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Results for "Available tak1 Inhibitors" in MCE Product Catalog:

249

Inhibitors & Agonists

4

Screening Libraries

1

Dye Reagents

1

Biochemical Assay Reagents

2

Peptides

1

MCE Kits

5

Natural
Products

Cat. No. Product Name Target Research Areas
  • 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-103490
    Takinib

    MAP3K Apoptosis Cancer
    Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM, which inhibits autophosphorylated and non-phosphorylated TAK1 that binds within the ATP-binding pocket and inhibits by slowing down the rate-limiting step of TAK1 activation.
  • 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-12686
    5Z-7-Oxozeaenol

    FR148083; L783279; LL-Z 1640-2

    MAP3K VEGFR Infection Inflammation/Immunology
    5Z-7-Oxozeaenol is a natural anti-protozoan compound from fungal origin, acting as a potent irreversible and selective inhibitor of TAK1 and VEGF-R2, with IC50s of 8 nM and 52 nM, respectively.
  • HY-114454
    INH14

    IKK Cancer Inflammation/Immunology
    INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity.
  • HY-10456
    TAK-715

    p38 MAPK Autophagy Inflammation/Immunology
    TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1.
  • HY-15504A
    RGB-286638 free base

    CDK GSK-3 MEK JAK Cancer
    RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
  • HY-15504
    RGB-286638

    CDK GSK-3 MEK JAK Cancer
    RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-107623
    TC-MCH 7c

    MCHR1 (GPR24) Metabolic Disease
    TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH1R antagonist with an IC50 of 5.6 nM for hMCH1R. TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively.
  • HY-12085
    Apremilast

    CC-10004

    Phosphodiesterase (PDE) Apoptosis TNF Receptor Inflammation/Immunology
    Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM.
  • HY-106080A
    Furegrelate sodium

    U-63557A

    Others Cardiovascular Disease
    Furegrelate Sodium (U-63557A) is a potent, orally available, and selective thromboxane synthase inhibitor. Furegrelate Sodium inhibits human platelet microsomal thromboxane A2 (TxA2) synthase with an IC50 of 15 nM. Furegrelate Sodium is being developed as an antiplatelet agent.
  • HY-14806
    Teneligliptin

    MP-513

    Dipeptidyl Peptidase Metabolic Disease
    Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM.
  • HY-14806S
    Teneligliptin D8

    MP-513 D8

    Dipeptidyl Peptidase Cardiovascular Disease
    Teneligliptin D8 (MP-513 D8) a deuterium labeled Teneligliptin (MP-513). Teneligliptin is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor.
  • HY-12085S
    Apremilast D5

    CC-10004 D5

    Phosphodiesterase (PDE) TNF Receptor Apoptosis Inflammation/Immunology
    Apremilast D5 (CC-10004 D5) is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-19373
    RWJ-445167

    3DP-10017

    Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  • HY-16787
    ICA-121431

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • HY-16635
    Setipiprant

    ACT-129968; KYTH-105

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Setipiprant is an orally available, selective CRTH2 antagonist.
  • HY-14543
    Sertindole

    Lu 23-174

    5-HT Receptor Dopamine Receptor Adrenergic Receptor Autophagy Neurological Disease Cancer
    Sertindole, a neuroleptic, is one of the newer antipsychotic medications available.
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

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

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-12507
    GSK-7975A

    Calcium Channel Inflammation/Immunology
    GSK-7975A is a potent and orally available CRAC channel inhibitor.
  • HY-10159
    Nilotinib

    AMN107

    Bcr-Abl Autophagy Cancer
    Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
  • HY-100830
    NCB-0846

    Wnt MAP4K Cancer
    NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-15564
    AR 231453

    GPR119 Metabolic Disease
    AR 231453 is a potent, selective and orally available GPR119 agonist.
  • HY-14857
    Carotegrast

    Integrin Inflammation/Immunology
    Carotegrast is an orally available α4 integrin receptor inhibitor with anti-inflammatories activities.
  • HY-10180
    MLN8054

    Aurora Kinase Cancer
    MLN8054 is a potent, selective and orally available aurora A kinase inhibitor with an IC50 of 4 nM.
  • HY-16445
    Sapacitabine

    CS682; CYC682

    Nucleoside Antimetabolite/Analog Cancer
    Sapacitabine is an orally available nucleoside analog prodrug that is structurally related to cytarabine.
  • HY-110095
    (±)-CPSI-1306

    Others Metabolic Disease Inflammation/Immunology
    (±)-CPSI-1306 is an orally available antagonist of macrophage migration inhibitory factor (MIF).
  • HY-16774
    Vericiguat

    BAY1021189

    Guanylate Cyclase Cardiovascular Disease
    Vericiguat (BAY1021189) is a potent, orally available and soluble guanylate cyclase stimulator.
  • HY-B1344
    Oxantel pamoate

    Oxantel embonate

    Parasite Infection
    Oxantel pamoate is a widely available dewormer, potently against Trichuris muris and Hookworms.
  • HY-11077
    SR 146131

    Cholecystokinin Receptor Metabolic Disease Endocrinology
    SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.
  • HY-12727
    EPZ015666

    GSK3235025

    Histone Methyltransferase Cancer
    EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 with an IC50 of 22 nM.
  • HY-15828
    NMS-1286937

    NMS-P937

    Polo-like Kinase (PLK) Apoptosis Cancer
    NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with an IC50 of 2 nM.
  • HY-19324
    EPZ031686

    Histone Methyltransferase Cancer
    EPZ031686 is an orally available SMYD3 inhibitor with an IC50 of 3 nM in cell-free assay.
  • HY-114332
    GNE-8505

    MAP3K Neurological Disease
    GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK).
  • HY-17359
    Deferasirox

    ICL 670

    Bacterial Ferroptosis Cancer
    Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload.
  • HY-B1215
    Dimenhydrinate

