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Results for "5�� reductase Inhibitors" in MCE Product Catalog:

1259

Inhibitors & Agonists

3

Screening Libraries

2

Biochemical Assay Reagents

32

Peptides

1

Inhibitory Antibodies

168

Natural
Products

Cat. No. Product Name Target Research Areas
  • 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-N2553
    4-Deoxypyridoxine 5'-phosphate

    LPL Receptor Metabolic Disease
    4-Deoxypyridoxine 5'-phosphate is a Pyridoxal 5'-phosphate analogue and a sphingosine 1-phosphate (S1P) inhibitor. 4-Deoxypyridoxine 5'-phosphate inhibits ornithine decarboxylase activity with a Ki of 60 μM. 4-Deoxypyridoxine 5'-phosphate is a competitive inhibitor of the activation of glutamate apodecarboxylase by Pyridoxal 5'-phosphate (Ki of 0.27 μM) and strongly inhibits glutamate-dependent labeling of glutamate decarboxylase.
  • HY-U00260
    CMI977

    LDP977

    Lipoxygenase Inflammation/Immunology
    CMI977 is a potent 5-Lipoxygenase (5-LO) inhibitor.
  • HY-114996
    ADAMTS-5 Inhibitor

    Others Inflammation/Immunology
    ADAMTS-5 Inhibitor is a potent ADAMTS-5 (aggrecanase-2) inhibitor, with an IC50 of 1.1 µM. ADAMTS-5 Inhibitor shows >40-fold functional selectivity over ADAMTS-4 (aggrecanase-1).
  • HY-U00156
    Lonapalene

    RS4317

    Lipoxygenase Inflammation/Immunology
    Lonapalene (RS4317) is a topically effective 5-lipoxygenase (5-LO) inhibitor.
  • HY-17511
    Potassium oxonate

    Potassium azaorotate; Potassium otastat

    Others Metabolic Disease
    Potassium oxonate is an inhibitor of uricase, inhibits the phosphorylation of 5-FU to 5-fluorouridine-5'-monophosphate catalyzed by pyrimidine phosphoribosyl-transferase in a different manner from allopurinol in cell-free extracts and intact cells in vitro.
  • HY-113957
    MPI_5a

    HDAC Cancer
    MPI_5a is a potent and selective HDAC6 inhibitor (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms. MPI_5a inhibits acyl-tubulin accumulation in cells with an IC50 value of 210 nM.
  • HY-P0081
    Bax inhibitor peptide V5

    BIP-V5; BAX Inhibiting Peptide V5

    Bcl-2 Family Cancer
    Bax inhibitor peptide V5 (BIP-V5) is a Bax-mediated apoptosis inhibitor, used for cancer treatment.
  • HY-N0172
    Caffeic acid

    TRP Channel Lipoxygenase Endogenous Metabolite Inflammation/Immunology Cancer
    Caffeic acid is an inhibitor of both TRPV1 ion channel and 5-Lipoxygenase (5-LO).
  • HY-90006
    5-Fluorouracil

    5-FU

    Nucleoside Antimetabolite/Analog HIV Apoptosis Endogenous Metabolite Cancer
    5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer. 5-Fluorouracil also inhibits HIV.
  • HY-12886
    Docebenone

    AA 861

    Lipoxygenase Ferroptosis Inflammation/Immunology
    Docebenone (AA 861) is a potent, selective and orally active 5-LO (5-lipoxygenase) inhibitor.
  • HY-101579
    LY 178002

    COX Lipoxygenase Phospholipase Inflammation/Immunology
    LY 178002 is a potent inhibitor of 5-lipoxygenase (5-LPO), phospholipase A2, with IC50 of 0.6 μM for 5-lipoxygenase, inhibits cellular production of LTB4 by human polymorphonuclear leukocytes, and shows relatively weak inhibition on cyclooxygenase.
  • HY-131446
    Chk1-IN-5

    Checkpoint Kinase (Chk) Cancer
    Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model.
  • HY-101853
    STAT5-IN-1

    STAT Cancer
    STAT5-IN-1 is a STAT5 inhibitor with an IC50 of 47 μM for STAT5β isoform.
  • HY-U00376
    5α-reductase-IN-1

    Others Metabolic Disease
    5α-reductase-IN-1 is an inhibitor of 5α-reductase, used for the research of patterned alopecia in combination with minoxidil.
  • HY-100148
    ICI 211965

