichloroacetate acid (DCA) subunit. AlbA-DCA can induce a marked increase in intracellular ROS and alleviate the accumulation of lactic acid in tumor microenvironment (TME), and also selectively kills cancer cells and induce apoptosis.
  • 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.
  • HY-12646
    Rhosin hydrochloride

    Ras Apoptosis Cancer
    Rhosin hydrochloride 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 hydrochloride induces cell apoptosis.
  • HY-15584B
    Taltobulin hydrochloride

    HTI-286 hydrochloride; SPA-110 hydrochloride

    Microtubule/Tubulin ADC Cytotoxin Apoptosis Cancer
    Taltobulin hydrochloride (HTI-286 hydrochloride), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin hydrochloride inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
  • HY-15584
    Taltobulin

    HTI-286; SPA-110

    Microtubule/Tubulin ADC Cytotoxin Apoptosis Cancer
    Taltobulin (HTI-286), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
  • HY-W014102
    L-Alanyl-L-glutamine

    Endogenous Metabolite Metabolic Disease Inflammation/Immunology
    L-Alanyl-L-glutamine, a glutamine dipeptide, is benefit for the antioxidant system, attenuating inflammation, and may modulate the heat shock protein (HSP) response in catabolic situations.
  • HY-103035
    BIO-32546

    Phosphodiesterase (PDE) Cancer
    BIO-32546 (example 12b, S-isomer) is an autotaxin (ATX) modulator, extracted from the patent US20170158687A1.
  • HY-129946
    Dopamine D2 receptor antagonist-1

    Dopamine Receptor Neurological Disease
    Dopamine D2 receptor antagonist-1 is a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R) with sub-mM affinity.
  • HY-114403
    VU6012962

    mGluR Neurological Disease
    VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM) with an IC50 of 347 nM.
  • HY-119433
    Asoprisnil

    J867

    Progesterone Receptor Endocrinology
    Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human.
  • HY-14316A
    Tebanicline dihydrochloride

    Ebanicline dihydrochloride; ABT-594 dihydrochloride

    nAChR Neurological Disease
    Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM.
  • HY-N2370
    24-Hydroxycholesterol

    iGluR LXR Neurological Disease
    24-Hydroxycholesterol is a natural sterol, which serves as a positive allosteric modulator of N-Methyl-d-Aspartate (NMDA) receptorsR, and a potent activator of the transcription factors LXR.
  • HY-128575
    BNC375

    nAChR Neurological Disease
    BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM.
  • HY-U00151
    Dopropidil

    Calcium Channel Cardiovascular Disease
    Dopropidil is a novel anti-anginal calcium ion modulating agent, possessing intracellular calcium antagonist activity and anti-ischemic effects in several predictive animal models.
  • HY-111498A
    RGX-104 free Acid

    LXR Cancer Inflammation/Immunology
    RGX-104 free Acid is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
  • HY-135273
    BCL2-IN-1

    Bcl-2 Family Cancer
    BCL2-IN-1 is a potent Bcl-2 inhibitor. BCL2-IN-1 binds Bcl-2 with a Ki of <0.01 nM.
  • HY-12041
    SP600125

    JNK Autophagy Apoptosis Ferroptosis Cancer
    SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 inhibits autophagy and activates apoptosis.
  • HY-13649
    Indibulin

    ZIO 301; D 24851

    Microtubule/Tubulin Apoptosis Cancer Neurological Disease
    Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis.
  • HY-121282
    Mepazine

    Pecazine

    MALT1 Apoptosis Cancer
    Mepazine (Pecazine) is a potent and selective MALT1 inhibitor. Mepazine inhibits GSTMALT1 full length and GSTMALT1 325-760 with IC50s of 0.83 and 0.42 μM, respectively. Mepazine affects viability of ABC-DLBCL cells by enhancing apoptosis.
  • HY-N0203
    Atractylenolide III

    ICodonolactone; 8β-Hydroxyasterolide

    Apoptosis Cancer
    Atractylenolide III is a major component of Atractylodes rhizome can induce apoptosis of the lung carcinoma cells.
  • HY-N1486
    Ursonic acid

    3-Ketoursolic acid

    Apoptosis Endogenous Metabolite Cancer
    Ursolic acid, a naturally occurring triterpenoid, induces the apoptosis of human cancer cells through multiple signaling pathways.
  • HY-N4313
    Eriosematin

    Apoptosis Metabolic Disease
    Eriosematin is a compound from the roots of Flemingia philippinensis with antiproliferative activity and apoptosis-inducing property.
  • HY-P1176A
    NTR 368 TFA

    Apoptosis Neurological Disease
    NTR 368 TFA is a peptide derived from p75 neurotrophin receptor (p75NTR) corresponding to residues 368-381 of the human receptor. NTR 368 TFA has helix forming propensity in the presence of micellar lipid. NTR 368 TFA is a potent inducer of neural apoptosis.
  • HY-10999A
    Trametinib (DMSO solvate)

    GSK-1120212 (DMSO solvate); JTP-74057 (DMSO solvate)

    MEK Apoptosis Cancer
    Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis.
  • HY-13556A
    Arzoxifene hydrochloride

    LY 353381 HCl; SERM 3

    Estrogen Receptor/ERR Cancer
    Arzoxifene hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol.
  • HY-14425
    NB001

    HTS 09836

    Adenylate Cyclase Neurological Disease
    NB001 (HTS 09836) is an adenylcyclase 1 (AC1) inhibitor which has effect on neural and non-neural pain by modulating AC1 activity.
  • HY-N2487
    5-Hydroxy-7-acetoxyflavone

    Others Cancer
    5-Hydroxy-7-acetoxyflavone, an active natural flavone derivative found in various plant sources, modulates several biological activities.
  • HY-14399
    Itanapraced

    CHF5074; CSP-1103

    γ-secretase Neurological Disease
    Itanapraced (CHF5074) is a novel γ-secretase modulator, reduces Aβ42 and Aβ40 secretion, with an IC50 of 3.6 and 18.4 μM, respectively.
  • HY-10043A
    gamma-secretase modulator 1 hydrochloride

    γ-secretase Neurological Disease
    gamma-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.
  • HY-N2032
    Euphorbiasteroid

    AMPK Cancer Infection Metabolic Disease
    Euphorbiasteroid is a tricyclic diperpene of Euphorbia lathyris L., inhibits tyrosinase, and increases the phosphorylation of AMPK, with anti-cancer, anti-virus, anti-obesity and multidrug resistance-modulating effect.
  • HY-101363
    1-BCP

    Piperonylic acid piperidide

    iGluR Neurological Disease
    1-BCP (Piperonylic acid piperidide) is a centrally active drug that modulates AMPA receptor gated currents. 1-BCP is a memory-enhancing agent.
  • HY-120722
    TCH-165

    Proteasome Cancer
    TCH-165 is a small molecule modulator of proteasome assembly, which increases 20S levels and facilitates 20S-mediated protein degradation.
  • HY-N0549
    (-)-α-Pinene

    GABA Receptor Bacterial Virus Protease Endogenous Metabolite Neurological Disease
    (-)-α-Pinene is a monoterpene and shows sleep enhancing property through a direct binding to GABAA-benzodiazepine (BZD) receptors by acting as a partial modulator at the BZD binding site.
  • HY-N0711
    Carvacrol

    Notch Apoptosis Fungal Endogenous Metabolite Cancer Inflammation/Immunology
    Carvacrol is a monoterpenoid phenol isolated from Lamiaceae family plants, with antioxidant, anti-inflammatory and anticancer properties. Carvacrol causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis.
  • HY-136531
    XMU-MP-3

    Btk Apoptosis Cancer
    XMU-MP-3 is a potent non-covalent BTK inhibitor with IC50s of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation in the presence of 10 μM ATP, respectively. XMU-MP-3 also induces apoptosis.
  • HY-19566
    NQDI-1

    MAP3K Apoptosis Cancer
    NQDI-1 inhibits apoptosis signal-regulating kinase 1 (ASK1) with a Ki of 500 nM and an IC50 of 3 μM.
  • 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-136313
    MC-VC-PAB-Tubulysin M

    Drug-Linker Conjugates for ADC Cancer
    MC-vc-PAB-Tubulysin M consists a cleavable ADC linker (MC-vc-PAB) and a cytotoxic tubulin inhibitor Tubulysin M (HY-N7053). Tubulysin M is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • HY-19322B
    PIM-447 dihydrochloride

    LGH447 dihydrochloride

    Pim Cancer
    PIM447 dihydrochloride (LGH447 dihydrochloride) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 dihydrochloride displays dual antimyeloma and bone-protective effects. PIM447 dihydrochloride induces apoptosis.
  • HY-117889
    PARP14 inhibitor H10

    PARP Apoptosis Cancer
    PARP14 inhibitor H10, compound H 10, is a selective inhibitor against PARP14 (IC50=490 nM), over other PARPs (≈24 fold over PARP1). PARP14 inhibitor H10 induces caspase-3/7-mediated cell apoptosis.
  • HY-12212
    Omaveloxolone

    RTA 408

    Keap1-Nrf2 STING Apoptosis Cancer Inflammation/Immunology
    Omaveloxolone (RTA 408) is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO). Omaveloxolone attenuates osteoclastogenesis by inhibiting STING dependent NF-κb signaling.
  • HY-14959
    Ulipristal

    CDB-3236; Deacetyl CDB-2914

    Progesterone Receptor Cancer Endocrinology
    Ulipristal (CDB 3236) is a selective progesterone receptor modulator (SPRM). Ulipristal binds to the progesteron receptor, thereby inhibiting PR-mediated gene expression, and interfering with progesterone activity in the reproductive system.
  • HY-133684
    N-Tetradecanoyl-L-homoserine lactone

    Bacterial
    N-Tetradecanoyl-L-homoserine lactone is a major chemical modulators of within and between cell communication and regulation. N-Tetradecanoyl-L-homoserine lactone can be used for the study of quorum sensing in vitro.
  • HY-103306
    Ryanodine

    Others Neurological Disease
    Ryanodine is a cell permeant ryanodine receptor modulator. Ryanodine can either stimulate or inhibit Ryanodine-mediated Ca 2+ release depending on its concentrations. Poisonous diterpenoid found in Ryania speciosa.
  • HY-133555
    mGluR2 antagonist 1

    mGluR Neurological Disease
    mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability.
  • HY-P0081
    Bax inhibitor peptide V5

    BIP-V5; BAX Inhibiting Peptide V5

    Bcl-2 Family Cancer
    Bax inhibitor peptide V5 (BIP-V5) is a Bax-mediated apoptosis inhibitor, used for cancer treatment.
  • HY-10933
    Ampalex

    CX516; BDP 12; Ampakine CX516

    iGluR Neurological Disease
    Ampalex (Ampakine CX516; CX516; BDP 12) is an ampakine and nootropic that acts as an AMPA receptor positive allosteric modulator as a treatment for Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).
  • HY-119165
    GSM-1

    γ-secretase Neurological Disease
    GSM-1 is a potent γ-secretase modulator. GSM-1 directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1).
  • HY-114406
    TD-106

    Ligand for E3 Ligase Cancer
    TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation.
  • HY-110285
    ML382

    Others Neurological Disease
    ML382 is a potent and selective MRGPRX1 (Mas-related G protein-coupled receptor X1, MrgX1) positive allosteric modulator, with an EC50 of 190 nM.
  • HY-12149
    A-867744

    nAChR Autophagy Neurological Disease
    A-867744 is a highly potent and selective type II positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptors (nAChR) with an EC50 of 1.0 μM.
  • HY-100765
    BI-0252

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis.
  • HY-B0146
    Verteporfin

    CL 318952

    YAP Apoptosis Autophagy Cancer
    Verteporfin (CL 318952) is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions. Verteporfin induces cell apoptosis. Verteporfinis an autophagy inhibitor that blocks autophagy at an early stage by inhibiting autophagosome formation.
  • HY-13628
    Etalocib

    LY293111; VML 295

    Leukotriene Receptor Apoptosis Cancer Inflammation/Immunology
    Etalocib (LY293111), an orally active leukotriene B4 receptor antagonist, inhibits the binding of [ 3H]LTB4, with a Ki of 25 nM. Etalocib (LY293111) prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib (LY293111) induces apoptosis.
  • HY-N7526
    Naphthazarin

    DHNQ; 5,8-Dihydroxy-1,4-naphthoquinone

    Apoptosis Cancer Neurological Disease
    Naphthazarin (DHNQ) is a naturally occurring compound. Naphthazarin is effective by various cellular mechanisms including oxidative stress, activation of mitochondrial apoptosis-inducing factor (AIF), depolymerization of microtubules, interference with lysosomal function and p53-dependent p21 activation. Naphthazarin triggers apoptosis and has anti-tumor effects.
  • HY-B1193
    Terfenadine

    (±)-Terfenadine; MDL-991

    Potassium Channel Histamine Receptor Na+/Ca2+ Exchanger Caspase Apoptosis Cancer Inflammation/Immunology Endocrinology
    Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca 2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
  • 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-100753
    STAT3-IN-1

    STAT Apoptosis Cancer
    STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor apoptosis.
  • HY-13719
    Oleandrin

    Na+/K+ ATPase Apoptosis Cancer
    Oleandrin inhibits the Na +, K +-ATPase activity with an IC50 of 620 nM. Oleandrin induces apoptosis via activating endoplasmic reticulum stress.
  • HY-13523
    PAC-1

    Procaspase activating compound 1

    Caspase Autophagy Apoptosis Cancer
    PAC-1 is an activator of procaspase-3 induces apoptosis in cancer cells with EC50 of 2.08 μM.
  • HY-113534
    MV1

    IAP Others
    MV1 is an antagonist of IAP (inhibitor of apoptosis protein), leads to protein knockdown of HaloTag-fused proteins when combined with HaloTag ligand.
  • HY-N0038
    Alantolactone

    (+)-Alantolactone; Alant camphor; Inula camphor

    STAT Apoptosis TGF-beta/Smad Cancer
    Alantolactone is a selective STAT3 inhibitor, with potent anticancer activity. Alantolactone induces apoptosis in cancer.
  • HY-13229
    BOC-D-FMK

    Caspase Cancer
    Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor; inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM.
  • HY-N2096
    Kavain

    GABA Receptor Neurological Disease
    Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic and sedative properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor.
  • HY-19845A
    Piperidine-MO-1

    Dopamine Receptor Neurological Disease
    Piperidine-MO-1 is a modulator of dopamine receptor extracted from patent WO/2005/121087A1, compound example 2; exhibits an ED50 of 68 μmol/kg on increase of DOPAC in the rat striatum.
  • HY-10167A
    Tecalcet Hydrochloride

    R-568 (hydrochloride)

    CaSR Others
    Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca 2+.
  • HY-117965
    Miricorilant

    CORT 118335

    Glucocorticoid Receptor Mineralocorticoid Receptor Endocrinology
    Miricorilant (CORT 118335) is a dual selective glucocorticoid (GR) modulator/mineralocorticoid (MR) antagonist. Miricorilant can be used for the research of hypothalamic-pituitary-adrenal (HPA) axis related disorders.
  • HY-P1125
    4-CMTB

    Others Others
    4-CMTB is a selective free fatty acid receptor 2 (FFA2/GPR43) agonist and a positive allosteric modulator (pEC50=6.38).
  • HY-128400
    4'-Methoxychalcone

    PARP Metabolic Disease Cancer
    4'-Methoxychalcone regulates adipocyte differentiation through PPARγ activation. 4'-Methoxychalcone modulates the expression and secretion of various adipokines in adipose tissue that are involved in insulin sensitivity.
  • HY-129395
    CC-92480

    E1/E2/E3 Enzyme Apoptosis Cancer
    CC-92480 is a cereblon E3 ubiquitin ligase modulating drug (CELMoD). CC-92480 shows high affinity to cereblon, resulting in potent antimyeloma activity.
  • HY-128128
    ASN04421891

    Others Neurological Disease
    ASN04421891 is a potent GPR17 receptor modulator, with an EC50 of 3.67 nM in [35S]GTPγS binding assay. ASN04421891 can be used for neurodegenerative diseases research.
  • HY-107409
    GNE 5729

    iGluR Neurological Disease
    GNE 5729 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively.
  • HY-122627
    Mcl1-IN-8

    Bcl-2 Family Cancer
    Mcl1-IN-8 (Comp8) is a Mcl-1-PUMA interface inhibitor, with a Ki of 0.3 μM. Mcl1-IN-8 (Comp8) exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells.
  • HY-N6785
    Okadaic acid

    Phosphatase Parasite Apoptosis Infection
    Okadaic acid is extracted from black sponges of the genus Halichondria. Okadaic acid is a non-comepetitive, selective and reversible serine/threonine-specific protein phosphatases 1 (PP1), PP2A and PP3 inhibitor with IC50s of 10-15 nM, 0.5 nM and 4 nM, respectively. Okadaic acid eliminate metazoan symbionts/parasites by apoptosis.
  • HY-116852
    Thiocolchicine

    Microtubule/Tubulin Cancer
    Thiocolchicine, a derivative modified in the C Ring of Colchicine (HY-16569) with enhanced biological properties. Thiocolchicine is a potent inhibitor of tubulin polymerization (IC50=2.5 µM) and competitively binds to tubulin with a Ki of 0.7 µM. Thiocolchicine induces cell apoptosis. Thiocolchicine can be used as an ADC cytotoxin in ADC technology.
  • HY-18204A
    LCZ696

    Sacubitril/Valsartan

    Angiotensin Receptor Neprilysin Apoptosis Cardiovascular Disease Endocrinology
    LCZ696 (Sacubitril/Valsartan), comprised Valsartan (an ARB) and Sacubitril (AHU377) in 1:1 molar ratio, is a first-in-class, orally bioavailable, and dual-acting angiotensin receptor-neprilysin (ARN) inhibitor for hypertension and heart failure. LCZ696 ameliorates diabetic cardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis.
  • 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-112256
    ACP-105

    Androgen Receptor Inflammation/Immunology
    ACP-105 is an orally available, selective amd potent androgen receptor modulator (SARM), with pEC50s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively.
  • HY-128770
    LY3154207

    Dopamine Receptor Neurological Disease
    LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM).
  • HY-N4157
    Isopteropodine

    mAChR 5-HT Receptor Neurological Disease
    Isopteropodine is heteroyohimbine-type oxindole alkaloid components of Uncaria tomentosa (Willd.) DC. Isopteropodine acts as positive modulators of muscarinic M1 and 5-HT2 receptors.
  • HY-110278
    ADX71743

    mGluR Neurological Disease
    ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity.
  • HY-W010104
    L-Methionine sulfoxide

    H-Met(O)-OH

    Endogenous Metabolite Metabolic Disease
    L-Methionine sulfoxide (H-Met(O)-OH), a metabolite of Methionine, induces M1/classical macrophage polarization, and modulates oxidative stress and purinergic signaling parameters.
  • HY-B0311
    Carbidopa

    (S)-(-)-Carbidopa

    Aryl Hydrocarbon Receptor Neurological Disease
    Carbidopa ((S)-(-)-Carbidopa), a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa inhibits pancreatic cancer cell and tumor growth.
  • HY-12151
    NS 1738

    NSC 213859

    nAChR Neurological Disease
    NS 1738 (NSC 213859) is a novel positive allosteric modulator of the α7 nAChR, with respect to positive modulation of α7 nAChR (EC50=3.4 μM in oocyte experiments).
  • HY-131181
    LEI-401

