1. Search Result

Search Result

Targets Recommended: E1/E2/E3 Enzyme Keap1-Nrf2

Results for "3-Aminopropionitrile fumarate 2:1" in MCE Product Catalog:

461

Inhibitors & Agonists

2

Screening Libraries

1

Biochemical Assay Reagents

34

Peptides

76

Natural
Products

8

Recombinant Proteins

Cat. No. Product Name Target Research Area
  • HY-107829
    3-Aminopropionitrile fumarate (2:1)

    Di-β-Aminopropionitrile fumarate; β-Aminopropionitrile fumarate; β-Ammoniumpropionitrile hemifumarate

    Others Others
    3-Aminopropionitrile fumarate (2:1) is a lathyrogen which inhibits crosslinking of collagen.
  • HY-113020
    21-Hydroxypregnenolone

    Endogenous Metabolite Metabolic Disease
    21-Hydroxypregnenolone is an essential intermediate in corticosterone synthesis.
  • HY-103394
    TC HSD 21

    Others Cancer
    TC HSD 21 is a potent 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) inhibitor with an IC50 of 14 nM. TC HSD 21 shows excellent selectivity over 17β-HSD isoenzymes and nuclear receptors.
  • HY-100207
    CP21R7

    CP21

    GSK-3 Cancer
    CP21R7 is potent GSK-3β inhibitor, with an IC50 of 1.8 nM; CP21R7 also shows inhibitory activitiy against PKCα, with an IC50 of 1900 nM.
  • HY-12484
    BMH-21

    DNA/RNA Synthesis Cancer
    BMH-21 is a small molecule DNA intercalator that binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription; does not cause phosphorylation of H2AX.
  • HY-B1214
    Prednisolone 21-acetate

    Others Inflammation/Immunology
    Prednisolone 21-acetate is an adrenal cortico hormones, with anti-inflammatory, anti-allergic and immune suppressive effects.
  • HY-N2275
    21-​O-​Tigloylgymnemagenin

    Others Others
    21-​O-​Tigloylgymnemagenin (Compound 7) is a acylated triterpenes isolated from Gymnema sylvestre.
  • HY-100234A
    DREADD agonist 21 dihydrochloride

    mAChR Neurological Disease
    DREADD agonist 21 dihydrochloride is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM).
  • HY-100234
    DREADD agonist 21

    mAChR Neurological Disease
    DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM).
  • HY-107470
    Antitumor agent-21

    Others Cancer Inflammation/Immunology
    Antitumor agent-21 is an aryl-quinolin derivative, with potential anticancer, anti-inflammatory, anti-proliferative, anti-hormonal effects and inhibition of vasculogenic mimicry .
  • HY-101386
    PZM21

    Opioid Receptor Neurological Disease
    PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.
  • HY-133322
    m-PEG21-acid

    PROTAC Linker Cancer
    m-PEG21-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-141025
    Bis-PEG21-acid

    PROTAC Linker Cancer
    Bis-PEG21-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140373
    Tos-PEG21-Tos

    PROTAC Linker Cancer
    Tos-PEG21-Tos is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-141237
    HO-PEG21-OH

    PROTAC Linker Cancer
    HO-PEG21-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-P1521
    β-Amyloid 15-21

    Beta-Amyloid (15-21)

    Amyloid-β Neurological Disease
    β-amyloid (15-21) is a fragment of Amyloid-β peptide, maybe used in the research of neurological disease.
  • HY-13023
    AMG-Tie2-1

    VEGFR
    AMG-Tie2-1 is an inhibitor of tunica interna endothelial cell kinase 2 (Tie2) and VEGF receptor 2 (VEGFR2) with IC50 values of 1 and 3 nM, respectively.
  • HY-B1832
    Prednisone acetate

    Prednisone 21-acetate

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    Prednisone acetate (Prednisone 21-acetate), the acetate salt form of prednisolone, is a glucocorticoid receptor agonist with anti-inflammatory and immunomodulating properties.
  • HY-B0775
    Betamethasone-17-butyrate-21-propionate

    Others Inflammation/Immunology
    Betamethasone-17-butyrate-21-propionate is a topical corticosteroid with potential in the treatment of inflammatory skin diseases.
  • HY-18061
    Ochromycinone

    (Rac)-STA-21

    STAT Bacterial Cancer Infection
    Ochromycinone ((Rac)-STA-21) is a natural antibiotic and a STAT3 inhibitor. Ochromycinone can inhibits STAT3 DNA binding activity, STAT3 dimerization. Ochromycinone has anticancer and antimicrobial activity.
  • HY-130827
    Bis-PEG21-NHS ester

    ADC Linker Cancer
    Bis-PEG21-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-17461A
    Cortisone acetate

    Cortisone 21-acetate

    Glucocorticoid Receptor Endogenous Metabolite Apoptosis Cancer Endocrinology
    Cortisone acetate (17-hydroxy-11-dehydrocorticosterone), a 21-carbon steroid hormone, is one of the main hormones released by the adrenal gland in response to stress.
  • HY-U00169
    Prednisolone farnesylate

    PNF21

    Others Inflammation/Immunology
    Prednisolone farnesylate (PNF21) is a new transdermal corticosteroid with anti-inflammatory activity.
  • HY-14564A
    GTS-21 dihydrochloride

    DMXB-A; DMBX-anabaseine

    nAChR Inflammation/Immunology
    GTS-21 dihydrochloride is a selective α7 nicotinic acetylcholine receptor agonist, has recently been established as a promising treatment for inflammation.
  • HY-W036553
    6-Hydroxypyridin-2(1H)-one hydrochloride

    Endogenous Metabolite Metabolic Disease
    6-Hydroxypyridin-2(1H)-one hydrochloride is an endogenous metabolite.
  • HY-14648A
    Dexamethasone acetate

    Dexamethasone 21-acetate; Hexadecadrol acetate

    Glucocorticoid Receptor Autophagy Mitophagy Bacterial Inflammation/Immunology Endocrinology Cancer
    Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist. Dexamethasone acetate has the potential for ophthalmic infections treatment.
  • HY-B0564
    Sodium nitroprusside

    Ro 21-2498

    Others Cancer Cardiovascular Disease
    Sodium nitroprusside (Ro 21-2498) is a potent vasodilator working through releasing NO spontaneously in blood.
  • HY-115514A
    BRK inhibitor P21d hydrochloride

    Others Cancer
    BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models.
  • HY-N4162
    3-Oxo-21α-methoxy-24,25,26,27-tetranortirucall-7-ene-23(21)-lactone

    Others Cancer
    3-Oxo-21α-methoxy-24,25,26,27-tetranortirucall-7-ene-23(21)-lactone is a cytotoxic tirucallane C26 triterpenoid isolated from the stem barks of Aphanamixis grandifolia.
  • HY-W015224
    Methyl 2-(1H-indol-3-yl)acetate

    Endogenous Metabolite Metabolic Disease
    Methyl 2-(1H-indol-3-yl)acetate is an endogenous metabolite.
  • HY-103252S
    Monomethyl fumarate D3

    Others Neurological Disease
    Monomethyl fumarate D3 is a deuterium labeled Monomethyl fumarate. Monomethyl fumarate is the primary metabolite of dimethyl fumarate.
  • HY-W010130
    7-Hydroxy-3,4-dihydro-2(1H)-quinolinone

    3,4-Dihydro-7-hydroxy-2(1H)-quinolinone

    Monoamine Oxidase Neurological Disease
    7-​Hydroxy-​3,​4-​dihydro-​2(1H)​-​quinolinone (3,4-Dihydro-7-hydroxy-2(1H)-quinolinone) is a weak MAO-A inhibitor, with an IC50 of 183 μM, and has no effect on MAO-B.
  • HY-W010155
    2-(1H-Indol-3-yl)ethan-1-ol

    Endogenous Metabolite Metabolic Disease
    2-(1H-Indol-3-yl)ethan-1-ol is an endogenous metabolite.
  • HY-123489
    3α,21-Dihydroxy-5α-pregnan-20-one

    THDOC

    GABA Receptor
    3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
  • HY-128835
    Phenol-amido-C1-PEG3-N3

    PROTAC Linker 21

    PROTAC Linker Cancer
    Phenol-amido-C1-PEG3-N3 (PROTAC Linker 21) is an PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-100113
    AT2 receptor agonist C21

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    AT2 receptor agonist C21 is a druglike selective angiotensin II AT2 receptor agonist with Ki values of 0.4 nM and >10 µM for the AT2 receptor and AT1 receptor, respectively.
  • 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-W062542
    2-(1-Methyl-1H-imidazol-4-yl)ethan-1-amine

    Endogenous Metabolite Metabolic Disease
    2-(1-Methyl-1H-imidazol-4-yl)ethan-1-amine is a histamine (Him) metabolite.
  • HY-103252
    Monomethyl fumarate

    GPR109A Drug Metabolite Inflammation/Immunology Neurological Disease
    Monomethyl fumarate, an active metabolite of Dimethyl fumarate (DMF), is a potent GPR109A agonist. Monomethyl fumarate has the potential for multiple neuroprotective pathways and other models of retinal disease.
  • HY-B1060
    6α-Methylprednisolone 21-hemisuccinate sodium salt

    Methylprednisolone sodium succinate; 6-Methylprednisolone succinate sodium

    Others Inflammation/Immunology
    6α-Methylprednisolone 21-hemisuccinate sodium salt is a glucocorticoid of slightly longer half-life than that of Prednisolone.
  • HY-P1454A
    Fz7-21 TFA

    (Ac)-LPSDDLEFWCHVMY-NH2 TFA

    Wnt Cancer
    Fz7-21 TFA ((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-B0021
    Doxifluridine

    Ro 21-9738; 5-Fluoro-5'-deoxyuridine; 5'-DFUR

    Nucleoside Antimetabolite/Analog Cancer
    Doxifluridine(Ro 21-9738; 5'-DFUR) is a thymidine phosphorylase activator for PC9-DPE2 cells with IC50 of 0.62 μM.
  • HY-P1024
    GLP-2(1-33)(human)

    GLP-2 (human); Glucagon-like peptide 2 (human)

    Glucagon Receptor Metabolic Disease
    GLP-2(1-33) (human) is an enteroendocrine hormone which can bind to the GLP-2 receptor and stimulate the growth of intestinal epithelium.
  • HY-B1155
    Hydrocortisone phosphate

    Hydrocortisone 21-phosphate; Cortisol 21-phosphate

    Glucocorticoid Receptor Metabolic Disease Endocrinology
    Hydrocortisone phosphate is the pharmaceutical term for cortisol, which is a steroid hormone, in the glucocorticoid class of hormones, increases blood sugar through gluconeogenesis, to suppress the immune system, and to aid in the metabolism of fat, protein, and carbohydrate.
  • HY-B1183
    Hydrocortisone acetate

    Hydrocortisone 21-acetate; Cortisol 21-acetate

    Glucocorticoid Receptor Endogenous Metabolite Inflammation/Immunology Endocrinology
    Hydrocortisone acetate is a corticosteroid, used to decrease swelling, itching, and pain that is caused by minor skin irritations or by hemorrhoids.
  • HY-101632
    Irindalone

    Lu 21-​098

    5-HT Receptor Neurological Disease
    Irindalone is a novel serotonin 5-HT2 antagonist.
  • HY-B1087
    Prednisolone hemisuccinate

    Prednisolone 21-hemisuccinate

    Others Inflammation/Immunology
    Prednisolone hemisuccinate is a synthetic glucocorticoid, a derivative of cortisol, which is used to treat a variety of inflammatory and auto-immune conditions.
  • HY-13571
    Betamethasone dipropionate

    Betamethasone 17,21-dipropionate

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology Cancer
    Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.
  • HY-N4328
    Pasakbumin B

    13α-(21)-Epoxyeurycomanone

    Others Inflammation/Immunology
    Pasakbumin B, a bioactive compound from Eurycoma longifolia Jack, exhibits potent antiulcer activity.
  • HY-W050145
    (1R,2S,3S,4R,5S)-6,8-Dioxabicyclo[3.2.1]octane-2,3,4-triol

    Endogenous Metabolite Metabolic Disease
    (1R,2S,3S,4R,5S)-6,8-Dioxabicyclo[3.2.1]octane-2,3,4-triol is an endogenous metabolite.
  • HY-B0890
    Zomepirac sodium salt

    McN-2783-21-98

    PGE synthase Inflammation/Immunology
    Zomepirac sodium salt is a pyrrole-acetic acid structurally related to tolmetin sodium; a prostaglandin synthetase inhibitor.
  • HY-B0645
    Prednisolone disodium phosphate

    Prednisolone 21-phosphate disodium

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    Prednisolone disodium phosphate is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties.
  • HY-17461
    Cortisone

    17-Hydroxy-11-dehydrocorticosterone; Kendall's compound E

    Glucocorticoid Receptor Endogenous Metabolite Inflammation/Immunology Endocrinology
    Cortisone is a 21-carbon steroid hormone.
  • HY-B0298A
    Clemastine fumarate

    HS-592 fumarate; Meclastine fumarate

    Histamine Receptor Autophagy Neurological Disease Endocrinology
    Clemastine (fumarate) (HS-592 (fumarate)) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.
  • HY-B2060A
    Tiamulin fumarate

    Thiamutilin fumarate

    Bacterial Antibiotic Infection Cancer
    Tiamulin fumarate (Thiamutilin fumarate) is a diterpenic veterinary drug widely used in swine for the control of infectious diseases, including swine dysentery and enzootic pneumonia.
  • HY-B1829A
    Dexamethasone phosphate disodium

    Dexamethasone 21-phosphate disodium salt

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    Dexamethasone phosphate disodium is a glucocorticoid receptor agonist.
  • HY-128682
    PGAM1-IN-2

    Phosphatase Cancer
    PGAM1-IN-2 is a phosphoglycerate mutase 1 (PGAM1) inhibitor with an IC50 of 2.1 μM.
  • HY-14734B
    Anamorelin Fumarate

    ONO-7643 fumarate; RC1291 fumarate

    GHSR Cancer Endocrinology
    Anamorelin Fumarate is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.
  • HY-100499
    Tyrphostin AG 528

    Tyrphostin B66; AG 528

    EGFR Cancer
    Tyrphostin AG 528 is an inhibitor of EGFR and ErbB2 with IC50s of 4.9 and 2.1 μM, respectively. Tyrphostin AG 528 (Tyrphostin B66) is a protein tyrosine kinase inhibitor, with IC50s of 4.9 μM for epidermal growth factor receptors (EGFR) and 2.1 μM for ErbB2. Tyrphostin AG 528 is also an anticancer agent.
  • HY-113697
    PF-05231023

    FGFR Metabolic Disease
    PF-05231023, a long-acting fibroblast growth factor 21 (FGF21) analog, is a FGF21-receptor agonist, suitable for development as a potential treatment for T2DM.
  • HY-B1651
    Iron(II) fumarate