    ZM-211965

    Lipoxygenase Inflammation/Immunology
    ICI 211965 (ZM-211965) is a selective and orally potent 5-Lipoxygenase (5-LPO) inhibitor.
  • HY-19969
    YM-90709

    Interleukin Related Inflammation/Immunology
    YM-90709 is a novel antagonist which inhibits the binding of interleukin-5 to interleukin-5 receptor.
  • HY-13012
    RepSox

    E-616452; SJN 2511

    TGF-β Receptor Cancer
    RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with IC50 of 4 nM.
  • HY-U00217
    AZD 4407

    ZD 4407

    Lipoxygenase Inflammation/Immunology
    AZD 4407 is a potent 5-lipoxygenase inhibitor.
  • HY-U00024
    Enazadrem

    Lipoxygenase Inflammation/Immunology
    Enazadrem is a 5-lipoxygenase inhibitor with antiinflammatory activities.
  • HY-14403
    ERK5-IN-1

    ERK Cancer
    ERK5-IN-1 is a potent ERK5 inhibitor with an IC50 of 87±7 nM. ERK5-IN-1 also inhibits LRRK2[G2019S] with an IC50 of 26 nM.
  • HY-15025A
    Sildenafil citrate

    UK-92480 citrate

    Phosphodiesterase (PDE) Autophagy Apoptosis Cardiovascular Disease Cancer
    Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.
  • HY-12056
    BIX02189

    MEK ERK Cancer
    BIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM.
  • HY-135386
    5β-​Dutasteride

    Drug Metabolite Inflammation/Immunology
    5β-Dutasteride is the S configuration of Dutasteride. 5β-Dutasteride is a potent inhibitor of both 5 alpha-reductase isozymes.
  • HY-U00347
    COX/5-LO-IN-1

    Atreleuton analog

    COX Lipoxygenase Inflammation/Immunology
    COX/5-LO-IN-1 (Atreleuton analog) is an inhibitor of cylooxygenase and 5-lipoxygenase (5-LO), used for the research of inflammatory and allergic disease states.
  • 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-13927
    Acetildenafil

    Phosphodiesterase (PDE)
    Acetildenafil is a derivative of the phosphodiesterase 5 (PDE5) inhibitor Sildenafil.
  • HY-112587
    MC3482

    Sirtuin Cancer
    MC3482 is a specific sirtuin5 (SIRT5) inhibitor.
  • HY-12055
    BIX02188

    MEK ERK Cancer
    BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM.
  • HY-112634
    SIRT5 inhibitor 1

    Sirtuin Others
    SIRT5 inhibitor 1 is a potent Human Sirtuin 5 deacylase inhibitor, with an IC50 of 0.11 μM.
  • HY-15881
    TCS JNK 5a

    JNK Inhibitor IX

    JNK Apoptosis Cancer
    TCS JNK 5a is a potent JNK3 inhibitor with a pIC50 of 6.7. TCS JNK 5a also inhibits JNK2 with a pIC50 of 6.5.
  • HY-N0198
    Nordihydroguaiaretic acid

    NDGA

    Lipoxygenase Autophagy Ferroptosis Cancer Neurological Disease
    Nordihydroguaiaretic acid is a 5-lipoxygenase (5LOX) (IC50=8 μM) and tyrosine kinase inhibitor.
  • HY-14930A
    Mirodenafil dihydrochloride

    SK-3530 dihydrochloride

    Phosphodiesterase (PDE) Others
    Mirodenafil dihydrochloride (SK3530 dihydrochloride) is a phosphodiesterase type 5 (PDE-5) inhibitor developed for the treatment of erectile dysfunction.
  • HY-15025
    Sildenafil

    UK-92480

    Phosphodiesterase (PDE) Autophagy Apoptosis Cardiovascular Disease Cancer
    Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.
  • HY-14164
    Zileuton

    A 64077; Abbott 64077

    Lipoxygenase Ferroptosis Inflammation/Immunology Cancer
    Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties.
  • HY-B1664
    Iopanoic acid

    Others Endocrinology
    Iopanoic acid is an inhibitor of 5'-Deiodinase and also an iodinated contrast medium.
  • HY-Y0051
    5-Hydroxymethylfurfural

    2-Hydroxymethyl-5-furfural; 2-Formyl-5-hydroxymethylfuran

    Fungal Others
    5-Hydroxymethylfurfural (2-Hydroxymethyl-5-furfural), derived from lignocellulosic biomass, inhibits yeast growth and fermentation as stressors.
  • 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-100422
    KDM5-IN-1