    Phospholipase Neurological Disease
    LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC50 of 27 nM. LEI-401 modulates emotional behavior in mice.
  • HY-122910
    RIPGBM

    Apoptosis Cancer
    RIPGBM is a selective inducer of apoptosis in glioblastoma multiforme (GBM) cancer stem cells (CSCs) with an EC50 of ≤500 nM.
  • HY-14590
    Kaempferol

    Kempferol; Robigenin

    Estrogen Receptor/ERR Autophagy Mitophagy Apoptosis HIV Parasite Endogenous Metabolite Cancer
    Kaempferol inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK.
  • HY-N0797
    (20S)-Protopanaxadiol

    20-Epiprotopanaxadiol; 20(S)-APPD

    P-glycoprotein Reactive Oxygen Species Apoptosis Cancer
    (20S)-Protopanaxadiol (20-Epiprotopanaxadiol) is an aglycon metabolic derivative of the protopanaxadiol-type ginseng saponin; apoptosis inducer.
  • HY-16518
    Voreloxin Hydrochloride

    SNS-595 Hydrochloride; Vosaroxin Hydrochloride; AG 7352 Hydrochloride

    Topoisomerase Apoptosis Cancer
    Voreloxin Hydrochloride is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis.
  • HY-N0016
    Glycitein

    Glycetein

    Apoptosis Cancer
    Glycitein is a soybean (yellow cultivar) isoflavonoid; used in combination with other isoflavonoids such as genistein and daidzein to study apoptosis and anti-oxidation processes.
  • HY-15491
    AG-024322

    COX Cancer
    AG-024322 is a potent ATP-competitive pan-CDK inhibitor against cell cycle kinases CDK1, CDK2, and CDK4 with Ki values in the 1-3 nM range. AG-024322 displays broad-spectrum anti-tumor activity and clear target modulation in vivo. AG-024322 induces cell apoptosis.
  • HY-10220
    SF1126

    PI3K Apoptosis Cancer
    SF1126 is a relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 prodrug, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment. SF1126 induces cell apoptosis.
  • 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-16636
    ML337

    mGluR Neurological Disease
    ML337 is a selective and brain-penetrant negative allosteric modulator of mGlu3, with an IC50 of 593 nM. ML337 possesses a favorable dystrophia myotonica protein kinase (DMPK) and ancillary pharmacology profile, and is centrally penetrant.
  • HY-15416
    NS309

    Potassium Channel Cardiovascular Disease
    NS309 is a positive modulator of small- and intermediate- conductance Ca2+-activated K+ channels (KCa2 and KCa3.1 channels); increases Ca2+ sensitivity. Displays no activity at BK channels.
  • HY-16950A
    (E/Z)-4-Hydroxytamoxifen

    Estrogen Receptor/ERR Cancer
    (E/Z)-4-Hydroxytamoxifen is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. (E/Z)-4-Hydroxytamoxifen is an estrogen receptor modulator.
  • HY-108703
    Foliglurax

    PXT002331

    mGluR Neurological Disease
    Foliglurax (PXT002331) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 79 nM. Antiparkinsonian effect.
  • HY-108243
    AZD5423

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    AZD5423 is an inhaled, potent, selective, and non-steroidal glucocorticoid receptor (GR) modulator (SGRM). AZD5423 effectively reduces allergen-induced responses in subjects with mild allergic asthma.
  • HY-107902
    RIG-1 modulator 1

    HBV HCV HIV Influenza Virus Infection
    RIG-1 modulator 1 is an anti-viral compound which can be useful for the treatment of viral infections including influenza virus, HBV, HCV and HIV extracted from patent WO 2015172099 A1.
  • HY-112209
    VU0467154

    mAChR Neurological Disease
    VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
  • HY-113320
    Etiocholanolone

    5β-Androsterone

    GABA Receptor Neurological Disease
    Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form.
  • HY-105858
    BNC210

    H-Ile-Trp-OH; IW-2143

    nAChR Neurological Disease
    BNC210 (H-Ile-Trp-OH; IW-2143) is a α7 nAChR negative allosteric modulator. BNC210 has potent activity in animal models of anxiety and depression.
  • HY-10863
    Anandamide

    Cannabinoid Receptor GPR55 Endogenous Metabolite Inflammation/Immunology
    Anandamide is an immune modulator in the central nervous system acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55).
  • HY-13738A
    Raloxifene hydrochloride

    Keoxifene hydrochloride; LY156758; LY139481 hydrochloride

    Estrogen Receptor/ERR Autophagy Endocrinology Cancer
    Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue.
  • HY-B1756
    Rotenone

    Mitochondrial Metabolism Autophagy Apoptosis Neurological Disease Cancer
    Rotenone is an mitochondrial electron transport chain complex I inhibitor. Rotenone induces apoptosis through enhancing mitochondrial reactive oxygen species production.
  • HY-N0882
    Desacetylcinobufotalin

    Deacetylcinobufotalin

    Apoptosis Cancer
    Desacetylcinobufotalin is a natural compound; apoptosis inducer and shows the marked inhibition effect to HepG2 cells and the IC50 value is 0.0279μmol/ml.
  • 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-Y0152
    Cinchonine

    (8R,9S)-Cinchonine; LA40221

    Apoptosis Parasite Cancer
    Cinchonine is a natural compound present in Cinchona bark. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells.
  • HY-14808
    Adarotene

    ST1926

    Apoptosis Cancer
    Adarotene is an effective apoptosis inducer, which surprisingly produces DNA damage and exhibites a potent antiproliferative activity on a large panel of human tumor cells.
  • HY-12795
    Vps34-IN-1

    PI3K Autophagy Cancer
    Vps34-IN-1 is an inhibitor of Vps34 extracted from patent WO2012085815A1, compound example 16a, with an IC50 of 4 nM. Vps34-IN-1 modulates autophagy.
  • HY-120530
    JNJ-46281222

    mGluR Neurological Disease
    JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator) with nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71).
  • HY-103040
    Zuranolone

    GABA Receptor Neurological Disease
    Zuranolone is an orally active and potent neuroactive steroid positive allosteric modulator of GABAA receptor, with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
  • HY-108337
    GNE-0723

    iGluR Neurological Disease
    GNE-0723 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM for GluN2C and GluN2D, respectively.
  • HY-125740
    Malvidin-3-glucoside chloride

    Malvidin-3-O-glucoside chloride; Oenin chloride

    Others Inflammation/Immunology
    Malvidin-3-glucoside chloride (Malvidin-3-O-glucoside chloride), a major wine anthocyanin, is effective in promoting resilience against stress by modulating brain synaptic plasticity and peripheral inflammation.
  • HY-128677
    NCC007

    Casein Kinase Neurological Disease
    NCC007 is a dual casein kinase Iα (CKIα) and δ (CKIδ) inhibitor with IC50s of 1.8 and 3.6 μM, respectively. NCC007 can be used in research of modulating mammalian circadian rhythms.
  • HY-103575A
    MFZ 10-7 hydrochloride

    mGluR Neurological Disease
    MFZ 10-7 hydrochloride is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a Ki of 0.67 nM for rat mGluR5. MFZ 10-7 hydrochloride inhibits cocaine-taking and cocaine-seeking behavior in rats.
  • HY-B2158
    Chlorotrianisene

    Estrogen Receptor/ERR COX Endocrinology Cardiovascular Disease
    Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood.
  • HY-124867
    D3-βArr

    TSH Receptor Endocrinology
    D3-βArr is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 by direct TSHR activation and potentiates TSH-mediated preosteoblast differentiation in vitro.
  • HY-129527
    GNE-9278

    iGluR Neurological Disease
    GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity.
  • HY-107198
    (2S)-6-Prenylnaringenin

    GABA Receptor Neurological Disease
    (2S)-6-Prenylnaringenin is the most efficient compound in forebrain. (2S)-6-Prenylnaringenin acts as a GABAA positive allosteric modulator at α+β- binding interface.
  • HY-108710
    VU0650786

    mGluR Neurological Disease
    VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents.
  • HY-100487
    TAK-243

    MLN7243

    E1/E2/E3 Enzyme NF-κB Apoptosis Cancer
    TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.
  • HY-17409
    Nystatin

    Fungal Antibiotic Infection
    Nystatin is an orally active polyene antifungal antibiotic effective against yeast and mycoplasma. Nystatin increases the permeability of plasma membranes to small monovalent ions, including chloridion. Nystatin is a cholesterol-sequestering agent, partially prevents Oxaliplatin-induced lipid raft aggregation, DR4 and DR5 clustering, and thereby reduces apoptosis.
  • HY-N0168
    Hesperetin

    p38 MAPK Apoptosis Autophagy Neurological Disease Cancer
    Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
  • HY-13216
    Pyroxamide

    HDAC Cancer
    Pyroxamide is a potent inhibitor of histone deacetylase 1 (HDAC1) with an ID50 of 100 nM. Pyroxamide can induce apoptosis and cell cycle arrest in leukemia.
  • HY-13680
    Meisoindigo

    Dian III; N-Methylisoindigotin; Natura-α

    Apoptosis Cancer
    Meisoindigo(Natura-α; N-Methylisoindigotin; Dian III), a derivative of Indigo naturalis, might induce apoptosis and myeloid differentiation of acute myeloid leukemia (AML).
  • HY-N1983
    Caudatin

    Apoptosis Cancer
    Caudatin is a steroidal cmpound found in Cynanchum auriculatum, causes cell cycle arrest and induces apoptosis, with anti-cancer and antiangiogenic properties.
  • HY-50714
    Quiflapon sodium

    MK-591 sodium

    FLAP Apoptosis Inflammation/Immunology
    Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.
  • 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-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-15843
    MIR96-IN-1

    MicroRNA Apoptosis Cancer
    MIR96-IN-1 selectively inhibits biogenesis of microRNA-96, upregulating a protein target (FOXO1) and inducing apoptosis in cancer cells.
  • HY-N2585
    Isodeoxyelephantopin

    Reactive Oxygen Species NF-κB Autophagy Cancer
    Isodeoxyelephantopin is a sesquiterpene lactone isolated from Elephantopus scaber. Isodeoxyelephantopin induces ROS generation, suppresses NF-κB activation. Isodeoxyelephantopin also modulates LncRNA expression and exhibit activities against breast cancer.
  • HY-108703A
    Foliglurax monohydrochloride

    PXT002331 (monohydrochloride)

    mGluR Neurological Disease
    Foliglurax monohydrochloride (PXT002331 monohydrochloride) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) , with an EC50 of 79 nM. Antiparkinsonian effect.
  • HY-12324
    SB269652

    Dopamine Receptor Neurological Disease
    SB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor (D2R); a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology.
  • HY-120012
    AZD9567

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    AZD9567 (compound 15) is a potent, oral active, non-steroidal and selective glucocorticoid receptor modulator (SGRM), with an IC50 of 3.8 nM. Exhibits excellent efficacy in the streptococcal cell wall (SCW) reactivation model of joint inflammation.
  • HY-101792A
    RG7800 hydrochloride

    RO6885247 hydrochloride

    DNA/RNA Synthesis Neurological Disease
    RG7800 hydrochloride is an orally active SMN2 splicing modulator, with EC1.5xs of 23 nM and 87 nM for SMN2 splicing and SMN protein; RG7800 hydrochloride has the potential to treat spinal muscular atrophy.
  • HY-15731
    Estetrol

    Estrogen Receptor/ERR Endogenous Metabolite Cardiovascular Disease
    Estetrol, a natural estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast.
  • HY-101281
    VU 6008667

    mAChR Neurological Disease
    VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration.
  • HY-13738
    Raloxifene

    Keoxifene; LY156758 free base; LY139481

    Estrogen Receptor/ERR Cancer
    Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research.
  • HY-B0311A
    Carbidopa monohydrate

    (S)-(-)-Carbidopa monohydrate

    Aryl Hydrocarbon Receptor Cancer Neurological Disease
    Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth.
  • HY-W011509
    CyPPA

    Potassium Channel Neurological Disease
    CyPPA is a positive modulator of hSK3 and hSK2, with EC50 values of 14 μM and 5.6 μM, repectively. CyPPA is inactive on both hSK1 and hIK channels[1].
  • HY-B1837
    Cyfluthrin

    Sodium Channel Infection
    Cyfluthrin is a type II pyrethroid and has effects on various insects. Cyfluthrin is a modulator of Nav1.8 sodium channels by repetitive stimulation. Cyfluthrin can be applied in agriculture,veterinary, insecticide,pyrethroid and stored product.
  • HY-12508
    CMPDA

    iGluR Neurological Disease
    CMPDA is a positive allosteric modulator of AMPA receptors with EC50s of 45.4 ± 4.2 nM/63.4 ± 5.6 nM for GluA2i/GluA2o receptor.
  • HY-135891
    AZD2423

    CCR Neurological Disease
    AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca 2+ flux .
  • HY-13963
    ZCL278

    Ras Cancer
    ZCL278 is a selective Cdc42 modulator that directly binds to Cdc42 and inhibits its functions with Kd of 11.4 μM for Cdc42-ZCL278 affinity in surface plasmon resonance (SPR) experiment.
  • HY-111772
    Elexacaftor

    VX-445

    CFTR Autophagy Others
    Elexacaftor (VX-445, Compound 1) is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR). Elexacaftor (VX-445, Compound 1) facilitates the processing and trafficking of CFTR to increase the amount of CFTR at the cell surface.
  • HY-N6687
    Calcimycin

    A-23187; Antibiotic A-23187

    Bacterial Fungal Apoptosis Autophagy Antibiotic Cancer Infection
    Calcimycin (A-23187) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin induces Ca 2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin also inhibits the activity of ATPase and uncouples oxidative phosphorylation of mammalian cells. Calcimycin induces apoptosis.
  • HY-10037
    Quiflapon

    MK-591

    FLAP Apoptosis Inflammation/Immunology
    Quiflapon (MK-591) is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.6 nM in a FLAP binding assay. Quiflapon is also a potent and orally active Leukotriene biosynthesis (LT) inhibitor, shows IC50 values of 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively. Quiflapon induces cell apoptosis.
  • 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-13948
    Angiotensin II human

    Angiotensin II; Ang II; DRVYIHPF

    Angiotensin Receptor Apoptosis Cardiovascular Disease Endocrinology Cancer
    Angiotensin II human (Angiotensin II) is a vasoconstrictor that mainly acts on the AT1 receptor. Angiotensin II human stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human also induces apoptosis.
  • HY-13948A
    Angiotensin II human acetate

    Angiotensin II acetate; Ang II acetate; DRVYIHPF acetate

    Angiotensin Receptor Apoptosis Cancer Endocrinology Cardiovascular Disease
    Angiotensin II human acetate (Angiotensin II acetate) is a vasoconstrictor that mainly acts on the AT1 receptor. Angiotensin II human acetate stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human acetate induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human acetate also induces 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-B0215
    Acetylcysteine

    N-Acetylcysteine; N-Acetyl-L-cysteine; NAC

    Reactive Oxygen Species Endogenous Metabolite Apoptosis Ferroptosis Influenza Virus Infection Neurological Disease
    Acetylcysteine (N-Acetylcysteine) is a mucolytic agent which reduces the thickness of the mucus. Acetylcysteine is a ROS inhibitor. Acetylcysteine is a cysteine precursor, prevents hemin-induced ferroptosis by neutralizing toxic lipids generated by arachidonate-dependent activity of 5-lipoxygenases. Acetylcysteine induces cell apoptosis. Acetylcysteine also has anti-influenza virus activities.
  • 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-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-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-B0011A
    Docetaxel Trihydrate

    RP-56976 Trihydrate

    Microtubule/Tubulin Apoptosis Cancer
    Docetaxel Trihydrate (RP-56976 Trihydrate) is an antineoplastic agent and inhibits microtubule depolymerization with an IC50 value of 0.2 μM. Docetaxel Trihydrate is a semisynthetic analog of taxol and attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel Trihydrate arrests the cell cycle at G2/M and leads to cell 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-N2500
    Deoxypodophyllotoxin

    Microtubule/Tubulin Apoptosis Autophagy Infection Cardiovascular Disease
    Deoxypodophyllotoxin (DPT), a derivative of podophyllotoxin, is a lignan with potent antimitotic, anti-inflammatory and antiviral properties isolated from rhizomes of Sinopodophullumhexandrum (Berberidaceae). Deoxypodophyllotoxin, targets the microtubule, has a major impact in oncology not only as anti-mitotics but also as potent inhibitors of angiogenesis. Deoxypodophyllotoxin induces cell autophagy and apoptosis. Deoxypodophyllotoxin evokes increase of intracellular Ca 2+ concentrations in DRG neurons.
  • HY-W015084
    β-Ionone

    Apoptosis Cancer
    β-Ionone, isolated from plant oils, is effective in the induction of apoptosis in gastric adenocarcinoma SGC7901 cells. Anti-cancer activity.
  • HY-N0006
    Demethoxycurcumin

    Curcumin II; Desmethoxycurcumin; Monodemethoxycurcumin

    Apoptosis Autophagy Bacterial Inflammation/Immunology Cancer
    Demethoxycurcumin(Curcumin II) is a major active curcuminoid; possess anti-inflammatory properties; also exert cytotoxic effects in human cancer cells via induction of apoptosis.
  • HY-118266
    BTdCPU

    Phosphatase Apoptosis Cancer
    BTdCPU is a potent heme-regulated eIF2α kinase (HRI) activator. BTdCPU promotes eIF2α phosphorylation and induced apoptosis in resistant cell.
  • 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-N5007
    Galgravin

    Others Cancer
    Galgravin is an active compound in Nectandra megapotamica, with anti-inflammatory activity. Galgravin displays in vitro cytotoxic activity and induce apoptosis in leukemia cells.
  • HY-N6940
    Prosapogenin A

    Progenin III

    Apoptosis Cancer
    Prosapogenin A, a natural product from Veratrum, induces apoptosis in human cancer cells in vitro via inhibition of the STAT3 signaling pathway and glycolysis.
  • HY-N2541
    Gymnemic acid I

    Others Metabolic Disease
    Gymnemic acid I is a bioactive triterpene saponin found in Gymnema sylvestre. Gymnemic acid I decreases the apoptosis under the high glucose stress.
  • HY-125848
    Ginsenoside F2

    Apoptosis Autophagy Endogenous Metabolite Cancer
    Ginsenoside F2, a metabolite from Ginsenoside Rb1, induces apoptosis accompanied by protective autophagy in breast cancer stem cells.
  • HY-N0784
    Ginkgolide B

    BN-52021

    Endogenous Metabolite Cancer
    Ginkgolide B (BN-52021), an important active terpenoid from Ginkgo biloba leaves, is reported to increase cell viability and decrease cell apoptosis.
  • HY-N4180
    Pennogenin 3-O-beta-chacotrioside

    Autophagy Cancer
    Pennogenin 3-O-beta-chacotrioside is an active component isolated from Paris polyphylla, modulates autophagy via increasing the expressions of autophagy-related proteins LC3 and Beclin-1. Anti-colorectal cancer activity.
  • HY-119332
    3-Keto petromyzonol