    Ferrous fumarate

    Others Metabolic Disease
    Iron(II) fumarate (Ferrous fumarate) is the iron(II) salt of fumaric acid. Iron(II) fumarate is an orally active dietary supplement and has the potential for iron deficiency anemia treatment.
  • HY-107649
    Zamifenacin fumarate

    UK-76654 fumarate

    mAChR Metabolic Disease
    Zamifenacin fumarate (UK-76654 fumarate) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome.
  • HY-13511A
    Rupatadine Fumarate

    UR-12592 fumarate

    Histamine Receptor Autophagy Inflammation/Immunology
    Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).
  • HY-14949C
    Cevipabulin fumarate

    TTI-237 fumarate

    Microtubule/Tubulin Cancer
    Cevipabulin fumarate (TTI-237 fumarate) is an oral, microtubule-active, antitumor compound and inhibits the binding of [ 3H]NSC 49842 to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line.
  • HY-U00266
    Cefetrizole

    Glucosidase Infection Metabolic Disease
    Ceftezole is an α-Glucosidase inhibitor with an IC50 and a Ki of 2.1 μM and 0.578 μM, respectively.
  • HY-101088
    CeMMEC13

    DNA/RNA Synthesis Cancer
    CeMMEC13 is a potent inhibitor of TAF1 (2) bromodomain, with an IC50 of 2.1 μM.
  • HY-B1618
    Corticosterone

    17-Deoxycortisol; 11β,21-Dihydroxyprogesterone; Kendall's compound B

    Glucocorticoid Receptor Endogenous Metabolite Neurological Disease Endocrinology
    Corticosterone is an adrenocortical steroid that has modest but significant activities as a mineralocorticoid and a glucocorticoid.
  • HY-W007686
    Imidazoleacetic acid hydrochloride

    Imidazolyl-4-acetic acid hydrochloride

    Endogenous Metabolite Metabolic Disease
    2-(1H-Imidazol-5-yl)acetic acid hydrochloride is an endogenous metabolite.
  • HY-15516
    Sotagliflozin

    LX-4211; LP-802034

    SGLT Metabolic Disease
    Sotagliflozin (LX-4211) is a potent dual SGLT2/1 inhibitor. Antidiabetic agents.
  • HY-14881A
    Bedaquiline fumarate

    R403323; TMC207 fumarate; R207910 fumarate

    Bacterial Antibiotic Infection
    Bedaquiline fumarate, a diarylquinoline antibiotic that targets ATP synthase, is effective for the treatment of Mycobacterium tuberculosis infections.
  • HY-15232A
    Tenofovir alafenamide fumarate

    GS-7340 (fumarate)

    HIV Reverse Transcriptase Infection
    Tenofovir alafenamide fumarate (GS-7340 fumarate) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-103085
    T-3775440 hydrochloride

    Histone Demethylase Cancer
    T-3775440 (hydrochloride) is an irreversible lysine-specific histone demethylase (LSD1) inhibitor with an IC50 value of 2.1 nM.
  • HY-W019696
    Monoethyl fumarate

    Others Others
    Monoethyl fumarate is the monoethyl ester form of fumaric acid. Monoethyl fumarate is a kind of effective preservative and polymerization agent for macromolecular material.
  • HY-A0030
    Fesoterodine fumarate

    mAChR Metabolic Disease Neurological Disease
    Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB).
  • HY-W010056
    Diethyl fumarate

    Endogenous Metabolite Metabolic Disease
    Diethyl fumarate is an endogenous metabolite.
  • HY-19635A
    G-5555 hydrochloride

    PAK Cancer
    G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.
  • HY-100736
    ML348

    GNF-Pf-1127

    Phospholipase Cancer
    ML348 is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor with an IC50 of 210 nM, and barely inhibits LYPLA2.
  • HY-15646
    UNC1999

    Histone Methyltransferase Autophagy Cancer
    UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH2/1 with IC50s of <10 nM and 45 nM, repectively.
  • HY-107348
    Etofylline clofibrate

    Others Cardiovascular Disease
    Etofylline clofibrate has ypolipidemic and antithrombotic effect. Etofylline clofibrate has an agonistic interaction with intimal PGI2.
  • HY-11042
    GNE-477

    PI3K mTOR Cancer
    GNE-477 is a potent and efficacious dual PI3K (IC50=4 nM)/mTOR(Ki=21 nM) inhibitor.
  • HY-N0581
    Qingyangshengenin A

    Others Neurological Disease
    Qingyangshengenin A, a C-21 steroidal glycoside isolated from the roots of Cynanchum otophyllum Schneid, has antiepileptic activity.
  • HY-B0157A
    Ketotifen fumarate

    HC 20511 fumarate

    Histamine Receptor Inflammation/Immunology Endocrinology
    Ketotifen (fumarate) is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer, which is used to prevent asthma attacks.
  • HY-101458
    IT1t

    CXCR HIV Inflammation/Immunology Endocrinology
    IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
  • HY-112583
    MIV-247

    Cathepsin Neurological Disease
    MIV-247 is a selective cathepsin S inhibitor with Kis of 2.1, 4.2 and 7.5 nM for human, mouse and cynomolgus monkey cathepsin S, respectively.
  • HY-101458A
    IT1t dihydrochloride

    CXCR HIV Inflammation/Immunology Endocrinology Cancer
    IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
  • HY-100611
    CaCCinh-A01

    Chloride Channel Inflammation/Immunology Cancer
    CaCCinh-A01 is an inhibitor of both TMEM16A and calcium-activated chloride channel (CaCC) with IC50s of 2.1 and 10 μM, respectively.
  • HY-19989A
    MK-571 sodium salt

    L-660711 sodium salt

    Leukotriene Receptor Inflammation/Immunology
    MK-571 sodium salt is a selective, orally active leukotriene D4 receptor antagonist, with Kis of 0.22 and 2.1 nM in guinea pig and human lung membranes.
  • HY-15542A
    FRAX597

    PAK Cancer
    FRAX597 is a potent group I p21-activated Kinases (PAKs) inhibitor with IC50 of 8, 13 and 19 nM for PAK1, 2 and 3.
  • HY-U00190
    Deprodone propionate

    RD20000

    Others Inflammation/Immunology
    Deprodone propionate (RD20000) is a corticosteroid which is obtained by esterifying with propionic acid the 17-position of the prednisolone skeleton and deoxidating its 21-position.
  • HY-15027
    5-Aminosalicylic Acid

    Mesalamine; 5-ASA; Mesalazine

    PPAR PAK NF-κB Endogenous Metabolite Inflammation/Immunology Cancer
    5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
  • HY-126325
    BY27

    Epigenetic Reader Domain Cancer
    BY27 is a potent and selective BET BD2 inhibitor, shows 38, 5, 7, and 21-fold BD1/BD2 selectivity for BRD2, BRD3, BRD4, and BRDT. Anti-cancer activity.
  • HY-126075A
    WS-383

    E1/E2/E3 Enzyme Cancer
    WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
  • HY-U00127
    Pyridazinediones-derivative-1

    Others Neurological Disease
    Pyridazinediones-derivative-1 has potential in treating neurodegenerative disorders. It shows an ED50 of 2.1 μM for inhibiting glutamate-induced contractions of isolated guineapig ileum.
  • HY-102028
    KY1220

    Wnt β-catenin Cancer
    KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway; with an IC50 of 2.1 μM in HEK293 reporter cells.
  • HY-P0274
    PGLa

    Bacterial Antibiotic Infection
    PGLa, a 21-residue peptide, is an antimicrobial peptide. PGLa is a member of the magainin family of antibiotic peptides found in frog skin and its secretions.
  • HY-N1902
    4-Hydroxyphenylacetic acid

    Keap1-Nrf2 Endogenous Metabolite Metabolic Disease
    4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2.
  • HY-15542B
    FRAX486

    PAK Cancer
    FRAX486 is a p21-activated kinase (PAK) inhibitor with IC50s of 14, 33 and 39 nM for PAK1, PAK2 and PAK3, respectively.
  • HY-P1308
    SLIGRL-NH2

    Protease-Activated Receptor-2 Activating Peptide

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    SLIGRL-NH2 (Protease-Activated Receptor-2 Activating Peptide) is an agonist of Protease-Activated Receptor-2 (PAR-2).
  • HY-19635
    G-5555

    PAK Cancer
    G-5555 is a potent p21-activated kinase 1 (PAK1) inhibitor with Kis of 3.7 nM and 11 nM for PAK1 and PAK2, respectively.
  • HY-100531
    DprE1-IN-2

    Bacterial Infection
    DprE1-IN-2 (compound 18) is a potent DprE1 inhibitor with an IC50 of 28 nM. DprE1-IN-2 has antituberculosis effect.
  • HY-112462
    Cdk1/2 Inhibitor III

    CDK Cancer
    Cdk1/2 Inhibitor III is a selective Cdk1/2 inhibitor, with an IC50 of 2.1 μM for CDK1/cyclin B.
  • HY-P0274A
    PGLa TFA

    Bacterial Antibiotic Infection
    PGLa TFA, a 21-residue peptide, is an antimicrobial peptide. PGLa TFA is a member of the magainin family of antibiotic peptides found in frog skin and its secretions.
  • HY-15889
    AMG 925

    FLT3 CDK Cancer
    AMG 925 is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively.
  • HY-114162A
    VTP50469 fumarate

    Epigenetic Reader Domain Apoptosis Cancer
    VTP50469 fumarate is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 fumarate has potently anti-leukemia activity.
  • HY-17363
    Dimethyl fumarate

    DMF

    Keap1-Nrf2 Endogenous Metabolite Inflammation/Immunology
    Dimethyl fumarate is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator and induces upregulation of antioxidant gene expression.
  • HY-107688A
    UB-165 fumarate

    nAChR Neurological Disease
    UB-165 fumarate is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for nicotine binding in rat brain.
  • HY-U00026
    Semotiadil recemate fumarate

    Calcium Channel Cardiovascular Disease
    Semotiadil recemate fumarate is the recemate of Semotiadil fumarate. Semotiadil fumarate is a novel vasoselective Ca 2+ channel antagonist.
  • HY-110318
    VUF11207 fumarate

    CXCR Cancer
    VUF11207 fumarate (Compound 29) is a CXCR7 agonist and a high-potency CXCR7 (pKi of 8.1) ligand that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7.
  • HY-B0010
    Formoterol Fumarate

    Formoterol

    Adrenergic Receptor Inflammation/Immunology Endocrinology
    Formoterol fumarate(Foradil) is a potent, selective and long-acting β2-adrenoceptor agonist.
  • HY-125884
    Pomalidomide-amido-C4-amido-C6-NH-Boc

    Cereblon Ligand-Linker Conjugates 21; E3 Ligase Ligand-Linker Conjugates 54

    E3 Ligase Ligand-Linker Conjugate Cancer
    Pomalidomide-amido-C4-amido-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
  • HY-114310
    VDR agonist 1

    VD/VDR Apoptosis Cancer
    VDR agonist 1 (compound 28) is a nonsteroidal Vitamin D receptor (VDR) agonist, with an IC50 of 690 nM in MCF-7 cells. VDR agonist 1 arrests the cell cycle through the up-regulation of p21 and p27, promotes apoptosis by increasing the expression of BAX and decrease the expression of Bcl-2.
  • HY-101217
    BI 689648

    Cytochrome P450 Endocrinology
    BI 689648 is a novel, highly selective aldosterone synthase inhibitor which can inhibit CYP11B1 and CYP11B2 with IC50s of 310 and 2.1 nM, respectively.
  • HY-15889A
    AMG 925 HCl

    FLT3 CDK Cancer
    AMG 925 HCl is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively.
  • HY-13223
    Crenolanib

    CP-868596

    FLT3 PDGFR Autophagy Cancer
    Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
  • HY-16966
    SBI-0206965

    ULK Autophagy Apoptosis Cancer
    SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50s of 108 nM for ULK1 kinase and 711 nM for the highly related kinase ULK2.
  • HY-P1308A
    SLIGRL-NH2 TFA

    Protease-Activated Receptor-2 Activating Peptide TFA

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    SLIGRL-NH2 TFA (Protease-Activated Receptor-2 Activating Peptide TFA) is an agonist of Protease-Activated Receptor-2 (PAR-2).
  • HY-10517
    Orantinib

    SU6668; TSU-68

    PDGFR FGFR VEGFR Apoptosis Cancer
    Orantinib (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with Kis of 2.1 μM, 8 nM and 1.2 μM for Flt-1, PDGFRβ and FGFR1, respectively.
  • HY-108708
    GeA-69

    PARP Cancer
    GeA-69 is a selective, highly cell permeable allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2, with a Kd of 2.1 µM.
  • HY-100614
    AS1517499

    STAT Inflammation/Immunology Cancer
    AS1517499 is a potent STAT6 inhibitor with an IC50 of 21 nM.
  • HY-126075
    WS-383 free base

    E1/E2/E3 Enzyme Cancer
    WS-383 free base is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 free base inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
  • HY-P1424
    Lei-Dab7

    Potassium Channel
    Lei-Dab7 is a high affinity, selective KCa2.2 (SK2) channel blocker (Kd=3.8 nM). Lei-Dab7 exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, Kv and Kir2.1. Lei-Dab7 increases theta-burst responses and increases LTP in rat hippocampal slices in vitro.
  • HY-112146
    MMG-11

    Toll-like Receptor (TLR) Inflammation/Immunology
    MMG-11 is a potent and selective human TLR2 antagonist with low cytotoxicity. MMG-11 inhibits both TLR2/1 and TLR2/6 signaling with IC50s of 1.7 µM for Pam3CSK4-induced hTLR2/1 and 5.7 µM for Pam2CSK4-induced hTLR2/6 responses.
  • HY-16901
    Firsocostat

    ND-630; GS-0976; NDI-010976

    Acetyl-CoA Carboxylase Metabolic Disease
    Firsocostat (ND-630; GS-0976; NDI-010976) is an acetyl-CoA carboxylase (ACC) inhibitor; inhibits human ACC1 and ACC2 with IC50 values of 2.1 and 6.1 nM, respectively.
  • HY-128710
    2'-Fluorothymidine

    2'-​Deoxy-​2'-​fluoro-​5-​Methyluridine

    Others Cancer
    2'-Fluorothymidine (2'-Fluoro-2'-deoxythymidine), a bioisostere of both thymidine (TdR) and methyluridine, is a putative highly selective substrate for thymidine kinase type 2 (TK2).
  • HY-17642
    Omidenepag

    Prostaglandin Receptor Endocrinology
    Omidenepag,a pharmacologically active form of Omidenepag Isopropyl, is a selective, non-prostanoid EP2 receptor agonist, with an EC50 of 1.1 nM. Omidenepag shows binding affinities (IC50) 10 nM for h-EP2.
  • HY-133148
    Lp-PLA2-IN-2