    Histamine Receptor Neurological Disease Endocrinology
    Dimenhydrinate is an anti-emetic and anti-histamine commonly available over-the-counter as a motion sickness remedy.
  • HY-19741
    A-1331852

    Bcl-2 Family Cancer
    A-1331852 is an orally available BCL-XL selective inhibitor with a Ki of less than 10 pM.
  • HY-109032
    Firuglipel

    GPR119 Metabolic Disease
    Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist.
  • HY-109018
    Velagliflozin

    SGLT Metabolic Disease
    Velagliflozin is an orally available sodium-glucose cotransporter 2 (SGLT2) inhibitor, with anti-diabetic activity.
  • HY-14870
    Selexipag

    NS-304; ACT-293987

    Prostaglandin Receptor Cardiovascular Disease Endocrinology
    Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor).
  • HY-13742
    Ropidoxuridine

    IPdR

    Others Cancer
    Ropidoxuridine (IPdR) is a novel orally available, halogenated thymidine analog and is a potential radiosensitizer for use in human tumors.
  • HY-109059
    Fulacimstat

    BAY1142524

    Others Cardiovascular Disease
    Fulacimstat is an orally available chymase inhibitor, with IC50s of 4, 3 nM for human and hamster chymase enzyme, respectively.
  • HY-13796
    IPSU

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.
  • HY-135813
    LtaS-IN-1

    Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-100388
    SHP099

    Phosphatase Cancer
    SHP099 is a potent, selective, orally available SHP2 inhibitor with an IC50 of 70 nM.
  • HY-101611
    MSC2530818

    CDK Cancer
    MSC2530818 is a potent, selective and orally available CDK8 inhibitor with an IC50 of 2.6 nM for CDK8.
  • HY-15599
    SSR128129E

    SSR

    FGFR Cancer
    SSR128129E is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
  • HY-15411
    MK-0557

    Neuropeptide Y Receptor Metabolic Disease Endocrinology
    MK-0557 is a highly selective, orally available neuropeptide Y5 receptor antagonist with a Ki of 1.6 nM.
  • HY-15291
    MBX-2982

    GPR119 Metabolic Disease
    MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist.
  • HY-50696
    Nutlin-3

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    Nutlin-3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.
  • HY-100388A
    SHP099 hydrochloride

    Phosphatase Cancer
    SHP099 hydrochloride is a potent, selective and orally available SHP2 inhibitor with an IC50 of 70 nM.
  • HY-32721
    Neratinib

    HKI-272

    EGFR Cancer
    Neratinib is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.
  • HY-104048
    QC6352

    Histone Demethylase Cancer
    QC6352 is an orally available, selective and potent KDM4C inhibitor with an IC50 of 35 nM.
  • HY-109082
    Cevidoplenib

    Syk Inflammation/Immunology
    Cevidoplenib is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential anti-inflammatory and immunomodulating activities.
  • HY-101474
    (±)-Zanubrutinib

    (±)-BGB-3111

    Btk Cancer
    (±)-Zanubrutinib ((±)-BGB-3111) is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
  • HY-15599A
    SSR128129E free acid

    SSR free acid

    FGFR Cancer
    SSR128129E free acid is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
  • HY-108339
    PF-06471553

    Acyltransferase Metabolic Disease
    PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM.
  • HY-12428
    A-1165442

    TRP Channel Neurological Disease
    A-1165442 is a potent, competitive and orally available TRPV1 antagonist with an IC50 of 9 nM for human TRPV1.
  • HY-18954
    NMS-P118

    PARP Cancer
    NMS-P118 is a potent, orally available, and highly selective PARP-1 Inhibitor for cancer therapy.
  • HY-103020
    BAY-1816032

    Others Cancer
    BAY-1816032 is a potent and oral available BUB1 (budding uninhibited by benzimidazoles 1) kinase inhibitor with an IC50 of 7 nM.
  • HY-18988
    ETC-159

    ETC-1922159

    Wnt Cancer
    ETC-159 is a potent, orally available PORCN inhibitor. It inhibits β-catenin reporter activity with an IC50 of 2.9 nM.
  • HY-101447A
    SI-2 hydrochloride

    EPH 116 hydrochloride

    Others Cancer
    SI-2 hydrochloride (EPH 116 hydrochloride) is a highly promising SRC-3 SMI: SRC-3 inhibitor (PPI), with IC50 values of 3-20 nM for breast cancer cell death. SI-2 hydrochloride (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability.
  • HY-101566A
    BAY-1895344 hydrochloride

    ATM/ATR Cancer
    BAY-1895344 hydrochloride is a potent, orally available and selective ATR inhibitor, with IC50 of 7 nM. Anti-tumor activity.
  • HY-15837
    SAR-260301

    PI3K Cancer
    SAR-260301 is an orally available and selective PI3Kβ inhibitor with an IC50 of 23 nM.
  • HY-B1110
    Nomifensine

    (±)-Nomifensin

    Dopamine Receptor Neurological Disease
    Nomifensine is a norepinephrine-dopamine reuptake inhibitor, increases the amount of synaptic norepinephrine and dopamine available to receptors by blocking the dopamine and norepinephrine reuptake transporters.
  • HY-100946
    CEP-40783

    RXDX-106

    TAM Receptor c-Met/HGFR Cancer
    CEP-40783 is a potent, selective and orally available inhibitor of AXL and c-Met with IC50 values of 7 nM and 12 nM, respectively.
  • HY-18072
    GSK2606414

    PERK Autophagy Apoptosis Cancer
    GSK2606414 is a cell-permeable and orally available protein kinase R-like endoplasmic reticulum (ER) kinase (PERK) inhibitor with an IC50 of 0.4 nM.
  • HY-100493
    BP-1-102

    STAT Cancer
    BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC50 of 6.8 μM.
  • HY-109096
    Nidufexor

    LMB763

    FXR Autophagy Inflammation/Immunology
    Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH).
  • HY-101566
    BAY-1895344

