1. Search Result
Search Result
Results for "

available

" in MCE Product Catalog:

251

Inhibitors & Agonists

7

Screening Libraries

1

Dye Reagents

1

Biochemical Assay Reagents

1

MCE Kits

7

Natural
Products

10

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • 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-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-114252
    Strophanthidin

    Na+/K+ ATPase Cardiovascular Disease
    Strophanthidin is a naturally available cardiac glycoside. Strophanthidin 0.1 and 1 nmol/L increases and 1~100 µmol/L inhibits the Na+/K+-ATPase activities, but Strophanthidin 10 and 100 nmol/L does not affect Na+/K+-ATPase activities in cardiac sarcolemmal. Strophanthidin increases both diastolic and systolic intracellular Ca 2+ concentration.
  • 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-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-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-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-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. BNC375 exhibits good CNS-drug like properties and clinical candidate potential. .
  • HY-14543S
    Sertindole-d4

    5-HT Receptor Dopamine Receptor Adrenergic Receptor Autophagy Neurological Disease Cancer
    Sertindole-d4 (Lu 23-174-d4) is the deuterium labeled Sertindole. Sertindole, a neuroleptic, is one of the newer antipsychotic medications available.
  • 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-100830
    NCB-0846

    Wnt MAP4K Cancer
    NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 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-12507
    GSK-7975A

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

    AMN107

    Bcr-Abl Autophagy Cancer
    Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
  • HY-101456
    PCPA methyl ester hydrochloride

    4-Chloro-DL-phenylalanine methyl ester hydrochloride

    Tryptophan Hydroxylase 5-HT Receptor Neurological Disease
    PCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride), a reversible tryptophan hydroxylase inhibitor, is a serotonin (5-HT) synthesis inhibitor. PCPA methyl ester hydrochloride crosses the blood brain barrier and reduces 5-HT central availability.
  • HY-110095
    (±)-CPSI-1306

    Others Metabolic Disease Inflammation/Immunology
    (±)-CPSI-1306 is an orally available antagonist of macrophage migration inhibitory factor (MIF).
  • HY-11077
    SR 146131

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

    GSK3235025

    Histone Methyltransferase Cancer
    EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 with an IC50 of 22 nM.
  • HY-101447A
    SI-2 hydrochloride

    EPH 116 hydrochloride

    Others Cancer
    SI-2 (EPH 116 hydrochloride) is a highly promising SRC-3 inhibitor (PPI), with IC50 values of 3-20 nM for breast cancer cell death. SI-2 (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability.
  • HY-15828
    Onvansertib

    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-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-109032
    Firuglipel

    GPR119 Metabolic Disease
    Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist.
  • HY-14857
    Carotegrast

    Integrin Inflammation/Immunology
    Carotegrast is an orally available α4 integrin receptor inhibitor with anti-inflammatories activities.
  • 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-114332
    GNE-8505

    MAP3K Neurological Disease
    GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK).
  • 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-109018
    Velagliflozin

    SGLT Metabolic Disease
    Velagliflozin is an orally available sodium-glucose cotransporter 2 (SGLT2) inhibitor, with anti-diabetic activity.
  • 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-W008235
    Fmoc-N-Me-Ala-OH

    Others Others
    Fmoc-N-Me-Ala-OH, an N-Fmoc-N-methyl amino acid, is available for the peptide-coupling reaction.
  • 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-14832
    Ataluren

    PTC124

    CFTR Autophagy Metabolic Disease
    Ataluren (PTC124) is an orally available CFTR-G542X nonsense allele inhibitor.
  • 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-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-W008558
    Fmoc-N-Me-Leu-OH

    Others Others
    Fmoc-N-Me-Leu-OH, an N-Fmoc-N-methyl amino acid, is available for the peptide-coupling reaction.
  • 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-120423
    AM-6538

    Cannabinoid Receptor Neurological Disease
    AM6538 is a long-acting, high affinity and pseudo-irreversible cannabinoid (CB) antagonist. AM6538 is a structural analog of rimonabant. AM6538 can be effectively used to evaluate the apparent efficacy of cannabinoid full and partial agonists. AM6538 may be useful in future studies that require temporary reductions in cannabinoid receptor availability.
  • HY-104048
    QC6352

    Histone Demethylase Cancer
    QC6352 is an orally available, selective and potent KDM4C inhibitor with an IC50 of 35 nM.
  • 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-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-B0177
    Tinidazole

    Bacterial Infection
    Tinidazole, an orally available antibacterial agent, is a 5-nitroimidazole with selective activity against anaerobic bacteria and protozoa.
  • 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-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-109082
    Cevidoplenib

