1. Search Result
Search Result
Results for "

mediator

" in MCE Product Catalog:

546

Inhibitors & Agonists

3

Screening Libraries

2

Dye Reagents

1

Biochemical Assay Reagents

47

Peptides

1

MCE Kits

3

Inhibitory Antibodies

143

Natural
Products

14

Recombinant Proteins

10

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-12512
    cGAMP

    Cyclic GMP-AMP; 3',3'-cGAMP

    STING Inflammation/Immunology
    cGAMP (Cyclic GMP-AMPP) functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators.
  • HY-110385
    cGAMP disodium

    Cyclic GMP-AMP disodium; 3',3'-cGAMP disodium

    STING Endogenous Metabolite Inflammation/Immunology
    cGAMP (Cyclic GMP-AMPP) disodium functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP diammonium activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators.
  • HY-110385A
    cGAMP diammonium

    Cyclic GMP-AMP diammonium; 3',3'-cGAMP diammonium

    STING Endogenous Metabolite Inflammation/Immunology
    cGAMP (Cyclic GMP-AMPP) diammonium functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP diammonium activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators.
  • HY-N0857
    Deoxyandrographolide

    Others Inflammation/Immunology Neurological Disease
    Deoxyandrographolide suppresses LPS induced increase in mRNA levels of iNOS as well as production of proinflammatory mediators TNF-α and IL-6. Deoxyandrographolide potentiates NGF-induced neurite outgrowth.
  • HY-10656
    SB-657510

    Urotensin Receptor Inflammation/Immunology
    SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The Ki values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells.
  • HY-125527
    Resolvin D1

    RvD1

    Endogenous Metabolite Inflammation/Immunology
    Resolvin D1 (RvD1), an endogenous pro-resolving mediator of inflammation, is derived from omega-3 docosahexaenoic acid during the resolution phase of acute inflammation. Resolvin D1 blocks proinflammatory neutrophil migration by regulating actin polymerization, reduces TNF-α–mediated inflammation in macrophages, and enhances phagocytosis of apoptotic cells by macrophages.
  • HY-W001174
    2,5-Dihydroxyacetophenone

    ERK NF-κB Inflammation/Immunology
    2,5-Dihydroxyacetophenone, isolated from Rehmanniae Radix Preparata, inhibits the production of inflammatory mediators in activated macrophages by blocking the ERK1/2 and NF-κB signaling pathways.
  • HY-108635
    C16-PAF

    PAF (C16)

    p38 MAPK MEK ERK Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease
    C16-PAF (PAF (C16)), a phospholipid mediator, is a platelet-activating factor and ligand for PAF G-protein-coupled receptor (PAFR). C16-PAF exhibits anti-apoptotic effect and inhibits caspase-dependent death by activating the PAFR. C16-PAF is a potent MAPK and MEK/ERK activator. C16-PAF induces increased vascular permeability.
  • HY-114041
    Resolvin E1

    RvE1

    Endogenous Metabolite Inflammation/Immunology
    Resolvin E1 (RvE1), a potent endogenous pro-resolving mediator of inflammation, is derived from omega-3 fatty acid eicosapentaenoic acid (EPA). Resolvin E1 is endogenously biosynthesized from EPA in the presence of Aspirin during the spontaneous resolution phase of acute inflammation, where specific cell-cell interactions occur. Resolvin E1 possesses unique counterregulatory actions that inhibit polymorphonuclear leukocyte (PMN) transendothelial migration. Resolvin E1 also acts as a potent inhibitor of leukocyte infiltration, dendritic cell migration, and IL-12 production.
  • HY-108496
    Sphingosine-1-phosphate

    S1P

    Endogenous Metabolite LPL Receptor Endocrinology
    Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca 2+ as an extracellular ligand for G protein-coupled receptors. Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids.
  • HY-108966
    Kushenol C

    Beta-secretase Inflammation/Immunology
    Kushenol C, isolated from the roots of Sophora flavescens, shows anti-Inflammatory and anti-oxidative stress activities. Kushenol C inhibits BACE1 (β-site APP cleaving enzyme 1) with an IC50 of 5.45 µM.
  • HY-W013812
    Ethyl linoleate

    Linoleic Acid ethyl ester

    Others Cardiovascular Disease
    Ethyl linoleate inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators.
  • HY-19817
    PRT4165

    NSC600157

    E1/E2/E3 Enzyme Cancer
    PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation.
  • HY-16661
    Skp2 Inhibitor C1

    SKPin C1

    E1/E2/E3 Enzyme Cancer
    Skp2 Inhibitor C1(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation, selectively inhibited Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts.
  • HY-B1404
    Nylidrin hydrochloride

    Buphenine hydrochloride

    Others Inflammation/Immunology
    Nylidrin hydrochloride was an effective inhibitor of IgE-mediated release of histamine from passively sensitized rat peritoneal mast cells and human basophils, and of IgG1-mediated release of histamine from passively sensitized guinea pig lung slices.
  • HY-19793
    RS-1

    RAD51 CRISPR/Cas9 Cancer
    RS-1 is a RAD51 activator, and also increases CRISPR/Cas9-mediated knock-in efficiencies.
  • HY-16697
    CID 16020046

    GPR55 Cancer
    CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca 2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function.
  • HY-14802
    Talarozole (R enantiomer)

    (R)-Talarozole

    Cytochrome P450 Cancer
    Talarozole R enantiomer is a potent and selective inhibitor of cytochrome P450 26-mediated breakdown of endogenous all-trans retinoic acid for the treatment of psoriasis and acne.
  • HY-B1232
    Metyrapone

    Su-4885

    Cytochrome P450 Autophagy Metabolic Disease Cancer
    Metyrapone is an inhibitor of cytochrome P450-mediated ω/ω-1 hydroxylase activity and CYP11B1.
  • HY-100013C
    2-PCCA hydrochloride

    Others Neurological Disease
    2-PCCA hydrochloride is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC50 of 116 nM in HEK293 cells.
  • HY-17413
    Zidovudine

    Azidothymidine; AZT; ZDV

    HIV CRISPR/Cas9 Infection
    Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection. Zidovudine increases CRISPR/Cas9-mediated editing frequency.
  • HY-108465
    Pyr3

    TRP Channel Others
    Pyr3 is a selective inhibitor of transient receptor potential canonical channel 3 (TRPC3), with an IC50 of 700 nM for TRPC3-mediated Ca 2+ influx.
  • HY-103710
    IBR2

    RAD51 Apoptosis Cancer
    IBR2 is a potent and specific RAD51 inhibitor and inhibits RAD51-mediated DNA double-strand break repair. IBR2 disrupts RAD51 multimerization, accelerates proteasome-mediated RAD51 protein degradation, inhibits cancer cell growth and induces apoptosis.
  • HY-N4113
    Glycycoumarin

    Autophagy Cancer
    Glycycoumarin is a major bioactive coumarin of licorice. Glycycoumarin inhibits hepatocyte lipoapoptosis through activation of autophagy and inhibition of ER stress-mediated JNK and GSK-3-mediated mitochondrial pathway. Glycycoumarin exerts anti-liver cancer activity by directly targeting T-LAK cell-originated protein kinase .
  • HY-132595
    Teprasiran

    QPI-1002

    MDM-2/p53 Cancer
    Teprasiran (QPI-1002) is a small interfering RNA that temporarily inhibits p53-mediated cell death that underlies acute kidney injury (AKI).
  • HY-120691A
    GSK205

    TRP Channel Metabolic Disease Inflammation/Immunology
    GSK205 is a potent, selective TRPV4 antagonist with an IC50 of 4.19  μM for inhibiting TRPV4-mediated Ca 2+ influx.
  • HY-N0341
    Scopolin

    Sirtuin Metabolic Disease
    Scopolin is a coumarin isolated from Arabidopsis thaliana (Arabidopsis) roots. Scopolin attenuated hepatic steatosis through activation of SIRT1-mediated signaling cascades.
  • HY-135653
    EC5026

    BPN-19186

    Epoxide Hydrolase Neurological Disease
    EC5026 (BPN-19186) is a first-in-class, non-opioid and orally active soluble Epoxide Hydrolase (sEH) inhibitor. EC5026 shows efficacy for inflammatory and neuropathic pain.
  • HY-129113
    α-​Chaconine

    COX Inflammation/Immunology
    α-Chaconine inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects.
  • HY-N3474
    Isolicoflavonol

    Others Others
    Isolicoflavonol potently inhibits hCES2A(Human carboxylesterase 2)-mediated fluorescein diacetate hydrolysis in a reversible and mixed inhibition manner, with Ki values less than 1.0 μM.
  • HY-18689
    SYM2206

    iGluR Neurological Disease
    SYM2206 is a potent and non-competitive AMPA receptor antagonist, with an IC50 of 1.6 μM. SYM2206 blocks Nav1.6-mediated persistent currents.
  • HY-134828
    AZ506

    Histone Methyltransferase Cancer
    AZ506 is a potent SMYD2 inhibitor with an IC50 of 17 nM. AZ506 inhibits SMYD2 methyltransferase activity in cells, leading to a decrease in the SMYD2-mediated methylation signal.
  • HY-101026
    CCT251236

    HSP Cancer
    CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC50 of 19 nM for inhibition of HSF1-mediated HSP72 induction.
  • HY-112125
    KRN2

    Others Inflammation/Immunology
    KRN2 is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 100 nM. KRN2 has potential to treat NFAT5-mediated Chronic Arthritis.
  • HY-111374
    NMDI14

    Others Cancer
    NMDI14 is a nonsense mediated RNA decay (NMD) inhibitor.
  • HY-10569
    Ponesimod

    ACT-128800

    LPL Receptor Inflammation/Immunology
    Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation.
  • HY-138657
    NCGC00378430

    Phosphatase Cancer
    NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor. NCGC00378430 partially reverses transcriptional and metabolic profiles mediated by SIX1 overexpression and reverses SIX1-induced TGF-β signaling and epithelial-mesenchymal transition (EMT). NCGC00378430 inhibits SIX1-mediated breast cancer metastasis in a mouse model.
  • HY-116213
    Sparstolonin B

    Toll-like Receptor (TLR) HIV Cancer Infection Inflammation/Immunology
    Sparstolonin B acts as a selective TLR2 and TLR4 antagonist and selectively blocks TLR2- and TLR4-mediated inflammatory signaling. Sparstolonin B has anti-HIV and anticancer activities.
  • HY-12483
    SR1664

    PPAR Metabolic Disease
    SR1664 is a PPARγ antagonist. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50=80 nM; Ki= 28.67 nM).
  • HY-119764
    Ikarugamycin

    Antibiotic Others
    Ikarugamycin is an antibiotic and a inhibitor of clathrin-mediated endocytosis (CME).
  • HY-B0119
    Risedronate sodium

    Risedronic Acid Sodium

    Others Others
    Risedronate sodium is a pyridinyl biphosphonate which inhibits osteoclast-mediated bone resorption.
  • HY-136390
    ML417

    Dopamine Receptor Neurological Disease
    ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons.
  • HY-115576
    P62-mediated mitophagy inducer

    PMI

    Mitophagy Neurological Disease
    P62-mediated mitophagy inducer is a mitophagy regulator which activates mitophagy without recruiting Parkin or collapsing ΔΨm and retains activity in cells devoid of a fully functional PINK1/Parkin pathway.
  • HY-18779
    PF-4840154

    TRP Channel Inflammation/Immunology
    PF-4840154 is a potent, selective agonist of the rat and human TrpA1 channel with EC50s of 97 and 23 nM, respectively. PF-4840154 elicits TrpA1-mediated nocifensive behaviour in mouse.
  • HY-N1514
    Ganoderenic acid B

    Others Cancer
    Ganoderenic acid B is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderenic acid B exhibits potent reversal effect on ABCB1-mediated multidrug resistance of HepG2/ADM cells to Doxorubicin.
  • HY-114504
    RVX-297

    Epigenetic Reader Domain Inflammation/Immunology
    RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models.
  • HY-112126
    KRN5

    Others Inflammation/Immunology
    KRN5, a derivative of KRN2, is an oral active Nuclear factor of activated T cells 5 (NFAT5) suppressor, with an IC50 of 750 nM. KRN5 has potential to treat NFAT5-mediated Chronic Arthritis.
  • HY-N6007
    Chrysosplenol D

    Apoptosis Cancer Infection Inflammation/Immunology
    Chrysosplenol D is a methoxy flavonoid that induces ERK1/2-mediated apoptosis in triple negative human breast cancer cells. Chrysosplenol D also exhibits anti-inflammatory and moderate antitrypanosomal activities.
  • HY-106182
    TBC3711

    Endothelin Receptor Endocrinology
    TBC3711 is a endothelin receptor modulator, used for the research of endothelin-mediated disorders.
  • HY-13021
    SRT3190

    CXCR Inflammation/Immunology Endocrinology
    SRT3190 is an antagonist of CXCR2, used in the research of chemokine mediated diseases.
  • HY-B0148
    Risedronic acid

    Risedronate

    Others Others
    Risedronic acid (Risedronate ) is a pyridinyl biphosphonate which inhibits osteoclast-mediated bone resorption.
  • HY-119500
    Ilimaquinone

    HIV Bacterial Cancer Infection Inflammation/Immunology
    Ilimaquinone, a marine sponge metabolite, displays anticancer activity via GADD153-mediated pathway. Ilimaquinone can induce vesiculation of the Golgi apparatus. Ilimaquinone exerts anti-HIV, anti-microbial, anti-inflammatory, and effects.
  • HY-N3239
    Mulberrofuran G

    NADPH Oxidase HBV
    Mulberrofuran G protects ischemic injury-induced cell death via inhibition of NOX4-mediated ROS generation and ER stress. Mulberrofuran G shows moderate inhibiting activity of hepatitis B virus (HBV) DNA replication with the
  • HY-N0327
    Lobetyolin

    Apoptosis Xanthine Oxidase Metabolic Disease
    Lobetyolin, a bioactive compound, is derived from Codonopsis pilosula. Lobetyolin has anti-inflammatory, anti-oxidative and xanthine oxidase inhibiting activities. Lobetyolin also induces the apoptosis via the inhibition of ASCT2-mediated glutamine metabolism.
  • HY-N2071
    Cedrol

    (+)-Cedrol; α-Cedrol

    Cytochrome P450 Fungal Infection Inflammation/Immunology Cancer
    Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes. Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities.
  • HY-100755
    KR-33493

    Others Neurological Disease
    KR-33493 is a potent inhibitor of Fas-mediated cell death (FAF1).
  • HY-139667
    PKM2-IN-3

    Pyruvate Kinase Neurological Disease
    PKM2-IN-3 is an inhibitor of PKM2 kinase with an IC50 value of 4.1 μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation.
  • HY-103254
    ML221

    Others Neurological Disease
    ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.
  • HY-N3513
    Mulberrin

    Kuwanon C

    Others Cardiovascular Disease
    Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.
  • HY-123905A
    LIN28 inhibitor LI71 enantiomer

    Others Cancer
    LIN28 inhibitor LI71 enantiomer is the enantiomer of LIN28 inhibitor LI71 with less active. LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM.
  • HY-N0534
    Vitexin-2"-O-rhamnoside

    Others Cardiovascular Disease
    Vitexin-2"-O-rhamnoside, a main flavonoid glycoside of the leaves of Cratagus pinnatifida Bge, contributes to the protection against H2O2-mediated oxidative stress damage and has potential to treat cardiovascular system diseases.
  • HY-101791
    P-gp inhibitor 1

    P-glycoprotein Cancer
    P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
  • HY-120528A
    GB-110 hydrochloride

    Protease-Activated Receptor (PAR) Cancer Inflammation/Immunology
    GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca 2+ release in HT29 cells with an EC50 of 0.28 μM.
  • HY-134656
    BC1618

    AMPK Mitophagy E1/E2/E3 Enzyme Metabolic Disease Inflammation/Immunology
    BC1618, an orally active Fbxo48 inhibitory compound, stimulates Ampk-dependent signaling (via preventing activated pAmpkα from Fbxo48-mediated degradation). BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity.
  • HY-120528
    GB-110

    Protease-Activated Receptor (PAR) Cancer Inflammation/Immunology
    GB-110 is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 selectively induces PAR2-mediated intracellular Ca 2+ release in HT29 cells with an EC50 of 0.28 μM.
  • HY-110281
    Dehydroascorbic acid

    Endogenous Metabolite Neurological Disease
    Dehydroascorbic acid, a blood-brain barrier transportable form of vitamin C, mediates potent cerebroprotection in experimental stroke.
  • HY-U00265
    3-CPs

    3-Carbethoxypsoralen; 3-Ethoxycarbonylpsoralen

    Others Infection
    3-CPs is a serotype capsular polysaccharide which can interfere with antibody-mediated bacterial killing.
  • 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-141512
    JB170

    PROTACs Aurora Kinase Cancer
    JB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC50=28 nM) by linking Alisertib, to the Cereblon-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase.
  • HY-N6894
    Pseudocoptisine acetate

    Isocoptisine acetate

    AChE Inflammation/Immunology
    Pseudocoptisine (Isocoptisine) acetate is a quaternary alkaloid with benzylisoquinoline skeleton, was isolated from Corydalis Tuber. Pseudocoptisine acetate inhibits acetylcholinesterase (AChE) activity with an IC50 of 12.8 μM. Anti-inflammatory and anti-amnestic effects.
  • HY-107587
    A-286982

    Integrin Inflammation/Immunology
    A-286982 is a potent and allosteric LFA-1/ICAM-1 interaction inhibitor with IC50s of 44 nM and 35 nM in an LFA-1/ICAM-1 binding and LFA-1-mediated cellular adhesion assay, respectively.
  • HY-102068
    Clathrin-IN-1

    HIV Infection
    Clathrin-IN-1 is a selective clathrin-mediated endocytosis (CME) inhibitor. Clathrin-IN-1 selectively inhibits amphiphysin association of clathrin terminal domain (TD) with an IC50 value of 12 μM. Clathrin-IN-1 acutely interferes with receptor-mediated endocytosis, entry of HIV, and synaptic vesicle recycling.
  • HY-114597
    PKF050-638