    ATM/ATR Cancer
    BAY-1895344 is a potent, orally available and selective ATR inhibitor, with IC50 of 7 nM. Anti-tumor activity.
  • HY-101773
    c-Met-IN-2

    c-Met/HGFR Cancer
    c-Met-IN-2 is a potent, selective and orally available c-Met inhibitor, with an IC50 of 0.6 nM, with antitumor activity.
  • HY-117632
    ABX-1431

    MAGL Neurological Disease
    ABX-1431 is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.
  • HY-14817
    Indeglitazar

    PPM 204

    PPAR Metabolic Disease
    Indeglitazar (PPM 204) is an orally available PPAR pan-agonist for all three PPARα, PPARδ and PPARγ.
  • 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-101918
    DS-1040 Tosylate

    Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-18728
    STF-31

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-12651
    Primaquine Diphosphate

    Primaquine phosphate; Primaquine bisphosphate

    Parasite Infection
    Primaquine is the only generally available anti-malarial that prevents relapse in vivax and ovale malaria, and the only potent gametocytocide in falciparum malaria.
  • HY-10804
    CCT 137690

    Aurora Kinase Apoptosis Cancer
    CCT 137690 is a potent and orally available aurora kinase inhibitor with IC50s of 15, 25, and 19 nM for aurora A, B and C, respectively.
  • HY-111360
    SPL-707

    Others Inflammation/Immunology
    SPL-707 is a potent, selective and orally available signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 80 nM.
  • HY-14272
    Ravuconazole

    BMS-207147; ER-30346

    Fungal Infection
    Ravuconazole (BMS-207147;ER-30346) is an orally available triazoleantifungle agent that potently inhibits a wide range of fungi.
  • HY-100209
    Sufugolix

    tak-013

    Others Endocrinology
    Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.1 nM.
  • HY-101782
    HSK0935

    HSK-0935; HSK 0935

    SGLT Metabolic Disease
    HSK0935 is a potent, highly selective and orally available SGLT2 inhibitor with an IC50 of 1.3 nM. Antihyperglycemic activities.
  • HY-101729
    Anti-Heart Failure Agent 1

    Others Cardiovascular Disease
    Anti-Heart Failure Agent 1 an orally available compound suitable for the treatment of heart failure without inducing nausea, vomiting and restlessness.
  • HY-19189
    Terbogrel

    BIBV 308SE

    Prostaglandin Receptor Cardiovascular Disease Endocrinology
    Terbogrel is an orally available thromboxane A2 receptor antagonist and a thromboxane A2 synthase inhibitor, with both IC50s of about 10 nM.
  • HY-19822
    Elacestrant

    RAD1901

    Estrogen Receptor/ERR Cancer
    Elacestrant (RAD1901) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.
  • HY-16785A
    Veledimex racemate

    INXN-1001 racemate; RG-115932 racemate

    Interleukin Related Cytochrome P450 Cancer Inflammation/Immunology
    Veledimex racemate (INXN-1001 racemate) is the racemate of veledimex. Veledimex is an orally available, small-molecule activator ligand for the RheoSwitch Therapeutic System.
  • HY-111409
    RIP1 kinase inhibitor 1

    RIP kinase Inflammation/Immunology
    RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pKi=9.04).
  • HY-15446
    Basimglurant

    RG7090; CTEP Derivative

    mGluR Neurological Disease
    Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM.
  • HY-19822A
    Elacestrant dihydrochloride

    RAD1901 dihydrochloride

    Estrogen Receptor/ERR Cancer
    Elacestrant dihydrochloride (RAD1901 dihydrochloride) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.
  • HY-128604
    XY101

    ROR Cancer
    XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC50 of 30 nM and a Kd of 380 nM.
  • HY-108413
    Talazoparib tosylate

    BMN 673ts

    PARP Cancer
    Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1.
  • HY-106392
    Lucerastat

    NB-DGJ; N-(n-Butyl)deoxygalactonojirimycin

    Others Metabolic Disease
    Lucerastat, the galactose form of Miglustat, is an orally-available inhibitor of glucosylceramide synthase (GCS). Lucerastat has the potential for Fabry disease study.
  • HY-16265
    JI-101

    Ephrin Receptor PDGFR VEGFR Cardiovascular Disease Cancer
    JI-101 is an orally available multi-kinase inhibitor of VEGFR2PDGFRβ and EphB4 with potent anti-cancer activity.
  • HY-B1028
    Pantethine

    D-Pantethine; LBF disulfide

    Endogenous Metabolite Others
    Pantethine is a dimeric form of pantothenic acid, is an intermediate in the production of Coenzyme A, is available as a dietary supplement, and is used to treat acne and improve the blood-cholesterol profile.
  • HY-A0076
    Tebipenem

    LJC 11036

    Bacterial Antibiotic Infection
    Tebipenem is an orally available carbapenem antibiotic, shows broad-spectrum activity against Gram-positive and -negative bacteria, except for Pseudomonas aeruginosa.
  • HY-19903
    ASP-9521

    Others Cancer
    ASP-9521 is a potent, selective and orally available AKR1C3 inhibitor with an IC50 of 11 nM for human AKR1C3.
  • HY-16511
    Upamostat

    WX-671

    Ser/Thr Protease PAI-1 Cancer
    Upamostat (WX-671) is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.
  • HY-101570
    Nedisertib

    M3814

    DNA-PK Cancer
    Nedisertib (M3814) is a potent, orally available and selective inhibitor of DNA-PK, with an IC50 of <3 nM. Anti-tumor activity.
  • HY-109754
    PF 03709270

    ulopenem etzadroxil

    Bacterial Infection
    PF 03709270 is an orally available ester prodrug form of sulopenem, with broad-spectrum antibacterial activity against most gram-positive and gram-negative bacteria.
  • HY-13041
    LX-1031

    Tryptophan Hydroxylase Neurological Disease
    LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally.
  • HY-14574
    PF-03814735