    Others Endocrinology
    3-Keto petromyzonol, a main component of Sea lamprey male sex pheromones, modulates both synthesis and release of gonadotropin releasing hormone (GnRH), and subsequently, hypothalamic-pituitary-gonadal (HPG) output in immature sea lamprey.
  • HY-107774
    BMS-986163

    iGluR Neurological Disease
    BMS-986163 is a negative allosteric modulator of GluN2B. The prodrug BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM).
  • HY-107091
    Aspartyl-alanyl-diketopiperazine

    DA-DKP

    Others Inflammation/Immunology
    Aspartyl-alanyl-diketopiperazine (DA-DKP) is an immunomodulatory molecule generated by cleavage and cyclization from the N-terminus of human albumin and can modulate the inflammatory immune response through a molecular pathway implicated in T- lymphocyte anergy.
  • HY-135585
    LY88074

    Others Endocrinology
    LY88074 (Compound 88074) is a Raloxifene analog lacking the basic side chain. Raloxifene is a selective estrogen receptor modulator, and reduces fracture risk at least in part by improving the mechanical properties of bone in a cell- and estrogen receptor-independent manner.
  • HY-122190
    TAK-071

    mAChR Neurological Disease
    TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM.
  • HY-16508
    Ulipristal acetate

    CDB-2914

    Progesterone Receptor Autophagy Endocrinology Cancer
    Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma.
  • HY-11048
    NS11394

    GABA Receptor Neurological Disease
    NS11394 is a potent and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of alpha(5) > alpha(3) > alpha(2) > alpha(1) at GABA(A) alpha subunit-containing receptors.
  • HY-W011100
    Cyclofenil

    Estrogen Receptor/ERR Influenza Virus Infection Endocrinology
    Cyclofenil is a selective estrogen receptor modulator and an ovulation-inducing agent. Cyclofenil shows an inhibitory effect on dengue virus replication in Vero cells with an EC50 of 1.62 μM. Cyclofenil has anti-dengue-virus activity.
  • 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-126222A
    MitoTam iodide, hydriodide

    Apoptosis Mitochondrial Metabolism Cancer
    MitoTam iodide, hydriodide is a tamoxifen derivative, an electron transport chain (ETC) inhibitor, spreduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology. MitoTam iodide, hydriodide is an effective anticancer agent, suppresses respiratory complexes (CI-respiration) and disrupts respiratory supercomplexes (SCs) formation in breast cancer cells. MitoTam iodide, hydriodide causes apoptosis.
  • HY-15149
    Romidepsin

    FK 228; FR 901228; NSC 630176

    HDAC Apoptosis Cancer
    Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively. Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis.
  • HY-N1243
    Tubulysin B

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin B is a highly cytotoxic peptide and potent microtubule destabilizing agents isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin B has IC50 values in the picomolar range against many cancer cell lines, including those with multidrug resistant properties.Tubulysin B is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • 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-B0097
    Floxuridine

    5-Fluorouracil 2'-deoxyriboside

    Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Bacterial CMV HSV 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-N0155
    Nobiletin

    ROR Reactive Oxygen Species Apoptosis Autophagy Cancer Inflammation/Immunology Neurological Disease
    Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphan receptors (RORs) agonist. Nobiletin can reduce reactive oxygen species (ROS) levels in differentiated C2C12 myotubes and has anti-inflammation and anti-cancer properties, including anti-angiogenesis, anti-proliferation, anti-metastasis and induced apoptosis.
  • HY-13259
    MG-132

    Z-Leu-leu-leu-al

    Proteasome Autophagy Apoptosis Cancer
    MG-132 (Z-Leu-leu-leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis.
  • HY-10221
    Vorinostat

    SAHA; Suberoylanilide hydroxamic acid

    HDAC Autophagy Mitophagy Filovirus Cancer Infection
    Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis. Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification.
  • HY-N7051
    Tubulysin H

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin H 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 H is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • HY-126222
    MitoTam bromide, hydrobromide

    Apoptosis Mitochondrial Metabolism Cancer
    MitoTam bromide, hydrobromide is a tamoxifen derivative, an electron transport chain (ETC) inhibitor, spreduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology. MitoTam bromide, hydrobromide is an effective anticancer agent, suppresses respiratory complexes (CI-respiration) and disrupts respiratory supercomplexes (SCs) formation in breast cancer cells. MitoTam bromide, hydrobromide causes apoptosis.
  • 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-16046
    Rimiducid

    AP1903

    FKBP Apoptosis Cancer
    Rimiducid (AP1903) is a dimerizer agent that acts by cross-linking the FKBP domains. Rimiducid (AP1903) dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis.
  • HY-121410
    Narasin

    Bacterial Parasite NF-κB Antibiotic Cancer Infection
    Narasin is a cationic ionophore and coccidiostat agent. Narasin inhibits NF-κB signaling and induces tumor cells apoptosis. Narasin has antimicrobial and anticancer activity.
  • HY-116514
    (S)-(−)-Perillyl alcohol

    Apoptosis Endogenous Metabolite Cancer
    (S)-(−)-Perillyl alcohol is a monoterpene found in lavender, inhibits farnesylation of Ras, upregulates the mannose-6-phosphate receptor and induces apoptosis. Anti-cancer activity.
  • HY-N0909
    Notoginsenoside R2

    20(S)-Notoginsenoside R2; Ginsenoside Ng-R2

    Others Neurological Disease
    Notoginsenoside R2 is a newly isolated notoginsenoside from Panax notoginseng, showed neuroprotective effects against 6-OHDA-induced oxidative stress and apoptosis.
  • HY-N2632
    Uvarigrin

    Apoptosis Cancer
    Uvarigrin, isolated from the roots of Uvaria calamistrata, induces tumor multidrug resistance cell apoptosis and triggers Caspase-9 activation.
  • 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-107324
    β-Elemene

    (-)-β-Elemene; Levo-β-elemene

    Apoptosis Cancer
    β-Elemene ((-)-β-Elemene; Levo-β-elemene) is isolated from natural plant Curcuma wenyujin with an antitumor activity. β-Elemene can induce cell apoptosis.
  • HY-15484
    Pifithrin-α hydrobromide

    Pifithrin hydrobromide; PFTα hydrobromide

    MDM-2/p53 Aryl Hydrocarbon Receptor Ferroptosis Cancer
    Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis. Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor (AhR) agonist.
  • HY-108277
    Ginsenoside F5

    Apoptosis Cancer
    Ginsenoside F5, from crude extracts of flower buds of Panax ginseng, remarkably inhibits the growth of HL-60 cells by the apoptosis pathway.
  • HY-129636A
    GABAB receptor antagonist 1

    GABA Receptor Neurological Disease
    GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.
  • HY-101281A
    (Rac)-VU 6008667

    mAChR Neurological Disease
    (Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC50=1.8 μM, pIC50= 5.75), has high CNS penetration.
  • HY-13580
    Budesonide

    Glucocorticoid Receptor Cancer Inflammation/Immunology
    Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
  • HY-123268
    Ro 363

    Adrenergic Receptor Cardiovascular Disease
    Ro 363 is a potent and highly selective β1-adrenoceptor agonist. RO 363 is an effective inotropic stimulant, and is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility.
  • 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-N6690
    Destruxin B

    Bcl-2 Family Caspase Apoptosis Cancer Infection
    Destruxin B, isolated from entomopathogenic fungus Metarhizium anisopliae, is one of the cyclodepsipeptides with insecticidal and anticancer activities. Destruxin B induces apoptosis via a Bcl-2 Family-dependent mitochondrial pathway in human nonsmall cell lung cancer cells. Destruxin B significantly activates caspase-3 and reduces tumor cell proliferation through caspase-mediated apoptosis, not only in vitro but also in vivo.
  • HY-N6687B
    Calcimycin hemimagnesium

    A-23187 hemimagnesium; Antibiotic A-23187 hemimagnesium

    Bacterial Fungal Apoptosis Autophagy Cancer Infection
    Calcimycin (A-23187) hemimagnesium is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hemimagnesium induces Ca 2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin hemimagnesium inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hemimagnesium also inhibits the activity of ATPase and uncouples oxidative phosphorylation of mammalian cells. Calcimycin hemimagnesium induces apoptosis.
  • 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-N0718
    Valepotriate

    Valtrate

    Others Cancer Neurological Disease
    Valepotriate, isolated from Valeriana jatamansi Jones, has anti-epileptic and anti-cancer activities.
  • HY-N2596
    Isoscabertopin

    Others Cancer Inflammation/Immunology
    Isoscabertopin is a sesquiterpene lactone isolated from Elephantopus scaber L and shows anti-tumor activities.
  • 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-N5074
    Terrestrosin D

    Apoptosis Cancer
    Terrestrosin D, a steroidal saponin from Tribulus terrestris L., induces cell cycle arrest and cancer cells apoptosis. Terrestrosin D has antiangiogenic activities.
  • HY-N2068
    Didymin

    Apoptosis Cancer
    Didymin, a dietary flavonoid glycoside from citrus fruits, possesses antioxidant properties. Didymin induces apoptosis by inhibiting N-Myc and upregulating RKIP in neuroblastoma.
  • HY-N0168A
    (Rac)-Hesperetin

    p38 MAPK Apoptosis Autophagy Cancer Neurological Disease
    (Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
  • HY-N0330
    Momordin Ic

    Apoptosis Cancer
    Momordin Ic is a principal saponin constituent of Fructus Kochiae, with with anti-cancer bioactivity. Momordin Ic induces apoptosis through oxidative stress-regulated mitochondrial dysfunction.
  • HY-N0011
    Baohuoside I

    Icariin-II; Icariside-II

    CXCR Apoptosis Cancer Inflammation/Immunology Endocrinology
    Baohuoside I, a flavonoid isolated from Epimedium koreanum Nakai, acts as an inhibitor of CXCR4, downregulates CXCR4 expression, induces apoptosis and shows anti-tumor activity.
  • HY-100844
    GS-444217

    MAP3K Apoptosis Cancer
    GS-444217 is a potent, orally available and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87 nM.
  • HY-17537
    APY29

    IRE1 Cancer
    APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain.
  • HY-N0029
    Forsythoside B

    TNF Receptor NF-κB Inflammation/Immunology
    Forsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant for treating inflammatory diseases and promoting blood circulation. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
  • HY-114739
    MA-0204

    PPAR Metabolic Disease
    MA-0204 is a potent, highly selective and orally available peroxisome proliferator activated receptor δ (PPARδ) modulator with EC50s of 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively. Potential treatment for Duchene Muscular Dystrophy (DMD).
  • HY-108523
    LG100754

    UVI 2112

    RAR/RXR Metabolic Disease
    LG100754 (UVI 2112) is a RXR dimers modulater. LG100754 acts as a RXR:RXR homodimer antagonist, but functions as a agonist towards RXR:PPARα and RXR:PPARγ heterodimers. LG100754 is an insulin sensitizer that functions through RXR.
  • HY-105296
    Blarcamesine

    AVex-73; AE-37

    Sigma Receptor mAChR
    Blarcamesine (AVex-73;AE-37) is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome.
  • HY-136151
    UNC10217938A

    Others Others
    UNC10217938A is a 3-deazapteridine analog with strong oligonucleotide enhancing effects. UNC10217938A enhances oligonucleotides effects by modulating their intracellular trafficking and release from endosomes. UNC10217938A also enhances the effects of antisense and siRNA oligonucleotides.
  • HY-135572
    TLX agonist 1

    Others Cancer Neurological Disease
    TLX agonist 1 (ccrp2) is an orphan nuclear receptor tailless (TLX, NR2E1) modulator (EC50=1μM; Kd= 650 nM). TLX agonist 1 potentiates TLX transcriptional repressive activity.
  • HY-114395
    NVS-ZP7-4

    Others Inflammation/Immunology
    NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
  • HY-116819
    VU0453379

    Glucagon Receptor Metabolic Disease
    VU0453379 is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM.
  • HY-N2416
    Taccalonolide A

    Microtubule/Tubulin Apoptosis Cancer
    Taccalonolide A is a microtubule stabilizer, which is a steroid isolated from Tacca chantrieri, with cytotoxic and antimalarial activities. Taccalonolide A causes G2-M accumulation, Bcl-2 phosphorylation and initiation of apoptosis. Taccalonolide A is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug resistance protein 7 (MRP7), with an IC50 of 622 nM for SK-OV-3 cells.
  • 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-N6687A
    Calcimycin hemicalcium salt

    A-23187 hemicalcium salt; Antibiotic A-23187 hemicalcium salt

    Bacterial Fungal Apoptosis Autophagy Antibiotic Cancer Infection
    Calcimycin hemicalcium salt (A-23187 hemicalcium salt) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hemicalcium salt induces Ca 2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin hemicalcium salt inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hemicalcium salt also inhibits the activity of ATPase and uncouples oxidative phosphorylation of mammalian cells. Calcimycin hemicalcium salt induces apoptosis.
  • HY-N1511
    Ganoderic acid D

    Sirtuin Apoptosis Cancer
    Ganoderic acid D, a highly oxygenated tetracyclic triterpenoid, is the major active component of Ganoderma lucidum. Ganoderic acid D upregulates the protein expression of SIRT3 and induces the deacetylated cyclophilin D (CypD) by SIRT3. Ganoderic acid D inhibits the energy reprogramming of colon cancer cells including glucose uptake, lactate production, pyruvate and acetyl-coenzyme production in colon cancer cells. Ganoderic acid D induces HeLa human cervical carcinoma apoptosis.
  • HY-N2360
    Hinokiflavone

    E1/E2/E3 Enzyme Cancer
    Hinokiflavone is a novel modulator of pre-mRNA splicing activity in vitro and in cellulo. Hinokiflavone blocks splicing of pre-mRNA substrates by inhibiting spliceosome assembly, specifically preventing B complex formation. Hinokiflavone is a SUMO protease inhibitor, inhibiting sentrin-specific protease 1 (SENP1) activity.
  • HY-18719D
    Endoxifen E-isomer

    E-Endoxifen

    Estrogen Receptor/ERR Cancer
    Endoxifen E-isomer is the E-isomer of (Z)-Endoxifen. (Z)-Endoxifen, an active metabolite generated via actions of CYP3A4/5 and CYP2D6, is a more potent selective estrogen receptor modulator (SERM) than Tamoxifen.
  • HY-100290
    5-HT1A modulator 1

    5-HT Receptor Neurological Disease
    5-HT1A modulator 1 displays very high affinities for the 5HT1A, adrenergic α1 and dopamine D2 receptor with IC50s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively.
  • HY-113066
    Guanosine 5'-diphosphate

    Endogenous Metabolite Inflammation/Immunology
    Guanosine 5'-diphosphate is a nucleoside diphosphate. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulating the interleukin-6 (IL-6)/stat-3 pathway.
  • HY-116463D
    (Rac)-E1R

    Sigma Receptor Neurological Disease
    (Rac)-E1R (Compound 2) is the racemate of E1R. (Rac)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
  • HY-14569
    CDPPB

    mGluR Neurological Disease
    CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5. CDPPB may provide an approach for development of antipsychotic agents.
  • HY-B0719
    Ingenol Mebutate

    Ingenol 3-angelate; PEP005

    PKC Cancer Inflammation/Immunology
    Ingenol Mebutate is an active ingredient in Euphorbia peplus, acts as a potent PKC modulator, with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively, and has antiinflammatory and antitumor activity.
  • HY-133558
    VII-31

    E1/E2/E3 Enzyme Apoptosis Cancer
    VII-31 is a potent NEDDylation pathway activator to inhibit the tumor progression in vitro and in vivo. VII-31 induces apoptosis via intrinsic and extrinsic pathways.
  • HY-128366
    Waltonitone

    Apoptosis Cancer
    Waltonitone is a ursane-type pentacyclic triterpene isolated from Gentian waltonii Burkill. Waltonitone significantly inhibits hepatocellular carcinoma cells growth and induces apoptosis in vitro and in vivo.
  • HY-10534
    Voreloxin

    SNS-595; Vosaroxin; AG 7352

    Topoisomerase Apoptosis Cancer
    Voreloxin (SNS-595; Vosaroxin; AG 7352) is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis.
  • HY-N1456
    Panaxydol

    Apoptosis Cancer
    Panaxydol is isolated from Panax ginseng roots. Panaxydol induces mitochondria-mediated apoptosis. Panaxydol has the potential to be an anticancer agent, especially for EGFR-addicted cancer.
  • HY-12287
    YH239-EE

    MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    YH239-EE, ethyl ester of the free carboxylic acid compound YH239, is a potent p53-MDM2 antagonizing and apoptosis-inducing agent.
  • HY-131143
    Cadein1

    Apoptosis Cancer
    Cadein1, an isoquinolinium derivative, leads to a G2/M delay and caspase-dependent apoptosis in cancer cells with non- functional p53.
  • HY-N2193
    Hirsutine

    Apoptosis Cancer Infection
    Hirsutine, an indole alkaloid of Uncaria rhynchophylla, exhibits anti-cancer activity. Hirsutine induces apoptosis and is a potent Dengue virus inhibitor exhibiting low cytotoxicity.
  • HY-15995
    Tubulysin A

    TubA

    Microtubule/Tubulin ADC Cytotoxin Apoptosis Cancer
    Tubulysin A(TubA) is a myxobacterial product that can function as an antiangiogenic agent in many in vitro assays; anti-microtubule, anti-mitotic, an apoptosis inducer, anticancer, anti-angiogenic, and antiproliferative.
  • HY-N4136
    Lonicerin

    Bacterial Infection
    Lonicerin is an anti-algE (alginate secretion protein) flavonoid with inhibitory activity for P. aeruginosa. Lonicerin prevents inflammation and apoptosis in LPS-induced acute lung injury.
  • HY-13281
    PIK-75 hydrochloride

    DNA-PK PI3K Apoptosis Cancer
    PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 hydrochloride induces apoptosis.
  • HY-13001
    Quizartinib

    AC220

    FLT3 Ligand for Target Protein for PROTAC Apoptosis Autophagy Cancer
    Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis.
  • HY-107834
    PIK-75

    DNA-PK PI3K Apoptosis Cancer
    PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 induces apoptosis.
  • HY-127019
    Nigericin

    Sodium Channel NOD-like Receptor (NLR) Bacterial Apoptosis Antibiotic Cancer Infection
    Nigericin is an antibiotic derived from Streptomyces hygroscopicus that act as a K +/H + ionophore, promoting K +/H + exchange across mitochondrial membranes.Nigericin can be a NLRP3 activator that induces the release of IL-1β as a NALP3-dependent manner. Nigericin triggers eryptosis, an effect paralleled by ROS formation, and in part due to induction of oxidative stress. Nigericin triggers apoptosis.
  • HY-P1222
    LL-37, Human

    Bacterial Infection
    LL-37, Human is a 37-residue, amphipathic, cathelicidin-derived antimicrobial peptide, which exhibits a broad spectrum of antimicrobial activity. LL-37, Human could help protect the cornea from infection and modulates wound healing.
  • HY-113066A
    Guanosine 5'-diphosphate disodium salt

    Endogenous Metabolite Inflammation/Immunology
    Guanosine 5'-diphosphate disodium salt is a nucleoside diphosphate. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulating the interleukin-6 (IL-6)/stat-3 pathway.
  • HY-107734
    L 152804

    Neuropeptide Y Receptor Metabolic Disease Endocrinology
    L 152804 is an orally active and selective neuropeptide Y Y5 receptor (NPY5-R) antagonist, with a Ki of 26 nM for hY5. L 152804 causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure.
  • HY-115467
    MitoBloCK-10