    HIV CRM1 Cancer
    PKF050-638 is a potent and selective inhibitor of HIV-1 Rev (IC50=0.04 μM). PKF050-638 inhibits the CRM1-mediated Rev nuclear export by disrupting CRM1-NES interaction.
  • HY-117656
    ESI-05

    NSC 116966

    Others Others
    ESI-05 (NSC 116966) is a specific antagonist of EPAC2 (exchange protein directly activated by cAMP 2), with an IC50 of 0.4 µM. ESI-05 (NSC 116966) inhibits cAMP-mediated activation of EPAC2 as well as EAPC2 mediated Rap1 activation.
  • HY-12378
    BQ-123

    Endothelin Receptor Cardiovascular Disease
    BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.
  • HY-N2345
    Procyanidin B3

    Histone Acetyltransferase Cancer
    Procyanidin B3 is a natural product, acts as a specific HAT inhibitor, binds to the other site of p300 instead of the active site, selectively inhibits p300-mediated androgen receptor acetylation. Procyanidin B3 has no effect on HDAC or HMT (histone methyltransferase).
  • 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-136244
    PF-06952229

    TGF-β Receptor Cancer
    PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor. PF-06952229 specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction. PF-06952229 is a promising antineoplastic agent for the study solid tumors, especifically metastatic breast cancer.
  • HY-13423
    Tenovin-1

    MDM-2/p53 Dihydroorotate Dehydrogenase Sirtuin Autophagy Cancer
    Tenovin-1, a p53 activator, protects p53 from MDM2-mediated degradation. Tenovin-1 acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also a dihydroorotate dehydrogenase (DHODH) inhibitor.
  • HY-110195
    Smurf1-IN-A01

    A01

    Others Others
    Smurf1-IN-A01 (A01) is an ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) inhibitor with a kd of 3.664 nM, which increases BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation.
  • 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-135231
    NL-1

    Mitochondrial Metabolism Autophagy Cancer
    NL-1 is a mitoNEET inhibitor with antileukemic effect. NL-1 inhibits REH and REH/Ara-C cells growth with IC50s of 47.35 µM and 56.26 µM, respectively. NL-1-mediated death in leukemic cells requires the activation of the autophagic pathway.
  • HY-15462
    SRT3109

    CXCR Inflammation/Immunology Endocrinology
    SRT3109 is an antagonist of CXCR2, with a pIC50 of 8.2, and used in the research of chemokine mediated diseases.
  • HY-P2273
    Calcitonin (human)

    CGRP Receptor Metabolic Disease
    Calcitonin (human) is a hypocalcemic hormone. Calcitonin (CT) inhibits the action of osteoclast mediated bone resorption.
  • HY-100456
    ZL006

    iGluR Neurological Disease
    ZL006 is a potent inhibitor of nNOS/PSD-95 interaction, and inhibits NMDA receptor-mediated NO synthesis.
  • HY-108347
    CP-100356 hydrochloride

    P-glycoprotein BCRP Metabolic Disease
    CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC50=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC50>15 µM).
  • HY-12378A
    BQ-123 TFA

    Endothelin Receptor Cardiovascular Disease
    BQ-123 TFA is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 TFA inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.
  • HY-136555
    GSK717

    NOD-like Receptor (NLR) Inflammation/Immunology
    GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells.
  • HY-16289
    Lodoxamide tromethamine

    U-42585E

    Histamine Receptor Inflammation/Immunology Endocrinology
    Lodoxamide tromethamine (U-42585E) is a medication for the treatment of prophylaxis of mast cell-mediated allergic disease.
  • HY-15530
    CID-2858522

    NF-κB Inflammation/Immunology Cancer
    CID-2858522 is a highly potent and selective antigen receptor-mediated NF-κB activation inhibitor with an IC50 of 70 nM.
  • HY-122627
    Mcl1-IN-8

    Bcl-2 Family Apoptosis 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-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-126972A
    RI(dl)-2 TFA

    RAD51 Cancer
    RI(dl)-2 TFA is a potent and selective RAD51-mediated D-loop formation inhibitor with an IC50 of 11.1 μM. RI(dl)-2 TFA does not influence RAD51 binding to ssDNA and inhibits homologous recombination (HR) activity in human cells (IC50 of 3.0 μM).
  • HY-19543
    Brusatol

    NSC 172924

    Keap1-Nrf2 Apoptosis Cancer
    Brusatol (NSC 172924) is a unique inhibitor of the Nrf2 pathway that sensitizes a broad spectrum of cancer cells to Cisplatin and other chemotherapeutic agents. Brusatol enhances the efficacy of chemotherapy by inhibiting the Nrf2-mediated defense mechanism. Brusatol can be developed into an adjuvant chemotherapeutic agent. Brusatol increases cellular apoptosis.
  • HY-W020790
    Sialyl-Lewis X

    sLeX

    Others Inflammation/Immunology
    Sialyl-Lewis X (sLeX) is a sialylated fucosylated tetrasaccharide, an endogenous antigen. Sialyl-Lewis X is a high-affinity ligand for selectins (E-, P-, and L-selectin). Sialyl-Lewis X binds to ELAM-1 and CD62 and has the ability to inhibits CD62-mediated neutrophil recruitment to sites of inflammation.
  • HY-15507
    VGX-1027

    GIT 27

    Interleukin Related TNF Receptor Metabolic Disease Inflammation/Immunology
    VGX-1027 is an orally active isoxazole compound that exhibits various immunomodulatory properties. VGX-1027 targets macrophages, reducing the production of the proinflammatory mediators TNF-α, IL-1β, IL-10. VGX-1027 has antidiabetogenic effects by limiting cytokine-mediated immunoinflammatory events.
  • 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-17013
    Dofequidar

    P-glycoprotein Cancer
    Dofequidar(MS-209) is a novel quinoline compound, which can reverse P-glycoprotein (P-gp)-mediated MDR.
  • HY-109804
    CORM-401

    Others Inflammation/Immunology
    CORM-401 is an oxidant-sensitive CO-releasing molecule, can be used in the research of inflammatory and oxidative stress-mediated pathologies.
  • HY-108869
    Fodipir

    DPDP

    Others Inflammation/Immunology
    Fodipir is an active metabolite of mangafodipir, involved in mangafodipir-mediated cytoprotection against 7β-hydroxycholesterol-induced cell death.
  • HY-113251
    2-Hydroxyestrone

    Catecholestrone

    Endogenous Metabolite Estrogen Receptor/ERR Cancer Endocrinology
    2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic.
  • HY-B1058
    Benfluorex hydrochloride

    JP-992 hydrochloride

    Others Metabolic Disease Cardiovascular Disease
    Benfluorex hydrochloride (JP-992 hydrochloride) is a hepatic nuclear factor 4 alpha (HNF4α) activator.
  • HY-P2230
    Angstrom6

    A6 Peptide

    PAI-1 Cancer
    Angstrom6 (A6 Peptide) is an 8 amino-acid peptide derived from single-chain urokinase plasminogen activator (scuPA) and interferes with the uPA/uPAR cascade and abrogates downstream effects. Angstrom6 binds to CD44 resulting in the inhibition of migration, invasion, and metastasis of tumor cells, and the modulation of CD44-mediated cell signaling.
  • HY-112683
    V-9302

    Others Cancer
    V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells.
  • 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-B1546
    Benzamil

    Benzylamiloride

    Sodium Channel Na+/Ca2+ Exchanger Neurological Disease
    Benzamil (Benzylamiloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM.
  • HY-112683A
    V-9302 hydrochloride

    Others Cancer
    V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells.
  • HY-W008634
    Bropirimine

    Toll-like Receptor (TLR) Cancer
    Bropirimine is a synthetic agonist for toll-like receptor 7 (TLR7). Bropirimine inhibits differentiation of osteoclast precursor cells into osteoclasts via TLR7-mediated production of IFN-β. Bropirimine is an orally active immunomodulator that has demonstrated anticancer activity in transitional cell carcinoma in situ (CIS) in both the bladder and upper urinary tract.
  • HY-B1546A
    Benzamil hydrochloride

    Benzylamiloride hydrochloride

    Na+/Ca2+ Exchanger Sodium Channel Neurological Disease
    Benzamil hydrochloride (Benzylamiloride hydrochloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil hydrochloride also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil hydrochloride inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM.
  • HY-101511
    TTT-28

    P-glycoprotein Cancer
    TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated Multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1.
  • HY-N10114
    Hyperectumine

    Others Inflammation/Immunology
    Hyperectumine exhibits moderate anti-inflammatory activity via suppression of LPS-activated inflammatory mediators in RAW 264.7 macrophage cells.
  • HY-P0206
    Bradykinin

    Bradykinin Receptor Endogenous Metabolite Cardiovascular Disease Endocrinology
    Bradykinin is an active peptide that is generated by the kallikrein-kinin system. It is a inflammatory mediator and also recognized as a neuromediator and regulator of several vascular and renal functions.
  • HY-112735
    Hexadimethrine bromide

    Polybrene; 1,5-Dimethyl-1,5-diazaundecamethylene polymethobromide

    Others Cancer
    Hexadimethrine bromide (Polybrene) is a cationic polymer used routinely to enhance the efficiency of retrovirus vector-mediated gene transfer.
  • HY-101508
    GNA002

    Histone Methyltransferase Cancer
    GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes.
  • 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-15478
    WZ811

    CXCR Cancer Endocrinology
    WZ811 is an orally active, highly potent competitive antagonist of CXCR4. WZ811 efficiently inhibits CXCR4/SDF-1 (or CXCL12)-mediated modulation of cAMP levels (EC50=1.2 nM) and SDF-1 induced Matrigel invasion in cells (EC50=5.2 nM).
  • HY-120645
    BMS-986122

    Opioid Receptor Neurological Disease
    BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mouse brain membranes.
  • HY-125918
    Bleomycin A5 hydrochloride

    Pingyangmycin hydrochloride

    Apoptosis Antibiotic Cancer Infection
    Bleomycin A5 (Pingyangmycin) hydrochloride is an anti-neoplastic glycoprotein antibiotic. Bleomycin A5 suppresses Drp1-mediated mitochondrial fission and induces apoptosis in human nasal polyp-derived fibroblasts. Bleomycin A5 hydrochloride has anticancer activities relying on its ability to produce RNA and DNA breaks, thus, leading to cell death..
  • HY-122614
    S29434

    NMDPEF

    Autophagy Neurological Disease
    S29434 (NMDPEF) is a potent, competitive, selective and cell-permeable inhibitor of quinone reductase 2 (QR2), with IC50s ranging from 5 to 16 nM for human QR2 at different organizational levels, and has good selectivity for QR2 over QR1. S29434 (NMDPEF) induces autophagy and inhibits QR2-mediated ROS production.
  • HY-13448
    Nedocromil

    FPL 59002

    Histamine Receptor Leukotriene Receptor Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Nedocromil suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
  • HY-16344
    Nedocromil sodium

    FPL 59002KP; Nedocromil disodium salt

    Histamine Receptor Leukotriene Receptor Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
  • HY-N9349
    Malvidin-3-O-arabinoside chloride

    AMPK Autophagy Metabolic Disease Inflammation/Immunology
    Malvidin-3-O-arabinoside chloride ameliorates ethyl carbamate-induced oxidative damage by stimulating AMPK-mediated autophagy.
  • HY-101503
    HTS01037

    FABP Metabolic Disease
    HTS01037 is an inhibitor of fatty acid binding; and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 with a Ki of 0.67 μM.
  • HY-N7617
    Toralactone

    Keap1-Nrf2 Cancer
    Toralactone, isolated from Cassia obtusifolia, mediates hepatoprotection via an Nrf2-dependent anti-oxidative mechanism.
  • HY-108730
    Avelumab

    Anti-Human PD-L1, Human Antibody; MSB 0010718C; MSB0010718C

    PD-1/PD-L1 Cancer Inflammation/Immunology
    Avelumab is a fully human IgG1 anti-PD-L1 monoclonal antibody with potential antibody-dependent cell-mediated cytotoxicity.
  • HY-112716
    N-alpha-Tosyl-L-lysine chloromethyl ketone hydrochloride

    Others Cancer
    N-alpha-Tosyl-L-lysine chloromethyl ketone (TLCK), a trypsin like protease inhibitor, sensitizes HeLa cells to Fas-mediated cell death.
  • HY-N6946
    Mitraphylline

    Others Inflammation/Immunology
    Mitraphylline is the major pentacyclic oxindolic alkaloid presented in Uncaria tomentosa. Mitraphylline inhibits lipopolysaccharide-mediated activation of primary human neutrophils.
  • HY-N1882
    4,5-Dimethoxycanthin-6-one

    Cytochrome P450 Metabolic Disease
    4,5-Dimethoxycanthin-6-one is a potent and uncompetitive inhibitor of CYP1A2-mediated phenacetin O-deethylation with an IC50 value of 1.7μM and a Ki value of 2.6 μM. 4,5-Dimethoxycanthin-6-one, as an alkaloid, is isolated from the wood of Picrasma quassioides BENNET (Simaroubaceae).
  • HY-101872A
    GSK-872 hydrochloride

    RIP kinase Inflammation/Immunology
    GSK-872 hydrochloride is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 hydrochloride decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury.
  • HY-110261
    GS143

    IKK E1/E2/E3 Enzyme NF-κB Inflammation/Immunology
    GS143 is a selec­tive IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCF βTrCP1-mediated IκBα ubiquitylation. GS143 sup­presses NF-κB acti­va­tion and tran­scrip­tion of tar­get genes and does not inhibit proteasome activity. GS143 has anti-asthma effect.
  • HY-110086
    RWJ 50271

    Integrin Inflammation/Immunology
    RWJ 50271 is an selective and orally active inhibitor of lymphocyte function-associated antigen-1/intercellular adhesion molecule-1(LFA-1/ICAM-1) interaction with an IC50 of 5.0 μM (HL60 cells). RWJ 50271 inhibits LFA-1/ICAM-1-mediated cell adhesion.
  • HY-123905
    LIN28 inhibitor LI71

    MicroRNA Cancer
    LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM. LIN28 inhibitor LI71 directly binds the cold shock domain (CSD) to suppress LIN28’s activity against let-7 in leukemia cells and embryonic stem cells.
  • HY-101872
    GSK-872

    RIP kinase Inflammation/Immunology
    GSK-872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury.
  • HY-N4231
    Lucyoside B

    NF-κB Inflammation/Immunology
    Lucyoside B inhibits the production of inflammatory mediators via both NF-κB and activator protein-1 pathways in activated macrophages.
  • HY-N2448
    Lindleyin

    Estrogen Receptor/ERR Endocrinology
    Lindleyin, isolated from Rhei rhizoma, mediates hormonal effects through estrogen receptors. Lindleyin binds to ERα with estrogenic activity.
  • HY-B2188
    S-Methyl-L-cysteine

    L-S-Methylcysteine

    Reactive Oxygen Species Metabolic Disease Neurological Disease
    S-Methyl-L-cysteine is a natural product that acts as a substrate in the catalytic antioxidant system mediated by methionine sulfoxide reductase A (MSRA), with antioxidative, neuroprotective, and anti-obesity activities.
  • HY-N0816
    Polyphyllin VI

    Apoptosis Pyroptosis Cancer
    Polyphyllin VI, an active saponin, possess anti-cancer activities. Polyphyllin VI induces G2/M cell cycle arrest and triggers apoptosis. Polyphyllin VI induces caspase-1-mediated pyroptosis via the induction of ROS/NF-κB/NLRP3/GSDMD signal axis in non-small cell lung cancer.
  • HY-117958
    HJC0197

    Ras Cancer Metabolic Disease Cardiovascular Disease
    HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP.
  • HY-108676
    NF023 hexasodium

    P2X Receptor Neurological Disease
    NF023 hexasodium is a selective and competitive P2X1 receptor antagonist, with IC50 values of 0.21 μM, 28.9 μM, > 50 μM and > 100 μM for human P2X1, P2X3, P2X2, and P2X4-mediated responses respectively.
  • HY-100237
    SZL P1-41

    E1/E2/E3 Enzyme Apoptosis Cancer
    SZL P1-41 is a specific Skp2 inhibitor, binds to the F-box domain of Skp2 to prevent Skp1 association and Skp2 SCF complex formation. SZL P1-41, like Skp2 deficiency, augments p27-mediated apoptosis/senescence, while it impairs Akt-driven glycolysis. Anti-tumor activities.
  • HY-107911
    Protamine sulfate

    Thrombin Metabolic Disease
    Protamine sulfate, polycationic peptide and a antiheparin agent, could neutralize the anticoagulant action of heparin and enhances lipid-mediated gene transfer.
  • HY-139024
    ACAT-IN-7

    Acyltransferase Inflammation/Immunology
    ACAT-IN-7 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-7 inhibits NF-κB mediated transcription.
  • HY-N0648
    Monotropein

    Others Inflammation/Immunology
    Monotropein is an iridoid glycoside isolated Morinda officinalis. Monotropein inhibits the expression of inflammatory mediators in dextran sulfate sodium (DSS)-induced colitis mouse model.
  • HY-139020
    ACAT-IN-3

    Acyltransferase Inflammation/Immunology
    ACAT-IN-3 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-3 inhibits NF-κB mediated transcription.
  • HY-136540
    Resolvin D3

    RvD3

    Others Inflammation/Immunology
    Resolvin D3 (RvD3) is a docosahexaenoic acid (DHA) derived mediator. Resolvin D3 is dysregulated in arthritis and reduces arthritic inflammation.
  • HY-N1480
    (-)-Fucose

    6-Desoxygalactose; L-(-)-Fucose; L-Galactomethylose

    Endogenous Metabolite Parasite Infection Metabolic Disease
    (-)-Fucose is classified as a member of the hexoses, plays a role in A and B blood group antigen substructure determination, selectin-mediated leukocyte-endothelial adhesion, and host-microbe interactions.
  • HY-70050A
    Alosetron

    GR 68755; GR 68755X

    5-HT Receptor Inflammation/Immunology Neurological Disease
    Alosetron (GR 68755) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects.
  • HY-115497
    BRD5529