    Phospholipase Inflammation/Immunology
    Lp-PLA2-IN-2 is a potent and selective lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 0f 120 nM for recombinant human Lp-PLA2.
  • HY-100830
    NCB-0846

    Wnt MAP4K Cancer
    NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.
  • HY-P1424A
    Lei-Dab7 TFA

    Potassium Channel
    Lei-Dab7 TFA is a high affinity, selective KCa2.2 (SK2) channel blocker (Kd=3.8 nM). Lei-Dab7 TFA exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, Kv and Kir2.1. Lei-Dab7 TFA increases theta-burst responses and increases LTP in rat hippocampal slices in vitro.
  • HY-B0580S
    Ketorolac D5

    COX Inflammation/Immunology
    Ketorolac D5 is a deuterium labeled Ketorolac. Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2.
  • HY-10959
    RG7112

    RO5045337

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    RG7112 is a potent, selective, first clinical, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC50 of 18 nM and a KD of 11 nM for binding to MDM2.
  • HY-133149
    Lp-PLA2-IN-3

    Phospholipase Cardiovascular Disease
    Lp-PLA2-IN-3 is a potent and orally bioavailable lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 of 14 nM for recombinant human Lp-PLA2 (rhLpPLA2).
  • HY-101140
    KI696

    Keap1-Nrf2 Metabolic Disease Inflammation/Immunology
    KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction. KI696 is a potent and selective inhibitor of the KEAP1/NRF2 interaction.
  • HY-22044
    ICA

    N-[4-(2-Pyridinyl)-2-thiazolyl]-2-pyridinamine

    Parasite Infection Cardiovascular Disease
    ICA (N-(pyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine) is a SK channel inhibitor that has antileishmanial activity with an IC50 of 2.1 µM.
  • HY-130607
    IDO1-IN-2

    Indoleamine 2,3-Dioxygenase (IDO) Cancer Inflammation/Immunology
    IDO1-IN-2 (compound 16) is a potent and selective IDO1 inhibitor with IC50s of 81 nM, 59 nM (mouse) and 28 nM (rat), respectively. IDO1-IN-2 has anti-cancer activity.
  • HY-W016103
    1-Hydroxy-2-naphthoic acid

    Endogenous Metabolite Metabolic Disease
    1-Hydroxy-2-naphthoic acid is an endogenous metabolite.
  • HY-15984
    VER-50589

    HSP Apoptosis Cancer
    VER-50589 is a Hsp90 inhibitor, with an IC50 of 21 nM and a Kd of 4.5 nM.
  • HY-P0009A
    Cetrorelix Acetate

    SB-075 acetate; NS-75A

    GNRH Receptor Neurological Disease Endocrinology
    Cetrorelix Acetate is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM.
  • HY-133145A
    hDDAH-1-IN-2 sulfate

    Others Cancer Inflammation/Immunology
    hDDAH-1-IN-2 is a selective, orally active human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1) inhibitor. hDDAH-1-IN-2 reveals an excellent profile regarding cell toxicity/viability.
  • HY-15177
    PF-04691502

    PI3K mTOR Autophagy Cancer
    PF-04691502 is a potent and selective inhibitor of PI3K and mTOR. PF-04691502 binds to human PI3Kα, β, δ, γ and mTOR with Kis of 1.8, 2.1, 1.6, 1.9 and 16 nM, respectively.
  • HY-133145
    hDDAH-1-IN-2

    Others Neurological Disease Inflammation/Immunology
    hDDAH-1-IN-2 is a selective, orally active human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1) inhibitor. hDDAH-1-IN-2 reveals an excellent profile regarding cell toxicity/viability.
  • HY-130296
    Palbociclib-propargyl

    PROTAC CDK6 ligand 1

    Ligand for Target Protein for PROTAC Cancer
    Palbociclib-propargyl is a ligand for target protein CDK6 for PROTAC, and binds to CRBN ligand via a PEG linker to make a PROTAC CP-10. CP-10 shows a DC50 of 2.1 nM for CDK6.
  • HY-78131A
    (S)-(+)-Ibuprofen

    (S)-Ibuprofen

    COX Inflammation/Immunology
    (S)-(+)-Ibuprofen is the S(+)-enantiomer of Ibuprofen that inhibits COX-1 and COX-2 activity with IC50s of 2.1 μM and 1.6 μM. (S)-(+)-Ibuprofen has analgesic, antiinflammatory and antipyretic effects.
  • HY-N7057
    Nonanoic acid

    Pelargonic acid

    Bacterial Infection
    Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2.
  • HY-10343
    Sotrastaurin

    AEB071

    PKC Inflammation/Immunology Cancer
    Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with Kis of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively.
  • HY-N0698
    Crocin II

    NO Synthase COX Cancer Inflammation/Immunology Neurological Disease
    Crocin II is isolated from the fruit of Gardenia jasminoides with antioxidant, anticancer, and antidepressant activity. Crocin II inhibits NO production with an IC50 value of 31.1 μM. Crocin II suppresses the expressions of protein and m-RNA of iNOS and COX-2.
  • HY-10799
    EG00229

    Others Cancer
    EG00229 is a neuropilin 1 (NRP1) receptor antagonist. EG00229 selectively inhibits VEGF-A binding to NRP1 b1 domain with an IC50 of 3 μM, but has no effect on VEGFA binding to VEGFR-1 and VEGFR-2.
  • HY-B0031S
    Quetiapine D4 fumarate

    5-HT Receptor Dopamine Receptor Neurological Disease
    Quetiapine D4 fumarate is the deuterium labeled Quetiapine fumarate. Quetiapine fumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects.
  • HY-18630A
    Ro 48-8071 fumarate

    Others Cancer
    Ro 48-8071 fumarate is an inhibitor of OSC (Oxidosqualene cyclase) with IC50 of appr 6.5 nM.
  • HY-100004
    Fumarate hydratase-IN-1

    Mitochondrial Metabolism Cancer
    Fumarate hydratase-IN-1 (compound 2) is a cell-permeable fumarate hydratase inhibitor. Fumarate hydratase-IN-1 has antiproliferative activity against several cancer cell lines with a mean IC50 of 2.2 μM.
  • HY-109105
    Tepilamide fumarate

    XP-23829

    Others Inflammation/Immunology
    Tepilamide fumarate (XP-23829) is an oral fumaric acid ester, acts as a prodrug of monomethyl fumarate, and is used in the research of moderate to severe chronic plaque psoriasis.
  • HY-15295
    Vonoprazan Fumarate

    TAK-438

    Proton Pump Endocrinology
    Vonoprazan Fumarate (TAK-438) is an orally active potassium-competitive acid blocker which inhibits H +, K +-ATPase activity with an IC50 of 19 nM.
  • HY-17013A
    Dofequidar fumarate

    MS-209

    P-glycoprotein Cancer
    Dofequidar fumarate(MS-209 fumarate), an orally active quinoline compound, has been reported to overcome MDR by inhibiting ABCB1/P-gp, ABCC1/MDR-associated protein 1, or both.
  • HY-U00400
    PF-592379

    Dopamine Receptor Neurological Disease
    PF-592379 is a potent dopamine D3 receptor agonist with an EC50 of 21 nM.
  • HY-19810
    MI-538

    Epigenetic Reader Domain Cancer
    MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM.
  • HY-112544
    IK1 inhibitor PA-6

    PA-6

    Potassium Channel Cardiovascular Disease
    IK1 inhibitor PA-6 (PA-6), a pentamidine analogue, is a selective and potent IK1 (KIR2.x ion-channel-carried inward rectifier current) inhibitor, with IC50 values of 12-15 nM for human and mouse KIR2.x currents. IK1 inhibitor PA-6 (PA-6) elevates KIR2.1 protein expression and induces intracellular KIR2.1 accumulation. IK1 inhibitor PA-6 (PA-6) has the potential to treat atrial fibrillation and arrhythmia.
  • HY-135967
    MTH1-IN-2

    DNA/RNA Synthesis Cancer
    MTH1-IN-2 is a MutT homolog 1 (MTH1) inhibitor extracted from patent WO2016135138A1, Compound (6), MTH1-IN-2 can be used for the research of cancer. Anti-tumor activity.
  • HY-135642
    SMS1-IN-1

    Others Inflammation/Immunology
    SMS1-IN-1, compound SAPA 1j, is a novel and the most potent sphingomyelin synthase 1 (SMS1) inhibitor with an IC50 value of 2.1 μM. SMS1-IN-1 has the potential for the treatment of atherosclerosis.
  • HY-130979
    EED226-COOH

    Ligand for Target Protein for PROTAC Cancer
    EED226-COOH is an EED226-derived ligand for target protein EED ligand for PROTAC, binds to a ligand for VHL via linker to form UNC6852 (HY-130708) to degrade PRC2.
  • HY-15793A
    Trans (2,3)-Dihydrotetrabenazine

    (2R,3R,11bR)-rel-Dihydrotetrabenazine; (2R,3R,11bR)-rel-DHTBZ

    Drug Metabolite Monoamine Transporter Neurological Disease
    Trans (2,3)-Dihydrotetrabenazine ((2R,3R,11bR)-rel-Dihydrotetrabenazine), a metabolite of Tetrabenazine, shows remarkable inhibition activity on vesicular monoamine transporter (VMAT2).
  • HY-129943
    Benzothiohydrazide

    Bacterial Infection
    Benzothiohydrazide is an analogue of anti–tubercular agent Isoniazid. Benzothiohydrazide exhibits anti–tubercular activity, with MICs of 132 μM and 264 μM for M. tuberculosis wild type (H37Rv) and clinical mutant strains (IC1 and IC2).
  • HY-15461
    Ertugliflozin

    PF-04971729

    SGLT Metabolic Disease
    Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2. Has the potential for the treatment of type 2 diabetes mellitus.
  • HY-120033
    RY796

    Sodium Channel Neurological Disease
    RY796 is a potent and selective voltage-gated potassium (KV2) channel inhibitor with IC50s of 0.25 μM and 0.09 μM for KV2.1 and KV2.2. RY796 has analgesic activity.
  • HY-N1064
    Xanthoplanine

    nAChR Neurological Disease
    Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC50 ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC50 values of 9 μM (alpha7) and 5 μM (alpha4beta2).
  • HY-P1271
    Catestatin

    nAChR Cardiovascular Disease
    Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
  • HY-12826
    Mcl1-IN-2

    Bcl-2 Family Cancer
    Mcl1-IN-2 is an inhibitor of myeloid cell factor 1 (Mcl-1).
  • HY-12453
    TBK1/IKKε-IN-2

    IKK Inflammation/Immunology
    TBK1/IKKε-IN-2 is a dual TBK1 and IKKε inhibitor.
  • HY-101299
    (+)-Dihydrexidine hydrochloride

    (+)-DAR-0100 (hydrochloride)

    Dopamine Receptor Neurological Disease
    (+)-Dihydrexidine hydrochloride ((+)-DAR-0100 hydrochloride) is a dopamine D1 receptor agonist with an EC50 of 72± 21 nM.
  • HY-111369
    CHK1-IN-2

    Checkpoint Kinase (Chk) Cancer
    CHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an IC50 of 6 nM.
  • HY-19837
    BMS-986120

    Protease-Activated Receptor (PAR) Inflammation/Immunology
    BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects.
  • HY-N0582
    Qingyangshengenin B

    Others Neurological Disease
    Qingyangshengenin B, a C-21 steroidal glycoside isolated from Qingyangshen. Qingyangshengenin B protects against Aβ toxicity, which decreases Aβ deposition by decreasing the expression of Aβ at the mRNA level. Qingyangshengenin B has antiepileptic activity.
  • HY-100026
    PQR620

    mTOR Cancer
    PQR620 is an orally bioavailable and selective brain penetrant inhibitor of mTORC1/2.
  • HY-100185
    SAR-100842

    LPL Receptor Inflammation/Immunology
    SAR-100842 is a lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor.
  • HY-15778
    AVE 0991

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC50 of 21 nM.
  • HY-10088
    Zibotentan

    ZD4054

    Endothelin Receptor Cancer Endocrinology
    Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).
  • HY-119759
    Lipoxamycin

    Fungal Infection
    Lipoxamycin is an antifungal antibiotic and a potent serine palmitoyltransferase inhibitor with an IC50 of 21 nM.
  • HY-P1271A
    Catestatin TFA

    nAChR Cardiovascular Disease
    Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
  • HY-112730
    PEO-IAA

    2-(1H-Indol-3-yl)-4-oxo-4-phenyl-butyric acid

    Others Others
    PEO-IAA is an indole-3-acetic acid (IAA) antagonist. PEO-IAA is an auxin antagonist that binds to transport inhibitor response 1/auxin signaling F-box proteins (TIR1/AFBs).
  • HY-114645
    PDK1-IN-RS2

    PDK-1 Cancer
    PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1.
  • HY-100489
    TBHQ

    tert-Butylhydroquinone

    Keap1-Nrf2 ERK Autophagy Apoptosis Ferroptosis Cancer
    TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2. TBHQ (tert-Butylhydroquinone) is also an ERK activator; rescues Dehydrocorydaline (DHC)-induced cell proliferation inhibitionin melanoma.
  • HY-10619
    Niraparib

    MK-4827

    PARP Apoptosis Cancer
    Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-10619A
    Niraparib hydrochloride

    MK-4827 hydrochloride

    PARP Apoptosis Cancer
    Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-136144
    FIDAS-5

    Wnt Cancer
    FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 has anticancer activities.
  • HY-15461A
    Ertugliflozin L-pyroglutamic acid

    PF-04971729 L-pyroglutamic acid

    SGLT Metabolic Disease
    Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2. Has the potential for the treatment of type 2 diabetes mellitus.
  • HY-119759A
    Lipoxamycin hemisulfate

    Fungal Infection
    Lipoxamycin hemisulfate is an antifungal antibiotic and a potent serine palmitoyltransferase inhibitor with an IC50 of 21 nM.
  • HY-P1545
    ACTH (1-17)

    α1-17-ACTH

    Melanocortin Receptor Cancer Neurological Disease Endocrinology
    ACTH (1-17), an adrenocorticotropin analogue, is a potent human melanocortin 1 (MC1) receptor agonist with a Ki of 0.21 nM.
  • HY-B0909
    Triflupromazine hydrochloride

    Dopamine Receptor Autophagy Neurological Disease
    Triflupromazine hydrochloride is an antipsychotic medication, which are Dopamine D1/D2 receptor antagonists.
  • HY-124798
    Rheb inhibitor NR1

    mTOR Cancer Inflammation/Immunology Neurological Disease
    Rheb inhibitor NR1 is a Rheb inhibitor with an IC50 of 2.1 µM in the Rheb-IVK assay. Rheb inhibitor NR1 also is a selective mTORC1 inhibitor. NR1 inhibits the phosphorylation of T389pS6K1 and increases the phosphorylation of S473pAKT in a dose-dependent manner.
  • HY-117474
    MJN110