    Aurora Kinase VEGFR Cancer
    PF-03814735 is a potent, orally available and reversible aurora A and aurora B inhibitor with IC50s of 0.8 and 0.5 nM, respectively.
  • HY-10792
    Eplivanserin

    SR-46349

    5-HT Receptor Neurological Disease
    Eplivanserin is a potent, selective and orally available 5-HT2 receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM.
  • HY-B0826
    Spirodiclofen

    BAJ-2740

    Parasite Infection
    Spirodiclofen is a broad spectrum acaricide acting via lipid biosynthesis inhibition (LBI) with no cross resistance to currently available acaricides and with additional insecticidal properties.
  • HY-A0176
    Glisoxepide

    Potassium Channel Metabolic Disease Cardiovascular Disease
    Glisoxepide, a sulphonamide derivative, is an orally available nonselective K(ATP) channel blocker, with antihyperglycemic activity and cardiovascular regulation effect.
  • HY-101437
    Ralfinamide

    FCE-26742A

    Sodium Channel Neurological Disease
    Ralfinamide (FCE-26742A) is an orally available Na + blocker derived from α-aminoamide, with function of suppressing pain.
  • HY-19803
    Naquotinib mesylate

    ASP8273 (mesylate)

    EGFR Cancer
    Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
  • HY-101437A
    Ralfinamide mesylate

    FCE-26742A mesylate

    Sodium Channel Neurological Disease
    Ralfinamide mesylate (FCE-26742A mesylate) is an orally available Na + channel blocker derived from α-aminoamide, with function of suppressing pain.
  • HY-112439
    PI3Kdelta inhibitor 1

    PI3K Cancer Inflammation/Immunology
    PI3Kdelta inhibitor 1 (Compound 5d) is a potent, selective and orally available PI3Kδ inhibitor with an IC50 of 1.3 nM.
  • HY-16686
    α-Tocopherol phosphate

    alpha-Tocopherol phosphate; TocP; vitamin E phosphate

    Others Others
    α-Tocopherol phosphate is the compound demonstrating the highest vitamin E activity, which is available both in its natural form as RRR-alpha-tocopherol isolated from plant sources.
  • HY-108532
    AC-261066

    RAR/RXR Cancer
    AC-261066 is a potent, orally available and isoform-selective retinoic acid beta2 (RARbeta2) receptor agonist, with a pEC50 of 8.0.
  • HY-19729
    Naquotinib

    ASP8273

    EGFR Cancer
    Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-13328
    Sapanisertib

    INK-128; MLN0128; tak-228

    mTOR Autophagy Cancer
    Sapanisertib (INK-128; MLN0128; TAK-228) is an orally available, ATP-dependent mTOR1/2 inhibitor with an IC50 of 1 nM for mTOR kinase.
  • HY-107781
    PAT-505

    Phosphodiesterase (PDE) Inflammation/Immunology
    PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma.
  • HY-B1141
    Eprodisate disodium

    NC-503

    Others Others
    Eprodisate disodium (NC-503) is the orally available disodium salt form of Eprodisate, a negatively charged sulfonated inhibitor of fibrillogenesis, that can be used in the treatment of amyloid A (AA) amyloidosis.
  • HY-10159S
    Nilotinib D6

    AMN107 D6

    Bcr-Abl Autophagy Cancer
    Nilotinib D6 (AMN107 D6) is a deuterium labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
  • HY-19612B
    DDP-38003 trihydrochloride

    Histone Demethylase Cancer
    DDP-38003 trihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
  • HY-13233B
    Talabostat isomer mesylate

    Others Others
    Talabostat isomer mesylate is an isomer of talabostat mesylate. Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM.
  • HY-19612A
    DDP-38003 dihydrochloride

    Histone Demethylase Cancer
    DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
  • HY-10286A
    Dutogliptin tartrate

    PHX-1149

    Dipeptidyl Peptidase Metabolic Disease
    Dutogliptin tartrate (PHX-1149) is an orally available, potent, and selective dipeptidyl peptidase-4 (DPP4) inhibitor for the treatment of type 2 diabetes mellitus.
  • HY-128575
    BNC375

    nAChR Neurological Disease
    BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM.
  • HY-U00002
    ZD-4190

    VEGFR EGFR Cancer
    ZD-4190 is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cancer.
  • HY-10011
    SCH 563705

    CXCR Inflammation/Immunology Endocrinology
    SCH 563705 is a potent and orally available CXCR2 and CXCR1 antagonist, with IC50s of 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively.
  • HY-105634
    Nomegestrol

    Progesterone Receptor Endocrinology
    Nomegestrol is a potent and orally available progestin, acts as a selective full progesterone receptor agonist, with a Kd of 5.44 nM for rat uterine progesterone receptor, and has moderate antiandrogenic activity and strong antiestrogenic activity.
  • HY-19822D
    Elacestrant S enantiomer

    RAD1901 S enantiomer

    Estrogen Receptor/ERR Cancer
    Elacestrant S enantiomer is an low activity enantiomer of elacestrant. Elacestrant (RAD1901) is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
  • HY-19822B
    Elacestrant S enantiomer dihydrochloride

    RAD1901 S enantiomer dihydrochloride; RAD 1901 S enantiomer dihydrochloride; RAD-1901 S enantiomer dihydrochloride

    Estrogen Receptor/ERR Cancer
    Elacestrant S enantiomer dihydrochloride is an low activity enantiomer of elacestrant dihydrochloride. Elacestrant (RAD1901) dihydrochloride is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
  • HY-112912
    P-gp modulator 1

    P-glycoprotein Cancer
    P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR).
  • HY-10286
    Dutogliptin

    PHX-1149 free base

    Dipeptidyl Peptidase Metabolic Disease
    Dutogliptin (PHX-1149 free base) is an orally available, potent, and selective dipeptidyl peptidase-4 (DPP4) inhibitor for the treatment of type 2 diabetes mellitus.
  • HY-100844
    GS-444217