    E1/E2/E3 Enzyme Inflammation/Immunology
    BRD5529 is a selective CARD9-E3 ubiquitin ligase TRIM62 protein-protein interaction inhibitor with an IC50 of 8.6 μM. BRD5529 directly and selectively binds CARD9, disrupts TRIM62 recruitment, inhibits TRIM62-mediated ubiquitinylation and activation of CARD9, and demonstrates cellular activity and selectivity in CARD9-dependent pathways.
  • HY-129624A
    Bisindolylmaleimide VIII acetate

    Ro 31-7549 acetate; Bis VIII acetate

    PKC Apoptosis Cancer Inflammation/Immunology
    Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively. Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.
  • HY-101906
    DC260126

    GPR40 Apoptosis Metabolic Disease
    DC260126 is a potent antagonist of GPR40 (FFAR1). DC260126 dose-dependently inhibits GPR40-mediated Ca 2+ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50: 6.28, 5.96, 7.07, 4.58 μM, respectively). DC260126 could protect MIN6 β cells from palmitate-induced ER stress and apoptosis.
  • HY-14754
    Salirasib

    S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS

    Ras Autophagy Cancer
    Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.
  • HY-W097009
    Violuric acid

    Others Others
    Violuric acid is a redox mediator used in the laccase system. The violuric acid assay is a method to ascertain that the high-redox potential of laccase is not lost during directed evolution.
  • HY-W010347
    L-Homocysteine

    Endogenous Metabolite Inflammation/Immunology
    L-Homocysteine, a homocysteine metabolite, is a homocysteine that has L configuration. L-Homocysteine induces upregulation of cathepsin V that mediates vascular endothelial inflammation in hyperhomocysteinaemia.
  • 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-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-P1514
    Peptide YY (PYY), human

    Neuropeptide Y Receptor Metabolic Disease Neurological Disease Endocrinology
    Peptide YY (PYY) is a gut hormone that regulates appetite and inhibits pancreatic secretion. Peptide YY (PYY) can mediate its effects through the Neuropeptide Y receptors.
  • HY-108643
    CMPD1

    MAPKAPK2 (MK2) Cancer
    CMPD1 is a selective and non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor with apparent Ki (Ki app) of 330 nM.
  • HY-70050C
    Alosetron Hydrochloride

    GR 68755C; GR 68755 Hydrochloride; GR 68755X Hydrochloride

    5-HT Receptor Neurological Disease
    Alosetron Hydrochloride (GR 68755C) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron Hydrochloride attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects.
  • HY-126396
    Sordarin sodium

    CaMK Fungal Antibiotic Infection Inflammation/Immunology
    Sordarin is a potent diphthamide-dependent eEF2 inhibitor with antifungal properties. Sordarin targets eEF2 so as to inhibit protein translation by blocking eEF2-mediated translocation of tRNAs. Sordarin inhibits translation specifically in certain fungi (e.g. C. albicansC. glabrata, and C. neoformans) while unable to do so in some other fungal species (e.g. Candida parapsilosis and Candida lusitaniae).
  • HY-110088
    SCH529074

    MDM-2/p53 Cancer
    SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC).
  • HY-139025
    ACAT-IN-8

    Acyltransferase Inflammation/Immunology
    ACAT-IN-8 (example 206) is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-8 inhibits NF-κB mediated transcription.
  • HY-W020005
    2-Carboxyphenol-d4

    Others Others
    2-Carboxyphenol-d4 is the deuterium labeled 2-Carboxyphenol. 2-Carboxyphenol is a plant hormone and mediates host responses against microbial pathogens.
  • HY-13991
    CCG-1423

    Ras Cancer
    CCG-1423 is a novel inhibitor of RhoA/C-mediated gene transcription that is capable of inhibiting invasion of PC-3 prostate cancer cells in a Matrigel model of metastasis.
  • HY-N0775
    Isocorynoxeine

    7-Isocorynoxeine

    5-HT Receptor Neurological Disease
    Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM.
  • HY-139021A
    ACAT-IN-4 hydrochloride

    Acyltransferase Inflammation/Immunology
    ACAT-IN-4 hydrochloride (Example 208) is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-4 hydrochloride inhibits NF-κB mediated transcription.
  • HY-N0805
    Alisol B 23-acetate

    23-Acetylalismol B; 23-O-Acetylalisol B; Alisol B monoacetate

    Others Others
    Alisol B 23-acetate (23-Acetylalismol B), a natural triterpenoid, produces protective effects against EE-induced cholestasis, due to FXR-mediated gene regulation.
  • HY-139021
    ACAT-IN-4

    Acyltransferase Inflammation/Immunology
    ACAT-IN-4 (Example 208) is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-4 inhibits NF-κB mediated transcription.
  • HY-B0649
    Propofol

    2,6-Diisopropylphenol

    GABA Receptor Endogenous Metabolite Neurological Disease
    Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic.
  • HY-115716
    EGFR-IN-17

    EGFR Cancer
    EGFR-IN-17 is a potent and selective inhibitor of the epidermal growth factor receptor ( IC50 0.0002 μM) to overcome C797S-mediated resistance.
  • 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-133807A
    (Rac)-Benpyrine

    TNF Receptor Inflammation/Immunology
    (Rac)-Benpyrine, a racemate of Benpyrine, is a potent and orally active TNF-α inhibitor. (Rac)-Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research.
  • HY-139022
    ACAT-IN-5

    Acyltransferase Inflammation/Immunology
    ACAT-IN-5 (example 19) is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-5 inhibits NF-κB mediated transcription.
  • HY-N0050
    Allomatrine

    (+)-Allomatrine

    Others Neurological Disease
    Allomatrine ((+)-Allomatrine) is an alkaloid from the bark of Sophora japonica. Allomatrine has antinociceptive properties mediated mainly through the activation ofκ-opioid receptors.
  • HY-W002116
    Methyl syringate

    TRP Channel Inflammation/Immunology
    Methyl syringate, a chemical marker of asphodel monofloral honey, is an efficient phenolic mediator for bacterial and fungal laccases. Methyl syringate is a TRPA1 agonist.
  • HY-132589
    Vutrisiran

    ALN-TTRsc02

    Others Neurological Disease
    Vutrisiran (ALN-TTRsc02) is a liver-directed, investigational, small interfering ribonucleic acid (siRNA) agent. Vutrisiran can be used for transthyretin (TTR)-mediated amyloidosis research.
  • HY-134665
    NITD-2

    DNA/RNA Synthesis Infection
    NITD-2, a dengue virus (DENV) polymerase inhibitor, inhibits the DENV RdRp-mediated RNA elongation. NITD-2 penetrates cell membrane poorly.
  • HY-103220
    6,2',4'-Trimethoxyflavone

    Aryl Hydrocarbon Receptor Cancer Neurological Disease
    6,2',4'-Trimethoxyflavone is a potent aryl hydrocarbon receptor (AHR) antagonist. 6,2',4'-Trimethoxyflavone represses AHR-mediated gene induction.
  • HY-W011890
    Cridanimod

    Progesterone Receptor IFNAR Inflammation/Immunology
    Cridanimod is a potent progesterone receptor (PR) activator mediated through induction of IFNα and IFNβ expression. Cridanimod is a small-molecule immunomodulator and interferon inducer.
  • HY-D0937
    Methoxy-PMS

    1-Methoxy PMS; 1-Methoxyphenazine methosulfate

    Reactive Oxygen Species Others
    Methoxy-PMS (1-Methoxy PMS), an active oxygen formation inducer, is stable electron-transport mediator between NAD(P)H and tetrazolium dyes.
  • HY-N2518
    Agnuside

    Agnoside

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Agnuside is a compound isolated from Vitex negundo, down-regulates pro-inflammatory mediators PGE2 and LTB4, and reduces the expression of cytokines, with anti-arthritic activity.
  • HY-118828
    12-Oxo phytodienoic acid

    12-OPDA

    Bacterial Infection
    12-Oxo phytodienoic acid is a biologically active, immediate precursor of 7-epi jasmonic acid. 12-Oxo phytodienoic acid plays an independent role in mediating resistance to pathogens and pests.
  • HY-P0197
    Neurokinin A

    Substance K; Neurokinin α; Neuromedin L

    Neurokinin Receptor Neurological Disease Endocrinology
    Neurokinin A (Substance K), a peptide neurotransmitter of the tachykinin family, acts via the NK-2 receptor. Neurokinin A acts as a major mediator in human airway and gastrointestinal tissues.
  • HY-N7152
    6-Dehydrogingerdione

    Apoptosis Cancer
    6-Dehydrogingerdione sensitizes human hepatoblastoma hep G2 cells to TRAIL-induced apoptosis via reactive oxygen species-mediated increase of DR5.
  • HY-N0425
    Epoxylathyrol

    P-glycoprotein Cancer
    Epoxylathyrol, an epoxylathyrane derivative isolated from the Euphorbia boetica, is a P-glycoprotein (P-gp) inhibitor. Epoxylathyrol is a P-gp-mediated multidrug resistance (MDR) reverser.
  • HY-12742
    SCR7

    DNA/RNA Synthesis CRISPR/Cas9 Apoptosis Cancer
    SCR7 is an unstable form that can be autocyclized into a stable form SCR7 pyrazine. 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-113509
    Lipoxin A4

    LXA4

    Interleukin Related Inflammation/Immunology
    Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties. Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways. Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC50 value of 25.74 nM.
  • HY-128892
    EN6

    Autophagy Proton Pump Neurological Disease
    EN6 is a small-molecule in vivo activator of autophagy that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal the vacuolar H + ATPase (v-ATPase). EN6-mediated ATP6V1A modification decouples the v-ATPase from the Rags, leading to inhibition of mTORC1 signaling, increased lysosomal acidification and activation of autophagy. EN6 clears TDP-43 aggregates, a causative agent in frontotemporal dementia, in a lysosome-dependent manner.
  • HY-111329
    JGB1741

    ILS-JGB-1741

    Sirtuin Apoptosis Cancer
    JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC50 of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC50>100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediated apoptosis with modulation of Bax/Bcl2 ratio, cytochrome c release and PARP cleavage. JGB1741 has the potential for breast cancer research.
  • HY-D1027
    Dansylcadaverine

    Monodansyl cadaverine

    Autophagy Others
    Dansylcadaverine (Monodansyl cadaverine) is an autofluorescent compound used for the labeling of autophagic vacuoles. Dansylcadaverine, a high affinity substrate of transglutaminases, can block the receptor-mediated endocytosis of many ligands.
  • HY-115604
    Pitstop 2

    Apoptosis Cancer
    Pitstop 2 is a clathrin inhibitor which inhibits clathrin-mediated endocytosis (CME) by associating with the terminal domain of clathrin. Pitstop 2 has the potential for anti-cancer research.
  • HY-116078
    CKD-519

    CETP Cardiovascular Disease
    CKD-519 is a selective and potent cholesteryl ester transfer protein (CETP) inhibitor, which inhibits CETP-mediated transfer of cholesteryl ester in human serum with an IC50 of 2.3 nM.
  • HY-101106
    AR7

    RAR/RXR Cancer Neurological Disease
    AR7 is an atypical RARA/RARα (retinoic acid receptor, alpha) antagonist. AR7 specifically activates chaperone-mediated-autophagy (CMA) activity without affecting macroautophagy.
  • HY-P1291
    PKI 14-22 amide,myristoylated

    PKA Cancer
    PKI 14-22 amide,myristoylated is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.
  • 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-12022
    3-Aminobenzamide

    PARP-IN-1

    PARP Cancer
    3-Aminobenzamide (PARP-IN-1) is a potent inhibitor of PARP with IC50 of appr 50 nM in CHO cells, and acts as a mediator of oxidant-induced myocyte dysfunction during reperfusion.
  • 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-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-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-134452
    MeAIB

    α-(Methylamino)isobutyric acid

    Others Others
    MeAIB (α-(Methylamino)isobutyric acid) is a specific substrate for amino acid transport system A (ATA1). ATA mediate the uptake of short-chain neutral amino acids in a Na +-dependent manner.
  • HY-N2197
    Hirsuteine

    Others Neurological Disease
    Hirsuteine is an indole alkaloid extracted from Uncaria genus. Hirsuteine non-competitively antagonizes nicotine-mediated dopamine release by blocking ion permeation through nicotinic receptor channel complexes.
  • HY-107498
    GNE-8324

    iGluR Neurological Disease
    GNE-8324 is a selective GluN2A positive allosteric modulator. GNE-8324 selectively enhances NMDA receptor (NMDAR)-mediated synaptic responses in inhibitory but not excitatory neurons.
  • 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-B0631
    Alendronic acid

    Others Cancer
    Alendronic acid, a bisphosphonate, is a farnesyl diphosphate synthase (FDPS) inhibitor. Alendronic acid inhibits osteoclast-mediated bone resorption. Alendronic acid shows efficacy in postmenopausal osteoporosis, malignant hypercalcemia and Paget’s disease.
  • HY-P0197A
    Neurokinin A TFA

    Substance K TFA; Neurokinin α TFA; Neuromedin L TFA

    Neurokinin Receptor Endocrinology Neurological Disease
    Neurokinin A TFA (Substance K TFA), a peptide neurotransmitter of the tachykinin family, acts via the NK-2 receptor. Neurokinin A acts as a major mediator in human airway and gastrointestinal tissues.
  • HY-Y0520
    Itaconic acid

    Endogenous Metabolite Inflammation/Immunology
    Itaconic acid, a precursor of polymers, chemicals, and fuels, can be synthesized by many fungi. Itaconic acid also is a macrophage-specific metabolite. Itaconic acid mediates crosstalk between macrophage metabolism and peritoneal tumors.
  • HY-103348
    Boc-Asp(OMe)-fluoromethyl ketone

    Boc-Asp(OMe)-FMK

    Caspase Inflammation/Immunology
    Boc-Asp(OME)-Fluoromethyl Ketone is a broad range caspase inhibitor that inhibits Fas-mediated phagocytosis and oxidative rupture inhibition, but does not affect the chemotactic activity of IL-8.
  • HY-P0188
    ω-Conotoxin MVIIC

    Calcium Channel Neurological Disease
    ω-Conotoxin MVIIC is a N- and P/Q-type Ca 2+ channel blocker, significantly suppresses the 11-keto-βboswellic acid-mediated inhibition of glutamate release.
  • HY-U00141
    ABTL-0812

    α-Hydroxylinoleic acid

    Autophagy Metabolic Disease
    ABTL-0812 (α-Hydroxylinoleic acid) induces endoplasmic reticulum (ER) stress-mediated autophagy. ABTL-0812 is a first-in-class small molecule with anti-cancer activity.
  • HY-B0268A
    Enoxacin hydrate

    Enoxacin sesquihydrate; AT-2266 hydrate; CI-919 hydrate

    Bacterial DNA/RNA Synthesis MicroRNA Antibiotic Infection Cancer
    Enoxacin hydrate (Enoxacin sesquihydrate), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin hydrate is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin hydrate has potent activities against gram-positive and -negative bacteria. Enoxacin hydrate is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing.
  • 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-B0268
    Enoxacin

    AT 2266; CI 919

    Bacterial DNA/RNA Synthesis MicroRNA Antibiotic Cancer Infection
    Enoxacin (AT 2266), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin has potent activities against gram-positive and -negative bacteria. Enoxacin is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing.
  • HY-B1218
    Sulfaphenazole

    Bacterial Infection
    Sulfaphenazole is a specific inhibitor of CYP2C9 which blocks atherogenic and pro-inflammatory effects of linoleic acid (increase in oxidative stress and activation of AP-1) mediated by CYP2C9.
  • HY-D1267
    PAO-Nap

    Apoptosis Cancer
    PAO-Nap is the modified PAO attached a naphthalimide fluorophore using aminocaproic acid as a linker. PAO induces oxidative stress-mediated apoptosis in HL-60 cells by selectively targeting thioredoxin reductase.
  • HY-100783A
    (-)-Bicuculline methochloride

    l-Bicuculline methochloride

    GABA Receptor Neurological Disease
    (-)-Bicuculline methochloride (l-Bicuculline methochloride) is a potent GABAA receptor antagonist. (-)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
  • HY-16126
    Carboxyamidotriazole

    L-651582; CAI

    Calcium Channel Cancer Inflammation/Immunology
    Carboxyamidotriazole (L-651582) is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole shows anti-tumor, anti-inflammatory and antiangiogenic effects.
  • HY-P0188A
    ω-Conotoxin MVIIC TFA

    Calcium Channel Neurological Disease
    ω-Conotoxin MVIIC TFA is a N- and P/Q-type Ca 2+ channel blocker, significantly suppresses the 11-keto-βboswellic acid-mediated inhibition of glutamate release.
  • HY-N0139
    Troxerutin

    Trihydroxyethylrutin

    NOD-like Receptor (NLR) Cancer Metabolic Disease Inflammation/Immunology Neurological Disease
    Troxerutin, also known as vitamin P4, is a tri-hydroxyethylated derivative of natural bioflavonoid rutins which can inhibit the production of reactive oxygen species (ROS) and depress ER stress-mediated NOD activation.
  • HY-102076
    0990CL

    Others Others
    0990CL is a specific heterotrimeric Gαi subunit inhibitor by direct interaction with Gαi. 0990CL is able to block α2AR mediated regulation of cAMP.
  • HY-100783
    (-)-Bicuculline methobromide

    l-Bicuculline methobromide

    GABA Receptor Neurological Disease
    (-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent GABAA receptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
  • HY-N4053
    Heraclenin

    Others Inflammation/Immunology
    Heraclenin, a natural furanocoumarin, significantly inhibits T cell receptor-mediated proliferation in human primary T cells in a concentration-dependent manner by targeting nuclear factor of activated T-cells (NFAT).
  • HY-141478
    Antitumor agent-28

    ATM/ATR Cancer
    Antitumor agent-28 selectively inhibits ataxia telangiectasia mutated (ATM) kinase. Antitumor agent-28 prevents ATM mediated disease and has potent anti-cancer activity.
  • HY-12809
    Optovin

    TRP Channel Neurological Disease
    Optovin is a reversible photoactivated TRPA1 ligand that enables light-mediated neuronal excitation. Optovin activates TRPA1 via structure-dependent photochemical reactions with redox-sensitive cysteine residues.
  • HY-132590
    Revusiran