    MAGL Neurological Disease
    MJN110 is an orally active and selective monoacylglycerol lipase (MAGL) inhibitor with IC50s of 9.1 nM and 2.1 nM for hMAGL and 2-arachidonoylglycerol (2-AG), respectively. MJN110 produces opioid-sparing effects and displays strong antihyperalgesic activity.
  • HY-120110
    IOX4

    HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology Neurological Disease
    IOX4 is a selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with an IC50 value of 1.6 nM, induces HIFα in cells and in wildtype mice with marked induction in the brain tissue. IOX4 competes with and displaces 2-oxoglutarate (2OG) at the active site of PHD2.
  • HY-15129
    O-Phospho-L-serine

    L-Serine O-phosphate; L-SOP

    mGluR Endogenous Metabolite Neurological Disease
    O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2.
  • HY-B0352A
    (S)-Mirtazapine

    (S)-Org3770; (S)-6-Azamianserin

    5-HT Receptor Neurological Disease
    (S)-Mirtazapine ((S)-Org3770) is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception. (S)-Mirtazapine is a stereoselective 5-HT2 receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2.
  • HY-10619B
    Niraparib tosylate

    MK-4827 tosylate

    PARP Apoptosis Cancer
    Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate (MK-4827 tosylate) leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-B0387
    Ibutilide fumarate

    U70226E

    Calcium Channel Cardiovascular Disease
    Ibutilide fumarate is a Class III antiarrhythmic agent that is indicated for acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm.
  • HY-13782
    Tenofovir Disoproxil Fumarate

    Tenofovir DF

    HIV Reverse Transcriptase HBV Infection
    Tenofovir Disoproxil Fumarate is a nucleotide reverse transcriptase inhibitor used to treat HIV and chronic Hepatitis B.
  • HY-127111
    NDI-091143

    ATP Citrate Lyase Cancer
    NDI-091143 is a potent and high-affinity human ATP-citrate lyase (ACLY) inhibitor with an IC50 of 2.1 nM (ADP-Glo assay), a Ki of 7.0 nM and a Kd of 2.2 nM. NDI-091143 inhibits ACLY catalysis allosterically, by stabilizing large conformational changes in the citrate domain that indirectly block the binding and recognition of citrate.
  • HY-13706
    CAY10471 Racemate

    TM30089 Racemate

    Prostaglandin Receptor Cancer Endocrinology
    CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist, with a Ki of 0.6 nM for hCRTH2, selective over human thromboxane A2 receptor TP (Ki, >10000 nM) or PGD2 receptor DP (Ki, 1200 nM). CAY10471 Racemate also has effect on mouse and rat orthologs of CRTH2.
  • HY-12201
    TAK-901

    Aurora Kinase Cancer
    TAK-901 is a multi-targeted aurora inhibitor with IC50s of 21 and 15 nM for aurora A and B, respectively.
  • HY-P1545A
    ACTH (1-17) (TFA)

    α1-17-ACTH TFA

    Melanocortin Receptor Cancer Neurological Disease Endocrinology
    ACTH (1-17) TFA, an adrenocorticotropin analogue, is a potent human melanocortin 1 (MC1) receptor agonist with a Ki of 0.21 nM.
  • HY-12216
    Resmetirom

    MGL-3196; VIA-3196

    Thyroid Hormone Receptor Cardiovascular Disease Endocrinology
    Resmetirom (MGL-3196) is a highly selective thyroid hormone receptor β (THR-β) agonist with an EC50 value of 0.21 μM.
  • HY-128703
    Bromodomain inhibitor-8

    Epigenetic Reader Domain Inflammation/Immunology
    Bromodomain inhibitor-8 (Intermediate 21) is a BET bromodomain inhibitor for treating autoimmune and inflammatory diseases.
  • HY-118284
    Vicagrel

    P2Y Receptor Cardiovascular Disease
    Vicagrel, an acetate derivative of Clopidogrel, is a P2Y12 platelet inhibitor potentially for the treatment of thrombosis, the substrate of carboxylesterase 2 (CES2). Vicagrel demonstrates a favorable safety profile and excellent anti-platelet activity, which could be an anti-platelet drug and for the unmet medical needs of cardiovascular diseases.
  • HY-114181
    IRAK4-IN-4

    IRAK Inflammation/Immunology
    IRAK4-IN-4 is an interleukin-1 receptor–associated kinase 4 (IRAK4) inhibitor extracted from patent CN107163044A, Compound15, has an IC50 of 2.8 nM. IRAK4-IN-4 also inhibits cyclic GMP-AMP synthase (cGAS) with an IC50 of 2.1 nM.
  • HY-N6837
    Fructo-​oligosaccharide DP7/GF6

    Others Others
    Fructo-oligosaccharide DP7/GF6 belongs to fructooligosaccharides (FOS) with degree of polymerization (DP=7). Fructo-oligosaccharides (FOS) are composed of 6 fructose units linked by (21)-β-glycosidic bonds and having a single D-glucosyl unit at the non-reducing end.
  • HY-101176
    2-Iodomelatonin

    Melatonin Receptor Cancer
    2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1  over MT2. 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues.
  • HY-13413
    Tofogliflozin (hydrate)

    CSG-452 hydrate

    SGLT Reactive Oxygen Species Metabolic Disease
    Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2 (SGLT2) inhibitor with an IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2. Tofogliflozin partially inhibits high glucose-induced reactive oxyen species (ROS) generation in tubular cells.
  • HY-111555
    AmPEG6C2-Aur0131

    Microtubule/Tubulin Drug-Linker Conjugates for ADC Cancer
    AmPEG6C2-Aur0131 is a drug-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0131 (an auristatin microtubule inhibitor), linked via the non-cleavable linker AmPEG6C2.
  • HY-N6834
    Fructo-​oligosaccharide DP10/GF9

    Others Others
    Fructo-oligosaccharide DP10/GF9 belongs to fructooligosaccharides (FOS) with degree of polymerization (DP=10). Fructo-oligosaccharides (FOS) are composed of 9 fructose units linked by (21)-β-glycosidic bonds and having a single D-glucosyl unit at the non-reducing end.
  • HY-108588
    NS5806

    Potassium Channel Cardiovascular Disease
    NS5806, a potent potassium current activator, increases KV4.3/KChIP2 peak current amplitudes with an EC50 of 5.3 μM. NS5806 slows KV4.3 and KV4.2 current dacay in channel complexes containing KChIP2.
  • HY-N7008
    Fructo-oligosaccharide DP11/GF10

    Others Metabolic Disease
    Fructo-oligosaccharide DP11/GF10 belongs to fructooligosaccharides (FOS) with degree of polymerization (DP=11). Fructo-oligosaccharides (FOS) are composed of 10 fructose units linked by (21)-β-glycosidic bonds and having a single D-glucosyl unit at the non-reducing end.
  • HY-N6836
    Fructo-oligosaccharide DP8/GF7

    Others Others
    Fructo-oligosaccharide DP8/GF7 belongs to fructooligosaccharides (FOS) with degree of polymerization (DP=8). Fructo-oligosaccharides (FOS) are composed of 7 fructose units linked by (21)-β-glycosidic bonds and having a single D-glucosyl unit at the non-reducing end.
  • HY-N6835
    Fructo-oligosaccharide DP9/GF8

    Others Others
    Fructo-oligosaccharide DP9/GF8 belongs to fructooligosaccharides (FOS) with degree of polymerization (DP=9). Fructo-oligosaccharides (FOS) are composed of 8 fructose units linked by (21)-β-glycosidic bonds and having a single D-glucosyl unit at the non-reducing end.
  • HY-N7009
    Fructo-oligosaccharide DP12/GF11

    Others Metabolic Disease
    Fructo-oligosaccharide DP12/GF11 belongs to fructooligosaccharides (FOS) with degree of polymerization (DP=12). Fructo-oligosaccharides (FOS) are composed of 11 fructose units linked by (21)-β-glycosidic bonds and having a single D-glucosyl unit at the non-reducing end.
  • HY-107453
    SirReal1-O-propargyl

    PROTAC Sirt2-binding moiety 1

    Ligand for Target Protein for PROTAC Cancer
    SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC50 of 2.4 μM. SirReal1-O-propargyl, the SirReal1-based moiety, binds to the cereblon ligand via a linker to form PROTAC to degrade Sirt2.
  • HY-P1858
    Urocortin III, mouse

    CRFR Neurological Disease Cardiovascular Disease Endocrinology
    Urocortin III, mouse is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2. Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics.
  • HY-108235
    Lanicemine

    AZD6765

    iGluR Neurological Disease
    Lanicemine (AZD6765) is a low-trapping NMDA channel blocker with a binding (Ki) of 0.56-2.1 μM.
  • HY-102054
    Acetylhydrolase-IN-1

    FAAH Cardiovascular Disease
    Acetylhydrolase-IN-1 is a 1-Alkyl-2-acetylglycerophosphocholine esterase (Alkylacetyl-GPC: acetylhydrolase) inhibtor.
  • HY-A0163
    Zuclopenthixol

    (Z)-Clopenthixol

    Dopamine Receptor Neurological Disease
    Zuclopenthixol is a thioxanthene derivative which acts as a mixed dopamine D1/D2 receptor antagonist.
  • HY-19366
    Nav1.7-IN-2

    Sodium Channel Neurological Disease
    Nav1.7-IN-2 is an inhibitor of voltage-gated sodium channels (Nav), in particular Nav 1.7, with IC50 of 80 nM.
  • HY-40354
    Tofacitinib

    Tasocitinib; CP-690550

    JAK Apoptosis Inflammation/Immunology Cancer
    Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
  • HY-112457
    MK-2 Inhibitor III

    MAPKAPK2 (MK2) Inflammation/Immunology
    MK-2 Inhibitor III (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 0.85 nM, and is exceptional selectivity against MK-3 (IC50=0.21 μM), MK-5 (IC50=0.081 μM), ERK2 (IC50=3.44 μM), MNK1(IC50=5.7 μM) as well as CDK2, JNK2, IKK2, MSK1, and MSK2.
  • HY-126245
    Keap1–Nrf2-IN-1

    Keap1-Nrf2 Metabolic Disease Inflammation/Immunology
    Keap1–Nrf2 IN-1 (compound35) is a Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2 (Keap1-Nrf2) protein-protein interaction inhibitor, and with an IC50 of 43 nM for Keap1 protein. Keap1–Nrf2 IN-1 (compound35) activates Nrf2-regulated cytoprotective response and antagonizes acetaminophen-induced liver injury both in cellular and in vivo models.
  • HY-123844
    dBET57

    PROTAC Epigenetic Reader Domain Cancer
    dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology. dBET57 mediates recruitment to the CRL4 CRBN E3 ubiquitin ligase, with a DC50/5h of 500 nM for BRD4BD1, and is inactive on BRD4BD2.
  • HY-114169
    WRG-28

    Discoidin Domain Receptor Cancer
    WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor with an IC50 of 230 nM. WRG-28 uniquely inhibits receptor-ligand interactions via allosteric modulation of the receptor. WRG-28 inhibits tumor invasion and migration, as well as tumor-supporting roles of the stroma, and inhibits metastatic breast tumor cell colonization in the lungs by targeting DDR2.
  • HY-78131AS
    (S)-(+)-Ibuprofen D3

    (S)-Ibuprofen D3

    COX Inflammation/Immunology
    (S)-(+)-Ibuprofen D3 ((S)-Ibuprofen D3) is a deuterium labeled (S)-(+)-Ibuprofen. (S)-(+)-Ibuprofen is the S(+)-enantiomer of Ibuprofen that inhibits COX-1 and COX-2 activity with IC50s of 2.1 μM and 1.6 μM. (S)-(+)-Ibuprofen has analgesic, antiinflammatory and antipyretic effects.
  • HY-112801
    F-1

    ALK ROS Cancer
    F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALK WT, ROS1 WT, ALK L1196M and ALK G1202R, respectively.
  • HY-117684A
    DDD107498 succinate

    DDD-498 succinate

    Parasite CaMK Autophagy Infection
    DDD107498 succinate (DDD-498 succinate) is a potent and orally active antimalarial agent, inhibits multiple life-cycle stages of the parasite, with an EC50 of 1 nM against P. falciparum 3D7. DDD107498 succinate inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC50 of 2 nM for WT-PfeEF2.
  • HY-P1858A
    Urocortin III, mouse TFA

    CRFR Neurological Disease Cardiovascular Disease Endocrinology
    Urocortin III, mouse TFA is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2. Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics.
  • HY-111422
    PLX51107

    Epigenetic Reader Domain Cancer
    PLX51107 is a potent and selective BET inhibitor, with Kds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range).
  • HY-14523
    LY 254155

    Antifolate Cancer
    LY 254155, an antifolate, inhibits hGARFT and binds to mFBP with Kis of 2.1±0.2 and 1.7±0.1 nM, respectively.
  • HY-12058
    AZD8330

    ARRY-424704; ARRY-704

    MEK Cancer
    AZD8330 (ARRY-424704) is a potent, uncompetitive MEK1/MEK2 inhibitor, with an IC50 of 7 nM.
  • HY-15869
    Inauhzin

    INZ

    Sirtuin MDM-2/p53 Cancer
    Inauhzin is a dual SirT1/IMPDH2 inhibitor, and acts as an activator p53, used in the research of cancer.
  • HY-100747
    PSB-12379

    CD73 Cancer
    PSB-12379 is a potent Ecto-5'-Nucleotidase (CD73) inhibitor with Kis of 9.03 nM (rat) and 2.21 nM (human).
  • HY-15434
    NG25

    MAP4K MAP3K Cancer Inflammation/Immunology
    NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.
  • HY-114926
    KT185

    MAGL Neurological Disease
    KT185 is an orally-bioavailable, brain-penetrant and selective ABHD6 inhibitor, with an IC50 0.21 nM in Neuro2A cells.
  • HY-135570
    DHODH-IN-2

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Influenza Virus Infection
    DHODH-IN-2 (compound 21d) is a human dihydroorotate dehydrogenase (HsDHODH) inhibitor, inhibits measles virus replication with a pMIC50 value of 8.6.
  • HY-100462
    PTP1B-IN-2

    Phosphatase Metabolic Disease
    PTP1B-IN-2 is a potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 50 nM.
  • HY-121744
    PS10

    PDHK Inflammation/Immunology
    PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM). PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy.PDK: pyruvate dehydrogenase kinase
  • HY-100005A
    Fumarate hydratase-IN-2 sodium salt