    Syk Inflammation/Immunology
    Cevidoplenib is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential anti-inflammatory and immunomodulating activities.
  • 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-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-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-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-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-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-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-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-101782
    HSK0935

    SGLT Metabolic Disease
    HSK0935 is a potent, highly selective and orally available SGLT2 inhibitor with an IC50 of 1.3 nM. Antihyperglycemic activities.
  • 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-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-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-15837
    SAR-260301

    PI3K Cancer
    SAR-260301 is an orally available and selective PI3Kβ inhibitor with an IC50 of 23 nM.
  • 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-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-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-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-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-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-16265
    JI-101

    Ephrin Receptor PDGFR VEGFR Cardiovascular Disease Cancer
    JI-101 is an orally available multi-kinase inhibitor of VEGFR2, PDGFRβ and EphB4 with potent anti-cancer activity.
  • HY-32721
    Neratinib

    HKI-272

    EGFR Cancer
    Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.
  • 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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-14574
    PF-03814735

    Aurora Kinase VEGFR Cancer
    PF-03814735 is a potent, orally available, ATP-competitive and reversible aurora A and aurora B inhibitor with IC50s of 0.8 and 0.5 nM, respectively.
  • 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-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-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-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-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-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-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-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-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-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-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-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-18988
    ETC-159

    ETC-1922159

    Porcupine Wnt Cancer
    ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor. ETC-159 inhibits β-catenin reporter activity with an IC50 of 2.9 nM.
  • 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-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-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-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-124502
    UNC4203

    TAM Receptor FLT3 Cancer
    UNC4203 is a potent, orally available and highly selective MERTK inhibitor, with IC50 of 1.2 nM, 140 nM, 42 nM and 90 nM for MERTK, AXL, TYRO3 and FLT3, 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-15564
    AR 231453

    GPR119 Metabolic Disease
    AR 231453 is a potent, specific and orally available GPR119 agonist. AR 231453 can stimulate β-cell replication and improve islet graft function s.
  • 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-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-19957
    Zoligratinib

    Debio 1347; CH5183284

    FGFR Cancer
    Zoligratinib (Debio 1347) 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-A0176S
    Glisoxepid-d4

    Potassium Channel Metabolic Disease Cardiovascular Disease
    Glisoxepid-d4 is the deuterium labeled Glisoxepide. Glisoxepide, a sulphonamide derivative, is an orally available nonselective K(ATP) channel blocker, with antihyperglycemic activity and cardiovascular regulation effect.
  • 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-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-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-114330
    ZK824859

    PAI-1 Ser/Thr Protease 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-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-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-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-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-132549S
    Nilotinib-d3

    Bcr-Abl Autophagy Cancer
    Nilotinib-d3 (AMN107-d3) is the deuterium labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
  • 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-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-19822B
    Elacestrant S enantiomer dihydrochloride

    RAD1901 S enantiomer dihydrochloride

    Estrogen Receptor/ERR Cancer
    Elacestrant S enantiomer dihydrochloride (RAD1901 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-W127442
    Etzadroxil

    Ethyl 2-Ethylbutyrate

    Others Others
    Etzadroxil (Ethyl 2-Ethylbutyrate) is a volatile ester compound. Sulopenem Etzadroxil is an orally available ester prodrug form of Sulopenem, an antibiotic with broad-spectrum activities against Gram-positive and Gram-negative bacteria.
  • 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-101212
    Fadraciclib

    CYC065

    CDK Cancer
    Fadraciclib (CYC065) is a second-generation, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50s of 5 and 26 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-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-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-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-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-19822D
    Elacestrant (S enantiomer)

    RAD1901 S enantiomer

    Estrogen Receptor/ERR Cancer
    Elacestrant S enantiomer (RAD1901 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-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-12296
    Navtemadlin

    AMG 232; KRT-232

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. Navtemadlin binds to MDM2 with a Kd of 0.045 nM.
  • 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-14272S
    Ravuconazole-d4

    Fungal Infection
    Ravuconazole-d4 (BMS-207147-d4) is the deuterium labeled Ravuconazole. Ravuconazole (BMS-207147) is an orally available triazoleantifungle agent that potently inhibits a wide range of fungi.
  • 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-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-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-109061
    Lazertinib

    YH25448; GNS-1480

    EGFR Cancer
    Lazertinib (YH25448) 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-B1693
    Levomepromazine

    Methotrimeprazine

    5-HT Receptor Dopamine Receptor Neurological Disease
    Levomepromazine (Methotrimeprazine) 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-14870S
    Selexipag-d8