    ALN-TTRSC

    Others Neurological Disease
    Revusiran (ALN-TTRSC) is a 1st-generation short interfering RNA, which directed against transthyretin (TTR) mRNA. Revusiran can be used for transthyretin (TTR)-mediated amyloidosis research.
  • HY-W011819
    Tetradecanedioic acid

    Endogenous Metabolite Metabolic Disease
    Tetradecanedioic acid is an endogenous metabolite and belongs to the class of organic compounds known as long-chain fatty acids. Tetradecanedioic acid can act as a candidate biomarker for organic anion-transporting polypeptide mediated drug-drug interactions .
  • HY-N4323
    14-Deoxyandrographolide

    Apoptosis 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-P1291A
    PKI 14-22 amide,myristoylated TFA

    PKA Cancer
    PKI 14-22 amide,myristoylated TFA is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated TFA reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.
  • HY-132966
    ASP2453

    Ras Cancer
    ASP2453 is a potent, selective and covalent KRAS G12C inhibitor. ASP2453 inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf with an IC50 value of 40 nM.
  • HY-134811
    KRAS G12D inhibitor 1

    Ras Cancer
    KRAS G12D inhibitor 1 (example 243) is a KRAS G12D inhibitor, with an IC50 of 0.8 nM for KRAS G12D-mediated ERK phosphorylation.
  • HY-B0890
    Zomepirac sodium salt

    McN-2783-21-98

    PGE synthase Inflammation/Immunology
    Zomepirac sodium salt (McN-2783-21-98) is a potent prostaglandin biosynthesis inhibitor. Zomepirac sodium salt is a non-steroidal anti-inflammatory drug (NSAID). Zomepirac sodium salt can cause immune-mediated liver injury.
  • HY-139569
    Ebaresdax

    Endogenous Metabolite Others
    Ebaresdax can inhibit peroxynitrite oxidation derived by SIN-1 and peroxynitrite mediated Cytotoxicity with IC50s of 3.7±0.80 and 0.13±0.02 uM, respectively.
  • 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-U00442
    CTX1

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    CTX1 is a p53 activator that overcomes HdmX-mediated p53 repression. CTX1 exhibits potent anti-cancer activity in a mouse acute myeloid leukemia (AML) model system.
  • HY-135336
    (R)-Verapamil hydrochloride

    (R)-(+)-Verapamil hydrochloride

    P-glycoprotein Apoptosis Cancer
    (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer drugs.
  • HY-W015343
    3-Methoxyphenylacetic acid

    m-Methoxyphenylacetic acid

    Others Others
    3-Methoxyphenylacetic acid (m-Methoxyphenylacetic acid), a m-hydroxyphenylacetic acid (m-OHPAA) derivative, is a phytotoxin in Rhizoctonia solani. 3-Methoxyphenylacetic acid is used to develop a toxin-mediated bioassay for resistance to rhizoctonia root rot.
  • HY-12521
    GSK-5498A

    CRAC Channel Inflammation/Immunology
    GSK-5498A is a selective small molecule blocker of CARC (IC50, 1 μM); inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.
  • HY-N0150
    Monensin sodium salt

    Monensin A sodium salt

    Bacterial Sodium Channel Antibiotic Infection Cancer
    Monensin sodium salt is an antibiotic secreted by the bacteria Streptomyces cinnamonensis. Monensin sodium salt is an ionophore that mediates Na +/H + exchange. Monensin sodium salt causes a marked enlargement of the multivesicular bodies (MVBs) and regulates exosome secretion.
  • 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-N6010
    8-Hydroxybergapten

    Others Others
    8-hydroxybergapten is O-methylated by cell-free extracts of Ruta cells to isopimpinellin, in reactions mediated by discrete O-methyltransferases. 8-hydroxybergapten has excellent anti-wrinkle effect.
  • HY-B2162
    Chondroitin sulfate

    Chondroitin polysulfate

    NO Synthase MMP Endogenous Metabolite Inflammation/Immunology
    Chondroitin sulfate, one of five classes of glycosaminoglycans, has been widely used in the treatment of osteoarthritis. Chondroitin sulfate reduces inflammation mediators and the apoptotic process and is able to reduce protein production of inflammatory cytokines, iNOS and MMPs.
  • HY-108464A
    Phenamil methanesulfonate

    Sodium Channel TRP Channel Metabolic Disease Inflammation/Immunology
    Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM. Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca 2+ transport with an IC50 of 140 nM in a Ca 2+ uptake assay. Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease.
  • HY-18758
    IN-1130

    TGF-β Receptor Cancer Inflammation/Immunology
    IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis.
  • HY-N4226
    1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid

    Others Inflammation/Immunology Cancer
    1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid is from Cordyceps bassiana, which is one of Cordyceps species with anti-oxidative, anti-cancer, anti-inflammatory, anti-diabetic, anti-obesity, anti-angiogenic, and anti-nociceptive activities. 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid targets to block AP-1-mediated luciferase activity, implying it has an anti-inflammatory function.
  • HY-N0109
    Salidroside

    Rhodioloside

    mTOR Apoptosis Cancer
    Salidroside is a prolyl endopeptidase Inhibitor. Salidroside alleviates cachexia symptoms in mouse models of cancer cachexia via activating mTOR signalling. Salidroside protects dopaminergic neurons by enhancing PINK1/Parkin-mediated mitophagy.
  • HY-139019
    ACAT-IN-2

    Acyltransferase Inflammation/Immunology
    ACAT-IN-2 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 187. ACAT-IN-2 inhibits NF-κB mediated transcription.
  • HY-116429
    Maresin 1

    Reactive Oxygen Species Inflammation/Immunology
    Maresin 1, produced by human Mφs from endogenous docosahexaenoic acid (DHA) and a specialized proresolving mediator, stimulates intracellular [Ca 2+] and secretion. Maresin 1 possesses anti-inflammatory activity.
  • HY-139026
    ACAT-IN-9

    Acyltransferase Inflammation/Immunology
    ACAT-IN-9 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 207. ACAT-IN-9 inhibits NF-κB mediated transcription.
  • HY-114492
    GSK547

    GSK'547

    RIP kinase Cancer
    GSK547 (GSK'547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIPK1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.
  • HY-125445
    PCTR1

    Others Inflammation/Immunology
    PCTR1 is a potent monocyte/macrophage agonist, regulating key anti-inflammatory and pro-resolving processes during bacterial infection. PCTR1 is a member of the protectin family of specialized pro-resolving mediators (SPMs).
  • HY-P1868
    α2β1 Integrin Ligand Peptide

    Integrin Infection
    α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
  • HY-N0042
    Ginsenoside Rc

    Panaxoside Rc

    GABA Receptor TNF Receptor Interleukin Related Cancer Inflammation/Immunology Neurological Disease
    Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptorA (GABAA)-mediated ion channel currents (IGABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β.
  • HY-122907
    JNJ4796

    Influenza Virus Infection
    JNJ4796 is an oral active fusion inhibitor of influenza virus, neutralizing influenza A group 1 viruses by inhibiting hemagglutinin (HA)-mediated fusion. JNJ4796 mimics the functionality of the broadly neutralizing antibodies (bnAbs).
  • HY-121885
    LMD-009

    CCR Metabolic Disease Endocrinology
    LMD-009 is a selective CCR8 nonpeptide agonist. LMD-009 mediates chemotaxis, inositol phosphate accumulation, and calcium release in high potencies with EC50s from 11 to 87 nM.
  • HY-N7126
    Citronellal

    Others Neurological Disease
    Citronellal is a monoterpenea from the essential oils in various aromatic species of plants, with depressant, hypnotic, and antinociceptive properties. Citronellal attenuates mechanical nociception, mediated in part by the NO-cGMP-ATP-sensitive K channel pathway.
  • HY-P1868A
    α2β1 Integrin Ligand Peptide TFA

    Integrin Others
    α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
  • HY-131059
    CBS1117

    Influenza Virus Infection
    CBS1117 is a virus entry inhibitor with an IC50 of 70 nM for influenza A virus, A/Puerto Rico/8/34 (H1N1). CBS1117 interferes with the hemagglutinin (HA)-mediated fusion process.
  • HY-139027
    ACAT-IN-10

    Acyltransferase Inflammation/Immunology
    ACAT-IN-10 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 197. ACAT-IN-10 weakly inhibits NF-κB mediated transcription.
  • HY-107790
    5-Methoxyflavone

    DNA/RNA Synthesis Neurological Disease
    5-Methoxyflavone, belonged to Flavonoid family, is a DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. possess central nervous system (CNS) depressant effect mediated through the ionotropic GABAA receptors.
  • 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-139027A
    ACAT-IN-10 dihydrochloride

    Acyltransferase Inflammation/Immunology
    ACAT-IN-10 dihydrochloride is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 197. ACAT-IN-10 dihydrochloride weakly inhibits NF-κB mediated transcription.
  • HY-139023
    ACAT-IN-6

    Acyltransferase Inflammation/Immunology
    ACAT-IN-6 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 200. ACAT-IN-6 potently inhibits NF-κB mediated transcription.
  • HY-N3307
    (+)-Medioresinol

    Bacterial Fungal Reactive Oxygen Species Apoptosis Infection Neurological Disease Cardiovascular Disease
    (+)-Medioresinol is a furofuran type lignan with antifungal, antibacterial and lesishmanicidal activities. (+)-Medioresinol leads to intracellular ROS accumulation and mitochondria-mediated apoptotic cell death in Candida albicans. (+)-Medioresinol can reduce the cardiovascular disease risk.
  • HY-126539
    UBE2T/FANCL-IN-1

    Others Cancer
    UBE2T/FANCL-IN-1 is a potent inhibitor of UBE2T/FANCL-mediated FANCD2 monoubiquitylation that sensitizes cells to the DNA cross-linking agent, Carboplatin.
  • HY-110105
    NS8593 hydrochloride

    Potassium Channel Neurological Disease
    NS8593 hydrochloride is a potent and selective small conductance Ca 2+-activated K + channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca 2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca 2+), and does not affect the Ca 2+-activated K + channels of intermediate and large conductance (hIK and hBK channels, respectively).
  • HY-70050B
    Alosetron ((Z)-2-butenedioate)

    GR 68755 ((Z)-2-butenedioate); GR 68755X ((Z)-2-butenedioate)

    5-HT Receptor Inflammation/Immunology Neurological Disease
    Alosetron (GR 68755) (Z)-2-butenedioate is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron (Z)-2-butenedioate is used for the research of irritable bowel syndrome (IBS). Alosetron (Z)-2-butenedioate blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron (Z)-2-butenedioate attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects.
  • HY-106178
    PMX-53

    3D53

    Complement System Cancer Inflammation/Immunology Cardiovascular Disease
    PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC50 of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects.
  • HY-70050
    Alosetron (Hydrochloride(1:X))

    GR 68755 (Hydrochloride(1:X)); GR 68755X (Hydrochloride(1:X))

    5-HT Receptor Inflammation/Immunology Neurological Disease
    Alosetron (GR 68755) Hydrochloride(1:X) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride(1:X) is used for the research of irritable bowel syndrome (IBS). Alosetron Hydrochloride(1:X) blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron Hydrochloride(1:X) attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects.
  • HY-12757
    YHO-13177

    BCRP Cancer
    YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells.
  • HY-109011
    Rosiptor

    AQX-1125

    Phosphatase Cancer
    Rosiptor (AQX-1125) is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects. Rosiptor (AQX-1125) inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro.
  • HY-135146
    GSK-3484862

    DNA Methyltransferase Cancer
    GSK-3484862 is a non-covalent inhibitor for Dnmt1. GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates global demethylation in murine embryonic stem cells.
  • 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-100807
    Quinolinic acid

    Endogenous Metabolite iGluR Inflammation/Immunology Neurological Disease
    Quinolinic acid is an endogenous N-methyl-D-aspartate (NMDA) receptor agonist synthesized from L-tryptophan via the kynurenine pathway and thereby has the potential of mediating N-methyl-D-aspartate neuronal damage and dysfunction.
  • HY-103269
    BAI1

    Bcl-2 Family Apoptosis Cancer
    BAI1 is a selective and allosteric inhibitor of BAX, an apoptosis regulator. BAI1 directly binds to BAX and allosterically inhibits BAX activation. BAI1 has the potential for the research of diseases mediated by BAX-dependent cell death.
  • HY-W001542
    5-Hydroxyoxindole

    Reactive Oxygen Species Cancer Metabolic Disease Neurological Disease
    5-Hydroxyoxindole is a structural analog of uric acid. 5-Hydroxyoxindole has DPPH radical scavenging activities and lipid peroxidation-inhibitory activities. 5-Hydroxyoxindole can be used for the research of oxidative stress-mediated disorders.
  • HY-133511
    MLS000544460

    Phosphatase Cancer
    MLS000544460 is a highly selective and reversible Eya2 phosphatase inhibitor with a Kd of 2.0 μM and an IC50 of 4 μM. MLS000544460 inhibit Eya2 phosphatase mediated cell migration and has anti-cancer activity.
  • HY-121192
    Capillarisin

    ROS Inflammation/Immunology Neurological Disease
    Capillarisin, as a constituent from Artemisiae Capillaris herba, is found to exert anti-inflammatory and antioxidant properties. Capillarisin can be used for the research of asthma-mediated complications and can be a potential neuroprotectant against bupivacaine-induced neurotoxicity.
  • HY-124416
    ML604086

    CCR Inflammation/Immunology Endocrinology
    ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca 2+ concentrations.
  • 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-132580
    Tofersen

    BIIB067; ISIS-SOD1Rx

    Others Neurological Disease
    Tofersen (BIIB067) is an antisense oligonucleotide that mediates RNase H-dependent degradation of superoxide dismutase 1 (SOD1) mRNA to reduce the synthesis of SOD1 protein. Tofersen can be used for the research of amyotrophic lateral sclerosis (ALS).
  • HY-N0656
    Usnic acid

    Bacterial Cancer Infection
    Usnic acid, a lichen-derived secondary metabolite, has a unique dibenzofuran skeleton. Usnic acid has excellent anticancer and antimicrobial properties. Usnic acid significantly inhibits RANKL-mediated osteoclast formation and function by reducing the transcriptional and translational expression of NFATc1.
  • HY-17043
    Loratadine

    Loratidine; SCH 29851

    Histamine Receptor Influenza Virus Infection Endocrinology Inflammation/Immunology
    Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
  • HY-19024
    Merbarone

    NSC 336628

    Topoisomerase Cancer
    Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage without stabilizing topo II-DNA covalent complexes. Merbarone is an anticancer agent.
  • HY-W011400
    TLR1

    MyD88 Inflammation/Immunology
    TLR1 (compound 4a) is a low molecular weight, cell-penetrating Toll/IL-1 receptor/resistance (TIR) domain/BB-Loop mimic. TLR1 inhibits IL-1 receptor-mediated responses.
  • HY-129055
    Isoeleutherin

    Fungal Inflammation/Immunology
    Isoeleutherin is a naphthopyran derivative isolated from E. americana Merr. Et Heyne with anti-fungal, anti-viral, and anti-tumor activities. Isoeleutherin plays an important role in selective modulation of T helper cell-mediated immune responses.
  • HY-P0242
    Neurokinin B

    Neurokinin Receptor Neurological Disease Endocrinology
    Neurokinin B belongs to the tachykinin family of peptides. Neurokinin B binds a family of GPCRs-including neurokinin receptor 1 (NK1R), NK2R, and NK3R-to mediate their biological effect.
  • HY-114492A
    (Rac)-GSK547

    RIP kinase Cancer
    (Rac)-GSK547 is the racemate of GSK547. GSK547 is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.
  • HY-128900
    11-cis-Vaccenyl acetate

    Endogenous Metabolite Others
    11-cis-Vaccenyl acetate is male-specific lipid that mediates aggregation behavior in both male and female flies, which activates a few dozen olfactory neurons located in T1 sensilla on the antenna of both male and female flies.
  • HY-B0268S
    Enoxacin-d8

    Bacterial DNA/RNA Synthesis MicroRNA Antibiotic Cancer Infection
    Enoxacin-d8 (AT 2266-d8) is the deuterium labeled Enoxacin. Enoxacin (AT 2266), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin has potent activities against gram-positive and -negative bacteria. Enoxacin is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing.
  • HY-12684
    CH-223191

    Aryl Hydrocarbon Receptor Cancer
    CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR). CH-223191 inhibits TCDD-mediated nuclear translocation and DNA binding of AhR, and inhibits TCDD-induced luciferase activity with an IC50 of 0.03 μM.
  • HY-19642
    Glesatinib

    MGCD265

    TAM Receptor c-Met/HGFR Cancer
    Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).
  • HY-128807
    E3 ligase Ligand 10

    Ligand for E3 Ligase Cancer
    E3 ligase Ligand 10 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 10 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
  • HY-129653
    E3 ligase Ligand 18

    Ligand for E3 Ligase Cancer
    E3 ligase Ligand 18 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 18 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
  • HY-128811
    E3 ligase Ligand 14

    Ligand for E3 Ligase Cancer
    E3 ligase Ligand 14 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 14 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
  • HY-19642A
    Glesatinib hydrochloride

    MGCD265 hydrochloride

    TAM Receptor c-Met/HGFR Cancer
    Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).
  • HY-43961
    E3 ligase Ligand 8

    Ligand for E3 Ligase Cancer
    E3 ligase Ligand 8 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 8 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
  • HY-128810
    E3 ligase Ligand 13

    Ligand for E3 Ligase Cancer
    E3 ligase Ligand 13 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 13 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
  • HY-122881
    HOIPIN-1

    JTP-0819958

    IKK Cancer
    HOIPIN-1 (JTP-0819958) is a selective linear ubiquitin chain assembly complex (LUBAC) inhibitor with an IC50 of 2.8 μM. HOIPIN-1 suppress LUBAC-mediated NF-kB activation in vitro.
  • HY-15337
    Hesperidin