    Mitochondrial Metabolism Cancer
    Fumarate hydratase-IN-2 sodium salt (compound 3) is a cell-permeable and competitive fumarate hydratase inhibitor (Ki=4.5 μM) with nutrient-dependent cytotoxicity .
  • HY-120348
    ML67-33

    Potassium Channel Neurological Disease Cardiovascular Disease
    ML67-33 is a selective activator of temperature- and mechano-sensitive K2P channels. ML67-33 rapidly and reversibly affects K2P2.1 (TREK-1) with EC50s of 36.3 μM and 9.7 μM in cell-free and HEK293 cells, respectively.
  • HY-B0352AS
    (S)-Mirtazapine D3

    (S)-Org3770 D3; (S)-6-Azamianserin D3

    5-HT Receptor Neurological Disease
    (S)-Mirtazapine D3 ((S)-Org3770 D3) is a deuterium labeled (S)-Mirtazapine. (S)-Mirtazapine is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception.(S)-Mirtazapine is a stereoselective 5-HT2 receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2.
  • HY-N0919
    Yangonin

    Cannabinoid Receptor NF-κB Autophagy Inflammation/Immunology
    Yangonin exhibits affinity for the human recombinant cannabinoid CB1 receptor with an IC50 and a Ki of 1.79 ± 0.53 μM and 0.72±0.21 μM, respectively.
  • HY-W020215
    Tricarballylic acid

    Mitochondrial Metabolism Inflammation/Immunology
    Tricarballylic acid, a conjugate acid of a tricarballylate, is a competitive inhibitor of the enzyme aconitate hydratase (aconitase; EC 4.2.1.3) with a Ki value of 0.52 mM.
  • HY-14719
    RO4987655

    CH4987655

    MEK Cancer
    RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM for inhibition of MEK1/MEK2.
  • HY-N2102
    Tenacissoside I

    Others Cancer
    Tenacissoside I is a C21 steroid from the Marsdenia tenacissima, which is detected at relatively high level in M. tenacissima.
  • HY-14218
    Ditolylguanidine

    1,3-Di-o-tolylguanidine; DTG

    Sigma Receptor Neurological Disease
    Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor).
  • HY-16504
    Treprostinil sodium

    UT-15

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Treprostinil sodium is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
  • HY-111655
    SKA-31

    Potassium Channel Cardiovascular Disease
    SKA-31 is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. SKA-31 potentiates endothelium-derived hyperpolarizing factor response and lowers blood pressure.
  • HY-100972
    ARV-771

    PROTAC Epigenetic Reader Domain Cancer
    ARV-771 is a potent BET degrader based on PROTAC technology with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.
  • HY-108938
    SDZ285428

    Cytochrome P450 Fungal Parasite Infection
    SDZ285428 is a CYP51 inhibitor. SDZ285428 inhibits Trypanosoma cruzi (TC) CYP51 with I/E2 <1 (5 min) and I/E2=9 (1 h). SDZ285428 inhibits Trypanosoma brucei (TB) CYP51 with I/E2 <1 (5 min) and I/E2=35 (1 h).
  • HY-15098
    Apoptozole

    Apoptosis Activator VII

    HSP Apoptosis Cancer
    Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with Kds of 0.21 and 0.14 μM, respectively, and can induce apoptosis.
  • HY-13419
    U-73122

    Phospholipase Lipoxygenase Ferroptosis Inflammation/Immunology
    U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50of 1-2.1 µM for PLC.
  • HY-133080
    BAY-784

    GNRH Receptor Cancer
    BAY-784 is a gonadotropin releasing hormone receptor (GnRH-R) antagonist probe with IC50s of 21 and 24 nM for human and rat GnRH-R, respectively.
  • HY-112444
    BACE1-IN-2

    Beta-secretase Neurological Disease
    BACE1-IN-2 is a 1,4-Oxazine β-Secretase 1 (BACE1) inhibitor with an IC50 of 22 nM.
  • HY-128585
    GNE684

    RIP kinase Cancer Inflammation/Immunology
    GNE684 is a potent inhibitor of potent receptor interacting protein 1 (RIP1), with mean Ki app values of 21 nM, 189 nM and 691 nM for human mouse and rat RIP1, respectively.
  • HY-N2990
    16α-Hydroxydehydrotrametenolic acid

    3β,16α-Dihydroxylanosta-7,9(11),24-trien-21-oic acid

    Others Inflammation/Immunology
    16α-Hydroxydehydrotrametenolic acid is a triterpene Acid in fermented mycelia of edible fungus Poria cocos.
  • HY-108596
    BL-1249

    Potassium Channel Inflammation/Immunology
    BL-1249 is a nonsteroidal anti-inflammatory drug (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM).
  • HY-N6696
    Aflatoxin B2

    Bacterial Antibiotic Cancer Infection
    Aflatoxin B2 is a major naturally produced aflatoxin. Aflatoxin B2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
  • HY-N6698
    Aflatoxin G2

    Bacterial Antibiotic Cancer Infection
    Aflatoxin G2 is a major naturally produced aflatoxin. Aflatoxin G2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
  • HY-107417
    Hypothemycin

    VEGFR MEK FLT3 PDGFR ERK Cancer
    Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively.
  • HY-U00444
    DDR1-IN-2

    Discoidin Domain Receptor Inflammation/Immunology
    DDR1-IN-2 is a potent inhibitor of discoidin domain receptor 1 (DDR1), with an IC50 of 13.1 nM, and also less potently inhibits DDR2, with an IC50 of 203 nM.
  • HY-16660
    INH1

    IBT13131

    Others Cancer
    INH1 is a small molecule targeting the Hec1/Nek2 mitotic pathway suppresses tumor cell growth in culture and in animal.
  • HY-140886
    1,1,1-Trifluoroethyl-PEG2-propargyl

    PROTAC Linker Cancer
    1,1,1-Trifluoroethyl-PEG2-propargyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-10535
    Evofosfamide

    TH-302

    Apoptosis Cancer
    Evofosfamide (TH-302) is a hypoxia-activated prodrug with IC50 of 10 μM and 1000 μM in hypoxia (N2) and normoxia (21% O2), respectively.
  • HY-108522
    PA452

    RAR/RXR Metabolic Disease
    PA452, retinoic X receptor (RXR) specific antagonist, inhibits the effect of Retinoic acid (RA) on Th1/Th2 development.
  • HY-140845
    1,1,1-Trifluoroethyl-PEG2-azide

    PROTAC Linker Cancer
    1,1,1-Trifluoroethyl-PEG2-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-100747A
    PSB-12379 disodium

    CD73 Cancer
    PSB-12379 disodium is a potent Ecto-5'-Nucleotidase (CD73) inhibitor with Kis of 9.03 nM (rat) and 2.21 nM (human).
  • HY-15431
    Capivasertib

    AZD5363

    Akt Autophagy Cancer
    Capivasertib (AZD5363) is a potent pan-AKT kinase inhibitor with IC50 of 3, 7 and 7 nM for Akt1,Akt2 and Akt3, respectively.
  • HY-100791
    NSC23005 sodium

    Others Cancer
    NSC23005 sodium is a novel and effective p18 inhibitor (ED50=5.21 nM) in promoting Hematopoietic stem cells (HSCs) expansion in both murine and human models.
  • HY-111390
    Dot1L-IN-2

    Histone Methyltransferase Cancer
    Dot1L-IN-2 is a potent, selective and orally bioavailable inhibitor of Dot1L (a histone methyltransferase), with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively.
  • HY-18106
    BM 957

    Bcl-2 Family Cancer
    BM 957 is a potent Bcl-2 and Bcl-xL inhibitor, with Kis of 1.2, <1 nM and IC50s of 5.4, 6.0 nM respectively.
  • HY-N6700
    Aflatoxin M2

    Others Cancer
    Aflatoxin M2 is a major metabolite of Aflatoxin B1. Aflatoxin M2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
  • HY-101265
    S1p receptor agonist 1

    LPL Receptor Inflammation/Immunology
    S1p receptor agonist 1 is a potent and orally active S1P receptor agonist, exhibits an activity of inducing S1P1 internalization (EC50=9.83 nM). S1p receptor agonist 1 has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). S1p receptor agonist 1 is extracted from patent WO2015039587A1, Compound 2.
  • HY-135366
    HPN-01

    IKK Inflammation/Immunology
    HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2.
  • HY-133143
    1,2-Bis(2-iodoethoxy)ethane

    PROTAC Linker Cancer
    1,2-Bis(2-iodoethoxy)ethane is a PEG-based PROTAC linker. 1,2-Bis(2-iodoethoxy)ethane can be used in the synthesis of MT802 (HY-122562) and SJF620 (HY-133137). MT-802 and SJF620 are potent PROTAC BTK degraders with DC50s of 1 nM and 7.9 nM, respectively.
  • HY-N6699
    Aflatoxin M1

    Bacterial Cancer Infection
    Aflatoxin M1 is a major metabolite of Aflatoxin B1. Aflatoxin M1 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
  • HY-10013B
    Taranabant ((1R,2R)stereoisomer)

    MK0364 (1R,2R)stereoisomer

    Cannabinoid Receptor Others
    Taranabant (1R,2R)stereoisomer is the R-enantiomer of Taranabant. Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist.
  • HY-100441
    Treprostinil

    LRX-15

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Treprostinil (LRX-15) is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
  • HY-15315A
    Baricitinib phosphate

    LY3009104 phosphate; INCB028050 phosphate

    JAK Inflammation/Immunology
    Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) is a selective orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.
  • HY-13560
    AVN-944

    VX-944

    Others Cancer
    AVN-944(VX-944) is a selective, noncompetitive inhibitor of the enzyme directed against human IMPDH with Ki of 6-10 nM for IMPDH1/IMPDH2.
  • HY-18717
    Mutant IDH1-IN-2

    Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-2 is a inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with IC50 of in LS-MS biochemical assay, IC50 of 16.6 nM in Fluorescence biochemical assay.
  • HY-104049
    Lanifibranor

    IVA337

    PPAR Metabolic Disease Cancer
    Lanifibranor is a pan peroxisome proliferator-activated receptor (PPAR) agonist with EC50s of 1.5, 0.87 and 0.21 μM for human PPARα, PPARσ and PPARγ, respectively.
  • HY-10215
    Luminespib

    NVP-AUY922; VER-52296

    HSP Autophagy Apoptosis Cancer
    Luminespib (NVP-AUY922) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively.
  • HY-103384
    TMCB

    Casein Kinase Cancer
    TMCB is a selective, ATP-competitive CK2 (casein kinase II) inhibitor with distinct Ki values of 83 nM and 21 nM for the two different catalytic CK2 subunits α and α', respectively.
  • HY-17363S
    Dimethyl fumarate D6

    DMF D6

    Keap1-Nrf2 Inflammation/Immunology
    Dimethyl fumarate D6 is a deuterium labeled Dimethyl fumarate. Dimethyl fumarate is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator and induces upregulation of antioxidant gene expression.
  • HY-N6805
    Isoeugenol acetate

    AChE Cancer Inflammation/Immunology
    Isoeugenol acetate, an essential oil constituent of nutmeg, clove, and cinnamon, shows excellent inhibitory effects against some metabolic enzymes such as acetylcholinesterase (AChE) enzymes (IC50=77 nM; Ki=16 nM), α-glycosidase (IC50=19.25 nM; Ki=21 nM), and α-amylase (IC50=411.5 nM). Isoeugenol acetate is used medical and cosmetics industries for its antioxidant, anticancer, antimicrobial and anti-inflammatory properties.
  • HY-W018781
    Benzamidine hydrochloride

    Ser/Thr Protease Cancer
    Benzamidine hydrochloride is an reversible competitive inhibitor of trypsin-like serine proteases, with Kis of 97 µM, 21 µM, 20 µM and 110 µM for uPA, trypsin, tryptase and factor Xa, respectively.
  • HY-135893
    SGK1-IN-2

    SGK Inflammation/Immunology
    SGK1-IN-2 (14h) is a selective SGK1 (serum and glucocorticoid regulated kinase 1) inhibitor, with an IC50 of 5 nM at 10 μM ATP concentration.
  • HY-P1180
    Pam3CSK4

    Pam3Cys-Ser-(Lys)4

    Toll-like Receptor (TLR) Infection Inflammation/Immunology
    Pam3CSK4 is a toll-like receptor 1/2 (TLR1/2) agonist with an EC50 of 0.47 ng/mL for human TLR1/2.
  • HY-18603
    FIIN-3

    EGFR FGFR Cancer
    FIIN-3 is an irreversible inhibitor of FGFR with an IC50 of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
  • HY-100529
    PD150606

    Proteasome Cancer
    PD 150606 is a selective, cell-permeable non-peptide calpain inhibitor with Ki values of 0.21 μM and 0.37 μM for μ- and m-calpains respectively, which is neuroprotective.
  • HY-129700
    MCL-1/BCL-2-IN-2

    Bcl-2 Family Cancer
    MCL-1/BCL-2-IN-2 (Compound 6) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor.
  • HY-101544
    ARQ 069

    FGFR Cancer
    ARQ 069, an analog of ARQ 523, inhibits FGFR in an enantiospecific manner. ARQ 069 targets the unphosphorylated, inactive forms of FGFR1/FGFR2 kinases (IC50s of 0.84 μM and 1.23 μM, respectively). ARQ 069 inhibits FGFR1/FGFR2 autophosphorylation (IC50s of 2.8 and 1.9 μM, respectively) through a mechanism in a non-ATP competitive dependent manner.
  • HY-135887
    ZX-29

    ALK Apoptosis Autophagy Cancer
    ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect.
  • HY-P1180A
    Pam3CSK4 TFA

    Pam3Cys-Ser-(Lys)4 TFA

    Toll-like Receptor (TLR) Infection Inflammation/Immunology
    Pam3CSK4 TFA is a toll-like receptor 1/2 (TLR1/2) agonist with an EC50 of 0.47 ng/mL for human TLR1/2.
  • HY-111940
    LUT014

    Raf Inflammation/Immunology
    LUT014 is a B-Raf inhibitor with an IC50 of 11.7 nM, and developed to reduce dose-limiting acneiform lesions associated EGFR Inhibitors treatment. Extracted from patent WO 2019026065A2 [1].
  • HY-13809
    BMS-833923

    XL-139

    Smo Apoptosis Cancer
    BMS-833923 (XL-139) is an orally bioavailable small-molecule inhibitor of Smoothened with potential antineoplastic activity; inhibits BODIPY cyclopamine binding to SMO in a dose-dependent manner with an IC50 of 21 nM.
  • HY-N1375
    Qingyangshengenin

    Others Cancer
    Qingyanshengenin (NSC 379666; compound 2), a pregnane glycoside, is a C21 steroidal aglycone isolated from the root of Cynanchumot ophyllum (Asclepiadaceae). Qingyanshengenin has anti-cancer activity.
  • HY-N6066
    Praeruptorin E