    MAP3K Apoptosis Cancer
    GS-444217 is a potent, orally available and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87 nM.
  • HY-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-17617
    Nastorazepide

    Z-360

    Cholecystokinin Receptor Cancer Endocrinology
    Nastorazepide (Z-360) is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity.
  • 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-12789
    Etrasimod

    APD334

    LPL Receptor Inflammation/Immunology
    Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.
  • HY-19957
    CH5183284

    Debio 1347

    FGFR Cancer
    CH5183284 is an orally available and selective FGFR inhibitor with IC50s of 9.3, 7.6, and 22 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
  • HY-40354A
    Tofacitinib citrate

    Tasocitinib citrate; CP-690550 citrate

    JAK Apoptosis Bacterial Fungal Influenza Virus Cancer Infection Inflammation/Immunology
    Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-19650
    Pumosetrag Hydrochloride

    MKC-733; DDP-733

    5-HT Receptor Metabolic Disease
    Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.
  • HY-114330A
    ZK824859 hydrochloride

    PAI-1 Inflammation/Immunology
    ZK824859 hydrochloride is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively.
  • HY-114330
    ZK824859

    PAI-1 Inflammation/Immunology
    ZK824859 is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively.
  • HY-12744A
    Genz-123346

    Others Metabolic Disease
    Genz-123346 is a potent, orally available glucosylceramide synthase inhibitor. Genz-123346 blocks the conversion of ceramide to glucosylceramide (GL1) and inhibits GM1 with an IC50 value of 14 nM.
  • HY-103007
    TC-G-1008

    GPR39-C3

    GHSR Metabolic Disease Endocrinology
    TC-G-1008 (GPR39-C3) is a potent and orally available GPR39 agonist with EC50 values of 0.4 and 0.8 nM for rat and human receptors respectively.
  • HY-109061
    Lazertinib

    YH25448; GNS-1480

    EGFR Cancer
    Lazertinib is a potent, highly mutant-selective, blood-brain barrier permeable, orally available and irreversible third-generation EGFR tyrosine kinase inhibitor, and can be used in the research of non-small cell lung cancer.
  • HY-12296
    AMG 232

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    AMG 232 is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. AMG 232 binds to MDM2 with a Kd of 0.045 nM.
  • HY-112256
    ACP-105

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

    Dopamine Receptor Neurological Disease
    LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM).
  • HY-126361
    ZK824190

    Ser/Thr Protease PAI-1 Inflammation/Immunology
    ZK824190 is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively.
  • HY-112823B
    HS-10296 hydrochloride

    EGFR Cancer
    HS-10296 hydrochloride is an orally available and third-Generation inhibitor of epidermal growth factor receptor (EGFR)-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.
  • HY-101212
    CYC065

    CDK Cancer
    CYC065 is a second-generation, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50s of 5 and 26 nM, respectively.
  • HY-13904
    Flumatinib

    HHGV678

    Bcr-Abl c-Kit PDGFR Cancer
    Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively.
  • HY-14182
    Vernakalant

    RSD1235

    Potassium Channel Cardiovascular Disease
    Vernakalant(RSD-1235) is an investigational mixed ion channel blocker that can terminate acute atrial fibrillation (AF) in humans at 2 to 5 mg/kg and may be more atrial-selective than available agents; in treatment of antiarrhythmic.
  • 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-101784
    NE 52-QQ57

    Others Inflammation/Immunology
    NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. NE 52-QQ57 has anti-inflammatory activity.
  • HY-13943
    CNX-774

    Btk Cancer
    CNX-774 is a potent, selective, and orally available small molecule inhibitor of Btk (IC50< 1 nM) that forms a ligand-directed covalent bond with Cys-481, a non-conserved amino acid within the active site of the enzyme.
  • HY-101026
    CCT251236

    HSP Cancer
    CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC50 of 19 nM for inhibition of HSF1-mediated HSP72 induction.
  • HY-13905
    Flumatinib mesylate

    HHGV678 mesylate

    Bcr-Abl c-Kit PDGFR Cancer
    Flumatinib mesylate (HHGV678 mesylate) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively.
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM [1].
  • HY-11021
    Elinogrel

    PRT060128

    P2Y Receptor Cardiovascular Disease
    Elinogrel (PRT060128) is a potent, direct acting, competitive, and reversible platelet P2Y12 antagonist (IC50=20 nM). It is orally and intravenously available and has potent antiplatelet effects.
  • HY-18708
    Erdafitinib

    JNJ-42756493

    FGFR Apoptosis Cancer
    Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.
  • HY-112823
    HS-10296

    EGFR Cancer
    HS-10296, an orally available and third-generation EGFR-activating mutations and T790M-resistant mutation inhibitor, shows limited activity against wild-type EGFR.
  • HY-111407
    MK-8353

    SCH900353

    ERK Cancer
    MK-8353 (SCH900353) is a potent, selective and orally available ERK1/2 inhibitor, with IC50s of 23.0 nM and 8.8 nM, respectively; MK-8353 has antitumor activity.
  • HY-10205
    Cediranib

    AZD2171

    VEGFR Autophagy PDGFR Cancer
    Cediranib (AZD2171) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
  • HY-10716A
    PF-03463275

    GlyT Neurological Disease
    PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research.
  • HY-135335
    3'-Hydroxy Repaglinide

    Drug Metabolite Metabolic Disease
    3'-Hydroxy Repaglinide is a main CYP2C8 metabolite of Repaglinide. Repaglinide is a carbamoylmethyl benzoic acid (CMBA) derivative, which recently has become available for the treatment of type II diabetes.
  • HY-18317
    JNJ-38158471

    VEGFR RET c-Kit Cancer
    JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively.
  • HY-13049
    Cediranib maleate