    Hesperetin 7-rutinoside

    Apoptosis Autophagy Reactive Oxygen Species Endogenous Metabolite Cancer
    Hesperidin (Hesperetin 7-rutinoside), a flavanone glycoside, is isolated from citrus fruits. Hesperidin has numerous biological properties, such as decreasing inflammatory mediators and exerting significant antioxidant effects. Hesperidin also exhibits antitumor and antiallergic activities.
  • 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-15529
    S0859

    Na+/HCO3- Cotransporter Cardiovascular Disease
    S0859 is a selective, high-affinity generic Na +/HCO3 - transporter (NBC) inhibitor. S0859 reversibly inhibits NBC-mediated intracellular pH (pHi) recovery (Ki=1.7 μM, full inhibition at approximately 30 μM).
  • HY-N0406
    2"-O-beta-L-galactopyranosylorientin

    Others Metabolic Disease
    2"-O-beta-L-galactopyranosylorientin is extracted from the flowers of Trollius ledebouri. 2"-O-beta-L-galactopyranosylorientin involves transporter mediated efflux in addition to passive diffusion and is the substrate of multidrug resistance protein 2 (MRP2).
  • HY-P0242A
    Neurokinin B TFA

    Neurokinin Receptor Neurological Disease Endocrinology
    Neurokinin B TFA belongs to the tachykinin family of peptides. Neurokinin B binds a family of GPCRs-including neurokinin receptor 1 (NK1R), NK2R, and NK3R-to mediate their biological effect.
  • 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-N0896
    Inulicin

    1-O-Acetylbritannilactone

    NF-κB COX Cancer Inflammation/Immunology
    Inulicin (1-O-Acetylbritannilactone) is an active compound that inhibits VEGF-mediated activation of Src and FAK. Inulicin (1-O-Acetylbritannilactone) inhibits LPS-induced PGE2 production and COX-2 expression, and NF-κB activation and translocation.
  • HY-141891
    M435-1279

    E1/E2/E3 Enzyme Cancer
    M435-1279 is a UBE2T inhibitor. M435-1279 inhibits the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1.
  • HY-10080
    Teglarinad chloride

    GMX1777; EB-1627

    NAMPT Cancer
    Teglarinad chloride (GMX1777) is a prodrug of GMX1778 (a nicotinamide phosphoribosyl transferase inhibitor). Teglarinad chloride exhibits antitumor activity in mice can be attributed to inhibition of NAMPT. Teglarinad chloride also enhances radiation efficacy, mediated by interference with DNA repair and antiangiogenesis.
  • 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-128806
    E3 ligase Ligand 9

    Ligand for E3 Ligase Cancer
    E3 ligase Ligand 9 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 9 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
  • HY-N6865
    Groenlandicine

    Topoisomerase Cancer Metabolic Disease
    Groenlandicine is a protoberberine alkaloid isolated from Coptidis Rhizoma. Groenlandicine exhibits moderate inhibitory effect with IC50 value of 154.2 μM for human recombinant aldose reductase (HRAR). Groenlandicine selectively induces topoisomerase I-mediated DNA cleavage.
  • HY-115770
    8-Methylsulfinyloctyl isothiocyanate

    Others Inflammation/Immunology
    8-Methylsulfinyloctyl isothiocyanate, an isothiocyanate, has antimicrobial activity and remarkable inhibitory activity against plant growth. 8-Methylsulfinyloctyl isothiocyanate impair COX-2 mediated inflammatory responses in LPS stimulated raw macrophages.
  • HY-50937
    ST 2825

    MyD88 Inflammation/Immunology
    ST 2825 is a specific MyD88 dimerization inhibitor. ST2825 interferes with recruitment of IRAK1 and IRAK4 by MyD88, causing inhibition of IL-1β-mediated activation of NF-κB transcriptional activity.
  • HY-103316A
    Ned 19

    Calcium Channel Cancer
    Ned 19 is a selective membrane-permeant non competitive NAADP antagonist and inhibits NAADP-mediated Ca 2+ signaling, with an IC50 of 65 nM. Ned 19 strongly inhibits tumor growth and vascularization as well as lung metastases in mice.
  • HY-118581
    Coralyne chloride

    Topoisomerase Cancer
    Coralyne chloride is a protoberberine alkaloid with potent anti-cancer activities. Coralyne chloride acts as a potent topoisomerase I poison and induces Top I mediated DNA cleavage. Coralyne chloride can be used for preparing coralyne derivatives as DNA binding fluorescent probes.
  • 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-A0150
    Alclometasone

    7a-​Chloro-​16a-​methyl prednisolone

    Glucocorticoid Receptor Inflammation/Immunology
    Alclometasone (7a-Chloro-16a-methyl prednisolone) is a glucocorticoid and inhibits the release of pro-inflammatory mediators from leukocytes. Alclometasone can be used to relieve corticosteroid-responsive dermatoses, including atopic dermatitis, eczema, psoriasis and allergic dermatitis.
  • HY-B0890S
    Zomepirac-d4 sodium salt

    PGE synthase Inflammation/Immunology
    Zomepirac-d4 sodium salt is the deuterium labeled Zomepirac sodium salt. Zomepirac sodium salt (McN-2783-21-98) is a potent prostaglandin biosynthesis inhibitor. Zomepirac sodium salt is a non-steroidal anti-inflammatory drug (NSAID). Zomepirac sodium salt can cause immune-mediated liver injury.
  • HY-44148
    FAK ligand-Linker Conjugate 1

    Target Protein Ligand-Linker Conjugates Cancer
    FAK ligand-Linker Conjugate 1 incorporates a ligand for FAK, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). FAK ligand-Linker Conjugate 1 can be extensively used for PROTAC-mediated protein degradation.
  • 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-124325
    PIP-199

    DNA Alkylator/Crosslinker Cancer
    PIP-199 is a selective inhibitor of RMI (RecQ-mediated genome instability protein) core complex/MM2 interaction, with an IC50 of 36 μM. PIP-199 can be used for the research of sensitizing resistant tumors to DNA crosslinking chemotherapeutics.
  • 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-114174
    Fmoc-Ala-Glu-Asn-Lys-NH2

    Amyloid-β Neurological Disease
    Fmoc-Ala-Glu-Asn-Lys-NH2 is a selective asparagine endopeptidase (AEP) inhibitor peptide and suppresses amyloid precursor protein (APP) cleavage. AEP, a pH-controlled cysteine proteinase, is activated during ageing and mediates APP proteolytic processing.
  • HY-P3137
    TRV056

    Angiotensin Receptor Cardiovascular Disease
    TRV056 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV056 is efficacious in stimulating cellular Gq-mediated signaling. TRV056 can be used to develop the Gq-biased AT1R agonists.
  • 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-P3136
    TRV055

    Angiotensin Receptor Cardiovascular Disease
    TRV055 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 is efficacious in stimulating cellular Gq-mediated signaling. TRV055 can be used to develop the Gq-biased AT1R agonists.
  • HY-B1899A
    Taurodeoxycholic acid sodium hydrate

    Sodium taurodeoxycholate monohydrate

    Caspase Apoptosis Metabolic Disease Inflammation/Immunology
    Taurodeoxycholic acid sodium hydrate (Sodium taurodeoxycholate monohydrate) prevents apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid sodium hydrate is investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.
  • HY-110249
    CINPA1

    Others Metabolic Disease
    CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function.
  • HY-N2625A
    Harmalol hydrochloride

    Others Others
    Harmalol hydrochloride, a beta carboline alkaloid, presents in several medicinal plants such as Peganum harmala. Harmalol hydrochloride, main metabolite of Harmaline, significantly inhibits the dioxin-mediated induction of CYP1A1 at the transcriptional and posttranslational levels. Harmalol hydrochloride possesses antioxidant and hydroxyl radical-scavenging properties.
  • 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-129393
    AB928

    Adenosine Receptor Inflammation/Immunology
    AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. AB928 relieves adenosine-mediated immune suppression. AB928 has immunomodulatory and antitumor activities.
  • HY-138161
    JR14a

    Complement System Inflammation/Immunology
    JR14a is a potent thiophene antagonist of human complement C3a receptor. JR14a shows selectivity for the human C3a receptor over C5a receptor. JR14a can suppress C3aR-mediated inflammation.
  • HY-121685A
    Tipepidine hydrochloride

    Potassium Channel Neurological Disease
    Tipepidine hydrochloride reversibly inhibits dopamine (DA) D2 receptor-mediated GIRK currents (IDA(GIRK)) with an IC50 of 7.0 μM. Tipepidine hydrochloride subsequently activates VTA dopamine neuron. Tipepidine hydrochloride, a non-narcotic antitussive, exerts an antidepressant-like effect.
  • HY-123159
    AKI603

    Aurora Kinase Cancer
    AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells.
  • HY-108022
    Azemiglitazone

    MSDC-0602

    Mitochondrial Metabolism Metabolic Disease
    Azemiglitazone (MSDC-0602), a PPARγ-sparing thiazolidinedione (TZD), interacts with the mitochondrial pyruvate carrier (MPC) and inhibits its activity and has the potential for type 2 diabetes study with reducing risk of PPARγ-mediated side effects.
  • HY-15724A
    Vercirnon sodium

    GSK-1605786 sodium; CCX282-B sodium; Traficet-EN sodium

    CCR Inflammation/Immunology Endocrinology
    Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
  • HY-15724
    Vercirnon

    GSK-1605786; CCX282-B; Traficet-EN

    CCR Inflammation/Immunology Endocrinology
    Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
  • HY-109097
    Otaplimastat

    SP-8203

    MMP iGluR Neurological Disease
    Otaplimastat (SP-8203), a matrix metalloproteinase (MMP) inhibitor, blocks N-methyl-D-aspartate (NMDA) receptor-mediated excitotoxicity in a competitive manner. Otaplimastat also exhibits anti-oxidant activity. Otaplimastat can be used for the research of brain ischemic injury.
  • HY-120084
    BTX161

    Casein Kinase Cancer
    BTX161, a Thalidomide analog, is a potent CKIα degrader. BTX161 mediates degradation of CKIα better than Lenalidomide in human AML cells and activates DNA damage response (DDR) and p53, while stabilizing the p53 antagonist MDM2.
  • HY-B0649S
    Propofol-d17

    GABA Receptor Endogenous Metabolite Neurological Disease
    Propofol-d17 (2,6-Diisopropylphenol-d17) is the deuterium labeled Propofol. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic.
  • HY-124899
    Hh-Ag1.5

    SAg1.5

    Hedgehog Metabolic Disease
    Hh-Ag1.5 (SAg1.5) is a potent Hedgehog (Hh) agonist with an EC50 of 1 nM. Hh-Ag1.5 mediated reprogramming breaks the quiescence of noninjured liver stem cells for rescuing liver failure.
  • HY-13323A
    CX-5461 dihydrochloride

    DNA/RNA Synthesis Cancer
    CX-5461 dihydrochloride is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC50s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC50 ≥25 μM).
  • HY-76200
    Voriconazole

    UK-109496

    Fungal Infection
    Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes.
  • HY-N1778
    3,4-Dimethoxycinnamic acid

    O-Methylferulic acid

    Reactive Oxygen Species Virus Protease Cancer Infection
    3,4-Dimethoxycinnamic acid (O-Methylferulic acid) is a monomer extracted and purified from Securidaca inappendiculata Hassk. 3,4-Dimethoxycinnamic acid exerts anti-apoptotic effects on L-02 cells via the ROS-mediated signaling pathway. Anti-apoptotic effects.
  • HY-13988
    AT-56

    PGE synthase Inflammation/Immunology
    AT-56 is a potent, selective and orally active inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS), with an IC50 of 95 μM and Ki of 75 μM. AT-56 could selectively suppress the drowsiness or pain reaction mediated by L-PGDS-catalyzed PGD2.
  • HY-N1778A
    (E)-3,4-Dimethoxycinnamic acid

    (E)-O-Methylferulic acid

    Reactive Oxygen Species Virus Protease Cancer Infection
    (E)-3,4-Dimethoxycinnamic acid is the less active isomer of 3,4-Dimethoxycinnamic acid. 3,4-Dimethoxycinnamic acid exerts anti-apoptotic effects on L-02 cells via the ROS-mediated signaling pathway. Anti-apoptotic effects.
  • HY-B1066
    Butylhydroxyanisole

    Butylated hydroxyanisole; BHA; E320

    Reactive Oxygen Species Ferroptosis Inflammation/Immunology Neurological Disease
    Butylhydroxyanisole (Butylated hydroxyanisole) is an antioxidant used as a food additive preservative. Butylhydroxyanisole mediates liver toxicity, retardation in reproductive organ development and learning, and sleep deficit. Butylhydroxyanisole exerts neurotoxic effects and leads to disruption of the brain and nerve development. Butylhydroxyanisole is a ferroptosis inducer.
  • HY-15838
    ID-8

    DYRK Cancer
    ID-8 is an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase (DYRK). ID-8 sustains embryonic stem cell (ESC) self-renewal and pluripotency. ID-8 enhances Wnt-mediated hESC survival and proliferation via inhibition of DYRKs.
  • HY-15310
    Ivermectin

    MK-933

    Parasite HIV Mitophagy HSV SARS-CoV Antibiotic Autophagy Infection Cancer
    Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.
  • HY-P0299
    LSKL, Inhibitor of Thrombospondin (TSP-1)

    TGF-β Receptor Cancer
    LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) can readily crosse the blood-brain barrier.
  • HY-P0299A
    LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)

    TGF-β Receptor Cancer
    LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier.
  • HY-110302
    6'-GNTI dihydrochloride

    Opioid Receptor Neurological Disease
    6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons.
  • HY-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-133557
    XZ739

    PROTACs Bcl-2 Family Apoptosis Cancer
    XZ739, a Cereblon-dependent PROTAC BCL-XL (Bcl-2 family member) 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-N2388
    Auraptene

    MMP Inflammation/Immunology Cancer
    Auraptene is the most abundant naturally occurring geranyloxycoumarin. Auraptene decreases the secretion of matrix metalloproteinase 2 (MMP-2) as well as key inflammatory mediators, including IL-6, IL-8, and chemokine (C-C motif) ligand-5(CCL5).
  • HY-N0349
    Methyl Paraben

    Methyl 4-hydroxybenzoate

    Bacterial Endogenous Metabolite Infection
    Methyl Paraben, isolated from the barks of Tsuga dumosa the methyl ester of p-hydroxybenzoic acid, is a standardized chemical allergen. Methyl Paraben is a stable, non-volatile compound used as an antimicrobial preservative in foods, drugs and cosmetics. The physiologic effect of Methyl Paraben is by means of increased histamine release, and cell-mediated immunity.
  • HY-30008
    Cycloleucine

    iGluR Cancer Infection Metabolic Disease Neurological Disease
    Cycloleucine is a specific inhibitor of S-adenosyl-methionine mediated methylation. Cycloleucine is antagonist of NMDA receptor associated glycine receptor, with a Ki of 600 μM. Cycloleucine is also a competitive inhibitor of ATP: L-methionine-S-adenosyl transferase in vitro. Cycloleucine has anxiolytic and cytostatic effects.
  • HY-136408
    Malonyl Coenzyme A lithium

    Others Metabolic Disease
    Malonyl Coenzyme A (lithium) is a coenzyme A derivative that is utilized in fatty acid and polyketide synthesis and in the transport of α-ketoglutarate across the mitochondrial membrane. Malonyl Coenzyme A (lithium) is formed by the Acetyl CoA Carboxylase-mediated carboxylation of acetyl CoA. Malonyl Coenzyme A (lithium) is exclusively used as the extender unit in the synthesis of bacterial aromatic polyketides.
  • HY-136172
    ESI-08

    Ras Cancer Metabolic Disease Cardiovascular Disease
    ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation.
  • HY-N2485
    4'-Methoxyresveratrol

    4'-O-Methylresveratrol

    Others Inflammation/Immunology
    4'-Methoxyresveratrol (4'-O-Methylresveratrol) is a polyphenol derived from Dipterocarpaceae, with antiandrogenic, antifungal and anti-inflammatory activities. 4'-Methoxyresveratrol alleviates AGE-induced inflammation through suppressing RAGE-mediated MAPK/NF-κB signaling pathway and NLRP3 inflammasome activation.
  • HY-103460
    IRL 2500

    Endothelin Receptor Cardiovascular Disease
    IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50 values of 1.3 and 94 nM for ETB and ETA receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo.
  • HY-126390
    (E/Z)-BCI

    NSC 150117

    Phosphatase Apoptosis Cancer Inflammation/Immunology
    (E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway.
  • HY-107701
    CGP 78608 hydrochloride

    iGluR Neurological Disease
    CGP 78608 hydrochloride is a highly potent and selective antagonist at the glycine-binding site of the NMDA receptor, with an IC50 of 6 nM. CGP 78608 acts as a potentiator of GluN1/GluN3A-mediated glycine currents, with an estimated EC50 in the low nM range (26.3 nM). Anticonvulsant activity.
  • HY-133807
    Benpyrine

    TNF Receptor Inflammation/Immunology
    Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 µM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research.
  • HY-100612
    T16Ainh-A01

    Chloride Channel Others
    T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor, inhibiting TMEM16A-mediated chloride currents with an IC50 value of ~1 µM. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC).
  • HY-103696
    PTC-028

    Apoptosis Cancer
    PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. PTC-028 selectively inhibits cancer cells whereas normal cells remain unaffected. PTC-028 downregulates BMI-1, inducing caspase-mediated apoptosis.
  • HY-115734
    Phenylpyropene C

    S14-95

    Acyltransferase Inflammation/Immunology
    Phenylpyropene C (S14-95), a JAK/STAT pathway inhibitor, can inhibit IFN-γ mediated expression of the reporter gene (IC50=5.4~10.8 μM). Phenylpyropene C also is an inhibitor of acyl-CoA, with an IC50 of 16.0 μM.
  • HY-12824
    RNPA1000

    Antibiotic Bacterial Infection
    RNPA1000, an antibiotic, is a potent RnpA inhibitor and inhibits RnpA-mediated cellular RNA degradation. RNPA1000 inhibits tRNA maturation with an IC50 of 175 μM. RNPA1000 displays broad-spectrum antimicrobial activities and inhibits staphylococcal and all Gram-positive bacterial pathogens activity.
  • HY-135336S
    (R)-Verapamil D7 hydrochloride