    Calcium Channel Cardiovascular Disease
    Praeruptorin E is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin C is a calcium antagonist with pD2 value of 5.2.
  • HY-13266A
    BS-181 hydrochloride

    CDK Cancer
    BS-181 hydrochloride is a highly selective CDK7 inhibitor with IC50 of 21 nM, and > 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
  • HY-N0417
    Cucurbitacin E

    α-Elaterin; α-Elaterine

    CDK Autophagy Cancer
    Cucurbitacin E is a natural compound which from the climbing stem of Cucumic melo L. Cucurbitacin E significantly suppresses the activity of the cyclin B1/CDC2 complex.
  • HY-12593
    GS967

    Sodium Channel Cardiovascular Disease
    GS967 (GS-458967) is a potent, and selective inhibitor of cardiac late sodium current (late INa ) with IC50 values of 0.13 and 0.21 μM for ventricular myocytes and isolated hearts, respectively.
  • HY-10167A
    Tecalcet Hydrochloride

    R-568 (hydrochloride)

    CaSR Others
    Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca 2+.
  • HY-N1713
    29-Nor-20-oxolupeol

    Others Neurological Disease
    29-Nor-20-oxolupeol, extracted from Impatiens basamina, reduces NO levels in LPS-activated murine microglial cells with an IC50 of 44.21 µM.
  • HY-108337
    GNE 0723

    iGluR Neurological Disease
    GNE 0723 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM for GluN2C and GluN2D, respectively.
  • HY-16962A
    CC-115 hydrochloride

    DNA-PK mTOR Cancer
    CC-115 hydrochloride is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
  • HY-16962
    CC-115

    DNA-PK mTOR Cancer
    CC-115 is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
  • HY-18976
    UF010

    HDAC Cancer
    UF010 is a potent and selective HDAC inhibitor with IC50 ~0.06 μM, 0.1 μM, 0.5 μM and 1.5 μM for HDACs 3, 2, 1 and 8, respectively.
  • HY-108704
    CT-721

    Bcr-Abl Cancer
    CT-721 is a potent and time-dependent Bcr-Abl kinase inhibitor with an IC50 of 21.3 nM for wild-type Bcr-Abl kinase, and possesses anti-chronic myeloid leukemia (CML) activities.
  • HY-N0590
    Corynoxeine

    ERK Cardiovascular Disease
    Corynoxeine, isolated from the hook of Uncaria rhynchophylla, is a potent ERK1/ERK2 inhibitor of key PDGF-BB-induced vascular smooth muscle cells (VSMCs) proliferation.
  • HY-101193
    Zinc Protoporphyrin

    Zn(II)-protoporphyrin IX; ZnPP; Zinc Protoporphyrin-9

    Reactive Oxygen Species Endogenous Metabolite Apoptosis Cancer Metabolic Disease Cardiovascular Disease
    Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is an orally active and competitive heme oxygenase-1 (HO-1) inhibitor and markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2. Zinc Protoporphyrin is used as a screening marker of iron deficiency in individual pregnant women and children, but also to assess population iron status in combination with haemoglobin concentration. Zinc Protoporphyrin has anti-cancer activity.
  • HY-131061
    BET bromodomain inhibitor 1

    Epigenetic Reader Domain Cancer
    BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity.
  • HY-N0632
    Esculentoside A

    COX NF-κB Inflammation/Immunology
    Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta. Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models, has selective inhibitory activity towards cyclooxygenase-2 (COX-2). Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways.
  • HY-P0289
    CEF3

    Influenza Virus Infection
    CEF3 (SIIPSGPLK) corresponds to aa 13-21 of the influenza A virus M1 protein. The matrix (M1) protein of influenza A virus is a multifunctional protein that plays essential structural and functional roles in the virus life cycle.
  • HY-13994
    Mps1-IN-2

    Mps1 Polo-like Kinase (PLK) Cancer
    Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC50 and a Kd of 145 nM and 12 nM for Mps1 and a Kd of 61 nM for Plk1.
  • HY-N2103
    Tenacissoside G

    Others Cancer
    Tenacissoside G is a C21 steroid from the stems of Marsdenia tenacissima. Tenacissoside G reverses multidrug resistance in P-glycoprotein (Pgp)-overexpressing multidrug-resistant cancer cells.
  • HY-12790
    CB1-IN-1

    BPRCB1184

    Cannabinoid Receptor Neurological Disease
    CB1-IN-1 (BPRCB1184) is a peripherally restricted CB1R antagonist, with Ki of 0.3 nM and 21 nM for CB1R (EC50 = 3 nM) and CB2R, respectively.
  • HY-10977
    Tivozanib

    AV-951; KRN951

    VEGFR Cancer
    Tivozanib (AV-951; KRN951) is a highly potent and selective VEGFR 1/2/3 inhibitor with IC50s of 0.21, 0.16, and 0.24 nM in cell assay, respectively.
  • HY-10963
    Momelotinib Mesylate

    CYT387 (Mesylate)

    JAK Autophagy Cancer
    Momelotinib Mesylate (CYT387 Mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.
  • HY-100018
    BAY1125976

    Akt Cancer
    BAY1125976 is a selective allosteric Akt1/Akt2 inhibitor; inhibits Akt1 and Akt2 activity with IC50 values of 5.2 nM and 18 nM at 10 μM ATP, respectively.
  • HY-100375
    Diroximel fumarate

    ALKS 8700; BIIB098

    Others Others
    Diroximel fumarate (ALKS 8700) is an orally-active and well-tolerated monomethyl fumarate (MMF) prodrug in a controlled-release formulation. Diroximel fumarate is considered as active equivalent to its active metabolite dimethyl fumarate (DMF). Diroximel fumarate has a favorable safety and efficacy profile, has the potential for the study of multiple sclerosis (MS).
  • HY-N4225
    Aaptamine

    Adrenergic Receptor Cancer Endocrinology
    Aaptamine, a spongean alkaloid isolated from a sea sponge Aaptos aaptos, is a competitive antagonist of α-adrenoceptor and activates the p21 promoter in a p53-independent manner.
  • HY-11079
    A-803467

    Sodium Channel Neurological Disease
    A 803467 is a selective Nav1.8 sodium channel blocker with an IC50 of 8 nM; over 100-fold more selective vs. human Nav1.2, 1.3, 1.5 and 1.7.
  • HY-B0190A
    Nafamostat mesylate

    FUT-175

    Ser/Thr Protease Apoptosis SARS-CoV Cardiovascular Disease Cancer
    Nafamostat mesylate, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat mesylate supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat mesylate blocks activation of SARS-CoV-2..
  • HY-B0190
    Nafamostat

    Ser/Thr Protease Apoptosis SARS-CoV Cardiovascular Disease
    Nafamostat, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat blocks activation of SARS-CoV-2.
  • HY-14691
    Refametinib

    BAY 869766; RDEA119

    MEK Cancer
    Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.
  • HY-B0190B
    Nafamostat hydrochloride

    Ser/Thr Protease Apoptosis SARS-CoV Cardiovascular Disease
    Nafamostat hydrochloride, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat hydrochloride supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat hydrochloride blocks activation of SARS-CoV-2..
  • HY-P1540
    Angiotensin III, human, mouse

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    Angiotensin III, human, mouse is a heptapeptide, acts as an endogenous angiotensin type 2 receptor (AT2R) agonist, with IC50s of 0.648 nM and 21.1 nM for AT2R and AT1R, respectively.
  • HY-12755
    ML141

    CID-2950007

    Ras Apoptosis Cancer
    ML141 (CID-2950007) is a potent, allosteric,selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines.
  • HY-17542
    PLpro inhibitor

    SARS-CoV Infection
    PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with an IC50 of 2.6 µM. PLpro inhibitor inhibits SARS-CoV-2 PLpro with an IC50 of 5.0 µM and an EC50 of 21.0 µM.
  • HY-101140A
    KI696 isomer

    Keap1-Nrf2 Metabolic Disease Inflammation/Immunology
    KI696 isomer is the less active isomer of KI696 (HY-101140). KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction.
  • HY-110346
    AZD5582 dihydrochloride

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

    IAP Apoptosis Cancer
    AZD5582 is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.
  • HY-12594
    Paritaprevir

    ABT-450; Veruprevir

    HCV Protease HCV Infection
    Paritaprevir (ABT-450) is a potent non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively.
  • HY-10961
    Momelotinib

    CYT387

    JAK Autophagy Apoptosis Cancer
    Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.
  • HY-133554
    ASK1-IN-1

    p38 MAPK Inflammation/Immunology
    ASK1-IN-1 is a CNS-penetrant ASK1 (apoptosis signal-regulating kinase 1) inhibitor, with good potency (cell IC50=138 nM; Biochemical IC50=21 nM).
  • HY-111746
    CWHM-1008

    Parasite Infection
    CWHM-1008 is a potent and orally active antimalarial agent, with EC50 values of 46 and 21 nM against drug-sensitive Plasmodium falciparum 3D7 and drug-resistant Dd2 strains, respectively.
  • HY-100013A1
    (1R,2R)-2-PCCA(hydrochloride)

    Others Neurological Disease
    (1R,2R)-2-PCCA hydrochloride is a diastereomer of 2-PCCA, and acts as a potent GPR88 receptor agonist, with an EC50 of 3 nM in cell-free assay, and 603 nM in cell assay.
  • HY-119412
    Biliatresone

    Others Metabolic Disease
    Biliatresone is a natural toxin isolated from Dysphania glomulifera and D. littoralis. Biliatresone, a 1,2-diaryl-2-propenone class of isoflavonoid, produces extrahepatic biliary atresia in a zebrafish model.
  • HY-118607
    VU041

    Potassium Channel Infection
    VU041 is a first submicromolar-affinity inhibitor of Anopheles (An.) gambiae and Aedes (Ae.) aegypti inward rectifier potassium 1 (Kir1) channels with IC50 values of 2.5 μM and 1.7 μM, respectively. VU041 inhibits appreciably is mammalian Kir2.1 (IC50 of 12.7 μM), and has less inhibitory effect on mammalian Kir1.1, Kir4.1, Kir6.2/SUR1, and Kir7.1. VU041 also induces impaired Malpighian tubule function.
  • HY-125843
    Pomalidomide-PEG1-C2-N3

    Cereblon Ligand-Linker Conjugates 13; E3 ligase Ligand-Linker Conjugates 50

    E3 Ligase Ligand-Linker Conjugate Cancer
    Pomalidomide-PEG1-C2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 1-unit PEG linker used in PROTAC technology. Pomalidomide-PEG1-C2-N3 can be used to design a selective CDK6 PROTAC degrader CP-10. CP-10 induces the degradation of CDK6 with an DC50 of 2.1 nM.
  • HY-111787
    CSF1R-IN-2

    Src c-Met/HGFR c-Fms Cancer
    CSF1R-IN-2 (compound 5) is an oral-active inhibitor of SRC, MET and c-FMS, with IC50 values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively.
  • HY-B1190A
    Cefadroxil hydrate

    BL-S 578 hydrate

    Bacterial Antibiotic Infection
    Cefadroxil hydrate (BL-S 578 hydrate) is an orally active and first-generation cephalosporin with a broad spectrum antibacterial activity. Cefadroxil hydrate (BL-S 578 hydrate) also acts as a substrate of the peptide transporter PEPT1 and PEPT2.
  • HY-103504
    (S)-SNAP5114

    GABA Receptor Neurological Disease
    (S)-SNAP5114 is a selective GABA transport inhibitor, with IC50 values of 5 μM and 21 μM for hGAT-3 and rGAT-2, respectively. (S)-SNAP5114 is an anticonvulsant drug.
  • 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-12274
    ML347

    LDN 193719

    TGF-β Receptor Cancer
    ML347(DN193719) is a highly selective ALK1/ALK2 inhibitor with IC50s of 46/32 nM; shows >300-fold selectivity for ALK2 vs.
  • HY-B0725
    Doxepin Hydrochloride

    Histamine Receptor Cytochrome P450 Neurological Disease
    Doxepin hydrochloride is an orally active tricyclic antidepressant used as a sedative. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2.
  • HY-10962
    Momelotinib sulfate

    CYT387 sulfate salt

    JAK Autophagy Apoptosis Cancer
    Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).
  • HY-100607A
    Landiolol hydrochloride

    ONO1101 hydrochloride

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Landiolol hydrochloride (ONO1101 hydrochloride) is a highly beta1 selective ultra-short acting beta-blocker (β1/β2 selectivity = 255:1, a half-life of 4 min), acts as an adrenoceptor antagonist.
  • HY-112051
    CU-CPT9b

    Toll-like Receptor (TLR) Inflammation/Immunology
    CU-CPT9b is a specific TLR8 antagonist, with an IC50 of 0.7 nM. CU-CPT9b shows high binding affinity towards TLR8 with a Kd of 21 nM.
  • HY-12518
    OF-1

    Epigenetic Reader Domain Cancer
    OF-1 is a selective BRPF1B and BRPF2 bromodomain inhibitor with Kd values of 100 nM/500 nM for BRPF1B/BRPF2; 39-fold selectivity over BRD4.
  • HY-15510B
    Tenovin-6 Hydrochloride

    Sirtuin MDM-2/p53 Autophagy Cancer
    Tenovin-6 Hydrochloride is an inhibitor of SIRT1 and SIRT2, slightly inhibits HDAC8, and is also a potent activator of p53, with IC50s of 21 μM, 10 μM, and 67 μM for SirT1, SirT2, and SirT3, respectively.
  • HY-112292
    GW806742X

    Mixed Lineage Kinase VEGFR Others
    GW806742X is a Mixed Lineage Kinase Domain-Like protein (MLKL) inhibitor which binds the MLKL pseudokinase domain with a Kd value of 9.3 μM and has anti-necroptosis activity. GW806742X has activity against VEGFR2.
  • HY-111055
    BIP-135

    GSK-3 Neurological Disease
    BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuroprotective effect.
  • HY-15510
    Tenovin-6

    Sirtuin MDM-2/p53 Autophagy Cancer
    Tenovin-6 is an inhibitor of SIRT1 and SIRT2, slightly inhibits HDAC8, and is also a potent activator of p53, with IC50s of 21 μM, 10 μM, and 67 μM for SirT1, SirT2, and SirT3, respectively.
  • HY-13030
    (+)-JQ-1

    JQ1

    Epigenetic Reader Domain Autophagy Ligand for Target Protein for PROTAC Cancer
    (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy.
  • HY-12498
    GV-58

    Calcium Channel Neurological Disease
    GV-58 is a potent, selective N- and P/Q-type Ca2+ channels agonist with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel; 20-fold less potent CDK inhibitor activity.
  • HY-129681
    MCL-1/BCL-2-IN-1