    Prostaglandin Receptor Cardiovascular Disease Endocrinology
    Selexipag-d8 (NS-304-d8) is the deuterium labeled Selexipag. Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor).
  • 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-17612
    Evenamide

    NW-3509

    Sodium Channel Neurological Disease
    Evenamide (NW-3509) is an orally available voltage-gated sodium channel (VGSC) blocker (Ki=0.4 µM) for the research of schizophrenia. Evenamide shows efficacy in a broad spectrum of rodent models of psychosis, mania, depression, and aggressiveness.
  • 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-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-123475A
    Sisunatovir hydrochloride

    RV521 hydrochloride

    RSV Infection
    Sisunatovir (RV521) hydrochloride, an orally available inhibitor of the RSV fusion (RSV-F) protein, exhibits potent efficacy against a panel of clinical isolates of RSV-A and RSV-B viruses, with IC50s of 1.4 nM and 1.0 nM, respectively.
  • 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-123475
    Sisunatovir

    RV521

    RSV Infection
    Sisunatovir (RV521), an orally available inhibitor of the RSV fusion (RSV-F) protein, exhibits potent efficacy against a panel of clinical isolates of RSV-A and RSV-B viruses, with IC50s of 1.4 nM and 1.0 nM, respectively.
  • 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-W017782
    2,5-Furandimethanol

    Others Others
    2,5-Furandimethanol is obtained from 5-Hydroxymethylfurfural. 5-hydroxymethylfurfural, as a building block, is considered an important intermediate due to its rich chemistry and potential availability from carbohydrates such as fructose, glucose, sucrose, cellulose and inulin.
  • HY-32721S
    Neratinib-d6

    EGFR Cancer
    Neratinib-d6 (HKI-272-d6) is the deuterium labeled Neratinib. Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.
  • HY-12206A
    Thioperamide maleate

    MR-12842 maleate

    Histamine Receptor Neurological Disease
    Thioperamide maleate (MR-12842 maleate) 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 maleate inhibits [ 3H]histamine synthesis with a Ki of 31 nM.
  • 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-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-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-101466A
    E7090 succinate

    FGFR Cancer
    E7090 succinate is an orally available, selective and potent inhibitor of FGFR1, FGFR2 and FGFR3 tyrosine kinase activities, with IC50 values of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/2/3/4, respectively.
  • 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-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-101466
    E7090

    FGFR Cancer
    E7090 is an orally available, potent, and selective FGFR inhibitor with IC50s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4, respectively.
  • 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 .
  • 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-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-138962
    κ-Carrageenan

    Others Cancer Inflammation/Immunology
    κ-Carrageenan is a natural polymer which predominantly available in red seaweeds. κ-Carrageenan is an effective drug carrier to deliver curcumin in cancer cells and to induce apoptosis. κ-carrageenan serves as a potential inflammatory agent that magnifies existing intestinal inflammation.
  • HY-12066
    GSK1292263

    GPR119 Metabolic Disease Inflammation/Immunology
    GSK-1292263 is an orally available GPR119 agonist with pEC50s of 6.9 and 6.7 for human and rat GPR119, respectively. GSK-1292263 can be used for the research of type 2 diabetes mellitus (T2DM).
  • HY-A0119
    Nitroprusside disodium dihydrate

    Sodium nitroprusside dihydrate; Sodium Nitroferricyanide(III) Dihydrate

    Autophagy Cardiovascular Disease Cancer
    Nitroprusside disodium dehydrate (Sodium nitroprusside dihydrate) is a vasodilator that available for the research of acute hypertension, heart failure. Nitroprusside disodium dehydrate induces autophagy in glutathione-depleted osteoblasts. Nitroprusside disodium dehydrate acts as a nitric oxide (NO) donor in a rat intestinal ischemia reperfusion model.
  • 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-101246
    RPI-1

    RET Cancer
    RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity.
  • HY-114452
    LY2940094

    BTRX-246040

    Opioid Receptor Neurological Disease
    LY2940094 (BTRX-246040) 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). LY2940094 reduces ethanol self-administration in animal models.
  • 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-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-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-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-19322B
    PIM-447 dihydrochloride

    LGH447 dihydrochloride

    Pim Apoptosis 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-111372A
    (Rac)-Finerenone

    (Rac)-BAY 94-8862

    Mineralocorticoid Receptor Cardiovascular Disease
    (Rac)-Finerenone ((Rac)-BAY 94-8862) is the racemate of Finerenone. Finerenone 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).
  • HY-15433A
    Quisinostat dihydrochloride