    Others Metabolic Disease
    MitoBloCK-10 (MB-10) is the first small molecule modulator to attenuate protein-associated motor (PAM) complex activity. MitoBloCK-10 (MB-10) inhibits Tim44 (C-terminal domain) binding to the precursor and to Hsp70.
  • HY-N4317
    Ethoxysanguinarine

    Apoptosis Cancer
    Ethoxysanguinarine is a benzophenanthridine alkaloid natural product that is mainly found in Macleaya cordata. Ethoxysanguinarine inhibits viability and induces apoptosis of colorectal cancer cells by inhibiting protein phosphatase 2A (CIP2A).
  • HY-N1429
    Taurochenodeoxycholic acid sodium salt

    12-Deoxycholyltaurine sodium salt

    Apoptosis Endogenous Metabolite Inflammation/Immunology
    Taurochenodeoxycholic acid sodium salt (12-Deoxycholyltaurine sodium salt) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid induces apoptosis and shows obvious anti-inflammatory and immune regulation properties.
  • HY-N2121
    Neoisoliquiritigenin

    Apoptosis Cancer
    Neoisoliquiritigenin, isolated from Spatholobus suberectus, inhibits cell proliferation and induces cell apoptosis in breast cancer by directly binding to GRP78 to regulate the β-catenin pathway.
  • HY-P2228
    Chlamydocin

    HDAC Apoptosis Cancer
    Chlamydocin, a fungal metabolite, is a highly potent HDAC inhibitor, with an IC50 of 1.3 nM. Chlamydocin exhibits potent antiproliferative and anticancer activities. Chlamydocin induces apoptosis by activating caspase-3.
  • HY-N2897
    Dihydrokaempferol

    Apoptosis Bcl-2 Family Inflammation/Immunology
    Dihydrokaempferol is isolated from Bauhinia championii (Benth). Dihydrokaempferol induces apoptosis and inhibits Bcl-2 and Bcl-xL expression. Dihydrokaempferol is a good candidate for new antiarthritic drugs.
  • HY-N0564
    Notopterol

    Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Notopterol is a coumarin extracted from N. incisum. Notopterol induces apoptosis and has antipyretic, analgesic and anti-inflammatory effects. Notopterol is used for acute myeloid leukemia (AML).
  • HY-122966
    Desmethylxanthohumol

    Apoptosis Cancer
    Desmethylxanthohumol is a prenylated hydroxychalcone isolated from hop cones (Humulus lupulus L.). Desmethylxanthohumol is a powerful apoptosis inducing agent. Desmethylxanthohumol has antiplasmodial, antiproliferative, and antioxidant bioactivities.
  • HY-18938
    Selonsertib

    GS-4997

    MAP3K Apoptosis Cancer
    Selonsertib, an orally bioavailable, selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.
  • HY-N2027
    Taurochenodeoxycholic acid

    12-Deoxycholyltaurine

    Apoptosis Endogenous Metabolite Inflammation/Immunology
    Taurochenodeoxycholic acid (12-Deoxycholyltaurine) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid induces apoptosis and shows obvious anti-inflammatory and immune regulation properties.
  • HY-N2058
    Neogambogic acid

    Bacterial Apoptosis Cancer Infection
    Neogambogic acid, an active ingredient in garcinia, induces apoptosis and has anticancer effect. Neogambogic acid has significant inhibitory activity toward methicillin-resistant Staphylococcus aureus (MRSA).
  • HY-14596
    Genistein

    NPI 031L

    EGFR Autophagy Apoptosis Endogenous Metabolite Cancer
    Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis.
  • HY-120508
    Pivanex

    AN-9; Pivalyloxymethyl butyrate

    HDAC Bcr-Abl Apoptosis Cancer Inflammation/Immunology
    Pivanex (AN-9), a derivative of Butyric acid, is an orally active HDAC inhibitor. Pivanex down-regulates bcr-abl protein and enhances apoptosis. Pivanex has antimetastic and antiangiogenic properties.
  • HY-N0513
    Loganic acid

    Others Inflammation/Immunology Cardiovascular Disease
    Loganic acid is an iridoid isolated from cornelian cherry fruits. Loganic acid can modulate diet-induced atherosclerosis and redox status. Loganic acid has strong free radical scavenging activity and remarkable cyto-protective effect against heavy metal mediated toxicity.
  • HY-128584
    VU6005806

    AZN-00016130

    mAChR Neurological Disease
    VU6005806 (AZN-00016130) is a potent muscarnic acethylcholine receptor subtype 4 (M4) positive allosteric modulator (PAM), with EC50s of 94 nM, 28 nM, 87 nM and 68 nM for human, rat, dog and cyno M4, respectively. Used in the research of neuropsychiatric disorders.
  • HY-P1303
    CART(62-76)(human,rat)

    5-HT Receptor Neurological Disease
    CART(62-76)(human,rat) is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain.
  • HY-14418
    VU0361737

    ML-128

    mGluR Neurological Disease
    VU 0361737 (ML-128) is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors.
  • HY-10936
    S 18986

    iGluR Neurological Disease
    S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests.
  • HY-123956
    HG-12-6

    IRAK Inflammation/Immunology
    HG-12-6 is a type II inhibitor of IRAK4. HG-12-6 shows preferential binding to unphosphorylated inactive IRAK4 with an IC50 of 165 nM. HG-12-6 can modulate IRAK4 activity in autoimmunity and inflammation.
  • HY-106901A
    Asoxime dichloride

    HI-6

    nAChR Neurological Disease
    Asoxime dichloride (HI-6) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride involves in modulating immunity response. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system.
  • 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-14804A
    Tasisulam sodium

    LY 573636 sodium

    Apoptosis Cancer
    Tasisulam is a anticancer agent and induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death. Tasisulam inhibits mitotic progression and induces vascular normalization.
  • HY-100599
    Urolithin A

    Drug Metabolite Reactive Oxygen Species DNA/RNA Synthesis Autophagy Apoptosis Endogenous Metabolite Cancer
    Urolithin A, a gut-microbial metabolite of ellagic acid, exerts anti-inflammatory, antiproliferative, and antioxidant properties. Urolithin A induces autophagy and apoptosis, suppresses cell cycle progression, and inhibits DNA synthesis.
  • HY-N2281
    Leachianone A

    Apoptosis Cancer Inflammation/Immunology
    Leachianone A, isolated from Radix Sophorae, has anti-malarial, anti-inflammatory, and cytotoxic potent. Leachianone A induces apoptosis involved both extrinsic and intrinsic pathways.
  • HY-33350
    Clofilium tosylate

    Potassium Channel Apoptosis Cancer Cardiovascular Disease
    Clofilium tosylate, a potassium channel blocker, induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3. Antiarrhythmic agent.
  • HY-N0332
    Ziyuglycoside II

    Reactive Oxygen Species Apoptosis Cancer Inflammation/Immunology
    Ziyuglycoside II is a triterpenoid saponin compound extracted from Sanguisorba officinalis L.. Ziyuglycoside II induces reactive oxygen species (ROS) production and apoptosis. Anti-inflammation and anti-cancer effect.
  • HY-14804
    Tasisulam

    LY 573636

    Apoptosis Cancer
    Tasisulam is a anticancer agent and induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death. Tasisulam inhibits mitotic progression and induces vascular normalization.
  • HY-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-N4323
    14-Deoxyandrographolide

    Others Metabolic Disease
    14-Deoxyandrographolide, a bioactive compound of Andrographis paniculata, has hepatoprotective efficacy. 14-Deoxyandrographolide desensitizes hepatocytes to TNF-α-mediated apoptosis through the release of TNFRSF1A release.
  • HY-122487
    Troriluzole

    BHV-4157

    Others Neurological Disease
    Troriluzole, a third-generation, tripeptide prodrug of Riluzole (HY-B0211), is an orally active glutamate modulator. Troriluzole reduces synaptic glutamate level and increases the synaptic glutamate absorption. Troriluzole has the potential for Alzheimer disease and generalized anxiety disorder (GAD).
  • HY-110155A
    (Rac)-LM11A-31 dihydrochloride

    Others Neurological Disease
    (Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist.
  • HY-P1222A
    LL-37, Human TFA

    Bacterial Infection
    LL-37, Human TFA is a 37-residue, amphipathic, cathelicidin-derived antimicrobial peptide, which exhibits a broad spectrum of antimicrobial activity. LL-37, Human TFA could help protect the cornea from infection and modulates wound healing.
  • 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-112163
    Zotatifin

    eFT226

    Eukaryotic Initiation Factor (eIF) SARS-CoV Apoptosis Cancer
    Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM) and interferes with the assembly of the eIF4F initiation complex. Zotatifin shows robust antiviral effects, it effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis (IC90=37 nM). Zotatifin induces cell apoptosis.
  • HY-128359
    ACBI1

    PROTAC Epigenetic Reader Domain Apoptosis Cancer
    ACBI1 is a potent PROTAC degrader of BAF ATPase subunits SMARCA2 and SMARCA4, also degrades the polybromo-associated BAF (PBAF) complex member PBRM1, with DC50s of 6 nM, 11 nM and 32 nM for SMARCA2, SMARCA4 and PBRM1 in MV-4-11 cells, respectively. ACBI1 is composed of a bromodomain ligand, a linker, and the E3 ubiquitin ligase VHL. ACBI1 can induce anti-proliferative effects and apoptosis.
  • HY-101287
    MPT0B392

    Microtubule/Tubulin JNK Apoptosis Caspase Cancer
    MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line.
  • HY-N2369
    Chelidonine

    Apoptosis Influenza Virus Cancer Infection
    Chelidonine is an isoquinoline alkaloid isolated from Chelidonium majus L., causes G2/M arrest and induces caspase-dependent and caspase-independent apoptosis, with anticancer and antiviral activity.
  • HY-114323
    PROTAC FLT-3 degrader 1

    PROTAC FLT3 Apoptosis Cancer
    PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction.
  • HY-N6074
    Soyasapogenol B

    Autophagy Apoptosis Cancer
    Soyasapogenol B, an ingredient of soybean, exerts anti-proliferative, anti-metastatic activities. Soyasapogenol B triggers endoplasmic reticulum stress, which mediates apoptosis and autophagy in colorectal cancer.
  • 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 (Dracohodin perochlorate) inhibits cell proliferation, induces cell cycle arrest and apoptosis .
  • 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-15658
    GSK2801

    Epigenetic Reader Domain Cancer
    GSK2801 is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with Kd values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4.
  • HY-128776
    Antitumor agent-19

    Others Cancer
    Antitumor agent-19 is an antitomor agent targeting tumor-associated macrophages (TAMs) to serve as an effective TAMs modulator. The EC50 values of Antitumor agent-19 in the RAW 264.7 cells and the BMDM cells are 17.18 μM and 18.87 μM, respectively.
  • HY-126145
    S1PR1 modulator 1

    LPL Receptor Inflammation/Immunology
    S1PR1 modulator 1 is a selective S1PR1 inhibitor, with a pIC50 of 7.6, with >40- and >80-fold selectivity, over the other S1PR isoforms S1PR2/3/4.
  • HY-P1303A
    CART(62-76)(human,rat) TFA

    5-HT Receptor Neurological Disease
    CART(62-76)(human,rat) TFA is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) TFA can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain.
  • HY-B0077
    Bendamustine hydrochloride

    SDX-105

    DNA Alkylator/Crosslinker Apoptosis Cancer
    Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties.
  • HY-N6681
    15-Acetoxyscirpenol

    Caspase Bacterial Apoptosis Antibiotic Infection
    15-acetoxyscirpenol, one of acetoxyscirpenol moiety mycotoxins (ASMs), strongly induces apoptosis and inhibits Jurkat T cell growth in a dose-dependent manner by activating other caspases independent of caspase-3.
  • HY-N4202
    Dihydrorotenone

    Mitochondrial Metabolism Apoptosis Neurological Disease
    Dihydrorotenone, a natural pesticide, is a potent mitochondrial inhibitor. Dihydrorotenone probably induces Parkinsonian syndrome. Dihydrorotenone induces human plasma cell apoptosis by triggering endoplasmic reticulum stress and activating p38 signaling pathway.
  • HY-100628A
    Mafosfamide sodium salt

    Z 7557 sodium salt; cis-Mafosfamide sodium salt

    DNA/RNA Synthesis DNA Alkylator/Crosslinker Apoptosis Cancer
    Mafosfamide sodium salt (Z 7557 sodium salt) targets nuclear DNA, forms DNA cross-links and inhibits DNA synthesis. Mafosfamide sodium salt, a cyclophosphamide analogue, induces apoptosis in lymphoblastoid cells. Mafosfamide sodium salt has antitumor activity.
  • HY-N6012
    Alkannin

    Apoptosis Cancer Inflammation/Immunology
    Alkannin, found in Alkanna tinctoria, is used as a food coloring. Alkannin shows anticancer activity, arrests cell cycle, and induces apoptosis. Alkannin improves hepatic inflammation in a Rho-kinase pathway.
  • HY-N7523
    Neoxanthin

    DNA/RNA Synthesis Apoptosis Cancer
    Neoxanthin is a major xanthophyll carotenoid and a precursor of the plant hormone abscisic acid in dark green leafy vegetables. Neoxanthin is a potent antioxidant and light-harvesting pigment. Neoxanthin induces apoptosis and has anticancer actions.
  • HY-N0194
    Asiatic acid

    Apoptosis Parasite Cancer Inflammation/Immunology
    Asiatic acid, a pentacyclic triterpene found in Centella asiatica, induces apoptosis in melanoma cells. Asiatic acid has the potential for skin cancer treatment. Asiatic acid also has anti-inflammatory activities.
  • HY-N1472
    Levistolide A

    Apoptosis Cancer
    Levistolide A (LA), a natural compound isolated from the traditional Chinese herb Ligusticum chuanxiong Hort, is used for treating cancer. Levistolide A can induce apoptosis via ROS-mediated ER stress pathway.
  • HY-111879
    Biotin-BS

    SNIPER Cancer
    Biotin-BS contains two different ligands, methyl-bestatin (MeBS) for cIAP1 and biotin, which are connected by linkers. MeBS as a ligand for cellular inhibitor of apoptosis protein 1 (cIAP1) ubiquitin ligase.
  • HY-N6258
    Kahweol

    AMPK Apoptosis Metabolic Disease
    Kahweol is one of the consituents of the coffee from Coffea Arabica with anti-inflammatory anti-angiogenic, and anti-cancerous activities. Kahweol inhibits adipogenesis and increase glucose uptake by AMP-activated protein kinase (AMPK) activation. Kahweol induces apoptosis.
  • HY-N0048
    Polyphyllin II

    Apoptosis Cancer
    Polyphyllin II is one of the most significant saponins in Rhizoma Paridis and has toxic effects on kinds of cancer cells. Polyphyllin II induces apoptosis through caspases activation and cell-cycle arrest.
  • HY-18633
    MDK83190

    Apoptosis Cancer
    MDK83190 is a potent apoptosis activator, induces Apaf-1 oligomerization, increases procaspase-9 processing and subsequent caspase-3 activation in a cyto c-dependent Manner.
  • HY-B2054
    Tebufenozide

    Apoptosis Others
    Tebufenozide is a nonsteroidal ecdysone agonist used to control pest. Tebufenozide has cytotoxic and induces apoptosis in HeLa and insect Tn5B1-4 cells.
  • HY-108431
    MN58b

    Apoptosis Cancer
    MN58b is a selective choline kinase α (CHKα) inhibitor, and results in inhibition of phosphocholine synthesis. MN58b reduces cell growth through the induction of apoptosis, and also has antitumoral activity.
  • HY-111617
    BTR-1

    Apoptosis Cancer
    BTR-1 is an active anti-cancer agent, causes S phase arrest, and affects DNA replication in leukemic cells. BTR-1 activates apoptosis and induces cell death.
  • HY-15141
    Staurosporine

    Antibiotic AM-2282; STS; AM-2282

    PKC PKA Apoptosis Bacterial Fungal Antibiotic Cancer Infection
    Staurosporine is a potent and non-selective inhibitor of protein kinases with IC50s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively. Staurosporine is an apoptosis inducer.
  • HY-12150
    CCMI

    nAChR Neurological Disease
    CCMI is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases with cognitive dysfunction.
  • HY-P1397
    RVD-Hpα

    Cannabinoid Receptor
    RVD-Hpα is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα increases intracellular Ca 2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα also high affinity CB2 positive allosteric modulator (Ki=50 nM).
  • HY-14417B
    VU0155041 sodium

    mGluR Neurological Disease
    VU0155041 sodium is a potent, selective and mixed allosteric agonist/positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 sodium is a partial agonist of mGluR4 that activates the receptor by interacting with a site that is distinct from the glutamate binding site.
  • HY-112306
    Ripretinib

    DCC-2618

    c-Kit PDGFR FLT3 VEGFR Apoptosis Cancer
    Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2). DCC-2618 exerts antineoplastic effect and induces apoptosis.
  • HY-101198
    Clobenpropit dihydrobromide

    Histamine Receptor Cancer Neurological Disease
    Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM). Clobenpropit dihydrobromide increases apoptosis.
  • HY-122575
    Aurintricarboxylic acid

    P2X Receptor Influenza Virus Topoisomerase Infection Inflammation/Immunology Neurological Disease
    Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway.
  • HY-N2503
    Ginsenoside F4

    Apoptosis MMP Inflammation/Immunology
    Ginsenoside F4 (GF4), ginseng saponinis, isolated from notoginseng or red ginseng. Ginsenoside F4 (GF4) has inhibitory effect on human lymphocytoma JK cell by inducing its apoptosis. Ginsenoside F4 (GF4) inhibits matrix metalloproteinase 13 (MMP 13) expression in IL-1β-treated chondrocytes and blocks cartilage breakdown in rabbit cartilage tissue culture, shows therapeutic potential for preventing cartilage collagen matrix breakdown in diseased tissues.
  • HY-111878
    BzNH-BS

    SNIPER Cancer
    BzNH-BS contains two different ligands, methyl-bestatin (MeBS) for cIAP1 and benzoyl-amide, which are connected by linkers. MeBS as a ligand for cellular inhibitor of apoptosis protein 1 (cIAP1) ubiquitin ligase.
  • HY-N0770
    Isoliensinine

    Apoptosis Cancer Inflammation/Immunology
    Isoliensinine is a bisbenzylisoquinoline alkaloid extracted from the seed embryo of Nelumbo nucifera, with anti-oxidant and anti-inflammatory and anti-cancer activities. Isoliensinine induces apoptosis in triple-negative human breast cancer cells.
  • HY-N0730
    Diosgenin glucoside

    Autophagy Inflammation/Immunology Neurological Disease
    Diosgenin glucoside, a saponin compound extracted from Tritulus terrestris L., provides neuroprotection by regulating microglial M1 polarization. Diosgenin glucoside protects against spinal cord injury by regulating autophagy and alleviating apoptosis .
  • 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-N3797A
    Echitamine chloride

    Apoptosis Cancer
    Echitamine chloride is the major monoterpene indole alkaloid present in Alstonia with potent anti-tumour activity. Echitamine chloride induces DNA fragmentation and cells apoptosis. Echitamine chloride inhibits pancreatic lipase with an IC50 of 10.92 µM.
  • 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-N2490
    Dehydrotrametenolic acid