    Bcl-2 Family Cancer
    MCL-1/BCL-2-IN-2 (Compound Nap-1) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor with IC50s of 4.45 and 3.18 μM, respectively.
  • HY-120356A
    T-1101 tosylate

    TAI-95 tosylate

    Apoptosis Cancer
    T-1101 tosylate (TAI-95 tosylate) is a Hec1/Nek2 (Highly expressed in cancer 1 / NIMA-related kinase 2) inhibitor with antitumor activity. T-1101 tosylate is inactive toward normal cells, kinases and hERG
  • HY-15729
    Rociletinib

    CO-1686; AVL-301; CNX-419

    EGFR Cancer
    Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
  • HY-N6725
    Sterigmatocystine

    DNA/RNA Synthesis Bacterial Apoptosis Antibiotic Cancer Infection
    Sterigmatocystine is a precursor of aflatoxins and a mycotoxin produced by common mold strains from Aspergillus versicolor. Sterigmatocystine, a inhibitor of G1 Phase and DNA synthesis, is used to inhibit p21 activity. Sterigmatocystine has teratogenic, and carcinogenic effects in animals.
  • HY-15778A
    AVE 0991 sodium salt

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    AVE 0991 sodium salt is a nonpeptide and orally active Ang-(1-7) receptor Mas agonist. AVE 0991 competes for high-affinity binding of [ 125I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC50 of 21±35 nM.
  • HY-100224
    SANT-1

    Smo Hedgehog Cancer
    SANT-1, a potent Smo antagonist, inhibits Hedgehog signaling. SANT-1 shows IC50s of 20 nM and 30 nM in Shh-LIGHT2 and SmoA1-LIGHT2 assay, respectively.
  • HY-100488
    Bay 59-3074

    Cannabinoid Receptor Cancer
    Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors, respectively. Bay 59-3074 has analgesic properties.
  • HY-120856
    ARN-3236

    Salt-inducible Kinase (SIK) Cancer Inflammation/Immunology
    ARN-3236 is an oral active and selective inhibitor of salt-inducible kinase 2 (SIK2), with IC50s of <1 nM, 21.63 nM and 6.63 nM for SIK2, SIK1 and SIK3, respectively. Has anti-cancer activity.
  • HY-101490
    PDE1-IN-2

    Phosphodiesterase (PDE) Neurological Disease
    PDE1-IN-2 is an inhibitor of PDE1 extracted from patent WO2016/55618 A1, example 31; has IC50 values of 6, 140 and 164 nM for PDE1C, PDE1B and PDE1A, respectvely.
  • HY-15729A
    Rociletinib hydrobromide

    CO-1686 (hydrobromide); AVL-301 hydrobromide; CNX-419 hydrobromide

    EGFR Cancer
    Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
  • HY-119744
    BAY 38-7271

    Cannabinoid Receptor Neurological Disease
    BAY 38-7271 is selective and highly potent and cannabinoid CB1/CB2 receptor agonist, with Kis of 1.85 nM and 5.96 nM for recombinant human CB1 receptor and CB2 receptor, respectively. BAY 38-7271 has strong neuroprotective properties.
  • HY-N2203
    Vitexin2''-​O-​p-​coumarate

    Others Others
    Vitexin2''-O-p-coumarate is isolated from fenugreek seeds. Vitexin2''-O-p-coumarate strongly promotes 2BS cell proliferation induced by H2O2.
  • HY-N0003
    Honokiol

    NSC 293100

    Akt ERK Autophagy HCV Cancer
    Honokiol is a bioactive, biphenolic phytochemical that possesses potent antioxidative, anti-inflammatory, antiangiogenic, and anticancer activities by targeting a variety of signaling molecules. It inhibits the activation of Akt and enhances the phosphorylation of ERK1/ERK2. Honokiol can readily cross the blood brain barrier.
  • HY-77251
    TAK1/MAP4K2 inhibitor 1

    MAP4K MAP3K Cancer
    TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.
  • HY-113973
    LPA2 antagonist 2

    LPL Receptor Cancer
    LPA2 antagonist 2 (H2L 5226501) is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM. LPA2 antagonist 2 is >480-fold more selective than LPA3 (IC50 of 13.85 μM).
  • HY-114363A
    SRI 31215 TFA

    c-Met/HGFR Cancer
    SRI 31215 (TFA), a triplex inhibitor of matriptase, hepsin and hepatocyte growth factor activator (HGFA) with IC50s of 0.69 μM, 0.65 μM, 0.3 μM, blocks pro-HGF activation and thus mimics the activity of HAI-1/2.
  • HY-117113
    JI051

    Notch Cancer
    JI051 is a stabilizer for the Hes1-PHB2 interaction, interacts with a cancer-associated protein chaperone prohibitin 2 (PHB2), induces cell-cycle arrest by inhibiting the Notch downstream effector gene Hes1. Anti-cancer activity.
  • HY-100862
    BRCA1-IN-2

    PARP Cancer
    BRCA1-IN-2 (compound 15) is a cell-permeable protein-protein interaction (PPI) inhibitor for BRCA1 with an IC50 of 0.31 μM and a Kd of 0.3 μM, which shows antitumor activities via the disruption of BRCA1 (BRCT)2/protein interactions.
  • HY-125835
    CP-10

    PROTAC CDK Cancer
    CP-10 is a PROTAC with highly selective, specific, and remarkable CDK6 degradation (DC50=2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated and overexpressed CDK6.
  • HY-15415
    KB-R7943 mesylate

    Na+/Ca2+ Exchanger Autophagy Cancer
    KB-R7943 mesylate is a widely used inhibitor of the reverse Na +/Ca 2+ exchanger (NCXrev) with IC50 of 5.7±2.1 µM. KB-R7943 mesylate induces cancer cell death via activating the JNK pathway and blocking autophagic flux.
  • HY-B0725S
    Doxepin D3 Hydrochloride

    Histamine Receptor Cytochrome P450 Neurological Disease
    Doxepin D3 Hydrochloride is a deuterium labeled Doxepin Hydrochloride. Doxepin hydrochloride is an orally active tricyclic antidepressant used as a sedative. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2.
  • HY-114398
    BAY-293

    Ras Cancer
    BAY-293, a valuable chemical probe, blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC50 of 21 nM. BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1). SOS1 is the guanine nucleotide exchange factor (GEF) and activator of RAS.
  • HY-126290A
    Tyk2-IN-9

    JAK Inflammation/Immunology
    Tyk2-IN-9 is a potent,selective and specific inhibitor of JAK kinases, inhibits Tyk2, JAK1 and JAK2 with IC50 values of 6 nM, 21nM and 6nM, respectively. Tyk2-IN-9, example 19, is extracted from patent US2017240552A1.
  • HY-114311
    FGFR1/DDR2 inhibitor 1

    FGFR Cancer
    FGFR1/DDR2 inhibitor 1 (compound 11k) is an inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM, 108.4 nM and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.
  • HY-112699
    AMPA receptor modulator-1

    iGluR Neurological Disease
    AMPA receptor modulator-1 is a potent, orally active and selective AMPAR regulatory protein TARP γ-8 negative modulator with a pIC50 of 9.7, more selective over GluA1/γ-2 (pIC50=5).
  • HY-126298
    RAF mutant-IN-1

    Raf Cancer
    RAF mutant-IN-1 is a RAF kinase inhibitor, extracted from patent WO2019107987A1, with IC50 values of 21 nM, 30 nM and 392 nM for C-RAF 340D/Y341D, B-RAF V600E and B-RAF WT, respectively.
  • HY-18086
    TCS PIM-1 1

    SC 204330

    Pim Cancer
    TCS PIM-1 1 (SC 204330) is a potent, selective and ATP-competitive Pim-1 kianse inhibitor with an IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC50s >20000 nM).
  • HY-B1836
    Mildronate

    Meldonium; MET-88; Quaterin

    Others Metabolic Disease Cardiovascular Disease
    Mildronate (Meldonium) functions as a cardioprotective drug by cpmpetetively inhibiting BBOX1 and OCTN2. Mildronate (Meldonium) exhibits IC50 values of 34-62 μM for human recombinant BBOX and an EC50 of 21 μM for human OCTN2. Mildronate (Meldonium) treatment-induced redirection of long-chain FA metabolism from mitochondria to peroxisomes.
  • HY-70059
    LY341495

    mGluR Neurological Disease
    LY341495 is a metabotropic glutamate receptor (mGluR) antagonist with IC50s of 21 nM, 14 nM, 7.8 μM, 8.2 μM, 170 nM, 990 nM, 22 μM for mGlu2, mGlu3, mGlu1a, mGlu5a, mGlu8, mGlu7, and mGlu4 receptors, respectively.
  • HY-13335
    PKCβ inhibitor 1

    PKC Apoptosis Cancer
    PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε).
  • HY-133020
    ARD-266

    PROTAC Androgen Receptor Cancer
    ARD-266 is a a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
  • HY-117147A
    GSK2945 hydrochloride

    Cytochrome P450 Metabolic Disease
    GSK2945 hydrochloride is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 hydrochloride enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.
  • HY-117147
    GSK2945

    Cytochrome P450 Metabolic Disease
    GSK2945 is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.
  • HY-B1836A
    Mildronate dihydrate

    Meldonium dihydrate; MET-88 dihydrate; Quaterin dihydrate

    Others Metabolic Disease Cardiovascular Disease
    Mildronate dihydrate (Meldonium dihydrate) functions as a cardioprotective drug by cpmpetetively inhibiting BBOX1 and OCTN2. Mildronate (Meldonium) exhibits IC50 values of 34-62 μM for human recombinant BBOX and an EC50 of 21 μM for human OCTN2. Mildronate (Meldonium) treatment-induced redirection of long-chain FA metabolism from mitochondria to peroxisomes.
  • HY-15768
    Ilomastat

    GM6001; Galardin

    MMP Cancer
    Ilomastat (GM6001) is a potent and broad spectrum matrix metalloprotease (MMP) inhibitor, inhibits MMPs (IC50s, 1.5 nM for MMP-1; 1.1 nM for MMP-2; 1.9 nM for MMP-3; 0.5 nM for MMP-9), with a Ki of 0.4 nM for human skin fibroblast collagenase (MMP-1).
  • HY-15785
    TAS-116

    HSP Cancer
    TAS-116 is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. TAS-116 demonstrates less ocular toxicity.
  • HY-N7378A
    N-Hydroxypipecolic acid potassium

    1-Hydroxy-2-piperidinecarboxylic acid potassium; NHP potassium

    Others Inflammation/Immunology
    N-Hydroxypipecolic acid potassium (1-Hydroxy-2-piperidinecarboxylic acid potassium), a plant metabolite and a systemic acquired resistance (SAR) regulator, orchestrates SAR establishment in concert with the immune signal salicylic acid. N-Hydroxypipecolic acid potassium accumulates systemically in the plant foliage in response to pathogen attack. N-Hydroxypipecolic acid potassium induces SAR to bacterial and oomycete infection.
  • HY-10969
    Obatoclax Mesylate

    GX15-070 Mesylate

    Bcl-2 Family Autophagy Parasite Cancer Infection
    Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2. Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity.
  • HY-B1452
    Licofelone

    ML-3000

    COX Lipoxygenase Apoptosis Cancer Inflammation/Immunology
    Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins.
  • HY-107322A
    Barnidipine

    Mepirodipine; YM-09730-5(Free base)

    Calcium Channel Cardiovascular Disease
    Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors. Barnidipine (Mepirodipine) is an antihypertensive drug and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action.
  • HY-107322
    Barnidipine hydrochloride

    Mepirodipine (hydrochloride); YM-09730-5

    Calcium Channel Cardiovascular Disease
    Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors. Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive drug and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action.
  • HY-110258
    ML334

    LH601A

    Keap1-Nrf2 Cancer
    ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity.
  • HY-10969A
    Obatoclax

    GX15-070

    Bcl-2 Family Autophagy Parasite Cancer Infection
    Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2. Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity.
  • HY-N7378
    N-Hydroxypipecolic acid

    1-Hydroxy-2-piperidinecarboxylic acid; NHP

    Others Inflammation/Immunology
    N-Hydroxypipecolic acid (1-Hydroxy-2-piperidinecarboxylic acid), a plant metabolite and a systemic acquired resistance (SAR) regulator, orchestrates SAR establishment in concert with the immune signal salicylic acid. N-Hydroxypipecolic acid accumulates systemically in the plant foliage in response to pathogen attack. N-Hydroxypipecolic acid induces SAR to bacterial and oomycete infection.
  • HY-16781
    Grapiprant

    CJ-023423; RQ-00000007; AAT-007

    Prostaglandin Receptor Metabolic Disease Endocrinology
    Grapiprant (CJ-023423) is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2). Grapiprant displaces [ 3H]-PGE2 (1 nM) binding to dog recombinant EP4 receptor with IC50 value of 35 nM and Ki value of 24 nM. Grapiprant has the potential for osteoarthritic pain and inflammation treatment[3] .
  • HY-100855
    DC_C66

    Histone Methyltransferase Cancer
    DC_C66 is a cell-permeable, selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 1.8 μM. DC_C66 has a good selectivity for CARM1 against PRMT1 (IC50=21 μM), PRMT6 (IC50= 47μM), and PRMT5.
  • HY-15303B
    Pritelivir mesylate hydrate

    BAY 57-1293 mesylate hydrate; AIC316 mesylate hydrate

    HSV Infection
    Pritelivir mesylate hydrate (BAY 57-1293 mesylate hydrate), an inhibitor of the viral helicase-primase complex, exhibits antiviral activity in vitro and in animal models of herpes simplex virus (HSV) infection. Pritelivir mesylate hydrate is active against herpes simplex virus types 1 and 2 (HSV-1 and HSV-2) with the IC50 of 0.02 μM against HSV1-2.
  • HY-118700
    2-Iminobiotin

    Guanidinobiotin

    NO Synthase Neurological Disease
    2-Iminobiotin (Guanidinobiotin) is a biotin (vitamin H or B7) analog. 2-Iminobiotin is a reversible nitric oxide synthases inhibitor with Kis of 21.8 and 37.5μM for murine iNOS and rat n-cNOS, respectively. 2-Iminobiotin superimposes on hypothermia protects human neuronal cells from hypoxia-induced cell damage.
  • HY-135396
    (1S,2S)-Bortezomib

    Proteasome Cancer
    (1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans.
  • HY-15303A
    Pritelivir mesylate

    BAY 57-1293 mesylate; AIC316 mesylate

    HSV Infection
    Pritelivir mesylate (BAY 57-1293 mesylate), an inhibitor of the viral helicase-primase complex, exhibits antiviral activity in vitro and in animal models of herpes simplex virus (HSV) infection. Pritelivir mesylate is active against herpes simplex virus types 1 and 2 (HSV-1 and HSV-2) with the IC50 of 0.02 μM against HSV1-2.
  • HY-N7018
    20-Hydroxyganoderic Acid G