    JNJ-26481585 dihydrochloride

    HDAC Apoptosis Autophagy 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 and HDAC11, respectively. Quisinostat dihydrochloride has a broad spectrum antitumoral activity.
  • 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-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-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-13007B
    PF-3758309 dihydrochloride

    PAK Apoptosis Cancer
    PF-3758309 dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
  • HY-130149
    Adagrasib

    MRTX849

    Ras Cancer
    Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib 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-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-114452A
    LY2940094 tartrate

    BTRX-246040 tartrate

    Opioid Receptor Neurological Disease
    LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models.
  • HY-13038A
    Fostamatinib

    R788

    Syk FLT3 Inflammation/Immunology Cancer
    Fostamatinib (R788) is the oral prodrug of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
  • 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-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-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-13038B
    Fostamatinib disodium hexahydrate

    R788 disodium hexahydrate

    Syk FLT3 Cancer Inflammation/Immunology
    Fostamatinib (R788) disodium hexahydrate is the oral prodrug of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
  • 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-14532
    Brincidofovir

    CMX001; HDP-CDV

    CMV HSV Infection
    Brincidofovir (CMX001), the lipid-conjugated prodrug of Cidofovir (HY-17438), is an orally available, long-acting antiviral. Brincidofovir shows activity against a broad spectrum of DNA viruses including cytomegalovirus (CMV), adenovirus (ADV), varicella zoster virus, herpes simplex virus, polyomaviruses, papillomaviruses, poxviruses, and mixed double-stranded DNA virus infections.
  • HY-13038
    Fostamatinib Disodium

    R788(Disodium)

    Syk FLT3 Inflammation/Immunology Cancer
    Fostamatinib Disodium (R788 Disodium) is the oral prodrug of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
  • 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-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-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-B0113A
    Omeprazole sodium

    H 16868 sodium

    Proton Pump Autophagy Bacterial Phospholipase 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. Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
  • 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-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-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-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-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
    KL1333

    Mitochondrial Metabolism Metabolic Disease
    KL1333, a derivative of β-lapachone, is an orally available NAD+ modulator. KL1333 reacts with NAD(P)H:quinone oxidoreductase 1 (NQO1) as a substrate, resulting in increases in intracellular NAD+ levels via NADH oxidation. KL1333 improves energy metabolism and mitochondrial dysfunction in MELAS fibroblasts. KL1333 protects against Cisplatin-induced ototoxicity in mouse cochlear cultures.
  • HY-B0113
    Omeprazole

    H 16868

    Proton Pump Autophagy Bacterial Phospholipase 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.Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
  • 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-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-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-12067
    R406

    Syk FLT3 Apoptosis Cancer Inflammation/Immunology
    R406 is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 reduces immune complex-mediated inflammation. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
  • HY-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-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-12972
    Mavelertinib

    PF-06747775

    EGFR Cancer
    Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC).
  • 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-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-139554
    Zifanocycline

    KBP-7072

    Bacterial Infection
    Zifanocycline (KBP-7072) is a semisynthetic third-generation aminomethylcycline antibiotic that inhibits the normal function of the bacterial ribosome. Zifanocycline exhibits a broad spectrum of in vitro antibacterial activity against Gram-positive and Gram-negative bacteria, including many multidrug-resistant pathogens. Zifanocycline is available in both oral and injectable formulations. Zifanocycline can be used for the research of acute bacterial skin and skin structure infections, community-acquired bacterial pneumonia, and complicated intra-abdominal infections.
  • 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-136927
    MSA-2

    STING Cancer Inflammation/Immunology
    MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models.
  • 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-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-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-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-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-11108
    R406 free base

    Syk FLT3 Apoptosis Inflammation/Immunology Cancer
    R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 free base reduces immune complex-mediated inflammation. R406 free base also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
  • HY-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-107535
    AS1269574

    GPR119 TRP Channel Metabolic Disease
    AS1269574 is a potent, orally available GPR119 agonist, with an EC50 of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates TRPA1 cation channels to stimulate glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induces glucose-dependent insulin secretion from pancreatic β-cells only under high-glucose conditions. AS1269574 has the potential for the research of type 2 diabetes.
  • 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-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-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-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-112823
    Almonertinib

    HS-10296

    EGFR Cancer
    Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer.
  • HY-112823B
    Almonertinib hydrochloride

    HS-10296 hydrochloride

    EGFR Cancer
    Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer.
  • HY-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-109014
    Tenofovir exalidex

    CMX-157

    HIV HBV Nucleoside Antimetabolite/Analog Infection
    Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV.
  • 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.