    Caspase Cancer Inflammation/Immunology
    Dehydrotrametenolic acid is a sterol isolated from the sclerotium of Poria cocos. Dehydrotrametenolic acid induces apoptosis through caspase-3 pathway. Dehydrotrametenolic acid has anti-tumor activity, anti-inflammatory, anti-diabetic effects.
  • HY-N1402
    Oxysophoridine

    Sophoridine N-oxide

    Others Inflammation/Immunology
    Oxysophoridine (Sophoridine N-oxide) is a bioactive alkaloid extracted from the Sophora alopecuroides Linn. Oxysophoridine (Sophoridine N-oxide) shows anti inflammatory, anti oxidative stress and anti apoptosis effects.
  • 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-N0800
    Protosappanin B

    (-)-Protosappanin B

    Apoptosis Cancer
    Protosappanin B is a phenolic compound extracted from Lignum Sappan. Anti-cancer activity. Protosappanin B induces apoptosis and causes G1 cell cycle arrest in human bladder cancer cells.
  • HY-N1988
    Cucurbitacin IIa

    Hemslecin A

    Survivin Apoptosis Cancer
    Cucurbitacin IIa is a triterpene isolated from Hemsleya amalils Diels, induces apoptosis of cancer cells, reduces expression of survivin, reduces phospho-Histone H3 and increases cleaved PARP in cancer cells.
  • HY-101021
    Ascochlorin

    Ilicicolin D

    STAT Apoptosis Cancer Inflammation/Immunology
    Ascochlorin (Ilicicolin D), an isoprenoid antibiotic, mediates its anti-tumor effects predominantly through the suppression of STAT3 signaling cascade. Ascochlorin induces apoptosis. Anti-inflammatory activity.
  • HY-129636
    (E)-GABAB receptor antagonist 1

    GABA Receptor Neurological Disease
    (E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM.
  • HY-N4098
    Incensole Acetate

    Apoptosis Neurological Disease
    Incensole acetate is a main constituent of Boswellia carterii resin, has neuroprotective effects against neuronal damage in traumatic and ischemic head injury. Incensole acetate reduces Aβ25–35-triggered apoptosis in hOBNSCs.
  • HY-13567
    Bendamustine

    SDX-105 free base

    DNA Alkylator/Crosslinker Apoptosis Cancer
    Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activats DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties.
  • HY-13520
    Nocodazole

    Oncodazole; R17934

    Microtubule/Tubulin Bcr-Abl CRISPR/Cas9 Autophagy Apoptosis Cancer
    Nocodazole is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, and activates CRISPR/Cas9.
  • HY-N1925
    Tea polyphenol

    Others Cancer Inflammation/Immunology
    Tea polyphenol is the floorboard of phenolic compounds in tea. Tea polyphenol exhibits biological activity including antioxidant and anti-cancer activities, inhibition of cell proliferation, induction of apoptosis, cell cycle arrest and modulation of carcinogen metabolism.
  • HY-N0605
    Ginsenoside Rh2

    20(S)-Ginsenoside Rh2; 20(S)-Rh2; Ginsenoside-Rh2

    Caspase Apoptosis Endogenous Metabolite Cancer
    Ginsenoside Rh2 is isolated from the root of Ginseng. Ginsenoside Rh2 induces the activation of caspase-8 and caspase-9. Ginsenoside Rh2 induces cancer cell apoptosis in a multi-path manner.
  • HY-125466
    cRIPGBM

    RIP kinase Apoptosis Cancer
    cRIPGBM, a proapoptotic derivative of RIPGBM, a cell type-selective inducer of apoptosis in GBM cancer stem cells (CSCs) by binding to receptor-interacting protein kinase 2 (RIPK2), with an EC50 of 68 nM in GBM-1 cells.
  • HY-133554
    ASK1-IN-1

    p38 MAPK Inflammation/Immunology
    ASK1-IN-1 is a CNS-penetrant ASK1 (apoptosis signal-regulating kinase 1) inhibitor, with good potency (cell IC50=138 nM; Biochemical IC50=21 nM).
  • HY-12048
    Chelerythrine chloride

    PKC Bcl-2 Family Apoptosis Autophagy Cancer Metabolic Disease Inflammation/Immunology
    Chelerythrine chloride is a potent, cell-permeable inhibitor of protein kinase C, with an IC50 of 660 nM. Chelerythrine chloride inhibits the Bcl-XL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from Bcl-XL. Chelerythrine chloride induces apoptosis and autophagy.
  • HY-N0220
    Dauricine

    NF-κB Apoptosis Cancer Inflammation/Immunology
    Dauricine, a bisbenzylisoquinoline alkaloid in Asiatic Moonseed Rhizome, possesses anti-inflammatory activity. Dauricine inhibits cell proliferation and invasion, and induces apoptosis by suppressing NF-κB activation in a dose- and time-dependent manner in colon cancer.
  • HY-B0849
    Azoxystrobin

    Fungal Reactive Oxygen Species Apoptosis
    Azoxystrobin is a broad-spectrum β-methoxyacrylate fungicide. Azoxystrobin inhibits mitochondrial respiration by binding to the Qo site of the cytochrome bc1 complex and inhibiting electron transfer. Azoxystrobin induces the production of reactive oxygen species (ROS) and induces cell apoptosis.
  • HY-100548
    GSK621

    AMPK Autophagy Apoptosis Cancer
    GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation.
  • HY-N6740
    Beta-Zearalanol

    Apoptosis Metabolic Disease
    Beta-Zearalenol is an mycotoxin produced by Fusarium spp, which causes apoptosis and oxidative stress in mammalian reproductive cells. Beta-Zearalenol is the derivative of zearalenone (ZEA) which can conjugate with glucuronic acid.
  • HY-N6777
    Penicillic acid

    Caspase Bacterial Apoptosis Antibiotic Cancer Infection
    Penicillic acid is a polyketide mycotoxin produced by several species of Aspergillus and Penicillium, which exhibits cytotoxicity in rat alveolar macrophages (AM) in vitro. Penicillic acid inhibits Fas ligand-induced apoptosis by blocking self-processing of caspase-8.
  • HY-14611
    3,3'-Difluorobenzaldazine

    DFB

    mGluR Neurological Disease
    3,3'-Difluorobenzaldazine (DFB) is a selective positive allosteric modulator of mGluR5. 3,3'-Difluorobenzaldazine potentiates 3- to 6-fold action for mGlu5 agonists (Glutamate, Quisqualate, and 3,5-Dihydroxyphenylglycine), with EC50s in the 2 to 5 μM range.
  • HY-B0723S
    Ospemifene D4

    FC-1271a D4

    Estrogen Receptor/ERR Cancer
    Ospemifene D4 (FC-1271a D4) is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects.
  • HY-120789
    PF-06648671

    γ-secretase Neurological Disease
    PF-06648671 is a novel, brain‐penetrable, and orally active γ‐secretase modulator (GSM). PF-06648671 reduces Aβ42 and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro. PF-06648671 is used for the study of Alzheimer’s disease.
  • HY-117639
    AUT1

    Potassium Channel Cancer
    AUT1 is a Kv3 potassium channel modulator, with pEC50s of 5.33 and 5.31 for human recombinant Kv3.1b and Kv3.2a, respectively, exhibits 10-fold lower potency at human recombinant Kv3.3 channel (pEC50, 4.5).
  • 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-14600
    Rosiglitazone maleate

    BRL 49653C

    PPAR TRP Channel Autophagy Ferroptosis Cancer Metabolic Disease Inflammation/Immunology
    Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
  • HY-124614
    GLP-26

    HBV Infection
    GLP-26 is a HBV capsid assembly modulators (CAM), inhibits HBV DNA replication in Hep AD38 system (IC50=3 nM), and reduces cccDNA by >90% at 1 μM. GLP-26 disrupts the encapsidation of pre-genomic RNA, causes nucleocapsid disassembly and reduces cccDNA pools.
  • HY-110279
    Ogerin

    Others Neurological Disease
    Ogerin is a selective GPR68 positive allosteric modulator, with a pEC50 of 6.83. Ogerin shows inverse agonist and antagonist activity (Ki, 220 nM) at A2A receptoor and weak antagonist activity (Ki, 736 nM) at 5-HT2B receptor. Ogerin blocks recall in fear conditioning in mice.
  • HY-104037
    Cintirorgon

    LYC-55716

    ROR Cancer
    Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival.
  • 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-135909
    TH1217

    ZINC1775962367

    SARS-CoV Cancer Infection
    TH1217 (ZINC1775962367) is a potent and selective dCTPase pyrophosphatase 1 (dCTPase) inhibitor, with an IC50 of 47 nM. TH1217 enhances the cytotoxic effect of cytidine analogues in leukemia cells. TH1217 also could modulate SARS-Cov-2 interactors, so it shows activity of against COVID-19.
  • HY-N0313
    Euphol

    Endogenous Metabolite MAGL Inflammation/Immunology
    Euphol is a tetracyclic triterpene alcohol isolated from the sap of Euphorbia tirucalli with anti-mutagenic, anti-inflammatory and immunomodulatory effects, orally active. Euphol inhibits the monoacylglycerol lipase (MGL) activity via a reversible mechanism (IC50=315 nM). MGL inhibition in the periphery modulates the endocannabinoid system to block the development of inflammatory pain.
  • HY-P1397A
    RVD-Hpα TFA

    Cannabinoid Receptor
    RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα TFA increases intracellular Ca 2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα TFA also high affinity CB2 positive allosteric modulator (Ki=50 nM).
  • HY-115579
    MALAT1-IN-1

    Others Cancer
    MALAT1-IN-1 (compounds 5) is a potent and specific Malat1 (Metastasis-associated lung adenocarcinoma transcript 1) inhibitor. MALAT1-IN-1 modulated Malat1 downstream genes in a dose-dependent manner without affecting expression of nuclear enriched abundant transcript 1 (Neat1) .
  • HY-119931
    2-Hydroxychalcone

    Bcl-2 Family Apoptosis NF-κB Cancer Metabolic Disease
    2-hydroxychalcone, a natural flavonoid, is a potent antioxidant, inhibiting lipid peroxidation. 2-Hydroxychalcone induces apoptosis by Bcl-2 downregulation. 2-Hydroxychalcone inhibits the activation of NF-kB.
  • HY-N3005
    Britannin

    Apoptosis Autophagy Cancer Inflammation/Immunology
    Britannin, isolated from Inula aucheriana, is a sesquiterpene lactone. Britannin induces apoptosis and autophagy by activating AMPK regulated by ROS in liver cancer cells. Britannin has anti-proliferative and anti-inflammatory activities.
  • HY-12033
    2-Methoxyestradiol

    2-ME2; NSC-659853

    Apoptosis Microtubule/Tubulin Autophagy Endogenous Metabolite Cancer
    2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules.
  • HY-N7045
    Isosilybin B

    Androgen Receptor Apoptosis Cancer
    Isosilybin B, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation.
  • HY-N3014
    Bruceine D

    Notch Apoptosis Cancer Infection
    Bruceine D is a Notch inhibitor with anti-cancer activity and induces apoptosis in several human cancer cells. Bruceine D is an effective botanical insect antifeedant with outstanding systemic properties, causing potent pest growth inhibitory activity.
  • 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-116506
    Bigelovin

    RAR/RXR Reactive Oxygen Species Apoptosis Autophagy Cancer
    Bigelovin, a sesquiterpene lactone isolated from Inula helianthus-aquatica, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.
  • HY-N1373
    Sophoridine

    Apoptosis Cancer
    Sophoridine is a quinolizidine alkaloid isolated from leafs of Leguminous plant Sophora alopecuroides.L. Sophoridine induces apoptosis. Sophoridine has the potential to be a novel, potent and selective antitumor drug candidate for pancreatic cancer with well-tolerated toxicity.
  • HY-100761
    SS28

    Microtubule/Tubulin Apoptosis Cancer
    SS28, a SRT501 analog with oral bioavailability, inhibits tubulin polymerization to cause cell cycle arrest at G2/M phase. SS28 results in apoptosis rather than necrosis tubulin.
  • HY-N5058
    Dehydroeffusol

    Apoptosis Cancer
    Dehydroeffusol is a phenanthrene from medicinal herb Juncus effuses. Dehydroeffusol inhibits gastric cancer cell growth and tumorigenicity by selectively inducing tumor-suppressive endoplasmic reticulum stress and a moderate apoptosis. It shows very low toxicity.
  • HY-114162A
    VTP50469 fumarate

    Epigenetic Reader Domain Apoptosis Cancer
    VTP50469 fumarate is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 fumarate has potently anti-leukemia activity.
  • HY-114162
    VTP50469

    Epigenetic Reader Domain Apoptosis Cancer
    VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 has potently anti-leukemia activity.
  • HY-N6073
    Soyasapogenol A

    Others Inflammation/Immunology
    Soyasapogenol A, a triterpene compound, isolated from the roots of Abrus cantoniensis. Soyasapogenol A directly prevents apoptosis of hepatocytes, and secondly, inhibits the elevation of plasma TNF-α, which consequently results in the prevention of liver damage in the Concanavalin A-induced hepatitis model.
  • HY-111183
    Neocarzinostatin

    DNA/RNA Synthesis Bacterial Apoptosis Antibiotic Cancer Infection
    Neocarzinostatin, a potent DNA-damaging, anti-tumor antibiotic, recognizes double-stranded DNA bulge and induces DNA double strand breaks (DSBs). Neocarzinostatin induces apoptosis. Neocarzinostatin has potential for EpCAM-positive cancers treatment .
  • 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-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-N0162
    Luteolin

    Luteoline; Luteolol; Digitoflavone

    Apoptosis Autophagy Endogenous Metabolite Cancer Inflammation/Immunology
    Luteolin (Luteolol) is a flavanoid with 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-112885A
    nor-NOHA acetate

    Nω-Hydroxy-nor-L-arginine acetate

    Arginase Apoptosis Cancer Metabolic Disease Inflammation/Immunology
    nor-NOHA acetate (Nω-Hydroxy-nor-L-arginine acetate) is a specific and reversible arginase inhibitor, induces apoptosis in ARG2-expressing cells under hypoxia but not normoxia. Anti-leukemic activity, effective in endothelial dysfunction, immunosuppression and metabolism.
  • 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-N2135
    Puerarin 6''-O-Xyloside

    Apoptosis Cancer Inflammation/Immunology
    Puerarin 6''-O-Xyloside, isolated from radix of Pueraria lobata (Willd.), possesses snti-osteoporotic and anti-tumor activity. Puerarin 6''-O-Xyloside induces the mitochondria-mediated apoptosis pathway..
  • HY-N5106
    (E)-Flavokawain A

    Apoptosis Cancer
    (E)-Flavokawain A, a chalcone extracted from Kava, has anticarcinogenic effect. (E)-Flavokawain A induces apoptosis in bladder cancer cells by involvement of bax protein-dependent and mitochondria-dependent apoptotic pathway and suppresses tumor growth in mice.
  • HY-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-N6576
    Hellebrigenin

    Apoptosis Cancer
    Hellebrigenin, one of bufadienolides belonging to cardioactive steroids, is isolated from traditional Chinese medicine Venenum Bufonis. Hellebrigenin induces DNA damage and cell cycle G2/M arrest. Hellebrigenin triggers mitochondria-mediated apoptosis.
  • 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-100513A
    Dehydroaltenusin

    Apoptosis DNA/RNA Synthesis Cancer
    Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM). Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis. Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo.
  • HY-126248
    Tankyrase-IN-2

    PARP Cancer
    Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model.
  • HY-P2076
    Dusquetide

    SGX942

    Bacterial Cancer Infection
    Dusquetide (SGX942) is a first-in-class innate defense regulator (IDR). Dusquetide modulates the innate immune response to both PAMPs and DAMPs by binding to p62. Dusquetide shows activity in both reducing inflammation and increasing clearance of bacterial infection. DAMPs: damage-associated molecular patterns; PAMPs: pathogen-associated molecular patterns
  • HY-123489
    3α,21-Dihydroxy-5α-pregnan-20-one

    THDOC

    GABA Receptor
    3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
  • HY-126327
    UNC4976

    Histone Methyltransferase Cancer
    UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA.
  • HY-N6706
    Enniatin complex

    Bacterial Acyltransferase Apoptosis Cancer Infection
    Enniatin complex is a mixture of cyclohexadepsipeptides isolated largely from Fusarium species of fungi, and has ionophoric, antibiotic, and in vitro hypolipidaemic properties. Enniatin complex inhibits enzymes like acyl-CoA: cholesterol acyl transferase and induces apoptosis in several cancer lines .
  • 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-N1453
    Hypocrellin B

    Apoptosis Cancer Infection
    Hypocrellin B, a pigment isolated from the fungi Hypocrella bambusae and Shiraia bambusicola, is an apoptosis inducer. Hypocrellin B can be used as a photosensitizer for photodynamic therapy of cancer. Hypocrellin B also has antimicrobial and antileishmanial activities.
  • 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-P1841
    Glucagon-Like Peptide (GLP) II, human

    Endogenous Metabolite Metabolic Disease
    Glucagon-Like Peptide (GLP) II, human is a 33-amino acid peptide derived from the C-terminal of proglucagon and mainly produced by the intestinal L cells. Glucagon-Like Peptide (GLP) II, human stimulates intestinal mucosal growth and decreases apoptosis of enterocytes .
  • HY-N6674
    Diazepinomicin

    ECO-4601; TLN-4601; BU 4664L

    Ras Apoptosis Cancer
    Diazepinomicin (TLN-4601) is a secondary metabolite produced by Micromonospora sp. Diazepinomicin (TLN-4601) inhibits the EGF-induced Ras-ERK MAPK signaling pathway and induces apoptosis. An anti-tumor agent for K-Ras mutant models.
  • HY-122661
    Mefuparib hydrochloride

    MPH

    PARP Apoptosis Cancer
    Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo.
  • 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-N6011
    9-Methoxycamptothecin

    Topoisomerase Apoptosis Cancer
    9-Methoxycamptothecin (MCPT), isolated from Nothapodytes foetida, has antitumor activities through topoisomerase inhibition. 9-Methoxycamptothecin (MCPT) induces strong G2/M arrest and apoptosis in cancer.
  • 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-N2342
    Procyanidin C1

    Apoptosis Cancer
    Procyanidin C1 is a natural polyphenol, causes DNA damage, cell cycle arrest, and induces apoptosis. Procyanidin C1 decreases the level of Bcl-2, but enhances BAX, caspase 3 and 9 expression in cancer 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-N2454
    β-Elemonic acid

    Apoptosis Reactive Oxygen Species COX Cancer Inflammation/Immunology
    β-Elemonic acid is a triterpene isolated from Boswellia papyrifera. β-Elemonic acid induces cell apoptosis, reactive oxygen species (ROS) and COX-2 expression and inhibits prolyl endopeptidase. β-Elemonic acid exhibits anticancer and anti-inflammatory effects.
  • 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-120394
    TVB-3166

    Fatty Acid Synthase (FASN) Apoptosis Cancer
    TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC50s of 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth.
  • 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-126741
    Azadirachtin

    Apoptosis Others
    Azadirachtin, one of the most promising botanical insecticides, is widely used for pest control. Azadirachtin induces apoptosis in insect cell lines, including Sf9, SL-1 and BTI-Tn-5B1-4.
  • HY-N5001
    Euphorbia Factor L2