    (R)-(+)-Verapamil D7 hydrochloride

    P-glycoprotein Apoptosis Cancer
    (R)-Verapamil D7 hydrochloride ((R)-(+)-Verapamil D7 hydrochloride) is a deuterium labeled (R)-Verapamil hydrochloride. (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer drugs.
  • 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-N0742
    Absinthin

    Others Others
    Absinthin is a structurally unique triterpene, and is responsible for the high bitter value of wormwood. Absinthin is an agonist of the bitter taste receptor hTAS2R46, which reduces cytosolic Ca 2+-rises induced by histamine by a receptor-specific mechanism mediated by hTAS2R46.
  • HY-126397
    MnTBAP chloride

    NF-κB Inflammation/Immunology
    MnTBAP chloride is a superoxide dismutase (SOD) mimetic and peroxynitrite scavenger. MnTBAP chloride is a manganic porphyrin complex and has anti-oxidative property. MnTBAP chloride mediates anti-inflammatory effects through upregulation of BMPR-II and inhibition of the NFκB signaling. MnTBAP chloride has the potential for the fibrotic response in chronic kidney diseases (CKDs) research.
  • HY-121993
    Combretastatin A-1

    Microtubule/Tubulin Cancer
    Combretastatin A-1 is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 exhibits anti-tumor and anti-vascular effects.
  • HY-112483
    QX77

    Autophagy Cancer
    QX77 is a chaperone-mediated autophagy (CMA) activator and upregulates LAMP2A expression in vitro. QX77 induces Rab11 upregulation, rescues Rab11 down-regulation and trafficking deficiency in cystinotic cells. QX77 can impede self-renewal and promote differentiation of ES cells.
  • HY-13306
    Pyrintegrin

    Integrin Metabolic Disease
    Pyrintegrin is an β1-integrin agonist and a 2,4-disubstituted pyrimidine that promotes embryonic stem cells survival. Pyrintegrin enhances cell-extracellular matrix (ECM) adhesion-mediated integrin signaling. Pyrintegrin can be used as a podocyte-protective agent and has robustly adipogenic.
  • HY-B1805
    Triclocarban

    3,4,4′-Trichlorocarbanilide

    Bacterial Infection
    Triclocarban (3,4,4′-Trichlorocarbanilide), a broad spectrum antibacterial compound, is widely used in a broad range of applications such as the production of soaps, skin creams, toothpastes and deodorants. Triclocarban is a potential endocrine-disrupting chemical with the capacity to modulate androgen and estrogen activities as well as other hormone-mediated biological processes.
  • HY-N2204
    Swertiajaponin

    Tyrosinase Inflammation/Immunology
    Swertiajaponin is a tyrosinase inhibitor, forms multiple hydrogen bonds and hydrophobic interactions with the binding pocket of tyrosinase, with an IC50 of 43.47 μM. Swertiajaponin also inhibits oxidative stress-mediated MAPK/MITF signaling, leading to decrease in tyrosinase protein level. Swertiajaponin suppresses melanin accumulation and exhibits strong anti-oxidative activity.
  • HY-W001160
    5-Hydroxyindole

    Others Others
    5-Hydroxyindole, a hydroxylated indole, can be found in a vast array of pharmacologically active agents and natural products. 5-Hydroxyindole slows desensitization of the 5-HT3 receptor-mediated ion current in N1E-115 neuroblastoma cells.
  • HY-116626
    SM-7368

    NF-κB p38 MAPK MMP Cancer
    SM-7368 is a potent NF-kB inhibitor that targets downstream of MAPK p38 activation. SM-7368 inhibits TNF-α-induced MMP-9 upregulation. SM-7368 can be used for the research of chemotherapies targeting TNF-α-mediated tumor invasion and metastasis .
  • HY-N7395
    Cyclic ADP-​ribose

    cADPR

    Calcium Channel TRP Channel Endogenous Metabolite Infection Endocrinology Inflammation/Immunology Neurological Disease Cardiovascular Disease
    Cyclic ADP-ribose (cADPR) is a potent second messenger for calcium mobilization that is synthesized from NAD + by an ADP-ribosyl cyclase. Cyclic ADP-ribose increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels.
  • 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-W008226
    Phloracetophenone

    2,4,6-trihydroxyacetophenone; 1-(2,4,6-Trihydroxyphenyl)ethanone

    Cytochrome P450 Bacterial Antibiotic Infection Metabolic Disease
    Phloracetophenone (2,4,6-trihydroxyacetophenone) is the aglycone part of acetophenone glycoside obtained from Curcuma comosa Roxb, with cholesterol-lowering activity. Phloracetophenone enhances cholesterol 7α-hydroxylase (CYP7A1) activity. Phloracetophenone stimulats bile secretion mediated through Mrp2.
  • HY-124617A
    AMXT-1501 tetrahydrochloride

    Apoptosis Cancer Inflammation/Immunology
    AMXT-1501 tetrahydrochloride is an orally active polyamine transport inhibitor. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells. Combination of DFMO and AMXT‐1501 induces caspase‐3 mediated apoptosis in NB cell lines.
  • HY-W054146
    RAMB4

    Proteasome Cancer
    RAMB4 is a ubiquitin-proteasome system (UPS)-stressor. RAMB4 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. RAMB4 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity.
  • HY-N6901
    Luteolin 7-sulfate

    Others Metabolic Disease
    Luteolin 7-sulfate is isolated from Phyllospadix iwatensis Makino, a marine plant. Luteolin 7-sulfate attenuates TYR gene expression through the intervention of a cAMP-responsive element binding protein (CREB)- and microphthalmia-associated transcription factor (MITF)-mediated signaling pathway, leading to the decreased melanin synthesis.
  • HY-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-109854A
    (R)-Lisofylline

    (R)-Lisophylline

    STAT Metabolic Disease Inflammation/Immunology
    (R)-Lisofylline ((R)-Lisophylline) is a (R)-enantiomer of the metabolite of Pentoxifylline with anti-inflammatory properties. (R)-Lisofylline is a lysophosphatidic acid acyltransferase inhibitor with an IC50 of 0.6 µM and interrupts IL-12 signaling-mediated STAT4 activation. (R)-Lisofylline has the potential for type 1 diabetes, autoimmune disorders research.
  • HY-116999
    IR415

    HBV Infection
    IR415 is a potent anti-HBV agent and inhibits HBV replication by blocking the HBx activity. IR415 selectively interacts with HBx (Kd=2 nM) and blocks HBV-mediated RNAi suppression, reverses the inhibitory effect of HBx protein on the activity of the dicer endoribonuclease. HBx: hepatitis B virus X protein.
  • HY-101911
    5-BDBD

    P2X Receptor Neurological Disease
    5-BDBD, a potent and selective P2X4 receptor antagonist, inhibits rP2X4R-mediated currents, with an IC50 of 0.75 μM. 5-BDBD completely blocks the basal and acute hyperalgesia induced by nitroglycerin (NTG).
  • HY-108497
    L-803087

    Somatostatin Receptor Cancer Neurological Disease
    L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 is >280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice.
  • HY-B0240
    Disulfiram

    Tetraethylthiuram disulfide; TETD

    Aldehyde Dehydrogenase (ALDH) Interleukin Related Pyroptosis Metabolic Disease Cancer
    Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells[1-4].
  • HY-16125
    Carboxyamidotriazole Orotate

    L-651582 Orotate; CAI Orotate

    Calcium Channel Cancer Inflammation/Immunology
    Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor. Carboxyamidotriazole Orotate is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory and antiangiogenic effects.
  • HY-N6966
    Ethyl Caffeate

    NF-κB NO Synthase COX PGE synthase Inflammation/Immunology Cancer
    Ethyl Caffeate is a natural phenolic compound isolated from Bidens pilosa. Ethyl caffeate suppresses NF-κB activation and its downstream inflammatory mediators, inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and prostaglandin E2 (PGE2) in vitro or in mouse skin.
  • HY-134130
    Integrin modulator 1

    Integrin Inflammation/Immunology
    Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM.
  • HY-123844
    dBET57

    PROTACs Epigenetic Reader Domain Cancer
    dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology. dBET57 mediates recruitment to the CRL4 Cereblon E3 ubiquitin ligase, with a DC50/5h of 500 nM for BRD4BD1, and is inactive on BRD4BD2.
  • HY-18684
    SIBA

    5'-Isobutylthioadenosine; 5'-Deoxy-5'-isobutylthioadenosine

    Nucleoside Antimetabolite/Analog HSV Infection Metabolic Disease
    SIBA (5'-Isobutylthioadenosine), a synthetic analogue of SAH (HY-19528), acts as an inhibitor of S-adenosylmethionine-mediated transmethylation. SIBA can interfere with a variety of enzymatic activities in vitro, such as SAH hydrolase, methylthioadenosine phosphorylase and cAMP phosphodiesterase. SIBA reversibly blocks the multiplication of herpes simplex type 1 virus (HSV).
  • HY-129851
    NTP42

    Prostaglandin Receptor Cardiovascular Disease
    NTP42 is a thromboxane A2 (TXA2) receptor antagonist with an IC50 of 3.278 nM for antagonizing T prostanoid receptor (TP)- mediated [Ca 2+] mobilization following stimulation of cells with the alternative TP agonist U46609. NTP42 can be used for the treatment of pulmonary arterial hypertension (PAH).
  • HY-P9968
    Nimotuzumab

    EGFR Cancer
    Nimotuzumab is a humanized IgG1 monoclonal antibody targeting EGFR with a KD of 0.21 nM. Nimotuzumab is directed against the extracellular domain of the EGFR blocking the binding to its ligands. Nimotuzumab, a strong antitumor drug, is cytolytic on target tumors by its capacity to cause antibody dependent cell mediated cytotoxicity (ADCC) and complement dependent cytotoxicity (CDC).
  • HY-123352
    ZK 216348

    (+)-ZK 216348

    Glucocorticoid Receptor Endocrinology Inflammation/Immunology
    ZK 216348 ((+)-ZK 216348) is a nonsteroidal selective glucocorticoid receptor agonist with an IC50 of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC50s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects.
  • HY-17043S
    Loratadine-d4

    Loratidine-d4; SCH 29851-d4

    Histamine Receptor Influenza Virus Infection Endocrinology Inflammation/Immunology
    Loratadine-d4 (Loratidine-d4) is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
  • HY-129390
    Orelabrutinib

    ICP-022

    Btk Cancer
    Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK.
  • HY-116767
    BLT-1

    Block lipid transport-1

    HCV Metabolic Disease Inflammation/Immunology
    BLT-1, a thiosemicarbazone copper chelator, is a selective scavenger receptor B, type 1 (SR-BI) inhibitor. BLT-1 inhibits the transfer of lipids between high-density lipoproteins (HDL) and cells mediated by SR-BI. BLT-1 is a potent HCV entry inhibitor.
  • HY-129241
    AGX51

    Others Cancer
    AGX51 is a first-in-class pan-Id (inhibitors of DNA-binding/differentiation proteins) antagonist and degrader. AGX51 inhibits the Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and reduces viability. AGX51 inhibits pathologic ocular neovascularization.
  • 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-131364
    Nur77 modulator 1

    Others Cancer
    Nur77 modulator 1 is a good Nur77 binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity.
  • HY-138761
    EP4 receptor antagonist 3

    Prostaglandin Receptor Cancer Inflammation/Immunology
    EP4 receptor antagonist 3 is a potent EP4 receptor antagonist, example 3,extracted from patent WO2010019796 A1. EP4 receptor antagonist 3 can be used for the reseacrh of EP4 receptor-mediated diseases, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer.
  • HY-100808
    D-Serine

    (R)-Serine

    iGluR Endogenous Metabolite Neurological Disease
    D-Serine ((R)-Serine), an endogenous amino acid involved in glia-synapse interactions that has unique neurotransmitter characteristics, is a potent co-agonist at the NMDA glutamate receptor. D-Serinee has a cardinal modulatory role in major NMDAR-dependent processes including NMDAR-mediated neurotransmission, neurotoxicity, synaptic plasticity, and cell migration.
  • HY-P9923
    Benralizumab

    MEDI-563; BIW-8405

    Interleukin Related Inflammation/Immunology
    Benralizumab (MEDI-563) is an interleukin-5 receptor α (IL-5Rα)-directed cytolytic monoclonal antibody that induces direct, rapid and nearly complete depletion of eosinophils via enhanced antibody-dependent cell-mediated cytotoxicity. Benralizumab can be used for severe eosinophilic asthma.
  • HY-112257
    S-23

    Androgen Receptor Metabolic Disease
    S-23 is an orally active selective androgen receptor modulator (SARM) with a Ki of 1.7 nM. S-23 induces androgen receptor (AR)-mediated transcriptional activation in CV-1 cells. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats.
  • HY-W018555
    D-Cysteine

    Endogenous Metabolite Bacterial Infection Neurological Disease
    D-Cysteine is the D-isomer of cysteine and a powerful inhibitor of Escherichia coli growth. D-cysteine is mediated by D-amino acid oxidase to produce H2S and is a neuroprotectant against cerebellar ataxias. D-Cysteine could inhibit the growth and cariogenic virulence of dual-species biofilms formed by S. mutans and S. sanguinis.
  • HY-17043S1
    Loratadine-d5

    Loratidine-d5; SCH 29851-d5

    Histamine Receptor Influenza Virus Infection Endocrinology Inflammation/Immunology
    Loratadine-d5 (Loratidine-d5) is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
  • HY-103524
    Valerenic acid

    (-)-Valerenic Acid

    GABA Receptor 5-HT Receptor Neurological Disease
    Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAA receptors. Valerenic acid is also a partial agonist of the 5-HT5a receptor. Valerenic acid mediates anxiolytic activity via GABAA receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties.
  • HY-119347
    Cirsilineol

    IFNAR STAT Cancer Inflammation/Immunology
    Cirsilineol, a natural flavone compound, selectively inhibits IFN-γ/STAT1/T-bet signaling in intestinal CD4 + T cells. Cirsilineol has potent immunosuppressive and anti-tumor properties. Cirsilineol significantly ameliorates trinitro-benzene sulfonic acid (TNBS)-induced T-cell-mediated experimental colitis in mice.
  • HY-114250
    Cantrixil

    TRX-E-002-1

    Apoptosis Cancer
    Cantrixil (TRX-E-002-1), an active enantiomer of TRX-E-002, is a second-generation super-benzopyran (SBP) compound. Cantrixil increases phosphorylated c-Jun levels resulting in caspase-mediated apoptosis in ovarian cancer cells. Cantrixil has potent pan anti-cancer activity against a broad range of cancer phenotypes.
  • HY-N5025
    Bullatine A

    P2X Receptor Apoptosis 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-W017316
    Terpinen-4-ol

    4-Carvomenthenol

    Endogenous Metabolite Cancer Inflammation/Immunology
    Terpinen-4-ol (4-Carvomenthenol), a naturally occurring monoterpene, is the main bioactive component of tea-tree oil. Terpinen-4-ol suppresses inflammatory mediator production by activated human monocytes. Terpinen-4-ol significantly enhances the effect of several chemotherapeutic and biological agents.
  • HY-U00364
    CI-949

    Histamine Receptor Prostaglandin Receptor Leukotriene Receptor Inflammation/Immunology Endocrinology
    CI-949 is an allergic mediator release inhibitor, which inhibits histamine, leukotriene C4/D4 (LTC4/LTD4), and thromboxane B2 (TXB2) release with IC50s of 11.4 μM, 0.5 μM and 0.1 μM, respectively.
  • HY-15519
    LBW242

    IAP FLT3 Cancer
    LBW242, a 3-mer and Smac mimetic, is a potent and orally active proapoptotic IAP inhibitor. LBW242 shows effects on mutant FLT3-expressing cells. LBW242 has activity against multiple myeloma, and potentiates TRAIL- and anticancer drug-mediated cell death of ovarian cancer cells.
  • HY-119198
    NSC745885

    Apoptosis Histone Methyltransferase Cancer
    NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers.
  • HY-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-114180
    RU.521

    RU320521

    Cyclic GMP-AMP Synthase Metabolic Disease
    RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. RU.521 suppresses dsDNA-activated reporter activity with an IC50 of 700 nM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS).
  • HY-115739
    RTIL 13

    Ras Cancer Neurological Disease
    RTIL 13 is a potent inhibitor of dynamin GTPase, with an IC50 of 2.3 µM for dynamin I GTPase. RTIL 13 also targets pleckstrin homology lipid binding domain. RTIL 13 can inhibit receptor-mediated and synaptic vesicle endocytosis, with IC50s of 9.3 μM and 7.1 μM, respectively.
  • HY-N7395A
    Cyclic ADP-​ribose ammonium

    cADPR ammonium

    Calcium Channel TRP Channel Endogenous Metabolite Infection Endocrinology Inflammation/Immunology Neurological Disease Cardiovascular Disease
    Cyclic ADP-ribose ammonium (cADPR ammonium) is a potent second messenger for calcium mobilization that is synthesized from NAD + by an ADP-ribosyl cyclase. Cyclic ADP-ribose ammonium increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels.
  • HY-14428
    ICG-001

    β-catenin Apoptosis Cancer
    ICG-001 is an inhibitor of β-catenin/TCF mediated transcription. ICG-001 works by specifically binding to cyclic AMP response element-binding protein with an IC50 of 3 μM. ICG-001 selectively blocks the β-catenin/CBP interaction without interfering with the β-catenin/p300 interaction.
  • HY-120079
    MSN-125

    Bcl-2 Family Apoptosis 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-132173
    GL0388

    Bcl-2 Family Cancer
    GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo.
  • HY-W015977
    Prion Protein 106-126 (human)

    PrP 106-126 (human)

    Apoptosis Neurological Disease
    Prion Protein 106-126 (human), a peptide fragment of prion, and can induct neuronal apoptosis, antiproteinase K digestion, fiber formation, and mediate the conversion of normal cellular prion protein (PrP c) into pathogenic isoform (PrP Sc). Prion Protein 106-126 (human) is generally used as the model to investigate neural degeneration of prion disease.
  • HY-15205
    Ganetespib

    STA-9090

    HSP Apoptosis Cancer
    Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3.
  • HY-15772A
    Osimertinib mesylate