    Histone Demethylase Cancer
    KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
  • HY-13419
    U-73122

    Phospholipase Lipoxygenase Ferroptosis Inflammation/Immunology
    U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50of 1-2.1 µM for PLC.
  • HY-111644
    6-Methyl-5-azacytidine

    DNA Methyltransferase Cancer
    6-Methyl-5-azacytidine is a potent DNMT inhibitor.
  • HY-15588
    L189

    DNA/RNA Synthesis Cancer
    L189 is a novel human DNA ligase inhibitor, inhibits hLigI/III/IV with IC50 of 5/9/5 μM.
  • HY-111482
    SM 16

    TGF-β Receptor Cancer Inflammation/Immunology Cardiovascular Disease
    SM 16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively.
  • HY-W004924
    5-Hydroxymethyluracil

    Endogenous Metabolite Others
    5-Hydroxymethyluracil is a product of oxidative DNA damage. 5-Hydroxymethyluracil can be used as a potential epigenetic mark enhancing or inhibiting transcription with bacterial RNA polymerase.
  • 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-135383A
    (3S,5R)-Pitavastatin calcium

    Others Metabolic Disease
    (3S,5R)-Pitavastatin cacium is the enantiomer of Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor.
  • HY-17469
    Gimeracil

    Gimestat

    Others Cancer
    Gimeracil(Gimestat) is an inhibitor of dihydropyrimidine dehydrogenase (DPYD), which degrades pyrimidine including 5-fluorouracil in the blood; inhibits homologous recombination.
  • HY-14164A
    Zileuton sodium

    A 64077 sodium; Abbott 64077 sodium

    Lipoxygenase Inflammation/Immunology
    Zileuton sodium (A 64077 sodium) is a potent and selective inhibitor of 5-lipoxygenase, exhibiting inflammatory activities.
  • HY-12953
    R-268712

    TGF-β Receptor Cancer
    R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
  • HY-101826
    ER21355

    Phosphodiesterase (PDE) Cancer
    ER21355 is an inhibitor of phosphodiesterase 5 (PDE5), used for treatment of prostatic diseases.
  • HY-15000
    EMD534085

    Kinesin Cancer
    EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC50 of 8 nM.
  • HY-B0352
    Mirtazapine

    Org3770; 6-Azamianserin

    5-HT Receptor Neurological Disease
    Mirtazapine is a 5-HT receptor inhibitor. Mirtazapine is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent by blocking 5-HT2 and 5-HT3 receptors.
  • HY-10533
    Eniluracil

    5-Ethynyluracil; GW776C85

    Others Cancer
    Eniluracil (5-Ethynyluracil), a uracil analogue and a mechanism-based irreversible inhibitor of dihydropyrimidine dehydrogenase (DPD), increases the oral bioavailability of 5-fluorouracil (5-FU) to 100%, facilitating uniform absorption and predictable toxicity.
  • HY-121721
    Inz-5

    Fungal Infection
    Inz-5 is a fungal-selective mitochondrial cytochrome bc1 inhibitor. Inz-5 impairs fungal virulence and prevents the evolution of drug resistance.
  • HY-U00308
    5-Lipoxygenase-In-1

    Lipoxygenase Inflammation/Immunology Cardiovascular Disease
    5-Lipoxygenase-In-1 is a 5-Lipoxygenase inhibitor extracted from patent EP 331232 A2, table 4, compound example 4.10.
  • HY-15414
    Vortioxetine

    Lu AA 21004

    5-HT Receptor Serotonin Transporter Neurological Disease
    Vortioxetine is a inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT, with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
  • HY-123772
    CDK5 inhibitor 20-223

    CDK Cancer
    CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent.
  • HY-10997S
    Ibrutinib D5

    PCI-32765 D5

    Btk Cancer
    Ibrutinib D5 (PCI-32765 D5) is a deuterium labeled Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor.
  • HY-103464
    5'-Fluoroindirubinoxime

    5'-FIO

    FLT3 Cancer
    5'-Fluoroindirubinoxime (5’-FIO, compound 13), an Indirubin (HY-N0117) derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM.
  • HY-16592
    Brefeldin A

    BFA; Cyanein; Decumbin

    Autophagy CRISPR/Cas9 Mitophagy HSV Antibiotic Cancer Infection
    Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A is a CRISPR/Cas9 activator. Brefeldin A inhibits HSV-1 and has anti-cancer activity.
  • HY-15665
    XMD17-109