    Apoptosis Cancer
    Euphorbia factor L2, a lathyrane diterpenoid isolated from caper euphorbia seed (the seeds of Euphorbia lathyris L.), has been traditionally applied to treat cancer. Euphorbia factor L2 shows potent cytotoxicity and induces apoptosis via a mitochondrial pathway.
  • HY-N0072
    Brazilin

    Apoptosis Autophagy Cancer Inflammation/Immunology
    Brazilin is a red dye precursor obtained from the heartwood of several species of tropical hardwoods. Brazilin inhibits the cells proliferation, promotes apoptosis, and induces autophagy through the AMPK/mTOR pathway. Brazilin shows chondroprotective and anti-inflammatory activities.
  • HY-100738
    Ubiquitin Isopeptidase Inhibitor I, G5

    NSC144303

    Apoptosis Cancer
    Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively.
  • HY-N0158
    Oxymatrine

    TGF-beta/Smad Influenza Virus Cancer Infection Inflammation/Immunology
    Oxymatrine, an alkaloid from the roots of Sophora species, with anti-inflammatory, antifibrosis, and antitumor effects, inhibits the iNOS expression and TGF-β/Smad pathway. Oxymatrine inhibits bocavirus minute virus of canines (MVC) replication, reduces viral gene expression and decreases apoptosis induced by viral infection.
  • HY-N3376
    Liriodenine

    Spermatheridine; VLT045

    Others Cancer
    Liriodenine (Spermatheridine; VLT045) is an aporphine alkaloid isolated from the plant Mitrephora sirikitiae and has anti-cancer activities. Liriodenine induces cell apoptosis, activates the intrinsic pathway by induction of caspase-3 and caspase-9.
  • HY-119695A
    Simvastatin acid ammonium

    Tenivastatin ammonium

    Endogenous Metabolite Cardiovascular Disease
    Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene.
  • HY-P1216
    HS014

    Melanocortin Receptor Neurological Disease
    HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats.
  • HY-10016
    E 2012

    γ-secretase Neurological Disease
    E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat.
  • HY-116463B
    (2S,3S)-E1R

    Sigma Receptor Neurological Disease
    (2S,3S)-E1R (Compound 2d) is an enantiomer of E1R. (2S,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
  • HY-124634
    PZ-2891

    Others Neurological Disease
    PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively.
  • HY-116463A
    (2R,3S)-E1R

    Sigma Receptor Neurological Disease
    (2R,3S)-E1R (Compound 2c) is an enantiomer of E1R. (2R,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
  • HY-116463C
    (2R,3R)-E1R

    Sigma Receptor Neurological Disease
    (2R,3R)-E1R (Compound 2b) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
  • HY-P2076A
    Dusquetide TFA

    SGX942 TFA

    Bacterial Cancer Infection
    Dusquetide (SGX942) TFA is a first-in-class innate defense regulator (IDR). Dusquetide TFA modulates the innate immune response to both PAMPs and DAMPs by binding to p62. Dusquetide TFA shows activity in both reducing inflammation and increasing clearance of bacterial infection. DAMPs: damage-associated molecular patterns; PAMPs: pathogen-associated molecular patterns
  • HY-W011733
    Tulobuterol hydrochloride

    C-78

    Adrenergic Receptor Influenza Virus Antibiotic Infection Endocrinology Inflammation/Immunology
    Tulobuterol hydrochloride (C-78) is a long-acting β2-adrenoceptor agonist, which reduces the frequency of exacerbations of chronic obstructive pulmonary disease and bronchial asthma. Tulobuterol hydrochloride is also a sympathomimetic agent used as a transdermal patch, increases normal diaphragm muscle strength. Tulobuterol hydrochloride inhibit rhinovirus replication and modulate airway inflammation.
  • HY-114395A
    (R)-NVS-ZP7-4

    Others Inflammation/Immunology
    (R)-NVS-ZP7-4 is the R-isomer of NVS-ZP7-4. NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
  • HY-N6779
    Patulin

    Terinin

    Bacterial Apoptosis Antibiotic Infection
    Patulin (Terinin) is a mycotoxin produced by fungi including the Aspergillus, Penicillium, and Byssochlamys species, is suspected to be clastogenic, mutagenic, teratogenic and cytotoxic. Patulin (Terinin) induces autophagy-dependent apoptosis through lysosomal-mitochondrial axis, and causes DNA damage.
  • 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-N0907
    Ginsenoside Rg6

    NF-κB Apoptosis Cancer Inflammation/Immunology
    Ginsenoside Rg6 is the component isolated from notoginseng. Ginsenoside Rg6 inhibits TNF-α-induced NF-κB transcriptional activity with an IC50 of 29.34±2.22 μM in HepG2 cells. Ginsenoside Rg6 also exhibits apoptosis-inducing effect.
  • HY-100399
    Nevanimibe

    PD-132301; ATR-101

    Acyltransferase Apoptosis Cancer
    Nevanimibe (PD-132301) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe induces cell apoptosis and has the potential for adrenocortical cancer.
  • HY-12842
    UC-112

    IAP 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-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-N4058
    Helichrysetin

    Others 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-128360
    dMCL1-2

    PROTAC Bcl-2 Family Apoptosis Cancer
    dMCL1-2 is a potent and selective degrader of myeloid cell leukemia 1 (MCL1) based on PROTAC, which binds to MCL1 with a KD of 30 nM. dMCL1-2 activats the cellular apoptosis machinery by degradation of MCL1.
  • HY-N2177
    3-Dehydrotrametenolic acid

    Lactate Dehydrogenase Apoptosis Cancer
    3-​Dehydrotrametenolic acid, isolated from the sclerotium of Poria cocos, is a lactate dehydrogenase (LDH) inhibitor. 3-​Dehydrotrametenolic acid promotes adipocyte differentiation in vitro and acts as an insulin sensitizer in vivo. 3-​Dehydrotrametenolic acid induces apoptosis and has anticancer activity.
  • HY-15128
    9-cis-Retinoic acid

    ALRT1057

    RAR/RXR Apoptosis Cancer Inflammation/Immunology Neurological Disease
    9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities.
  • HY-N2166
    Tomatine

    α-Tomatine; Lycopersicin; Tomatin

    Proteasome Neurological Disease
    Tomatine is a glycoalkaloid, found in the tomato plant (Lycopersicon esculentum Mill.). Tomatine elicits neurotoxicity in RIP1 kinase and caspase-independent manner. Tomatine promotes the upregulation of nuclear apoptosis inducing factor (AIF) in neuroblastoma cells. Tomatine also inhibits 20S proteasome activity.
  • HY-100399A
    Nevanimibe hydrochloride

    PD-132301 hydrochloride; ATR101 hydrochloride

    Acyltransferase Apoptosis Cancer
    Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe hydrochloride inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe hydrochloride induces cell apoptosis and has the potential for adrenocortical cancer.
  • HY-N6866
    Gomisin N

    Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Gomisin N, isolated from Schisandra chinensis, produces beneficial sedative and hypnotic bioactivity. Gomisin N has the potential for use in the treatment of allergy. Gomisin N is an anti-cancer drug candidate capable of inhibiting the proliferation and inducing the apoptosis in cancer.
  • HY-N6861
    Lucidenic acid B

    Apoptosis Cancer
    Lucidenic acid B is a natural compound isolated from Ganoderma lucidum, induces apoptosis of cancer cells, and causes the activation of caspase-9 and caspase-3, and cleavage of PARP. Lucidenic acid B does not affect the cell cycle profile, or the number of necrotic cells.
  • 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-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-108638
    NSC 146109 hydrochloride

    MDM-2/p53 Cancer
    NSC 146109 hydrochloride is a small-molecule p53 activator that target MDMX and could be of value in treating breast cancer. NSC 146109 hydrochloride is a pseudourea derivative, promotes breast cancer cells to undergo apoptosis through activating p53 and inducing expression of proapoptotic genes[1].
  • HY-N1306
    Sideroxylin

    Bacterial Reactive Oxygen Species Apoptosis Cancer Infection
    Sideroxylin is a C-methylated flavone isolated from Callistemon lanceolatus and exerts antimicrobial activity against Staphylococcus aureus. Sideroxylin inhibits ovarian cancer cell proliferation and induces apoptosis, causing DNA fragmentation, depolarization of the mitochondrial membrane, the generation of reactive oxygen species (ROS).
  • HY-19980
    PRIMA-1Met

    APR-246

    MDM-2/p53 Autophagy Apoptosis Ferroptosis Cancer
    PRIMA-1Met restores wild-type conformation and function to mutant p53, and triggers apoptosis in tumor cells. PRIMA-1Met also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance.
  • HY-N3417
    Kongensin A

    HSP RIP kinase Apoptosis Cancer Inflammation/Immunology
    Kongensin A is a natural product isolated from Croton kongensis. Kongensin A is an effective, covalent HSP90 inhibitor that blocks RIP3-dependent necroptosishas. Kongensin A is a potent necroptosis inhibitor and an apoptosis inducer. Kongensin A has potential anti-necroptosis and anti-inflammation applications.
  • HY-136657
    SC-43

    STAT Phosphatase Apoptosis Cancer
    SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects.
  • 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-10619B
    Niraparib tosylate

    MK-4827 tosylate

    PARP Apoptosis Cancer
    Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-118342
    PQCA

    mAChR Neurological Disease
    PQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. PQCA has an EC50 value of 49 nM and 135 nM on rhesus and human M1 receptor, respectively, and is inactive for other muscarinic receptors. PQCA improves cognitive performance and cerebral blood flow in rat, cynomolgus macaque, and rhesus macaque. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease.
  • HY-B2163
    Astaxanthin

    PPAR Reactive Oxygen Species Cancer Cardiovascular Disease
    Astaxanthin, a red dietary carotenoid isolated from Haematococcus pluvialis, is a modulator of PPARγ and a potent antioxidant with antiproliferative, neuroprotective and anti-inflammatory activity. Astaxanthin has potential in the study of various diseases, such as cancers and Parkinson’s disease, cardiovascular disease. Due to its bright red colour, Astaxanthin could be used as a food colorant in animal feeds.
  • HY-106225
    Rotigaptide

    ZP123

    Gap Junction Protein Cardiovascular Disease
    Rotigaptide (ZP123) is a novel and specific modulator of connexin 43 (Cx43). Rotigaptide prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress. Rotigaptide is a potent antiarrhythmic peptide (AAP) with improved stability and has the potential for the investigation of cardiac arrhythmias-specifically atrial fibrillation.
  • HY-102070
    NS13001

    Potassium Channel Neurological Disease
    NS13001 is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC50s are 1.8 and 0.14 μM for SK2 and SK3, respectively. NS13001 holds promise as a potential therapeutic agent for treatment of spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias.
  • HY-20878
    Tyrphostin AG 879

    AG 879

    Trk Receptor EGFR Apoptosis Cancer
    Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation (IC50 of 10 μM), but not TrKB and TrKC. Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC50 of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR. Tyrphostin AG 879 has anticancer activity.
  • HY-P1095
    Ivachtin

    Caspase-3 Inhibitor VII

    Caspase Neurological Disease Cardiovascular Disease
    Ivachtin (Caspase-3 Inhibitor VII; compound 7a) is a nonpeptide, noncompetitive and reversibl caspase-3 inhibitor with an IC50 of 23 nM. Ivachtin has modest selectivity for the remaining caspases.
  • HY-15346
    Copanlisib

    BAY 80-6946

    PI3K 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-133121
    WDR5-IN-1

    Histone Methyltransferase Apoptosis Cancer
    WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines.
  • HY-50688
    SB-265610

    CXCR Inflammation/Immunology
    SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC50s of 3.7 nM and 70 nM, respectively.
  • HY-117071
    Dabuzalgron

    Ro 115-1240

    Adrenergic Receptor Endocrinology Cardiovascular Disease
    Dabuzalgron (Ro 115-1240) is an orally active and selective α-1A adrenergic receptor agonist for the treatment of urinary incontinence. Dabuzalgron protects against Doxorubicin-induced cardiotoxicity by preserving mitochondrial function.
  • HY-15346A
    Copanlisib dihydrochloride

    BAY 80-6946 dihydrochloride

    PI3K 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-N3584
    Paris saponin VII

    Chonglou Saponin VII

    Akt p38 MAPK P-glycoprotein Bcl-2 Family Caspase PARP Autophagy 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-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 blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 induces cell apoptosis.
  • 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-W005288
    4-Vinylphenol

    Apoptosis Endogenous Metabolite Cancer
    4-Vinylphenol is found in the medicinal herb Hedyotis diffusa Willd, wild rice and is also the metabolite of p-coumaric and ferulic acid by lactic acid bacteria in wine. 4-Vinylphenol induces apoptosis and inhibits blood vessels formation and suppresses invasive breast tumor growth in vivo.
  • HY-B1899A
    Taurodeoxycholic acid sodium hydrate

    Sodium taurodeoxycholate monohydrate

    Caspase Metabolic Disease Inflammation/Immunology
    Taurodeoxycholic acid sodium hydrate (Sodium taurodeoxycholate monohydrate) prevents apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid sodium hydrate is investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.
  • HY-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-P1216A
    HS014 TFA

    Melanocortin Receptor Neurological Disease
    HS014 TFA is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA modulates the behavioral effects of morphine in mice. HS014 TFA increases food intake in free-feeding rats.
  • HY-131337
    RhlR antagonist 1

    Bacterial Infection
    RhlR antagonist 1 is a potent RhlR antagonist with an IC50 of 26 μM. RhlR antagonist 1 displays selective RhlR antagonism over LasR and PqsR, strong inhibition of biofilm formation in static and dynamic settings, and reduces production of virulence factors such as rhamnolipid and pyocyanin in P. aeruginosa. RhlR antagonist 1 can be utilized for developing QS-modulating molecules in the control of P. aeruginosa infections.
  • HY-B1640
    Ethacrynic acid

    Gutathione S-transferase NF-κB Calcium Channel Cancer Inflammation/Immunology
    Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
  • HY-130609
    Aβ42-IN-1

    γ-secretase Neurological Disease
    Aβ42-IN-1, compound 1v, is a novel, potent and orally active γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC50 value of 0.091 µM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile.
  • HY-121955
    FW1256

    NF-κB Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    FW1256 is a phenyl analogue and a slow-releasing hydrogen sulfide (H2S) donor. FW1256 inhibits NF-κB activity and induces cell apoptosis. FW1256 exerts potent anti-inflammatory effects and has the potential for cancer and cardiovascular disease treatment.
  • HY-10619
    Niraparib

    MK-4827

    PARP Apoptosis Cancer
    Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-P1740
    RGD peptide (GRGDNP)

    Integrin Apoptosis Inflammation/Immunology
    RGD peptide (GRGDNP) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation. RGD peptide (GRGDNP) promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing.
  • HY-10619A
    Niraparib hydrochloride

    MK-4827 hydrochloride

    PARP Apoptosis Cancer
    Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • 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-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-W004520
    Phenazine methylsulfate

    5-Methylphenazinium methylsulfate

    Bacterial Antibiotic Apoptosis
    Phenazine methylsulfate is a free radical generator. Phenazine methylsulfate has been used as an electron transfer reactant in cell viability assays. Phenazine methylsulfate induces ssDNA break formation in the presence of the reducing agent NADPH. Phenazine methylsulfate induces oxidative DNA damage in an alkaline comet assay and apoptosis.
  • HY-13007
    PF-3758309

    PAK Apoptosis Cancer
    PF-3758309 is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
  • HY-103248
    Toyocamycin

    Vengicide

    IRE1 Fungal Antibiotic Cancer Infection
    Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage, with an IC50 of 80 nM. Toyocamycin (Vengicide) induces apoptosis. Toyocamycin (Vengicide) shows no effect on IRE1α auto-phosphorylation.
  • HY-124136
    WYC-209

    RAR/RXR Apoptosis Autophagy Cancer
    WYC-209, a synthetic retinoid, is a retinoic acid receptor (RAR) agonist. WYC-209 induces apoptosis primarily via the caspase 3 pathway (IC50=0.19 μM for inmalignant murine melanoma TRCs), and has long-term effects with little toxicity.
  • HY-N7450
    Icariside D2

    Angiotensin-converting Enzyme (ACE) Apoptosis HIV Cancer Infection Inflammation/Immunology
    Icariside D2, isolated from Annona glabra fruit, inhibits angiotensin-converting enzyme. Icariside D2 shows significant cytotoxic activity on the HL-60 cell line with the IC50 value of 9.0 ± 1.0 μM. Icariside D2 induces apoptosis .
  • HY-125355
    SEC

    Apoptosis Cancer
    SEC induces activation of ANXA7 GTPase via the AMPK/mTORC1/STAT3 signaling pathway. SEC selectively promotes apoptosis in cancer cells, expressing a high level of ITGB4 by inducing ITGB4 nuclear translocation.
  • HY-13434
    Ionomycin

    SQ23377

    Calcium Channel PKC Bacterial Apoptosis Antibiotic Cancer Infection
    Ionomycin (SQ23377) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin (SQ23377) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin also induces the activation of protein kinase C (PKC).
  • 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-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-101034
    CHMFL-ABL/KIT-155

    CHMFL-ABL-KIT-155

    Bcr-Abl c-Kit Apoptosis Cancer
    CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis.
  • HY-B0075S
    Melatonin D4

    N-Acetyl-5-methoxytryptamine D4

    Melatonin Receptor Autophagy Mitophagy Cancer Inflammation/Immunology Neurological Disease
    Melatonin D4 is deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Antioxidative and anti-inflammatory properties. Melatonin is a selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation.
  • HY-P1380A
    Difopein TFA

    Apoptosis Cancer
    Difopein (TFA), a specific and competitive inhibitor of 14-3-3 protein (a highly conserved eukaryotic regulatory molecule), blocking the ability of 14-3-3 to bind to target proteins and inhibits 14-3-3/Ligand interactions. Difopein (TFA) leads to induction of apoptosis and enhances the ability of cisplatin to kill cells.
  • HY-77293
    (E)-[6]-Dehydroparadol

    Apoptosis Cancer
    (E)-[6]-Dehydroparadol, extracted from patent US 9272994, compound M15, shows growth inhibition and induction of apoptosis against human cancer cells with IC50 values of 43.02 μM in HCT-116 cell and 41.59 μM in H-1299 cell, respectively.
  • HY-10227
    Bortezomib

    PS-341; LDP-341; NSC 681239

    Proteasome NF-κB Apoptosis Autophagy Cancer
    Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first therapeutic proteasome inhibitor to be used in humans. Anti-cancer activity.
  • HY-16322
    Minodronic acid

    YM-529

    P2X Receptor Apoptosis Cancer
    Minodronic acid (YM-529) is a third-generation bisphosphonate that directly and indirectly prevents proliferation, induces apoptosis, and inhibits metastasis of various types of cancer cells. Minodronic acid (YM-529) is an antagonist of purinergic P2X2/3 receptors involved in pain.
  • HY-103258
    TC ASK 10

    MAP3K Apoptosis Cancer
    TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM).
  • HY-N2435
    [8]-Shogaol

    COX Apoptosis Cancer
    [8]-Shogaol, one of the pungent phenolic compounds in ginger, exhibits anti-platelet activity (IC50=5 μM) and inhibits COX-2 (IC50=17.5 μM). [8]-Shogaol induces apoptosis in human leukemia cells.
  • HY-19759
    SRT 2183