    AZD-2171 maleate

    VEGFR Autophagy PDGFR Cancer
    Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
  • HY-131063
    CDK6/9-IN-1

    CDK Cancer
    CDK6/9-IN-1 (compound 66) is an oral available and dual CDK 6 and CDK 9 inhibitor, with IC50 values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively.
  • HY-102037
    SSTR5 antagonist 1

    Somatostatin Receptor Metabolic Disease Endocrinology
    SSTR5 antagonist 1 is a potent, selective, and orally available somatostatin receptor subtype 5 (SSTR5) antagonist with IC50s of 9.6 and 57 nM for hSSTR5 and mSSTR5, respectively. (Compound 25a)
  • HY-B1693
    Levomepromazine

    Methotrimeprazine

    5-HT Receptor Dopamine Receptor Neurological Disease
    Methotrimeprazine (Levomepromazine) is an orally available neuroleptic agent, which is commonly used to relieve nausea and vomiting in palliative care settings. Levomepromazine has antagonist actions at multiple neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin and histamine receptors.
  • HY-112134
    CSN5i-3

    Others Cancer
    CSN5i-3 is a potent, selective and orally available inhibitor of CSN5/Jab1, and inhibits CSN-catalysed Cul1 deneddylation with an IC50 value of 5.8 nM.
  • HY-106673
    Hydrocortisone buteprate

    Hydrocortisone probutate; HBP

    Others Inflammation/Immunology
    Hydrocortisone buteprate (Hydrocortisone probutate) is a medium potent, non-halogenated double-ester of hydrocortisone with a favorable benefit/risk ratio for the treatment of inflammatory skin disorders. Hydrocortisone buteprate (Hydrocortisone probutate) is available as a 0.1% cream or ointment formulation.
  • HY-112296
    T025

    CDK Cancer
    T025 is an orally available and highly potent Cdc2-like kinase (CLK) inhibitor with Kds of 4.8, 0.096, 6.5, and 0.61 nM for CLK1, CLK2, CLK3, and CLK4, respectively.
  • HY-12206
    Thioperamide

    MR-12842

    Histamine Receptor Neurological Disease
    Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide inhibits [ 3H]histamine synthesis with a Ki of 31 nM.
  • HY-112134A
    (R)-CSN5i-3

    Others Cancer
    (R)-CSN5i-3 is the (R)-enantiomer of CSN5i-3. CSN5i-3 is a potent, selective and orally available inhibitor of CSN5.
  • HY-114739
    MA-0204

    PPAR Metabolic Disease
    MA-0204 is a potent, highly selective and orally available peroxisome proliferator activated receptor δ (PPARδ) modulator with EC50s of 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively. Potential treatment for Duchene Muscular Dystrophy (DMD).
  • HY-17606
    Cenerimod

    ACT-334441

    LPL Receptor Inflammation/Immunology
    Cenerimod (ACT-334441) is a potent and orally available sphingosine 1-phosphate 1 receptor (S1P1) agonist extracted from patent WO 2016184939 A1 and WO 2011007324 A1, example 1, with an EC50 of 2.7 nM.
  • HY-18662
    RQ-00203078

    TRP Channel Cancer
    RQ-00203078 is a highly selective, potent and orally available TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively), exhibits >350-fold selectivity for TRPM8 over TRPV4, TRPV1 and TRPA1.
  • HY-120394
    TVB-3166

    Fatty Acid Synthase (FASN) Apoptosis Cancer
    TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC50s of 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth.
  • HY-136660
    mTOR inhibitor-7

    mTOR Neurological Disease
    mTOR inhibitor-7 is an orally available, and brain-penetrant mTOR inhibitor extracted from patent WO2017198346A1, compound example 44, has an IC50 of 5 nM for mTOR. mTOR inhibitor-7 can be used for the research of neurological disorder.
  • HY-120062
    TVB-3664

    Fatty Acid Synthase (FASN) Cancer
    TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC50 values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression.
  • HY-12678
    Entrectinib

    NMS-E628; RXDX-101

    ROS Trk Receptor ALK Autophagy Cancer
    Entrectinib (NMS-E628) is a potent, orally available, and CNS-active pan-Trk, ROS1, and ALK inhibitor. Entrectinib inhibits TrkA, TrkB, TrkC, ROS1 and ALK with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Antitumor activity.
  • HY-111388
    SEL120-34A

    CDK Cancer
    SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.
  • HY-108015
    RO5263397

    Others Neurological Disease
    RO5263397 is a potent, selective, and orally available TAAR1 agonist, with EC50s of 17 and 35 nM for human TAAR1 and rat TAAR1, respectively. RO5263397 regulates wakefulness and EEG spectral composition. Antidepressant-like effect.
  • HY-15433
    Quisinostat

    JNJ-26481585

    HDAC Cancer
    Quisinostat (JNJ-26481585) is an orally available, potent HDAC inhibitor with IC50s of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10, HDAC11, respectively.
  • HY-111388B
    SEL120-34A HCl

    CDK Cancer
    SEL120-34A HCl is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.
  • HY-13314
    Tesevatinib

    XL-647; EXEL-7647; KD-019

    EGFR VEGFR Ephrin Receptor Cancer
    Tesevatinib (XL-647; EXEL-7647; KD-019) is an orally available, multi-target tyrosine kinase inhibitor; inhibits EGFR, ErbB2, KDR, Flt4 and EphB4 kinase with IC50s of 0.3, 16, 1.5, 8.7, and 1.4 nM.
  • HY-114452
    LY-2940094

    Opioid Receptor Neurological Disease
    LY-2940094 is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY-2940094 reduces ethanol self-administration in animal models.
  • HY-100653A
    AZD5153 6-Hydroxy-2-naphthoic acid

    AZD-5153 HNT salt

    Epigenetic Reader Domain Cancer
    AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM.
  • HY-B0113A
    Omeprazole sodium