    Others Inflammation/Immunology
    20-Hydroxyganoderic Acid G is a lanostane triterpenoid obtained from the EtOH extract of fruiting bodies of the Ganoderma curtisii. 20-Hydroxyganoderic Acid G inhibits BV-2 microglia cells activated by LPS with an IC50 of 21.33 μM. 20-Hydroxyganoderic Acid G has therapeutic potential in the drug discovery of nerve inflammation diseases associated with microglia activated by LPS.
  • 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-N0381
    Maackiain

    DL-​Maackiain

    Parasite Infection
    Maackiain (DL-Maackiain) is isolated from Maackia amurensis Rupr.et Maxim. Maackiain (DL-Maackiain) is a larvicidal agent against Aedes aegypti mosquito.xp Parasitol with a LD50 of  21.95 µg/mL. Maackiain (DL-Maackiain) induces fragmentations of DNA to oligonucleosomal-sized fragments that like a characteristic of apoptosis in the HL-60 cells.
  • HY-15303
    Pritelivir

    BAY 57-1293; AIC316

    HSV Infection
    Pritelivir (BAY 57-1293; AIC316), an inhibitor of the viral helicase-primase complex, exhibits antiviral activity in vitro and in animal models of herpes simplex virus (HSV) infection. Pritelivir is active against herpes simplex virus types 1 and 2 (HSV-1 and HSV-2) with the IC50 of 0.02 μM against HSV1-2.
  • HY-N2284
    Sophoflavescenol

    AChE Beta-secretase Phosphodiesterase (PDE) Cancer
    Sophoflavescenol is a prenylated flavonol, which shows great inhibitory activity with IC50 of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC50s of 0.30 µM, 0.17 µM, 17.89 µg/mL, 10.98 µM, 8.37 µM and 8.21 µM, respectively.
  • HY-135774
    6-Hydroxybenzbromarone

    Drug Metabolite Phosphatase Cardiovascular Disease
    6-Hydroxybenzbromarone is the major metabolite of Benzbromarone with a longer half-life and greater pharmacological potency than the parent compound. 6-Hydroxybenzbromarone is a protein Eyes Absent 3 (EYA3) inhibitor with an IC50 value of 21.5 μM. 6-Hydroxybenzbromarone is an angiogenic agent, has strong inhibitory effects on cell migration, tubulogenesis, and angiogenic sprouting.
  • HY-114226
    Olutasidenib

    FT-2102

    Isocitrate Dehydrogenase (IDH) Cancer Inflammation/Immunology
    Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) .
  • HY-N0397
    Harpagide

    Parasite Infection Inflammation/Immunology
    Harpagide is a class of iridoid glycoside isolated from Scrophularia cryptophila and has antiparasitic activity, which exhibits good in vitro trypanocidal activities against African trypanosomes (T.b. rhodesiense) with an IC50 of 21 μg/mL. Harpagide exerts significant antileishmanial activity against L. donovani with an IC50 value of 2.0 μg/mL. Harpagide also possess significant anti-inflammatory activities.
  • HY-118700A
    2-Iminobiotin hydrobromide

    Guanidinobiotin hydrobromide

    NO Synthase Neurological Disease
    2-Iminobiotin hydrobromide (Guanidinobiotin hydrobromide) is a biotin (vitamin H or B7) analog. 2-Iminobiotin hydrobromide is a reversible nitric oxide synthases inhibitor with Kis of 21.8 and 37.5 μM for murine iNOS and rat n-cNOS, respectively. 2-Iminobiotin hydrobromide superimposes on hypothermia protects human neuronal cells from hypoxia-induced cell damage.
  • HY-N0087
    Gambogic Acid

    Beta-Guttiferrin

    Bcl-2 Family Autophagy Cancer
    Gambogic Acid (Beta-Guttiferrin) is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic Acid (Beta-Guttiferrin) inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50s of 1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM and 0.79 μM.
  • HY-N0460
    1-Caffeoylquinic acid

    NF-κB Cancer
    1-Caffeoylquinic acid is an effective NF-κB inhibitor, shows significant binding affinity to the RH domain of p105 with Ki of 0.002 μM and binding energy of 1.50 Kcal/mol. 1-Caffeoylquinic acid has anti-oxidative stress ability. 1-Caffeoylquinic acid inhibits PD-1/PD-L1 interact.
  • HY-W008364
    Olivetol

    Cytochrome P450 Cannabinoid Receptor Neurological Disease
    Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2. Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively.
  • 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-N2443
    Tribuloside

    Bacterial Infection Neurological Disease
    Tribuloside, is isolated fromPotentilla multifid. Tribuloside exhibits anti-mycobacterial activity against the non-pathogenic Mycobacterium species with a minimum inhibitory concentration (MIC) 5.0 mg/mL. Tribuloside has 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity. Tribuloside possesses antidepressant effect, improves behavior and BrdU immunoreactive cells of depression model rats.
  • HY-13422
    Zatebradine hydrochloride

    UL-FS-49; UL-FS-49CL

    HCN Channel Cardiovascular Disease
    Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively.
  • 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-107479
    (R)-JNJ-31020028

    Neuropeptide Y Receptor Neurological Disease
    (R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects.
  • HY-117386
    Methoxyfenozide

    Bacterial
    Methoxyfenozide, a diacylhydrazine insecticide, selectively binds to lepidopteran ecdysone receptors (EcRs) over dipteran EcRs with Kd values of 0.5 and 124 nM, respectively. Methoxyfenozide is lethal to neonatal larvae of S. exigua, S. frugiperda, T. ni, O. nubilalis, L. pomonella, H. zea, and H. virescens (LC50s=0.35, 0.2, 0.11, 0.18, 0.21, 0.79, and 3.12 mg/L, respectively).
  • HY-107523
    WAY-213613

    EAAT2 Neurological Disease
    WAY-213613 is a potent, selective nonsubstrate reuptake inhibitor of GLT-1/EAAT2 with IC50 of 85 nM EAAT2. It displays 59- and 44-fold selectivity over EAAT1 and EAAT3 (IC50s are 5 and 3.8 μM, respectively). WAY-213613 shows no activity at ionotropic and metabotropic glutamate receptors. It is a potential tool for the elucidation of EAAT2 function.
  • HY-133045
    VHL Ligand 8

    Ligand for E3 Ligase Cancer
    VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
  • HY-125876
    PROTAC Bcl2 degrader-1

    PROTAC Bcl-2 Family Cancer
    PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1.
  • HY-121618
    α-Thujone

    GABA Receptor Reactive Oxygen Species Parasite Apoptosis Autophagy Cancer Infection Neurological Disease
    α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and easily penetrates the blood-brain barrier.
  • HY-107523A
    WAY-213613 hydrochloride

    EAAT2 Neurological Disease
    WAY-213613 hydrochloride is a potent, selective nonsubstrate reuptake inhibitor of GLT-1/EAAT2 with IC50 of 85 nM EAAT2. It displays 59- and 44-fold selectivity over EAAT1 and EAAT3 (IC50s are 5 and 3.8 μM, respectively). WAY-213613 hydrochloride shows no activity at ionotropic and metabotropic glutamate receptors. It is a potential tool for the elucidation of EAAT2 function.
  • HY-101561
    Avapritinib

    BLU-285

    c-Kit PDGFR Cancer
    Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2.
  • HY-15826
    SGC-CBP30

    Epigenetic Reader Domain Histone Acetyltransferase Cancer Inflammation/Immunology
    SGC-CBP30 is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects.
  • HY-13422A
    Zatebradine

    UL-FS-49 free base; UL-FS-49CL free base

    HCN Channel Cardiovascular Disease
    Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 value of 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively.
  • HY-14743B
    Golotimod hydrochloride

    SCV 07 hydrochloride; Gamma-D-glutamyl-L-tryptophan hydrochloride

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod hydrochloride (SCV 07 hydrochloride), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod hydrochloride (SCV 07 hydrochloride) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod hydrochloride (SCV 07 hydrochloride) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-B1639
    Enoximone

    Phosphodiesterase (PDE) Inflammation/Immunology Cardiovascular Disease
    Enoximone is an inotropic vasodilating agent and a selective and orally active phosphodiesterase III (PDE3) inhibitor with an IC50 of 5.9 μM. Enoximone induces vasodilatation and increases intracellular levels of cAMP by inhibiting cGMP-inhibited PDE. Enoximone also exhibits PDE4 inhibitory effect with an IC50 of 21.1 μM for myocardial PDE4A. Enoximone has the potential for congestive heart failure research and has bronchodilatory, antiasthma and anti-inflammatory effects.
  • HY-112429
    HJB97

    Epigenetic Reader Domain Cancer
    HJB97 is a high-affinity BET inhibitor with Kis of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively. HJB97 is employed for the design of potential PROTAC BET degrader and has antitumor activity.
  • HY-130538
    1-Naphthohydroxamic acid

    HDAC Cancer
    1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC50 of 14 μM. 1-Naphthohydroxamic acid is more selectively for HDAC8 than class I HDAC1 and class II HDAC6 (IC50 >100 μM). 1-Naphthohydroxamic acid does not increase global histone H4 acetylation and also does not reduce total intracellular HDAC activity.1-Naphthohydroxamic acid can induce tubulin acetylation.
  • HY-133044
    Boc-Pip-alkyne-Ph-COOH

    PROTAC Linker Cancer
    Boc-Pip-alkyne-Ph-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-Pip-alkyne-Ph-COOH can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 effectively induces degradation of androgen receptor (AR) protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
  • HY-14743A
    Golotimod TFA

    SCV 07 TFA; Gamma-D-glutamyl-L-tryptophan TFA

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod TFA (SCV 07 TFA), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod TFA (SCV 07 TFA) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod TFA (SCV 07 TFA) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-14743
    Golotimod

    SCV 07; Gamma-D-glutamyl-L-tryptophan

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-100034
    NSC 663284

    DA-3003-1

    Phosphatase Histone Methyltransferase Cancer
    NSC 663284 is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively. NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM).
  • HY-112614
    ATM Inhibitor-1

    ATM/ATR Cancer
    ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM, shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM). ATM Inhibitor-1 exhibits anti-tumor activity.
  • HY-B0498
    Bindarit

    AF2838

    CCR Inflammation/Immunology Neurological Disease Cancer Endocrinology
    Bindarit (AF2838) is a selective inhibitor of the monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8, and no effect on other CC and CXC chemokines such as MIP-1α/CCL3, MIP-1β/CCL4, MIP-3/CCL23. Bindarit also has anti-inflammatory activity.
  • HY-103286
    PD176252

    Bombesin Receptor Cancer
    PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.
  • HY-17499
    EGFR-IN-12

    EGFR Apoptosis Cancer
    EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFR L858R and EGFR L861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity.
  • HY-112306
    Ripretinib

    DCC-2618

    c-Kit PDGFR FLT3 VEGFR Apoptosis Cancer
    Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2). DCC-2618 exerts antineoplastic effect and induces apoptosis.
  • HY-119109
    Laminaran

    Others Cancer
    Laminaran is a neutral water-soluble β-1-3-glucan and a typical ligand for Dectin-1 isolated from the brown alga D. dichotoma, has potent immunomodulating, radioprotective, and anticancer activities. Laminaran is made up of β (1→3)-glucan with β (1→6)-branches and can be catalyzed by enzymes such as laminarinase (EC 3.2.1.6) that breaks the β (1→3) bonds. Laminaran is a promising immune stimulatory molecule for use in cancer immunotherapy.
  • 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-10122
    Silodosin

    KAD 3213; KMD 3213

    Adrenergic Receptor Cancer Endocrinology
    Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH.
  • HY-13775
    XL019

    JAK Apoptosis Cancer
    XL019 is a potent,orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.
  • HY-110368
    BS-181 dihydrochloride

    CDK Cancer
    BS-181 dihydrochloride is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880 nM, 3000 nM and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 dihydrochloride inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 dihydrochloride has the potential for the research of cancer therapy.
  • HY-13266
    BS-181

    CDK Cancer
    BS-181 is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880, 3000 and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 has the potential for the research of cancer therapy.
  • HY-124322
    NB-360

    Beta-secretase Inflammation/Immunology Neurological Disease
    NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC50: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E.
  • HY-126251
    CDK9-IN-7

    CDK Apoptosis Cancer
    CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC.
  • HY-100858
    PP7

    Influenza Virus Infection
    PP7 is a potent PB1-PB2 interaction inhibitor with an IC50 of 8.6 μM, and their inhibition against viral polymerase activity (IC50=9.5 μM). PP7 shows antiviral activities against influenza A virus (IAV), including A(H1N1)pdm09 (EC50=1.4 μM), A(H7N9) and A(H9N2) subtypes.
  • HY-120874
    PF-06372865

    GABA Receptor Neurological Disease
    PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 has the potential for epilepsy.
  • HY-135856
    SARS-CoV-IN-2

    SARS-CoV Parasite HIV Infection
    SARS-CoV-IN-2 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-2 shows anti-Coronavirus activity with an EC50 of 1.9 μM in Vero cells. SARS-CoV-IN-2 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 21.5 and 30 nM; and IC90s of 51.0 and 99.9 nM; respectively. SARS-CoV-IN-2 reduces HIV-1-induced cytopathic effect with an EC50 of 2.9 μM in MT-4 cells. Antimalarial and Antiviral Activities.
  • HY-105285
    Piromelatine

    Neu-P11

    Melatonin Receptor 5-HT Receptor P2X Receptor TRP Channel Sodium Channel Neurological Disease
    Piromelatine (Neu-P11) is a melatonin MT1/MT2 receptor agonist, serotonin 5-HT1A/5-HT1D agonist, and serotonin 5-HT2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.
  • HY-10624
    THIQ

    Melanocortin Receptor Metabolic Disease
    THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC50=1.2 nM, EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants.
  • HY-120877
    MRT199665

    Salt-inducible Kinase (SIK) AMPK Apoptosis Cancer
    MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370.
  • HY-N1992
    Theaflavin 3,3'-digallate

    TF3

    Akt NF-κB MEK ERK Cancer
    Theaflavin 3,3'-digallate (TF3), the typical pigment in black tea, is a good antitumor agent. Theaflavin 3,3'-digallate is generally regarded as the effective component for the inhibitory effects against carcinogenesis without adverse side effects by affecting multiple signal transduction pathways, such as upregulating p53 and p21, inhibiting phosphorylation of the cell survival protein Akt and MAPK pathway, downregulation of NF-κB, shifting the ratio between pro-/antiapoptotic proteins. Theaflavin 3,3'-digallate causes a rapid and sustained decrease in phospho-ERK1/2 and -MEK1/2 protein expression. Theaflavin 3,3'-digallate inhibits HCT116 cell growth with an IC50 of 17.26 μM.