    AZD-9291 mesylate; Mereletinib mesylate

    EGFR Cancer
    Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
  • HY-14340
    WAY-181187

    SAX-187

    5-HT Receptor Neurological Disease
    WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist.
  • HY-124952
    iKIX1

    Fungal Infection
    iKIX1 is an antifungal agent and resensitizes drug-resistant C. glabrata to azole antifungals in vitro. iKIX1 inhibits the interaction between the KIX domain of the mediator subunit CgGal11A and the activation domain of CgPdr1, the IC50 and Ki values are 190.2 μM and 18 μM, respectively. iKIX1 is used for the study of multidrug resistance and C. glabrata infection.
  • HY-139297
    SCR130

    DNA/RNA Synthesis Apoptosis Cancer
    SCR130 is a SCR7-based DNA nonhomologous end-joining (NHEJ) inhibitor. SCR130 inhibits the end-joining of DNA in a Ligase IV-dependent manner. SCR130 is specific to Ligase IV, and shows minimal or no effect on Ligase III and Ligase I mediated joining. SCR130 induces cell apoptosis and has anticancer activity.
  • HY-13200A
    BRL-15572 hydrochloride

    5-HT Receptor Neurological Disease
    BRL-15572 hydrochloride is a selective antagonist of h5-HT1D, displays high affinity for h5-HT1D receptors. BRL-15572 hydrochloride could be useful pharmacological agents to characterise 5-HT1D receptor mediated responses.
  • HY-138364
    YUM70

    HSP Apoptosis Cancer
    YUM70 is a potent and selective inhibitor of glucose-regulated protein 78 (GRP78), with an IC50 of 1.5 μM for inhibiting GRP78 ATPase activity of the full-length protein. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer. YUM70 also has in vivo efficacy in a pancreatic cancer xenograft model.
  • HY-12511
    SKF-86002

    p38 MAPK Inflammation/Immunology
    SKF-86002 is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.
  • HY-N6246
    Asperulosidic Acid

    NF-κB ERK Cancer Inflammation/Immunology
    Asperulosidic Acid (ASPA), a bioactive iridoid glycoside, is extracted from the herbs of Hedyotis diffusa Willd. Asperulosidic Acid (ASPA) has anti-tumor, anti-oxidant, and anti-inflammatory activities. ASPA is related to the inhibition of inflammatory cytokines (TNF-α, IL-6) and mediators via suppression of the NF-κB and mitogen-activated protein kinase (MAPK) signaling pathways.
  • HY-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-115452
    G5-7

    JAK Apoptosis Cancer
    G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr 1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study.
  • HY-15772
    Osimertinib

    AZD-9291; Mereletinib

    EGFR Cancer
    Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
  • HY-N6052
    (+)-Medicarpin

    Estrogen Receptor/ERR Cancer
    (+)-Medicarpin, a pterocarpan, is a type of isoflavonoid isolated from several medicinal plant species with various biological effects, including Sophora japonica, Zollernia paraensis and Platymiscium yucatamun, Machaerium aristulatum, Platymiscium floribundum, and so on. (+)-Medicarpin potently inhibits osteoclastogenesis and promotes bone healing and increases bone mass by osteoblast differentiation with estrogen receptor (ER) β-mediated osteogenic action.
  • HY-107692
    SB 218795

    Neurokinin Receptor Neurological Disease
    SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit.
  • HY-14621
    Zingerone

    Vanillylacetone; Gingerone

    NF-κB Cancer Metabolic Disease Inflammation/Immunology
    Zingerone (Vanillylacetone) is a nontoxic methoxyphenol isolated from Zingiber officinale, with potent anti-inflammatory, antidiabetic, antilipolytic, antidiarrhoeic, antispasmodic and anti-tumor properties. Zingerone alleviates oxidative stress and inflammation, down-regulates NF-κB mediated signaling pathways. Zingerone acts as an anti-mitotic agent, and inhibits the growth of neuroblastoma cells.
  • HY-117203A
    CDK12-IN-E9

    CDK Cancer
    CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM.
  • HY-117388
    THI0019

    Integrin Inflammation/Immunology
    THI0019 is a potent integrin α4β1 (VLA-4) agonist with an EC50 range of 1-2 μM. THI0019 induces stem/progenitor cells adhesion. THI0019 also regulates adhesion mediated by α4β7, α5β1 and αLβ2.
  • HY-13200
    BRL-15572 dihydrochloride

    5-HT Receptor Neurological Disease
    BRL-15572 dihydrochloride is a selective antagonist of h5-HT1D, displays high affinity for h5-HT1D receptors. BRL-15572 dihydrochloride could be useful pharmacological agents to characterise 5-HT1D receptor mediated responses.
  • HY-108641
    SKF-86002 dihydrochloride

    p38 MAPK Inflammation/Immunology
    SKF-86002 dihydrochloride is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 dihydrochloride inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 dihydrochloride inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.
  • HY-108618
    BC11-38

    Phosphodiesterase (PDE) Endocrinology
    BC11-38 is a potent, selective, and biologically active PDE11 inhibitor, with IC50s of 0.28 µM and >100 µM for PDE11 and PDE1-10, respectively. BC11-38 elevates cAMP levels, PKA-mediated ATF-1 phosphorylation, and cortisol production in H295R cells.
  • HY-129555
    Surfactin

    Bacterial HSV Antibiotic Infection
    Surfactin is a potent cyclic lipopeptide biosurfactants consists of four isomers (Surfactin A, B, C and D), which mediates flux of mono-and divalent cations, such as calcium, across lipid bilayer membranes. Surfactin can act as an antimicrobial adjuvant with anti-bacterial, anti-fungal, antimycoplasma and hemolytic effects. Surfactin also has antiviral activity against a variety of enveloped viruses.
  • HY-116364A
    AZT triphosphate TEA

    3'-Azido-3'-deoxythymidine-5'-triphosphate TEA

    HIV DNA/RNA Synthesis HBV Reactive Oxygen Species Apoptosis Infection
    AZT triphosphate TFA (3'-Azido-3'-deoxythymidine-5'-triphosphate TFA) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TFA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TFA also inhibits the DNA polymerase of HBV. AZT triphosphate TFA activates the mitochondria-mediated apoptosis pathway.
  • HY-N2013
    Aristolactam I

    Aristololactam; Aristolactam

    Caspase Apoptosis Inflammation/Immunology
    Aristololactam I (AL-I), is the main metabolite of aristolochic acid I (AA-I), participates in the processes that lead to renal damage. Aristololactam I (AL-I) directly injures renal proximal tubule cells, the cytotoxic potency of AL-I is higher than that of AA-I and that the cytotoxic effects of these molecules are mediated through the induction of apoptosis in a caspase-3-dependent pathway.
  • HY-100421
    CPI-455

    Histone Demethylase Cancer
    CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents.
  • 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-108497A
    L-803087 TFA

    Somatostatin Receptor Cancer Neurological Disease
    L-803087 TFA is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 TFA is >280-fold more selective for sst4 receptor than other somatostatin receptors. L-803087 TFA facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice.
  • HY-13954
    A 839977

    P2X Receptor Neurological Disease Inflammation/Immunology
    A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta.
  • HY-N2259
    Curcumenol

    (+)-Curcumenol

    Cytochrome P450 Cancer Inflammation/Immunology Neurological Disease
    Curcumenol ((+)-Curcumenol) is a potent CYP3A4 inhibitor with an IC50 of 12.6 μM, which is one of constituents in the plants of medicinally important genus of Curcuma zedoaria, with neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. Curcumenol ((+)-Curcumenol) suppresses Akt-mediated NF-κB activation and p38 MAPK signaling pathway in LPS-stimulated BV-2 microglial cells.
  • HY-13425
    Deguelin

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

    Akt Autophagy Apoptosis Cancer
    Deguelin, a naturally occurring rotenoid, acts as a chemopreventive agent by blocking multiple pathways like PI3K-Akt, IKK-NF-κB, and MAPK-mTOR-survivin-mediated apoptosis. Deguelin binding to Hsp90 leads to a decreased expression of numerous oncogenic proteins, including MEK1/2, Akt, HIF1α, COX-2, and NF-κB.
  • HY-P1432A
    K-(D-1-Nal)-FwLL-NH2 TFA

    GHSR
    K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
  • HY-N0074
    Byakangelicol

    COX Inflammation/Immunology
    Byakangelicol, isolated from Angelica dahurica, inhibits interleukin-1beta (IL-1beta) -induced prostaglandin E2 (PGE2) release in A549 cells mediated by suppression of cyclooxygenase-2 (COX-2) expression and the activity of COX-2 enzyme. Byakangelicol has therapeutic potential as an anti-inflammatory drug on airway inflammation.
  • HY-116683
    116-9e

    MAL2-11B

    HSP DNA/RNA Synthesis Cancer Infection
    116-9e (MAL2-11B) is a Hsp70 co-chaperone DNAJA1 inhibitor. 116-9e inhibits Simian Virus 40 (SV40) replication and DNA synthesis. 116-9e inhibits tumor antigen (TAg)’s endogenous ATPase activity and the TAg-mediated activation of Hsp70.
  • 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-10294
    Relacatib

    SB-462795

    Cathepsin Cancer Metabolic Disease
    Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo.
  • 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-15486
    Salubrinal

    Phosphatase HSV Autophagy Apoptosis Cancer Infection Inflammation/Immunology
    Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation. Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis. Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5.
  • HY-16910
    WIKI4

    PARP β-catenin Cancer
    WIKI4 is a potent tankyrase inhibitor with an IC50 of 26 nM for TNKS2. WIKI4 potently inhibits Wnt/β-catenin signaling and that its half-maximal response dose is 75 nM. WIKI4 mediates its effects on Wnt/β-catenin signaling by inhibiting the enzymatic activity of TNKS2. WIKI4 is cytotoxic to SCLC cells with an IC50 value of 0.02 μM.
  • HY-16291
    APTO-253

    LOR-253; LT-253

    c-Myc KLF Apoptosis Cancer Inflammation/Immunology
    APTO-253 (LOR-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. APTO-253 has antiarthritic activity.
  • HY-N0631
    Cornuside

    p38 MAPK NF-κB Inflammation/Immunology
    Cornuside is a secoiridoid glucoside isolated from the fruit of Cornus officinalis Sieb. et Zucc., which is a traditional oriental medicine for treating inflammatory diseases and invigorating blood circulation. Cornuside inhibits mast cell-mediated allergic response by down-regulating MAPK and NF-κB signaling pathways. Cornuside has anti-allergic effects in vivo and in vitro which suggests a therapeutic application of this agent in inflammatory allergic diseases.
  • HY-120836
    AOH1160

    DNA/RNA Synthesis Apoptosis Cancer
    AOH1160 is a potent, first-in-class, orally available small molecule proliferating cell nuclear antigen (PCNA) inhibitor, interferes with DNA replication, blocks homologous recombination-mediated DNA repair, causes cell-cycle arrest and induces apoptosis. AOH1160 selectively kills many types of cancer cells (mean GI50=330 nM) without causing significant toxicity to a broad range of nonmalignant cells.
  • HY-W017212
    Methyl cinnamate

    Methyl 3-phenylpropenoate

    Tyrosinase Bacterial AMPK Infection Metabolic Disease
    Methyl cinnamate (Methyl 3-phenylpropenoate), an active component of Zanthoxylum armatum, is a widely used natural flavor compound. Methyl cinnamate (Methyl 3-phenylpropenoate) possesses antimicrobial activity and is a tyrosinase inhibitor that can prevent food browning. Methyl cinnamate (Methyl 3-phenylpropenoate) has antiadipogenic activity through mechanisms mediated, in part, by the CaMKK2-AMPK signaling pathway.
  • HY-134923
    CA77.1

    Autophagy Neurological Disease
    CA77.1 is a potent, brain-penetrant and orally active chaperone-mediated autophagy (CMA) activator with favorable pharmacokinetics. CA77.1 is a derivative of AR7 (HY-101106) and can increase the expression of the lysosomal receptor LAMP2A in lysosomes. CA77.1 improves behavior and neuropathology in PS19 mice model and can be used for alzheimer's disease research.
  • HY-10496
    SC75741

    NF-κB Influenza Virus Infection Cancer
    SC75741 is a broad and efficient NF-κB inhibitor with an IC50 of 200 nM for p65. SC75741 blocks influenza viruses (IV) replication. SC75741 impairs DNA binding of the NF-κB subunit p65, resulting in reduced expression of cytokines, chemokines, and pro-apoptotic factors. SC75741 subsequently inhibits caspase activation and blocks caspase-mediated nuclear export of viral ribonucleoproteins.
  • HY-101222
    SB-203186 hydrochloride

    5-HT Receptor Neurological Disease Cardiovascular Disease
    SB-203186 hydrochloride is a potent, selective and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively.
  • HY-16146
    Combretastatin A-1 phosphate tetrasodium

    OXi-4503 tetrasodium

    Microtubule/Tubulin Cancer
    Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a prodrug of Combretastatin A-1, is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 phosphate tetrasodium inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 phosphate tetrasodium exhibits anti-tumor and anti-vascular effects.
  • HY-117287
    Deucravacitinib

    BMS-986165

    JAK Interleukin Related IFNAR Inflammation/Immunology
    Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways.
  • HY-N0057
    3,4-Dicaffeoylquinic acid

    3,4-Di-O-caffeoylquinic acid; Isochlorogenic acid B

    Glucosidase Influenza Virus Apoptosis Endogenous Metabolite Cancer Infection
    3,4-Dicaffeoylquinic acid (3,4-Di-O-caffeoylquinic acid), naturally isolated from Laggera alata, has antioxidative, DNA protective, neuroprotective and hepatoprotective properties. 3,4-Dicaffeoylquinic acid exerts apoptosis-mediated cytotoxicity and α-glucosidase inhibitory effects. 3,4-Dicaffeoylquinic acid possesses a unique mechanism of anti-influenza viral activity, that is, enhancing viral clearance by increasing TRAIL.
  • HY-N2787
    8-​Prenylnaringenin

    Apoptosis Cancer
    8-prenylnaringenin is a prenylflavonoid isolated from hop cones (Humulus lupulus), with cytotoxicity. 8-prenylnaringenin has anti-proliferative activity against HCT-116 colon cancer cells via induction of intrinsic and extrinsic pathway-mediated apoptosis. 8-Prenylnaringenin also promotes recovery from immobilization-induced disuse muscle atrophy through activation of the Akt phosphorylation pathway in mice .
  • HY-15772S
    Osimertinib D6

    AZD-9291 D6; Mereletinib D6

    EGFR Cancer
    Osimertinib D6 (AZD-9291 D6) is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
  • HY-12067
    R406

    Syk FLT3 Apoptosis Cancer Inflammation/Immunology
    R406 is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 reduces immune complex-mediated inflammation. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
  • HY-100609
    4-P-PDOT

    Melatonin Receptor Neurological Disease
    4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity).
  • HY-N2205
    Esculentoside H

    NF-κB JNK Cancer
    Esculentoside H (EsH) is a saponin isolated from the root extract of perennial plant Phytolacca esculenta. Esculentoside H (EH) has anti-tumor activity, the mechanism is related to the capacity for TNFrelease. Esculentoside H (EsH) suppresses colon cancer cell migration through blockage of the JNK1/2 and NF-κB signaling-mediated matrix metalloproteinases-9 (MMP-9) expression.
  • HY-131001
    DPNB-ABT594

    nAChR Neurological Disease
    DPNB-ABT594 is a nitrobenzyl-caged ABT594 (HY-14316A) and activates nAChRs containing the α4β2 subunits with good selectivity than the α7 subunit. DPNB-ABT594 can be used to map the distribution of nAChRs on neurons of the medial habenula (MHb) and helps to gain a deeper understanding of the nAChR‐mediated Ca 2+ signalling in the MHb.
  • 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-139108
    DCH36_06

    Histone Acetyltransferase Apoptosis Cancer
    DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity.
  • HY-113330
    12S-HHT

    12(S)-HHTrE

    Leukotriene Receptor Endogenous Metabolite Inflammation/Immunology
    12S-HHT (12(S)-HHTrE) is an enzymatic product of prostaglandin H2 (PGH2) derived from cyclooxygenase (COX)-mediated arachidonic acid metabolism. 12S-HHT is an endogenous ligand for BLT2 that fully activates BLT2 in vivo. 12S-HHT suppresses UV-induced IL-6 synthesis in keratinocytes, exerting an anti-inflammatory activity.
  • HY-135331
    N-Desmethyl-Apalutamide

    Androgen Receptor Cytochrome P450 Cancer
    N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration.
  • HY-113618A
    RO2959 hydrochloride

    CRAC Channel Interleukin Related Cardiovascular Disease
    RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 hydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 hydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways.
  • HY-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-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-12397
    ZK159222

    VD/VDR Endocrinology
    ZK159222, a 25-carboxylic ester analogue of 1α,25-(OH)2D3, is a potent 1α,25-(OH)2D3 receptor (VDR) antagonist. The mechanism of ZK159222 antagonistic action is mediated by a lack of ligand-induced vitamin D receptor interaction with coactivators. ZK159222 has a partial agonistic character.
  • HY-101092
    QS-21

    Stimulon

    NOD-like Receptor (NLR) Inflammation/Immunology
    QS-21, an immunostimulatory saponin, could be used as a potent vaccine adjuvant. QS-21 stimulates Th2 humoral and Th1 cell-mediated immune responses through action on antigen presenting cells (APCs) and T cells. QS-21 can activate the NLRP3 inflammasome with subsequent release of caspase-1 dependent cytokines, IL-1β and IL-18.
  • HY-N4126
    6-Demethoxytangeretin

    ALK Cancer Inflammation/Immunology Neurological Disease
    6-Demethoxytangeretin is a citrus flavonoid isolated from Citrus depressa. 6-Demethoxytangeretin exerts anti-inflammatory activity and anti-allergic activity, suppresses production and gene expression of interleukin-6 in human mast cell-1 via anaplastic lymphoma kinase (ALK) and mitogen-activated protein kinase (MAPK) pathways. 6-Demethoxytangeretin facilitates the CRE-mediated transcription associated with learning and memory in cultured hippocampal neurons.
  • HY-109010
    Poseltinib