    H 16868 sodium

    Proton Pump Autophagy Bacterial Cancer Infection Metabolic Disease
    Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria.
  • HY-103023
    CLP290

    Potassium Channel Neurological Disease
    CLP290 is an orally available activator of the neuron-specific K +-Cl cotransporter KCC2, displays potential for treatment of a wide range of neurological and psychiatric indications. CLP290 can significantly lower blood arginine-vasopressin (AVP) and glucose levels in STZ rats.
  • HY-112233
    O-304

    AMPK Metabolic Disease Cardiovascular Disease
    O-304 is a first-in-class, orally available pan-AMPK activator, which increases AMPK activity by suppressing the dephosphorylation of pAMPK. O-304 exhibits a great potential as a drug to treat type 2 diabetes (T2D) and associated cardiovascular complications [1].
  • HY-13007
    PF-3758309

    PAK Apoptosis Cancer
    PF-3758309 is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
  • HY-B0113
    Omeprazole

    H 16868

    Proton Pump Autophagy Bacterial Cancer Infection Metabolic Disease
    Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria.
  • HY-10811
    GNE-493

    PI3K mTOR Cancer
    GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
  • HY-10942
    VER-82576

    NVP-BEP800

    HSP Cancer
    VER-82576 (NVP-BEP800) is a potent, orally available and selective Hsp90 inhibitor, with an IC50 of 58 nM for Hsp90β; VER-82576 also slightly blocks Grp94 and Trap-1, with IC50s of 4.1 and 5.5 μM, respectively.
  • HY-19322B
    PIM-447 dihydrochloride

    LGH447 dihydrochloride

    Pim Cancer
    PIM447 dihydrochloride (LGH447 dihydrochloride) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 dihydrochloride displays dual antimyeloma and bone-protective effects. PIM447 dihydrochloride induces apoptosis.
  • HY-19322
    PIM447

    LGH447

    Pim Apoptosis Cancer
    PIM447 (LGH447) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis.
  • HY-12143
    Vofopitant dihydrochloride

    GR 205171A

    Neurokinin Receptor Cancer Neurological Disease Endocrinology
    Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [ 3H]SP binding to the NK1 receptor with pKi values of 9.5 and 10.6 in rat and human membranes respectively, acts as a potential broad-spectrum anti-emetic agent.
  • HY-N7347
    (-)-Hydroxycitric acid lactone

    Garcinia lactone

    ATP Citrate Lyase Metabolic Disease
    (-)-Hydroxycitric acid lactone (Garcinia lactone) is an anti-obesity agent and a popular weight loss food supplement. (-)-Hydroxycitric acid lactone is a potent inhibitor of ATP-citrate lyase. (-)-Hydroxycitric acid lactone catalyzes the extramitochondrial cleavage of citrate to oxaloacetate and acetyl-CoA, limits the availability of acetyl-CoA units required for fatty acid synthesis.
  • HY-N6660
    Tricaprin

    Glyceryl tridecanoate

    Endogenous Metabolite Metabolic Disease
    Tricaprin (Glyceryl tridecanoate) is an orally available precursor of decanoic acid (DA) and can be hydrolyzed to DA. Tricaprin (Glyceryl tridecanoate) is a major component of medium chain triglyceride (MCT) with antiandrogen and antihyperglycemic properties.Tricaprin (Glyceryl tridecanoate) has a safe use in in foods, drugs, cosmetics as an additive.
  • HY-130992
    Androgen receptor antagonist 1

    Androgen Receptor Ligand for Target Protein for PROTAC Cancer
    Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.
  • HY-130149
    MRTX849

    Ras Cancer
    MRTX849 is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. MRTX849 covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction.
  • HY-15433A
    Quisinostat dihydrochloride

    JNJ-26481585 dihydrochloride

    HDAC Cancer
    Quisinostat dihydrochloride (JNJ-26481585 dihydrochloride) is an orally available, potent pan-HDAC inhibitor with IC50s of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10, HDAC11, respectively. Quisinostat dihydrochloride has a broad spectrum antitumoral activity.
  • HY-108006
    Mirogabalin besylate

    DS 5565 besylate

    Calcium Channel Neurological Disease
    Mirogabalin besylate is a selective and orally available ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively.
  • HY-135111
    4-Desmethoxy Omeprazole

    Drug Metabolite Cancer Infection Metabolic Disease
    4-Desmethoxy Omeprazole is the active metabolite of Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria.
  • HY-13007A
    PF-3758309 hydrochloride

    PAK Apoptosis Cancer
    PF-3758309 hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
  • HY-50101A
    Mavorixafor trihydrochloride

    AMD-070 trihydrochloride

    CXCR HIV Infection Endocrinology
    Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
  • HY-130240
    GCN2-IN-6

    Eukaryotic Initiation Factor (eIF) Cancer
    GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells).
  • HY-50101
    Mavorixafor

    AMD-070

    CXCR HIV Infection Endocrinology
    Mavorixafor (AMD-070) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
  • HY-117259
    ALZ-801

    Amyloid-β Neurological Disease
    ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated prodrug of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound. ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease.
  • HY-B0113S
    Omeprazole D3

    H 16868 D3

    Proton Pump Bacterial Autophagy Cancer Infection Metabolic Disease
    Omeprazole D3 (H 16868 D3) is deuterium labeled Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria.
  • HY-15292
    S107

    Others Cardiovascular Disease
    S107 is an orally available, blood brain barrier-permeable compound, which stabilizes RyR2 channels by enhancing the binding of calstabin2 to the mutant Ryr2-R2474S channel. S107 inhibits Ca 2+ leakage from the sarcoplasmic reticulum (SR) and prevents cardiac arrhythmias and raises the seizure threshold.
  • HY-13011
    Alectinib

    CH5424802; RO5424802; AF802

    ALK Cancer
    Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively. Alectinib demonstrates effective central nervous system (CNS) penetration.
  • HY-128357
    ACX-362E