    Sirtuin Apoptosis Cancer
    SRT 2183 is a selective Sirtuin-1 (SIRT1) activator with an EC1.5 value of 0.36 μM. SRT 2183 induces growth arrest and apoptosis, concomitant with deacetylation of STAT3 and NF-κB, and reduction of c-Myc protein levels.
  • HY-136477
    Pentagamavunon-1

    PGV-1

    Apoptosis COX VEGFR NF-κB Cancer
    Pentagamavunon-1 (PGV-1), a Curcumin analog with oral activity, targets on several molecular mechanisms to induce apoptosis including inhibition of angiogenic factors cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF). PGV-1 inhibits NF-κB activation.
  • 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-N6022
    Byakangelicin

    Others Metabolic Disease
    Byakangelicin, one of the active compounds found in the roots of Angelica gigas, can serve as a modulator to improve brain accumulation of diverse active compounds (Umb, Cur, and Dox) and enhance therapeutic effects. Byakangelicin is likely to increase the expression of all PXR target genes (such as MDR1) and induce a wide range of drug-drug interactions. Byakangelicin can inhibit the effects of sex hormones, it may increase the catabolism of endogenous hormones.
  • 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-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-B0075
    Melatonin

    N-Acetyl-5-methoxytryptamine

    Melatonin Receptor Autophagy Mitophagy Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation.
  • HY-N2638
    Ilexsaponin A

    Others Cardiovascular Disease
    Ilexsaponin A, isolated from the root of Ilex pubescens, attenuates ischemia-reperfusion-induced myocardial injury through anti-apoptotic pathway. Ilexsaponin A can reduce myocardial infarct size, lower the serum levels of LDH, AST and CK-MB, increase cellular viability and inhibit apoptosis in hypoxia/reoxygenation cardiomyocytes.
  • HY-P1740A
    RGD peptide (GRGDNP) (TFA)

    Integrin Apoptosis Inflammation/Immunology Cancer
    RGD peptide (GRGDNP) (TFA) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation. RGD peptide (GRGDNP) (TFA) promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing.
  • HY-N7038
    Phytohemagglutinin

    PHA-M

    Apoptosis Cancer Inflammation/Immunology
    Phytohemagglutinin (PHA-M), a lectin extract from the red kidney bean and a standard T cell mitogen, as an inhibitor of both T- and B-cell tumors. Phytohemagglutinin can inhibit incorporation of 3H-thymidine and mediate apoptosis of B- and T-cell tumor lines. Anti-tumor activity.
  • HY-N2450
    Sulforaphene

    Apoptosis EGFR ERK NF-κB Cancer
    Sulforaphene, isolated from radish seeds, exhibits an ED50 against velvetleaf seedlings approximately 2 x 10 -4 M. Sulforaphene promotes cancer cells apoptosis and inhibits migration via inhibiting EGFR, p-ERK1/2, NF‐κB and other signals.
  • HY-118341
    Clitocine

    Apoptosis Bcl-2 Family Cancer
    Clitocine, an adenosine nucleoside analog, is a potent and efficacious readthrough agent. Clitocine 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-100912
    W-7 hydrochloride

    CaMK Phosphodiesterase (PDE) Myosin Apoptosis Cancer
    W-7 hydrochloride is a selective calmodulin antagonist. W-7 hydrochloride inhibits the Ca 2+-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC50 values of 28 μM and 51 µM, respectively. W-7 hydrochloride induces apoptosis and has antitumor activity.
  • HY-105755
    Antimycin A3

    Mitochondrial Metabolism Cancer Infection
    Antimycin A3, an antibiotic isolated from a number of Streptomyces species, shows antifungal activities. Antimycin A3 is a potent inhibitor of respiration. Antimycin A3 inhibits the electron transfer activity of ubiquinol-cytochrome c oxidoreductase. Antimycin A3 inhibits ATP-citrate lyase with a Ki value of 60.1 µM.
  • HY-133146
    DJ001

    Phosphatase Inflammation/Immunology
    DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC50 of 1.43 μM. DJ001 displays no inhibitory activity against other phosphatases, with only modest inhibitory activity against Protein Phosphatase 5. DJ001 promotes promote hematopoietic stem cell regeneration.
  • HY-16576
    TCS-PIM-1-4a

    SMI-4a

    Pim Apoptosis Cancer
    TCS-PIM-1-4a (SMI-4a) is a pan-Pim kinases inhibitor that blocks mTORC1 activity via activation of AMPK. TCS-PIM-1-4a kills a wide range of both myeloid and lymphoid cell lines (IC50 values ranging from 0.8 μM to 40 μM).
  • 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-16210
    Forodesine

    BCX-1777; Immucillin-H

    Nucleoside Antimetabolite/Analog Apoptosis Cancer
    Forodesine (BCX-1777) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine is a potent human lymphocyte proliferation inhibitor. Forodesine could induce apoptosis in leukemic cells by increasing the dGTP levels.
  • 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-B0294
    Flubendazole

    Parasite Microtubule/Tubulin Apoptosis Cancer Infection
    Flubendazole is a safe and efficacious anthelmintic drug, which is widely used for anthelmintic to human, rodents and ruminants. Flubendazole exerts anticancer activities by mechanisms including inhibition of microtubule function. Flubendazole induces p53-mediated apoptosis and arrests G2/M cell cycle.
  • HY-16291
    APTO-253

    LOR-253; LT-253

    c-Myc KLF Apoptosis Cancer
    APTO-253 is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through induction of the Krüppel-like factor 4 (KLF4) tumor suppressor.
  • HY-B0656
    Rabeprazole

    LY307640

    Proton Pump Apoptosis Cancer Inflammation/Immunology
    Rabeprazole (LY307640) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H +/K +-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux.
  • 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-W058849
    MT 63-78

    AMPK mTOR Apoptosis Cancer
    MT 63-78 is a specific and potent direct AMPK activator with an EC50 of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects.
  • HY-B0656A
    Rabeprazole sodium

    LY307640 sodium

    Proton Pump Apoptosis Inflammation/Immunology Cancer
    Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H +/K +-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux.
  • HY-110084
    BTZO-1

    Apoptosis Cardiovascular Disease
    BTZO-1 binds to Macrophage migration inhibitory factor (MIF) with a Kd value of 68.6 nM, and its binding requires the N-terminal Pro1. BTZO-1 can activate antioxidant response element (ARE)-mediated gene expression and suppress oxidative stress-induced cardiomyocyte apoptosis in vitro.
  • HY-13404
    Capmatinib

    INC280; INCB28060

    c-Met/HGFR Apoptosis Cancer
    Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib (INC280; INCB28060) potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity.
  • HY-N6704
    Enniatin A1

    ERK Apoptosis Cancer
    Enniatin A1 isolated from Fusarium mycotoxins is a cyclic hexadepsipeptide consisting of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids. Enniatin A1 possesses anticarcinogenic properties by induction of apoptosis and disruption of ERK signalling pathway. Enniatin A1 inhibits ACAT with an IC50 of 49 μM in rat liver microsomes.
  • HY-16209
    Forodesine hydrochloride

    BCX-1777 hydrochloride; Immucillin-H hydrochloride

    Nucleoside Antimetabolite/Analog Apoptosis Cancer
    Forodesine hydrochloride (BCX-1777 hydrochloride) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine hydrochloride is a potent human lymphocyte proliferation inhibitor. Forodesine hydrochloride could induce apoptosis in leukemic cells by increasing the dGTP levels.
  • HY-136658
    STAT3-IN-7

    STAT Apoptosis Cancer
    STAT3-IN-7 is a Sorafenib analogue and potently inhibits the phosphorylation of STAT3. STAT3-IN-7 induces cell apoptosis through SHP-1 dependent STAT3 inactivation. STAT3-IN-7 does not inhibit kinase activity and has anticancer effects.
  • HY-114310
    VDR agonist 1

    VD/VDR Apoptosis Cancer
    VDR agonist 1 (compound 28) is a nonsteroidal Vitamin D receptor (VDR) agonist, with an IC50 of 690 nM in MCF-7 cells. VDR agonist 1 arrests the cell cycle through the up-regulation of p21 and p27, promotes apoptosis by increasing the expression of BAX and decrease the expression of Bcl-2.
  • HY-135581
    Raloxifene 6-glucuronide

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-107390A
    AX-024 hydrochloride

    TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • 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-128895
    NQO1 activator 1

    Others Metabolic Disease
    NQO1 activator 1 is an orally available NAD + modulator. It reacts with NAD(P)H:quinone oxidoreductase 1 (NQO1) as a substrate, resulting in increases in intracellular NAD + levels via NADH oxidation. Elevated NAD + levels triggers the activation of SIRT1 and AMPK, and subsequently activates PGC-1α. NQO1 activator 1 improves energy metabolism and mitochondrial dysfunction in MELAS fibroblasts.
  • HY-111751
    JNJ-61432059

    iGluR Neurological Disease
    JNJ-61432059 is an oral active and selective negative modulator of AMPAR associated with trans-membrane AMPAR regulatory protein (TARP) γ-8, with a pIC50 of 9.7 for GluA1/γ-8. Exhibits time- and dose-dependent AMPAR/γ-8 receptor occupancy in mouse hippocampus, resulting in robust seizure protection in corneal kindling and pentylenetetrazole (PTZ) anticonvulsant models.
  • HY-N2499
    Dehydrotumulosic acid

    Others Metabolic Disease
    Dehydrotumulosic acid, one of the effective constituents of Poria cocos, was isolated from the chloroform-soluble material of ethanol extract of the fungus. Poria cocos, a popular Chinese medicinal herb of fungal origin, has been included in many combinations with other CM herbs for its traditionally claimed activities of inducing diuresis, excreting dampness, invigorating the spleen and tranquilizing the mind and its modern pharmacological use of modulating the immune system of the body.
  • HY-19620
    Branaplam

    LMI070; NVS-SM1

    DNA/RNA Synthesis Potassium Channel Cancer
    Branaplam (LMI070; NVS-SM1) is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model.
  • HY-135582
    Raloxifene 4'-glucuronide

    Estrogen Receptor/ERR Endocrinology
    Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
  • HY-103484
    GATA4-NKX2-5-IN-1

    Others Cardiovascular Disease
    GATA4-NKX2-5-IN-1 (Compound 3) dose-dependently inhibits the GATA4–NKX2-5 transcriptional synergy with an IC50 of 3 μM. GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression.
  • HY-107390
    AX-024

    TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-136563
    RA375

    Proteasome Apoptosis Reactive Oxygen Species Cancer
    RA375 is a RPN13 (26S proteasome regulatory subunit) inhibitor. RA375 activates UPR signaling, ROS production and apoptosis. RA375 exhibits ten-fold greater activity against cancer lines than RA190, reflecting its nitro ring substituents and the addition of a chloroacetamide warhead.
  • 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-N0179
    Ecdysone

    α-Ecdysone

    Endogenous Metabolite Apoptosis Metabolic Disease
    Ecdysone (α-Ecdysone), a major steroid hormone in insects and herbs, triggers mineralocorticoid receptor (MR) activation and induces cellular apoptosis. Ecdysone plays essential roles in coordinating developmental transitions and homeostatic sleep regulation through its active metabolite 20-hydroxyecdysone (Crustecdysone; 20E; HY-N6979).
  • HY-135897
    Urolithin C

    Calcium Channel Reactive Oxygen Species Apoptosis Endogenous Metabolite Metabolic Disease
    Urolithin C, a gut-microbial metabolite of Ellagic acid, is a glucose-dependent activator of insulin secretion. Urolithin C is a L-type Ca 2+ channel opener and enhances Ca 2+ influx. Urolithin C induces cell apoptosis through a mitochondria-mediated pathway and also stimulates reactive oxygen species (ROS) formation.
  • 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-13007A
    PF-3758309 hydrochloride

    PAK Apoptosis Cancer
    PF-3758309 hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
  • HY-N0817
    Polyphyllin G

    Apoptosis Autophagy Bacterial Cancer Inflammation/Immunology
    Polyphyllin G is isolated from the rhizomes of Paris yunnanensis, with antimicrobial and anticancer activity. Polyphyllin G prevents the growth of both Gram-positive and Gram-negative bacteria with minimum inhibitory concentrations (MICs). Polyphyllin G induces apoptosis dependent on the activations of caspase-8, -3, and -9, induces autophagy.
  • HY-117433
    4-Hydroperoxy cyclophosphamide

    DNA Alkylator/Crosslinker Apoptosis Reactive Oxygen Species Drug Metabolite
    4-Hydroperoxy cyclophosphamide is the active metabolite form of the prodrug Cyclophosphamide. 4-Hydroperoxy cyclophosphamide crosslinks DNA and induces T cell apoptosis independent of death receptor activation, but activates mitochondrial death pathways through production of reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide is used to treat lymphomas and autoimmune disorders.
  • HY-N6693
    Valinomycin

    NSC 122023

    Bacterial Apoptosis Antibiotic 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-A0004
    Decitabine

    5-Aza-2'-deoxycytidine; NSC 127716

    DNA Methyltransferase Apoptosis Nucleoside Antimetabolite/Analog Cancer
    Decitabine (NSC 127716) is a deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity.
  • HY-N2292
    Kinsenoside

    Keap1-Nrf2 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-N4286
    4-Methyldaphnetin

    Apoptosis Cancer
    4-Methyldaphnetin is a precursor in the synthesis of derivatives of 4-methyl coumarin. 4-Methyldaphnetin has potent, selective anti-proliferative and apoptosis-inducing effects on several cancer cell lines. 4-Methyldaphnetin possesses radical scavenging property and strongly inhibits membrane lipid peroxidation.
  • HY-P2343
    BH3 hydrochloride

    Apoptosis Cancer
    BH3 hydrochloride, a BBB penetrated peptide, provoke apoptosis either by direct activation of pro-apoptotic Bax/Bak or by neutralizing anti-apoptotic Bcl-2 proteins (Bcl-2, Bcl-XL, Bcl-w, Mcl-1 and A-1) via their BH3 domian.
  • HY-N1535
    Ponicidin

    Rubescensine B

    Apoptosis Cancer Inflammation/Immunology
    Ponicidin (Rubescensine B) is a diterpenoid derived from Rabdosia rubescens, and exhibits immunoregulatory, anti-inflammatory, anti-viral and anti-cancer activity. Ponicidin (Rubescensine B) induces apoptosis of gastric carcinoma cell, decreases the phosphorylation of JAK2 and STAT3, and shows no effect on protein levels of JAK2 and STAT3.
  • HY-N7363
    Isolongifolene

    (-)-Isolongifolene

    Others 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-108538
    Ethacrynic acid D5

    Gutathione S-transferase NF-κB Calcium Channel Inflammation/Immunology
    Ethacrynic acid D5 is a deuterium labeled Ethacrynic acid. Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
  • HY-113466
    4-Hydroxynonenal

    4-HNE

    Aldehyde Dehydrogenase (ALDH) Endogenous Metabolite Cancer Neurological Disease Cardiovascular Disease
    4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.
  • HY-12355
    Siponimod

    BAF-312

    LPL Receptor Others
    Siponimod (BAF-312) is a potent and selective sphingosine-1-phosphate (S1P) receptor modulator. It is selective for S1P1 and S1P5 receptors over S1P2, S1P3, and S1P4 (EC50s of 0.39, 0.98, >10,000, >1,000, and 750 nM, respectively). Used to treat adult multiple sclerosis.
  • HY-110143
    CLP257

    Potassium Channel Neurological Disease
    CLP257 is a selective K +-Cl cotransporter KCC2 activator with an EC50 of 616 nM. CLP257 is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally.
  • HY-13456
    LY-404187

    iGluR Neurological Disease
    LY-404187 is a potent, selective and centrally active positive allosteric modulator of AMPA receptors, with the EC50s of 5.65, 0.15, 1.44, 1.66 and 0.21 µM for GluR1i, GluR2i, GluR2o, GluR3i and GluR4i, respectively. LY-404187 has therapeutic potential in a number of psychiatric disorders and neurodegenerative diseases.
  • HY-N2492
    (E)-Methyl 4-coumarate

    Methyl trans-p-coumarate

    Bacterial Apoptosis Cancer Infection
    (E)-Methyl 4-coumarate (Methyl 4-hydroxycinnamate), found in several plants, such as green onion (Allium cepa) or noni (Morinda citrifolia L.) leaves. (E)-Methyl 4-coumarate cooperates with Carnosic Acid in inducing apoptosis and killing acute myeloid leukemia cells, but not normal peripheral blood mononuclear cells. Antioxidant and antimicrobial activity.
  • HY-90006
    5-Fluorouracil

    5-FU

    Nucleoside Antimetabolite/Analog HIV Apoptosis Endogenous Metabolite Cancer
    5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer. 5-Fluorouracil also inhibits HIV.
  • HY-N7071A
    Maduramicin ammonium

    Maduramycin ammonium

    Bacterial Apoptosis Antibiotic Infection
    Maduramicin ammonium (Maduramycin ammonium) is isolated from the actinomycete Actinomadura rubra. Maduramicin ammonium (Maduramycin ammonium) is an anticoccidial agent for the the treatment of Eimeria spp., E. adenoeides, E. gallopavonis, and E. dispersa infection. Maduramicin ammonium (Maduramycin ammonium) induces cell apoptosis in chicken myocardial cells via intrinsic and extrinsic pathways.
  • HY-N0749
    Jatrorrhizine

    Others Neurological Disease
    Jatrorrhizine is a potent and orally active uptake-2 transporter inhibitor, it can be isolated from various Chinese medicinal plants. Jatrorrhizine exhibits a critical neuroprotective role in H2O2-induced apoptosis via inhibition of MAPK pathway in HT22 hippocampal neurons.
  • HY-B1452
    Licofelone

    ML-3000

    COX Lipoxygenase Apoptosis Cancer Inflammation/Immunology
    Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins.
  • HY-N6796
    Manumycin A

    Farnesyl Transferase Ras Apoptosis Cancer Infection
    Manumycin A is an antibiotic. Manumycin A acts as a selective, competitive inhibitor of protein farnesyltransferase (FTase) with respect to farnesylpyrophosphate (Ki =1.2 μM), and as a noncompetitive inhibitor with respect to the Ras protein. Manumycin A induces apoptosis and exerts antitumor activity . Manumycin A suppresses exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling.
  • HY-N0636
    Eriocitrin

    Apoptosis Cancer
    Eriocitrin is a flavonoid isolated from lemon, which is a strong antioxidant agent. Eriocitrin could inhibit the proliferation of hepatocellular carcinoma cell lines by arresting cell cycle in S phase through up-regulation of p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating mitochondria-involved intrinsic signaling pathway.
  • HY-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-13516
    Aloperine

    Apoptosis Autophagy Filovirus HIV Cancer Infection Inflammation/Immunology
    Aloperine is an alkaloid in sophora plants such as Sophora alopecuroides L, which has shown anti-cancer, anti-inflammatory and anti-virus properties. Aloperine is widely used to treat patients with allergic contact dermatitis eczema and other skin inflammation in China. Aloperine induces apoptosis and autophagy in HL-60 cells.
  • HY-116364
    AZT triphosphate

    3'-Azido-3'-deoxythymidine-5'-triphosphate

    HIV DNA/RNA Synthesis HBV Reactive Oxygen Species Apoptosis Infection
    AZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate also inhibits the DNA polymerase of HBV. AZT triphosphate activates the mitochondria-mediated apoptosis pathway.
  • HY-N0740
    Jatrorrhizine chloride