    HM71224; LY3337641

    Btk BMX Kinase Toll-like Receptor (TLR) Metabolic Disease
    Poseltinib, an orally active, selective and irreversible Bruton’s tyrosine kinase (BTK) inhibitor (IC50 =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. Poseltinib can covalently bind to the active site (cysteine 481 residue) of BTK, and reveales potent inhibition of B cell receptor (BCR), Fc receptor (FcR), Toll-like receptor (TLR) mediated signaling.
  • HY-135646
    Eleutheroside B1

    Influenza Virus Infection Inflammation/Immunology
    Eleutheroside B1, a coumarin compound, has a wide spectrum of anti-human influenza virus efficacy, with an IC50 value of 64-125 µg/ml. Eleutheroside B1 mediates its anti-influenza activity through POLR2A and N-glycosylation. Eleutheroside B1 inhibits the mRNA expression of several chemokine genes and the influenza nucleoprotein (NP) gene, and exhibits low cytotoxicity. Antiviral and anti-inflammatory activities.
  • HY-120214
    TAS05567

    Syk Inflammation/Immunology
    TAS05567 is a potent, highly selective, ATP-competitive and orally active Syk inhibitor with an IC50 of 0.37 nM. In a panel of 192 kinases, TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, JAK2, KDR and RET with IC50s of 10 nM, 4.8 nM, 600 nM and 29 nM, respectively). TAS05567 can be used for humoral immune-mediated inflammatory conditions such as autoimmune and allergic diseases.
  • HY-N0492S
    α-Lipoic Acid-d5

    Thioctic acid-d5; (±)-α-Lipoic acid-d5; DL-α-Lipoic acid-d5

    NF-κB HIV Mitochondrial Metabolism Endogenous Metabolite Apoptosis Cancer Infection Inflammation/Immunology
    α-Lipoic Acid-d5 (Thioctic acid-d5) is the deuterium labeled α-Lipoic Acid. 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-122882
    HOIPIN-8

    E1/E2/E3 Enzyme Inflammation/Immunology
    HOIPIN-8 is a potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM. HOIPIN-8 is a HOIPIN-1 derivative with enhanced the potency by 255-fold in the petit-LUBAC inhibition, and 10-fold and 4-fold in the LUBAC- and TNF-α-mediated NF-κB activation, respectively than HOIPIN-1. HOIPIN-1 is a promising tool to explore the cellular functions of LUBAC.
  • HY-134820
    MLT-943

    MALT1 Inflammation/Immunology
    MLT-943 is a potent, selective and orally active MALT1 protease inhibitor. MLT-943 inhibits stimulated-IL-2 secretion in PBMC or in whole blood with a similar IC50 across species (0.07-0.09 μM in PBMC, 0.6-0.8 μM in whole blood). MLT-943 has anti-inflammatory activities and can be used for FcgR-mediated inflammation research.
  • HY-133987
    AP-1/NF-κB activation inhibitor 1

    NF-κB Inflammation/Immunology
    AP-1/NF-κB activation inhibitor 1 is a potent AP-1 and NF-κB mediated transcriptional activation inhibitor (IC50=1 μM), without blocking basal transcription driven by the β-actin promoter. AP-1/NF-κB activation inhibitor 1 has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells.
  • HY-106005
    MMV390048

    Parasite PI4K Infection
    MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kd app=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent.
  • HY-N0751
    Scutellarin

    STAT Akt HIV Cancer Infection
    Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. Scutellarin is active against HIV-1IIIB, HIV-1(74V) and HIV-1KM018 with EC50s of 26 μM, 253 μM and 136 μM, respectively.
  • HY-113618B
    RO2959 monohydrochloride

    CRAC Channel Interleukin Related Cardiovascular Disease
    RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways.
  • HY-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-13509
    CCG-50014

    RGS Protein Inflammation/Immunology
    CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site. CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test.
  • HY-N2025
    Oroxin A

    PPAR Glucosidase Metabolic Disease
    Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity. Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence.
  • HY-128121
    MLS1547

    Dopamine Receptor Neurological Disease
    MLS1547 is a highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist (Ki=1.2 μM). MLS1547 stimulates D2R G protein-mediated signaling (EC50=0.37 μM in a calcium mobilization assay). MLS1547 acts as an antagonist for dopamine (DA)-stimulated β-arrestin recruitment to the D2R (IC50=9.9 μM).
  • HY-N1372A
    Fangchinoline

    HIV FAK Apoptosis Autophagy Cancer Infection
    Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing. Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK. Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer.
  • HY-B0837
    Emamectin Benzoate

    MK-244

    Parasite GABA Receptor Reactive Oxygen Species Apoptosis Infection Neurological Disease
    Emamectin Benzoate (MK-244) is an orally active nervoussystem toxicant by binding g-aminobutyric (GABA) receptor in insects. Emamectin Benzoate is one of semi-synthetic derivative of Avermectin (HY-15311) with a broadspectrum of insecticidal and acaricidal activity. Emamectin Benzoate induces ROS-mediated DNA damage and cell apoptosis. Emamectin Benzoate, a mixture of the natural Emamectin B1a benzoate and Emamectin B1b benzoate, has the main component of Emamectin B1a benzoate.
  • HY-N7176
    Kaempferol 3-O-β-D-glucuronide

    Kaempferol-3-glucuronide; Kaempferol-3-O-glucuronide

    Interleukin Related Inflammation/Immunology
    Kaempferol 3-O-β-D-glucuronide (Kaempferol-3-glucuronide), one conjugated kaempferol metabolite, has anti-inflammatory effect. Kaempferol 3-O-β-D-glucuronide significantly inhibits various pro-inflammatory mediators like IL-1β, NO, PGE2, and LTB4. Kaempferol 3-O-β-D-glucuronide upregulates the secretion of anti-inflammatory cytokine IL-10.
  • HY-N1912
    Andropanolide

    NF-κB Inflammation/Immunology
    Andrographolide (Andro) is a small antagonist for NF-κB activation by covalent modifying reduced cysteine 62 of p50. Andrographolide is a bicyclic diterpenoid lactone mainly produced from the plant Andrographis (Andrographis paniculate). Andrographolide suppresses the activation of NF-κB in stimulated endothelial cells, which reduces the expression of cell adhesion molecule E-selectin and prevents E-selectin-mediated leukocyte adhesion, but has no effect on IκBα degradation, p50 and p65 nuclear translocation.
  • HY-13811
    NSC697923

    E1/E2/E3 Enzyme Apoptosis Cancer
    NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity.
  • HY-N0376
    Liquiritin

    Reactive Oxygen Species Cancer Inflammation/Immunology Neurological Disease
    Liquiritin, a flavonoid isolated from Glycyrrhiza, is a potent and competitive AKR1C1 inhibitor with IC50s of 0.62 μM, 0.61 μM, and 3.72μM for AKR1C1, AKR1C2 and AKR1C3, respectively. Liquiritin efficiently inhibits progesterone metabolism mediated by AKR1C1 in vivo. Liquiritin acts as an antioxidant and has neuroprotective, anti-cancer and anti-inflammatory activity.
  • HY-103160A
    EHNA hydrochloride

    Adenosine Deaminase Phosphodiesterase (PDE) Influenza Virus Cancer Infection Neurological Disease Cardiovascular Disease
    EHNA hydrochloride is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA hydrochloride exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity. EHNA hydrochloride play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects.
  • HY-11108
    R406 free base

    Syk FLT3 Apoptosis Inflammation/Immunology Cancer
    R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 free base reduces immune complex-mediated inflammation. R406 free base also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
  • HY-P0262
    Galantide

    Neuropeptide Y Receptor Metabolic Disease Inflammation/Immunology Neurological Disease Endocrinology
    Galantide, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide appears to bind to a single population of SP receptors (KD~40 nM).
  • HY-P9976
    Isatuximab

    Apoptosis Cancer
    Isatuximab is a monoclonal antibody targeting the transmembrane receptor and ectoenzyme CD38, a protein highly expressed on hematological malignant cells, including those in multiple myeloma (MM). Isatuximab has antitumor activity via multiple biological mechanisms, including antibody-dependent cellular-mediated cytotoxicity, complement-dependent cytotoxicity, antibody-dependent cellular phagocytosis, and direct induction of apoptosis without crosslinking. Isatuximab also directly inhibits CD38 ectoenzyme activity, which is implicated in many cellular functions.
  • HY-13207
    ONX-0914

    PR-957

    Proteasome Bacterial HIV Infection Inflammation/Immunology
    ONX-0914 (PR-957) is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1.
  • 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-119101
    AZD-5672

    CCR Potassium Channel P-glycoprotein Inflammation/Immunology
    AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis.
  • HY-122156
    IMB-301

    HIV Infection
    IMB-301 is a specific HIV-1 replication inhibitor that binds to hA3G (human APOBEC3G), interrupts the hA3G-Vif interaction and inhibits Vif-mediated degradation of hA3G. IMB-301 inhibits the replication of HIV-1 in H9 cells (IC50=8.63 uM). Human APOBEC3G is a restriction factor that inhibits human immunodeficiency 1 virus (HIV-1) replication.
  • HY-W017316S
    Terpinen-4-ol-d7

    Endogenous Metabolite Cancer Inflammation/Immunology
    Terpinen-4-ol-d7 (4-Carvomenthenol-d7) is the deuterium labeled Terpinen-4-ol. Terpinen-4-ol (4-Carvomenthenol), a naturally occurring monoterpene, is the main bioactive component of tea-tree oil. Terpinen-4-ol suppresses inflammatory mediator production by activated human monocytes. Terpinen-4-ol significantly enhances the effect of several chemotherapeutic and biological agents.
  • HY-B0151
    Pregnenolone

    3β-Hydroxy-5-pregnen-20-one

    Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
  • HY-N0261
    Aurantio-obtusin

    Others Inflammation/Immunology Cardiovascular Disease
    Aurantio-obtusin is an anthraquinone isolated from Semen Cassiae, with anti-Inflammatory, anti-oxidative, anti-coagulating and anti-hypertension activities. Aurantio-obtusin relaxes systemic arteries through endothelial PI3K/AKT/eNOS-dependent signaling pathway in rats, thus acts as a new potential vasodilator. Aurantio-obtusin inhibits allergic responses in IgE-mediated mast cells and anaphylactic models and is potential for treatment for allergy-related diseases.
  • HY-130269
    β-Naphthoflavone-CH2-OH

    β-NF-CH2-OH

    Ligand for E3 Ligase Cancer
    β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) is a ligand for arylhydrocarbon receptor (AhR) E3 ligase. β-Naphthoflavone-CH2-OH can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1) that recruit the AhR E3 ligase complex by incorporating AhR ligands into chimeric molecules. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
  • HY-10002A
    (1S)-Calcitriol

    1α,25-Dihydroxy-3-epi-vitamin-D3

    Others Others
    (1S)-Calcitriol (1α,25-Dihydroxy-3-epi-vitamin-D3) is a natural metabolite of 1α,25-dihydroxyvitamin D3 (1α,25(OH)2D3). (1S)-Calcitriol exhibits potent vitamin D receptor (VDR)-mediated actions such as inhibition of keratinocyte growth or suppression of parathyroid hormone secretion.
  • HY-101513
    eIF4A3-IN-1

    Eukaryotic Initiation Factor (eIF) Autophagy Cancer
    eIF4A3-IN-1 (compound 53a) is a selective eukaryotic initiation factor 4A3 (eIF4A3) inhibitor (IC50=0.26 μM; Kd=0.043 μM), which binds to a non-ATP binding site of eIF4A3 and shows significant cellular nonsense-mediated RNA decay (NMD) inhibition at 10 and 3 μM and can be as a probe for further study of eIF4A3, the exon junction complex (EJC), and NMD.
  • HY-13207A
    ONX-0914 TFA

    PR-957 TFA

    Proteasome Bacterial HIV Infection Inflammation/Immunology
    ONX-0914 (PR-957) TFA is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 TFA blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 TFA is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 TFA reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1.
  • HY-N6588
    3,4,5-Tricaffeoylquinic acid

    3,4,5-triCQA

    Akt NF-κB Inflammation/Immunology
    3,4,5-Tricaffeoylquinic acid (3,4,5-triCQA) inhibits tumor necrosis factor-α-stimulated production of inflammatory mediators in keratinocytes via suppression of Akt- and NF-κB-pathways. 3,4,5-Tricaffeoylquinic acid induces cell cycle arrest at G0/G1, actin cytoskeleton organization, chromatin remodeling, neuronal differentiation, and bone morphogenetic protein signaling in human neural stem cells. 3,4,5-Tricaffeoylquinic acid has the potential for the research of aging-associated diseases.
  • HY-112345
    PD-089828

    FGFR PDGFR EGFR Src Cancer
    PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity.
  • HY-B1739
    Pregnenolone monosulfate

    3β-Hydroxy-5-pregnen-20-one monosulfate

    Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate can protect the brain from cannabis intoxication. Pregnenolone monosulfate is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
  • HY-119293
    K777

    Cathepsin CCR Cytochrome P450 Cancer Infection
    K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively.
  • HY-135699
    TD52

    Apoptosis Phosphatase Akt Cancer
    TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity.
  • HY-15814
    HG-7-85-01

    Bcr-Abl PDGFR c-Kit Src JAK Apoptosis Cancer
    HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression.
  • HY-110189
    Pregnenolone monosulfate sodium salt

    3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt

    Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone monosulfate sodium salt (3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication. Pregnenolone monosulfate sodium salt is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
  • HY-16659
    EHT 1864

    Ras Neurological Disease Cancer
    EHT 1864 is an inhibitor of Rac family small GTPases. EHT 1864 directly binds and impairs the ability of this small GTPase to engage critical downstream effectors required for growth transformation. The Kd values are 40, 50, 60, and 230 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. EHT 1864 also potently inhibits other Rac-dependent transformation processes, Tiam1- and Ras-mediated growth transformation. EHT 1864 prevents Aβ 40 and Aβ 42 production in vivo.
  • HY-19975
    RN-1734

    TRP Channel Neurological Disease
    RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM). RN-1734 clearly decreases the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells.
  • HY-135680
    I-OMe-Tyrphostin AG 538

    I-OMe-AG 538

    IGF-1R Cancer Metabolic Disease
    I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50 of 1 µM.
  • HY-12398A
    TEI-9648

    VD/VDR Metabolic Disease Inflammation/Immunology
    TEI-9648, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9648 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9648 also inhibits HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9648 has the potential for bone metabolism research.
  • HY-12398
    TEI-9647

    VD/VDR Metabolic Disease Inflammation/Immunology
    TEI-9647, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9647 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9647 inhibits bone resorption and HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9647 has the potential for suppressing the excessive bone resorption and osteoclast formation in Paget's disease.
  • HY-13453
    BAY 11-7082

    BAY 11-7821

    IKK Deubiquitinase Autophagy Apoptosis Cancer Inflammation/Immunology
    BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
  • HY-19369
    L-685458

    L-685,458

    γ-secretase Apoptosis Neurological Disease Cancer
    L-685458 is a potent transition state analog (TSA) γ-secretase inhibitor (GSI). L-685458 inhibits amyloid β-protein precursor γ-secretase activity with IC50 of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested. L685458 inhibits γ-secretase-mediated cleavage of APP-C99 and Notch-100 with IC50s of 301.3 nM and 351.3 nM, respectively. L-685458 can be used for the research of alzheimer’s disease (AD) and cancers.
  • HY-P1454
    Fz7-21

    Ac-LPSDDLEFWCHVMY-NH2

    Wnt Cancer
    Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2), a peptide antagonist of Frizzled 7 (FZD 7) receptors, selectively binds to FZD7 CRD subclass. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC50=100 nM) or transfected with a construct expressing WNT3A or WNT1. Fz7-21 also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells (IC50=50 nM).
  • HY-P1454A
    Fz7-21 TFA

    Ac-LPSDDLEFWCHVMY-NH2 TFA

    Wnt Cancer
    Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) TFA , a peptide antagonist of Frizzled 7 (FZD 7) receptors, selectively binds to FZD7 CRD subclass. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC50=100 nM) or transfected with a construct expressing WNT3A or WNT1. Fz7-21 also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells (IC50=50 nM).
  • HY-P2141
    TRV-120027

    Angiotensin Receptor Cardiovascular Disease
    TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment.
  • HY-P2141A
    TRV-120027 TFA

    Angiotensin Receptor Cardiovascular Disease
    TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment.
  • HY-15568A
    A-317491 sodium salt hydrate

    P2X Receptor Inflammation/Immunology Neurological Disease
    A-317491 sodium salt hydrate is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 sodium salt hydrate is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 sodium salt hydrate reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.
  • HY-15568
    A-317491

    P2X Receptor Inflammation/Immunology Neurological Disease
    A-317491 is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.
  • HY-13948
    Angiotensin II human

    Angiotensin II; Ang II; DRVYIHPF

    Angiotensin Receptor Apoptosis Cardiovascular Disease Endocrinology Cancer
    Angiotensin II (Angiotensin II) is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). 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. Angiotensin II induces capillary formation from endothelial cells via the LOX-1 dependent redox-sensitive pathway.
  • HY-13948B
    Angiotensin II human TFA

    Angiotensin II TFA; Ang II TFA; DRVYIHPF TFA

    Angiotensin Receptor Apoptosis Cancer Endocrinology Cardiovascular Disease
    Angiotensin II human (Angiotensin II) TFA is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human TFA plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human TFA stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human TFA 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 TFA also induces apoptosis. Angiotensin II human TFA induces capillary formation from endothelial cells via the LOX-1 dependent redox-sensitive pathway.
  • HY-13948A
    Angiotensin II human acetate

    Angiotensin II acetate; Ang II acetate; DRVYIHPF acetate

    Angiotensin Receptor Apoptosis Cancer Endocrinology Cardiovascular Disease
    Angiotensin II human (Angiotensin II) acetate is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human acetate plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). 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. Angiotensin II human acetate induces capillary formation from endothelial cells via the LOX-1 dependent redox-sensitive pathway.
  • HY-112608
    CHMFL-PI3KD-317

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