    Bacterial DNA/RNA Synthesis Infection
    ACX-362E is an orally available DNA polymerase IIIC (pol IIIC) inhibitor, acts as an antimicrobial agent to treat Gram-positive infections, with a MIC50 of 2 μg/mL for C. difficile. ACX-362E displays very potent in vitro and in vivo activities against broad spectrum of C. difficile pathogens.
  • HY-111372
    Finerenone

    BAY 94-8862

    Mineralocorticoid Receptor Cardiovascular Disease
    Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease.
  • HY-13440
    AMG 511

    PI3K Cancer
    AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model.
  • HY-13011A
    Alectinib Hydrochloride

    CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride

    ALK Cancer
    Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively. Alectinib demonstrates effective central nervous system (CNS) penetration.
  • HY-19834
    Fenebrutinib

    GDC-0853

    Btk Cancer
    Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research.
  • HY-100867
    TAK-659

    Syk FLT3 Cancer
    TAK-659 is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL).
  • HY-111509
    TAK-828F

    ROR Inflammation/Immunology
    TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (binding IC50=1.9 nM, reporter gene IC50=6.1 nM). TAK-828F shows excellent RORγt isoforms selectivity (>5000-fold selectivity against human RORα and RORβ).
  • HY-10472
    LY2811376

    Beta-secretase Neurological Disease
    LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC50 of 239 nM-249 nM, that acts to decrease Aβ secretion with EC50 of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.
  • HY-100867A
    TAK-659 hydrochloride

    Syk FLT3 Cancer
    TAK-659 hydrochloride is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 hydrochloride induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL).
  • HY-119726
    Fosmanogepix

    APX001; E1211

    Fungal Infection
    Fosmanogepix (APX001) is a first-in-class and orally available broad-spectrum antifungal agent, which targets the highly conserved Gwt1 fungal enzyme. Fosmanogepix (APX001) is an N-phosphonooxymethyl prodrug which is rapidly and completely metabolized by systemic alkaline phosphatases to the active moiety, APX001A. Fosmanogepix (APX001) can be used in development for the treatment of invasive fungal infections.
  • HY-122872
    MKK7-COV-9

    p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • HY-15160A
    TAK-960 hydrochloride

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

    Polo-like Kinase (PLK) Cancer
    TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
  • HY-19835
    LY2922470

    GPR40 Metabolic Disease
    LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively. LY2922470 reduces glucose levels along with significant increases in insulin and GLP-1, is potential for the treatment of type 2 diabetes mellitus (T2DM).
  • HY-15160
    TAK-960

    Polo-like Kinase (PLK) Cancer
    TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
  • HY-107390A
    AX-024 hydrochloride

    TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-120836
    AOH1160

    DNA/RNA Synthesis Apoptosis Cancer
    AOH1160 is a potent, first-in-class, orally available small molecule proliferating cell nuclear antigen (PCNA) inhibitor, interferes with DNA replication, blocks homologous recombination-mediated DNA repair, causes cell-cycle arrest and induces apoptosis. AOH1160 selectively kills many types of cancer cells (mean GI50=330 nM) without causing significant toxicity to a broad range of nonmalignant cells.
  • HY-128895
    NQO1 activator 1

    Others Metabolic Disease
    NQO1 activator 1 is an orally available NAD + modulator. It reacts with NAD(P)H:quinone oxidoreductase 1 (NQO1) as a substrate, resulting in increases in intracellular NAD + levels via NADH oxidation. Elevated NAD + levels triggers the activation of SIRT1 and AMPK, and subsequently activates PGC-1α. NQO1 activator 1 improves energy metabolism and mitochondrial dysfunction in MELAS fibroblasts.
  • HY-107390
    AX-024

    TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-104036
    IDH-305

    Isocitrate Dehydrogenase (IDH) Cancer
    IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC50= 27 nM (IDH1 R132H), 28 nM (IDH1 R132C), 6.14 µM (IDH1 WT)).
  • HY-15160C
    TAK-960 monohydrochloride

    Polo-like Kinase (PLK) Cancer
    TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
  • HY-13803C
    Tazemetostat hydrobromide

    EPZ-6438 hydrobromide; E-7438 hydrobromide

    Histone Methyltransferase Cancer
    Tazemetostat hydrobromide (EPZ-6438 hydrobromide) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat hydrobromide inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide inhibits Rat EZH2 with an IC50 of 4 nM. Tazemetostat hydrobromide also inhibits EZH1 with an IC50 of 392 nM.
  • HY-13803A
    Tazemetostat trihydrochloride

    EPZ-6438 trihydrochloride; E-7438 trihydrochloride

    Histone Methyltransferase Cancer
    Tazemetostat trihydrochloride (EPZ-6438 trihydrochloride) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat trihydrochloride inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki of 2.5 nM. Tazemetostat trihydrochloride inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat trihydrochloride inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM.
  • HY-101562
    GDC-0077

    RG6114

    PI3K Apoptosis Cancer
    GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα.
  • HY-76474
    BAY 61-3606

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

    Syk Apoptosis Inflammation/Immunology Cancer
    BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM. BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
  • HY-101514
    β3-AR agonist 1

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold).
  • HY-13803
    Tazemetostat

    EPZ-6438; E-7438

    Histone Methyltransferase Cancer
    Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat (EPZ-6438) inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat (EPZ-6438) inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat (EPZ-6438) inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM.
  • HY-112289
    IDH889

    Isocitrate Dehydrogenase (IDH) Cancer
    IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM.
  • HY-19896
    COTI-2

    MDM-2/p53 Apoptosis Cancer
    COTI-2, an anti-cancer drug with low toxicity, is an orally available third generation activator of p53 mutant forms. COTI-2 acts both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation.
  • HY-104042
    Vorasidenib

    AG-881

    Isocitrate Dehydrogenase (IDH) Cancer
    Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K.
  • HY-120944
    BAY-7598

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