    Others Neurological Disease
    Jatrorrhizine chloride is a potent and orally active uptake-2 transporter inhibitor, it can be isolated from various Chinese medicinal plants. Jatrorrhizine chloride exhibits a critical neuroprotective role in H2O2-induced apoptosis via inhibition of MAPK pathway in HT22 hippocampal neurons.
  • HY-10253
    AG1024

    Tyrphostin AG 1024

    IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 7 μM. AG1024 inhibits phosphorylation of insulin receptor (IR; IC50=57 μM). AG1024 induces apoptosis and has anti-cancer activity.
  • 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-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-125858
    MI-1061

    MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53, induces apoptosis, and has anti-tumor activity.
  • HY-14743B
    Golotimod hydrochloride

    SCV 07 hydrochloride; Gamma-D-glutamyl-L-tryptophan hydrochloride

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod hydrochloride (SCV 07 hydrochloride), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod hydrochloride (SCV 07 hydrochloride) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod hydrochloride (SCV 07 hydrochloride) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-120355A
    AP14145 hydrochloride

    Potassium Channel Cardiovascular Disease
    AP14145 hydrochloride is a potent KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF).
  • HY-136190
    TRPC6-PAM-C20

    TRP Channel
    TRPC6-PAM-C20 is a selective TRPC6 positive allosteric modulator. TRPC6-PAM-C20 selectively activates TRPC6 over other TRP channels and also activates TRPA1. TRPC6-PAM-C20 induces transient increase in intracellular Ca 2+ in HEK cells expressing TRPC6 (EC50=2.37 μM).
  • HY-12700
    RO5256390

    Others Neurological Disease
    RO5256390 is an agonist of trace amine-associated receptor 1 (TAAR1), a highly conserved G-protein-coupled receptor (GPCR) bound by endogenous trace amines. RO5256390 can be used to reduce multiple behavioral effects of drugs of abuse through their actions on the mesocorticolimbic system. RO5256390 is a modulator of monoaminergic neurotransmission, blocks psychostimulant-induced hyperactivity and produces a brain activation pattern reminiscent of the antipsychotic drug olanzapine, suggesting antipsychotic-like properties.
  • HY-105231
    Bryostatin 1

    PKC HIV Cancer Infection Inflammation/Immunology Neurological Disease
    Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties.
  • HY-P0063
    Copper tripeptide

    GHK-Cu

    Endogenous Metabolite Inflammation/Immunology
    Copper tripeptide (GHK-Cu), a naturally occurring tripeptide, is first isolated from human plasma, but can be found in saliva and urine. During wound healing, Copper tripeptide may be freed from existing extracellular proteins via proteolysis and serves as a chemoattractant for inflammatory and endothelial cells. Copper tripeptide has been shown to increase messenger RNA production for collagen, elastin, proteoglycans, and glycosaminoglycans in fibroblasts. Copper tripeptide is a Natural Modulator of Multiple Cellular Pathways in Skin Regeneration.
  • HY-117482
    BPN-15606

    γ-secretase Neurological Disease
    BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
  • HY-130609A
    Aβ42-IN-1 free base

    γ-secretase Neurological Disease
    Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease.
  • HY-50859
    Ruxolitinib sulfate

    INCB018424 sulfate

    JAK Autophagy Cancer
    Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.
  • HY-129602
    SD-36

    PROTAC STAT Apoptosis Cancer
    SD-36 is a potent and efficacious PROTAC STAT3 degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of CRBN ligand Lenalidomide for E3 ubiquitin ligase.
  • HY-135775
    BMVC

    G-quadruplex Telomerase DNA/RNA Synthesis Cancer
    BMVC is a potent G-quadruplex (G4) stabilizer and a selective telomerase inhibitor with an IC50 of ~0.2 μM. BMVC inhibits Taq DNA polymerase with an IC50 of ~2.5 μM. BMVC increases the melting temperature of G4 structure of telomere and accelerates telomere length shortening. Anticancer activities.
  • HY-12170
    Prinomastat

    AG3340; KB-R9896

    MMP Cancer
    Prinomastat (AG3340) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat crosses blood-brain barrier. Antitumor avtivity.
  • HY-12170A
    Prinomastat hydrochloride

    AG3340 hydrochloride; KB-R9896 hydrochloride

    MMP Cancer
    Prinomastat hydrochloride (AG3340 hydrochloride) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat hydrochloride inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat hydrochloride can cross blood-brain barrier. Antitumor avtivity.
  • HY-133129
    MS1943

    Histone Methyltransferase Cancer
    MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines. MS1943 effectively blocks proliferation of multiple TNBC and other cancer cell lines.
  • HY-N5025
    Bullatine A

    P2X Receptor Cancer Inflammation/Immunology
    Bullatine A, a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A is a potent P2X7 antagonist, inhibits ATP-induced cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A attenuates pain hypersensitivity, regardless of the pain models employed.
  • HY-135746
    OR-1896

    Potassium Channel Phosphodiesterase (PDE) Drug Metabolite Cardiovascular Disease
    OR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) III isoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K + channels and has Ca 2+-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation.
  • HY-13434A
    Ionomycin calcium

    SQ23377 calcium

    Calcium Channel PKC Bacterial Apoptosis Antibiotic Cancer Infection
    Ionomycin calcium (SQ23377 calcium) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin calcium (SQ23377 calcium) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin calcium (SQ23377 calcium) also induces the activation of protein kinase C (PKC).
  • HY-122611
    CSRM617

    Androgen Receptor Apoptosis Cancer
    CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
  • HY-135954A
    PDK4-IN-1 hydrochloride

    PDHK Apoptosis Cancer Metabolic Disease Inflammation/Immunology
    PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity.
  • HY-W040129
    Chromomycin A3

    Bacterial Fungal Antibiotic Cancer Infection
    Chromomycin A3 is an aureolic acid-type antitumor antibiotic. Chromomycin A3 forms dimeric complexes with divalent cations, such as Mg 2+, which strongly binds to the GC rich sequence of DNA to inhibit DNA replication and transcription. Chromomycin A3 has a variety of utilities as a staining agent for human sperm chromatin, autophagy inducing agent, and apoptosis inhibitor.
  • HY-101518
    APG-115

    AA-115

    MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    APG-115 (AA-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC50 and Ki values of 3.8 nM and 1 nM, respectively. APG-115 blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner.
  • HY-N1987
    Cucurbitacin IIb

    Apoptosis Inflammation/Immunology
    Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α.
  • HY-N0831
    Jaceosidin

    Bcl-2 Family COX Apoptosis Cancer Inflammation/Immunology
    Jaceosidin is a flavonoid isolated from Artemisia vestita, induces apoptosis in cancer cells, activates Bax and down-regulates Mcl-1 and c-FLIP expression. Jaceosidin exhibits anti-cancer, anti-inflammatory activities, decreases leves of inflammatory markers, and suppresses COX-2 expression and NF-κB activation.
  • HY-N6939
    Pseudolaric Acid B

    HBV Fungal Apoptosis Autophagy Ferroptosis Cancer Infection Inflammation/Immunology
    Pseudolaric Acid B is a diterpene isolated from the root of Pseudolarix kaempferi Gorden (pinaceae), has anti-cancer, antifungal, and antifertile activities, and shows immunosuppressive activity on T lymphocytes. Pseudolaric Acid B inhibits hepatitis B virus (HBV) secretion through apoptosis and cell cycle arrest. Pseudolaric Acid B induces autophagy.
  • HY-N6736
    K-252c

    PKC Bacterial Apoptosis Cancer Infection
    K-252c, a staurosporine analog isolated from Nocardiopsis sp., is a cell-permeable PKC inhibitor, with an IC50 of 2.45 µM. K-252c induces apoptosis in human chronic myelogenous leukemia cancer cells. K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase.
  • HY-B0011
    Docetaxel

    RP-56976

    Microtubule/Tubulin Apoptosis Endogenous Metabolite Cancer
    Docetaxel (RP-56976) is a microtubule depolymerization inhibitor, with an IC50 of 0.2 μM. Docetaxel is a semisynthetic analog of taxol and attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel arrests the cell cycle at G2/M and leads to cell apoptosis. Docetaxel has anti-cancer activity.
  • HY-N0747
    Oxypeucedanin

    Potassium Channel Cancer Cardiovascular Disease
    Oxypeucedanin is a furocoumarin derivative isolated from Angelica dahurica. Oxypeucedanin is a selective open-channel blocker, inhibits the hKv1.5 current with an IC50 value of 76 nM. Oxypeucedanin prolongs cardiac action potential duration (APD), is a potential antiarrhythmic agent for atrial fibrillation. Oxypeucedanin induces cell apoptosis through inhibition of cancer cell migration.
  • 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-N6790
    Nonactin

    Ammonium ionophore I

    Potassium Channel Mitochondrial Metabolism Bacterial Influenza Virus Apoptosis Antibiotic Cancer Infection
    Nonactin is a naturally occurring macrotetrolide antibiotic from Streptomyces griseus. Nonactin acts as an ionophore for monovalent cations, including K +, and NH4 +. Nonactin is able to uncouple the oxidative phosphorylation of mitochondria. Nonactin selectively induces apoptosis in cell lines harboring active mutant β-catenin. Nonactin inhibits the surface expression of endogenous HSP60.
  • HY-101761
    TM5441

    PAI-1 Apoptosis Cancer
    TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence.
  • HY-135396
    (1S,2S)-Bortezomib

    Proteasome 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-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-135954
    PDK4-IN-1

    PDHK Apoptosis Cancer Metabolic Disease Inflammation/Immunology
    PDK4-IN-1 is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity.
  • HY-130173
    Bafilomycin C1

    Bacterial Fungal Na+/K+ ATPase Cancer Infection
    Bafilomycin C1 is a macrolide antibiotic isolated from Streptomyces sp. Bafilomycin C1 is a potent, specific and reversible inhibitor of vacuolar-type H +-ATPases (V-ATPases). Bafilomycin C1 inhibits growth of gram-positive bacteria and fungi. Bafilomycin C1 induces cell apoptosis and can be used for the study of hepatocellular carcinoma (HCC).
  • HY-17408
    Mevastatin

    Compactin; ML236B

    HMG-CoA Reductase (HMGCR) Bacterial Autophagy Apoptosis Antibiotic Cancer Infection Metabolic Disease Neurological Disease Cardiovascular Disease
    Mevastatin (Compactin) is a first HMG-CoA reductase inhibitor that belongs to the statins class. Mevastatin is a lipid-lowering agent, and induces apoptosis, arrests cancer cells in G0/G1 phase. Mevastatin also increases endothelial nitric oxide synthase (eNOS) mRNA and protein levels. Mevastatin has antitumor activity and has the potential for cardiovascular diseases treatment.
  • HY-N2132
    Flavokawain B

    Flavokavain B

    Apoptosis Cancer
    Flavokawain B (Flavokavain B) is a chalcone isolated from the root extracts of kava-kava plant and a potent apoptosis inducer for inhibiting the growth of various cancer cell lines. Flavokawain B (Flavokavain B) shows strong antiangiogenic activity. Flavokawain B (Flavokavain B) inhibits human brain endothelial cell (HUVEC) migration and tube formation with very low and non-toxic concentrations.
  • HY-15079
    Talampanel

    GYKI-53773; LY-300164

    iGluR Neurological Disease
    Talampanel (LY300164) is an orally and selective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor antagonis with anti-seizure activity. Talampanel (IVAX) has neuroprotective effects in rodent stroke models. Talampanel attenuates caspase-3 dependent apoptosis in mouse brain.
  • HY-N0381
    Maackiain

    DL-​Maackiain

    Parasite Infection
    Maackiain (DL-Maackiain) is isolated from Maackia amurensis Rupr.et Maxim. Maackiain (DL-Maackiain) is a larvicidal agent against Aedes aegypti mosquito.xp Parasitol with a LD50 of  21.95 µg/mL. Maackiain (DL-Maackiain) induces fragmentations of DNA to oligonucleosomal-sized fragments that like a characteristic of apoptosis in the HL-60 cells.
  • HY-W046353
    2-Methoxycinnamaldehyde

    o-Methoxycinnamaldehyde

    Apoptosis Cancer
    2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound of Cinnamomum cassia, with antitumor activity. 2-Methoxycinnamaldehyde inhibits proliferation and induces apoptosis by mitochondrial membrane potential (ΔΨm) loss, activation of both caspase-3 and caspase-9. 2-Methoxycinnamaldehyde effectively inhibits platelet-derived growth factor (PDGF)-induced HASMC migration.
  • HY-13716
    Noscapine

    (S,R)-Noscapine

    Opioid Receptor Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can crosse the blood-brain barrier.
  • HY-B0656S
    Rabeprazole D4

    LY307640 D4

    Proton Pump Apoptosis Cancer Inflammation/Immunology
    Rabeprazole D4 (LY307640 D4) is a deuterium labeled Rabeprazole. Rabeprazole is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H +/K +-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux.
  • HY-N0331
    Ziyuglycoside I

    MDM-2/p53 Apoptosis Cancer
    Ziyuglycoside I isolated from S. officinalis root, has anti-wrinkle activity, and increases the expression of type I collagen. Ziyuglycoside I could be used as an active ingredient for cosmetics. Ziyuglycoside I triggers cell cycle arrest and apoptosis mediated by p53, it can be a potential drug candidate for treating triple-negative breast cancer (TNBC).
  • HY-114413
    YZ129

    HSP Apoptosis Cancer
    YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathway against glioblastoma, directly binding to heat shock protein 90 (HSP90) with an IC50 of 820 nM on NFAT nuclear translocation. YZ129-induced GBM cell-cycle arrest at the G2/M phase promotes apoptosis and inhibited tumor cell proliferation and migration.
  • HY-102078
    ZINC69391

    Ras Apoptosis Cancer
    ZINC69391, a specific Rac1 inhibitor, interferes with Rac1-GEF interaction by masking Trp56 residue on Rac1 surface. ZINC69391 interferes with the interaction of Rac1 with Dock180 and reduces Rac1-GTP levels. ZINC69391 induces apoptosis, and shows antiproliferative and antimetastatic effects.
  • HY-13716A
    Noscapine hydrochloride

    (S,R)-Noscapine hydrochloride

    Opioid Receptor Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Noscapine hydrochloride ((S,R)-Noscapine hydrochloride) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine hydrochloride exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine hydrochloride disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine hydrochloride possesses anticancer, neuroprotective, anti-inflammatory activities, and can crosse the blood-brain barrier.
  • HY-P1218
    Phrixotoxin 3

    Sodium Channel Neurological Disease
    Phrixotoxin 3 is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.
  • HY-100588
    VU0364770

    mGluR Neurological Disease
    VU0364770 is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.
  • HY-110155
    LM11A-31 dihydrochloride

    Others Neurological Disease
    LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.
  • HY-P1218A
    Phrixotoxin 3 TFA

    Sodium Channel Neurological Disease
    Phrixotoxin 3 TFA is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 TFA modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.
  • HY-14743A
    Golotimod TFA

    SCV 07 TFA; Gamma-D-glutamyl-L-tryptophan TFA

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod TFA (SCV 07 TFA), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod TFA (SCV 07 TFA) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod TFA (SCV 07 TFA) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-14743
    Golotimod

    SCV 07; Gamma-D-glutamyl-L-tryptophan

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-117482A
    BPN-15606 besylate

    γ-secretase Neurological Disease
    BPN-15606 besylate is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
  • HY-100588A
    VU0364770 hydrochloride

    mGluR Neurological Disease
    VU0364770 hydrochloride is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 hydrochloride exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 hydrochloride exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 hydrochloride also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.
  • 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-100991
    FG 7142

    ZK 39106; LSU-65

    GABA Receptor Neurological Disease
    FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex.
  • HY-103387
    DuP-697

    COX Apoptosis Cancer Inflammation/Immunology
    DuP-697 is a member of the vicinal diaryl heterocycles and a potent, irreversible, selective and orally active COX-2 inhibitor (IC50 of 10 nM and 800 nM for human COX-2 and COX-1, respectively). DuP-697 exerts antiproliferative (IC50 of 42.8 nM), antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. DuP-697 inhibits prostaglandin synthesis and has anti-inflammatory, anticancer and antipyretic effects.
  • HY-126390
    (E/Z)-BCI

    NSC 150117

    Phosphatase Cancer Inflammation/Immunology
    (E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway.
  • HY-N0484
    Liensinine

    Autophagy Mitophagy Cancer Cardiovascular Disease
    Liensinine is an autophagy/mitophagy inhibitor. Liensinine, a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn, has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc.
  • HY-107845
    SCR7 pyrazine

    CRISPR/Cas9 DNA/RNA Synthesis Apoptosis Cancer
    SCR7 pyrazine is a DNA ligase IV inhibitor that blocks nonhomologous end-joining (NHEJ) in a ligase IV-dependent manner. SCR7 pyrazine is also a CRISPR/Cas9 enhancer which increases the efficiency of Cas9-mediated homology-directed repair (HDR). SCR7 pyrazine induces cell apoptosis and has anticancer activity.
  • HY-18174A
    Prexasertib dihydrochloride

    LY2606368 dihydrochloride

    Checkpoint Kinase (Chk) Apoptosis Cancer
    Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dihydrochloride inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity.
  • 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-13027
    DAPT

    GSI-IX

    γ-secretase Amyloid-β Autophagy Notch Apoptosis Cancer Inflammation/Immunology Neurological Disease
    DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC50s of 115 nM and 200 nM for total amyloid-β (Aβ) and 42, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment.
  • HY-15142
    Doxorubicin hydrochloride

    Hydroxydaunorubicin hydrochloride

    Topoisomerase ADC Cytotoxin AMPK Autophagy Apoptosis HIV HBV Mitophagy Bacterial Antibiotic Cancer Infection
    Doxorubicin hydrochloride (Hydroxydaunorubicin hydrochloride), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy. Doxorubicin hydrochloride inhibits human DNA topoisomerase I with an IC50 of 0.8 μM.
  • 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-N2013
    Aristolactam I

    Aristololactam; Aristolactam

    Caspase Inflammation/Immunology
    Aristololactam I (AL-I), is the main metabolite of aristolochic acid I (AA-I), participates in the processes that lead to renal damage. Aristololactam I (AL-I) directly injures renal proximal tubule cells, the cytotoxic potency of AL-I is higher than that of AA-I and that the cytotoxic effects of these molecules are mediated through the induction of apoptosis in a caspase-3-dependent pathway.
  • HY-18174B
    Prexasertib Mesylate Hydrate

    LY2606368 Mesylate Hydrate; LY2940930

    Checkpoint Kinase (Chk) Apoptosis Cancer
    Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity.
  • HY-125374
    Larotaxel

    XRP9881

    Apoptosis Cancer
    Larotaxel (XRP9881) is a taxane analogue with preclinical activity against taxane-resistant breast cancer. Larotaxel (XRP9881) exerts its cytotoxic effect by promoting tubulin assembly and stabilizing microtubules, ultimately leading to cell death by apoptosis. It presents the ability to cross the blood brain barrier and has a much lower affinity for P-glycoprotein 1 than Docetaxel.
  • HY-18980
    Rottlerin

    Mallotoxin; NSC 56346; NSC 94525

    PKC Autophagy Apoptosis Infection Cancer
    Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation.
  • HY-129624A
    Bisindolylmaleimide VIII acetate

    Ro 31-7549 acetate; Bis VIII acetate