    ERK Cancer
    XMD17-109 is a novel, specific ERK-5 inhibitor, with an IC50 of 162 nM.
  • HY-100025A
    HLCL-61 hydrochloride

    Histone Methyltransferase Apoptosis Cancer
    HLCL-61 hydrochloride is a first-in-class inhibitor of protein arginine methyltransferase 5 (PRMT5).
  • HY-101496
    MT-DADMe-ImmA

    MTDIA; Methylthio-DADMe-Immucillin A

    Others Cancer
    MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM.
  • HY-100240
    Lodelaben

    SC-39026; Declaben

    Elastase Metabolic Disease Cardiovascular Disease
    Lodelaben is a human neutrophil elastase inhibitor with an IC50 and Ki of 0.5 and 1.5 μM, respectively.
  • HY-A0060
    Malotilate

    NKK 105

    Lipoxygenase Cancer
    Malotilate is a liver protein metabolism improved compound, which selectively inhibit the 5-lipoxygenase.
  • HY-10586
    5-Azacytidine

    Azacitidine; 5-AzaC; Ladakamycin

    Nucleoside Antimetabolite/Analog DNA Methyltransferase Bacterial Autophagy Antibiotic Cancer Infection
    5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes. 5-Azacytidine induces cell autophagy.
  • HY-P0222
    PKI(5-24)

    PKA Others
    PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
  • HY-107856
    5-Fluorouridine

    Others Cancer
    5-Fluorouridine is a metabolite of 5-fluorouracil with anticancer activity. 5-fluorouridine inhibits rRNA synthesis of human colon carcinoma cells. 5-Fluorouridine exhibits cytotoxic effect on growth of L1210 cells with an IC50 of 2 nM.
  • HY-15414A
    Vortioxetine hydrobromide

    Lu AA21004 hydrobromide

    5-HT Receptor Serotonin Transporter Neurological Disease
    Vortioxetine hydrobromide is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
  • HY-12803
    Fulvene-5

    NADPH Oxidase Reactive Oxygen Species Cancer
    Fulvene-5 is a potent NADPH oxidase 4 (NOX4) inhibitor with antioxidant properties. Fulvene-5 is a reactive oxygen species (ROS) modifying agent and a potent radioprotector. Fulvene-5 has antitumor activity.
  • HY-N2513
    β-Boswellic acid

    Lipoxygenase DNA/RNA Synthesis Cancer
    β-Boswellic acid is isolated from the gum resin of Boswellia serrate. β-Boswellic acid is a nonreducing-type inhibitor of the 5-lipoxygenase (5-LO) product formation either interacting directly with the 5-LO or blocking its translocation. β-Boswellic acid inhibits the synthesis of DNA, RNA and protein in human leukemia HL-60 cells.
  • HY-111926
    N6-Methyladenosine 5'-monophosphate disodium salt

    Others Metabolic Disease
    N6-Methyladenosine 5'-monophosphate disodium salt is an activator of glycogen phosphorylase b, with a Ka value of 22 µM. N6-Methyladenosine 5'-monophosphate disodium salt is a non-competitive rat adenylate kinase II inhibitor.
  • HY-100693
    SYP-5

    HIF/HIF Prolyl-Hydroxylase Cancer
    SYP-5 is a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis.
  • HY-110399
    Cirsiliol

    Lipoxygenase Neurological Disease
    Cirsiliol is a potent and selective 5-lipoxygenase inhibitor and a competitive low affinity benzodiazepine receptor ligand.
  • HY-12392
    Iprindole

    5-HT Receptor Metabolic Disease Neurological Disease
    Iprindole, a tricyclic indole antidepressant, is a weak inhibitor of the uptake of noradrenaline and 5-HT.
  • HY-100996
    10074-G5

    c-Myc Autophagy Cancer
    10074-G5 is an inhibitor of c-Myc-Max dimerization with an IC50 of 146 μM.
  • HY-18252
    Avanafil

    TA1790

    Phosphodiesterase (PDE) Cardiovascular Disease
    Avanafil(TA-1790) is a potent and highly selective phosphodiesterase-5(PDE-5) inhibitor(IC50=5.2 nM) for erectile dysfunction; lower selectivity against PDE1, PDE6, and PDE11.
  • HY-100933
    MY-5445

    Phosphodiesterase (PDE) Cardiovascular Disease
    MY-5445 is a specific phosphodiesterase type 5 (PDE5) inhibitor. MY-5445 selectively inhibits cGMP PDE with a Ki of 1.3 μM.
  • HY-101297
    Z-IETD-FMK

    Z-IE(OMe)TD(OMe)-FMK

    Caspase Cancer
    Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a selective and cell permeable caspase-8 inhibitor. Z-IETD-FMK is also a granzyme B inhibitor.
  • HY-135383
    (3S,5S)-Pitavastatin calcium

    Others Metabolic Disease
    (3S,5S)-Pitavastatin cacium is the 3-epimer of Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor.
  • HY-11108
    R406 free base

    Syk Apoptosis Inflammation/Immunology Cancer
    R406 free base is a potent Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3.
  • HY-P1111
    Lyn peptide inhibitor

    Src Interleukin Related Inflammation/Immunology
    Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of  asthma, allergic, and other eosinophilic disorders.
  • HY-W010918
    Adenosine 5'-diphosphate

    Adenosine diphosphate; ADP

    Endogenous Metabolite Others
    Adenosine 5'-diphosphate (Adenosine diphosphate) is a nucleoside diphosphate. Adenosine 5'-diphosphate is the product of ATP dephosphorylation by ATPases. Adenosine 5'-diphosphate induces human platelet aggregation and inhibits stimulated adenylate cyclase by an action at P2T-purinoceptors.
  • HY-P0222A
    PKI(5-24) TFA

    PKA Others
    PKI(5-24) TFA is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) TFA corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
  • HY-135780
    3'-Deoxyuridine-5'-triphosphate

    3'-dUTP

    Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Endogenous Metabolite Metabolic Disease
    3'-Deoxyuridine-5'-triphosphate (3'-dUTP) is a nucleotide analogue that inhibits DNA-dependent RNA polymerases I and II. 3'-Deoxyuridine-5'-triphosphate strongly and competitively inhibits the incorporations of UTP into RNA with a Ki value of 2.0 μM.
  • HY-102048
    STAT5-IN-2

    STAT Cancer
    STAT5-IN-2 is a STAT5 inhibitor with EC50s of 9 μM and 5 μM in K562 and KU812 cells, respectively. Potent antileukemic effect.
  • HY-15424
    5-Iodotubercidin

    NSC 113939; 5-ITu

    Adenosine Kinase Cancer
    5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC50 of 26 nM. 5-Iodotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by causing inactivation of phosphorylase and activation of glycogen synthase. 5-Iodotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC and Haspin.
  • HY-105024
    FPL 62064

    Lipoxygenase COX Inflammation/Immunology
    FPL 62064 is a potent 5-lipoxygenase (5-LOX) and COX dual inhibitor, with IC50 values of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and prostaglandin synthetase (cyclooxygenase), respectively. FPL 62064 has potent anti-inflammatory activity.
  • HY-13406
    TAK-779

    Takeda 779

    CCR HIV CXCR Infection Inflammation/Immunology Endocrinology
    TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.
  • HY-120137
    CMP-5

    Histone Methyltransferase Cancer
    CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected.
  • HY-50714
    Quiflapon sodium

    MK-591 sodium

    FLAP Apoptosis Inflammation/Immunology
    Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.
  • HY-13327
    Evacetrapib

    LY2484595

    CETP Cardiovascular Disease
    Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.
  • HY-100562
    Flopropione

    5-HT Receptor COMT Neurological Disease
    Flopropione is a 5-HT receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor. Flopropione also as an antispasmodic agent.
  • HY-101587
    PGS-IN-1

    KME-4

    PGE synthase Lipoxygenase Inflammation/Immunology
    PGS-IN-1 is a potent inhibitor of prostaglandin synthetase (PGS) with an IC50 of 0.28 μM; also inhibits 5-lipoxygenase with an IC50 of 1.05 μM.
  • HY-111643
    6-Amino-5-azacytidine

    Bacterial Infection
    6-Amino-5-azacytidine inhibits the growth of bacteria E. coli.
  • HY-123210
    Lodenafil

    Hydroxyhomosildenafil

    Phosphodiesterase (PDE) Endocrinology
    Lodenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).
  • HY-B0346
    Propylthiouracil

    6-n-Propylthiouracil; 6-Propyl-2-thiouracil; PTU

    Others Endocrinology
    Propylthiouracil(6-Propyl-2-thiouracil) is a thyroperoxidase and 5'-deiodinase inhibitor.
  • HY-15414S
    Vortioxetine D8

    Lu AA 21004 D8

    5-HT Receptor Serotonin Transporter Neurological Disease
    Vortioxetine D8 is a deuterium labeled Vortioxetine. Vortioxetine is an inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT, with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
  • HY-101157
    Propargyl-PEG5-acid

    ADC Linker Cancer
    Propargyl-PEG5-acid is a non-cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG5-acid can used to synthesize ADC inhibitors of Galectin-3.
  • HY-130802
    5-Aminouridine

    Fungal Influenza Virus Cancer Infection
    5-Aminouridine can modify nucleobases and can be incorporated into the target DNA. 5-Aminouridine exhibits a wide range of biological activity and it inhibits the growth of tumors, fungi and viruses.
  • HY-107777
    LLY-283

    Histone Methyltransferase Cancer
    LLY-283 is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM and a Kd of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity.
  • HY-101945
    A-69412

    Lipoxygenase Inflammation/Immunology
    A-69412 is a reversible, specific inhibitor of the hydrophilic 5-lipoxygenase (5-LO). A-69412 has the potential to treat asthma and ulcerative colitis, and possibly other inflammatory and allergic conditions.
  • HY-136144
    FIDAS-5

    Wnt Cancer
    FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 has anticancer activities.
  • HY-12220
    MM-102

    HMTase Inhibitor IX

    Histone Methyltransferase Cancer
    MM-102 (HMTase Inhibitor IX) is a potent WDR5/MLL interaction inhibitor, achieves IC50= 2.4 nM with an estimated Ki< 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.
  • HY-W011044
    CID 5951923

    KLF Cancer
    CID 5951923 is a potent inhibitor of Krüppel-like factor 5 (KLF5), with an IC50 of 603 nM. CID 5951923 can inhibit proliferation of cancer cells in vitro.
  • HY-13227
    SD-208

    TGF-β Receptor Cancer
    SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.
  • HY-101423
    NIH-12848

    Others Cardiovascular Disease
    NIH-12848 is a putative phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) inhibitor with an IC50 of 1 μM.
  • HY-19776
    3α-Aminocholestane

    Phosphatase Cancer
    3α-Aminocholestane is a selective SH2 domain-containing inositol-5′-phosphatase 1 (SHIP1) inhibitor with an IC50 of ~2.5 μM.
  • HY-P1111A
    Lyn peptide inhibitor TFA

    Src Interleukin Related Inflammation/Immunology
    Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor TFA can be used for study of  asthma, allergic, and other eosinophilic disorders.
  • HY-13032
    Molibresib

    I-BET762; GSK525762; GSK525762A

    Epigenetic Reader Domain Cancer
    Molibresib (I-BET762; GSK525762) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
  • HY-111471A
    JAK-IN-5 hydrochloride

    JAK Inflammation/Immunology
    JAK-IN-5 hydrochloride is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283.
  • HY-14775
    Nesbuvir

    HCV-796

    HCV Infection
    Nesbuvir is a nonnucleoside inhibitor of the hepatitis C virus (HCV) nonstructural protein 5B (NS5B) polymerase.
  • HY-11018
    Risperidone

    R 64 766

    5-HT Receptor Dopamine Receptor P-glycoprotein Neurological Disease
    Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-128729
    DNA2 inhibitor C5

    Others Cancer
    DNA2 inhibitor C5 is a potent, competitive and specific inhibitor of DNA2 nuclease activity with an IC50 of 20 μM. DNA2 inhibitor C5 inhibits nuclease, DNA dependent ATPase, helicase, and DNA binding activities of DNA2. DNA2 inhibitor C5 is a promising lead compound to develop sensitizers for cancer chemotherapeutics that cause replication stress.
  • HY-W014316
    5-Bromo-5-nitro-1,3-dioxane

    Bacterial Fungal Infection
    5-Bromo-5-nitro-1,3-dioxane, an antimicrobial compound, is effective against Gram-positive and Gram-negative bacteria and fungi, including yeast. 5-Bromo-5-nitro-1,3-dioxane inhibits enzyme activity and subsequent inhibition of microbial growth by the oxidation of essential protein thiol.
  • HY-12429
    Beclabuvir

    BMS-791325

    HCV Infection
    Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM. 
  • HY-100714A
    D-AP5

    D-APV; D-2-Amino-5-phosphonovaleric acid

    iGluR Neurological Disease
    D-AP5 (D-APV) is a selective and competitive NMDA receptor antagonist with a Kd of 1.4 μM. D-AP5 (D-APV) inhibits the glutamate binding site of NMDA receptors.
  • HY-117853
    Atreleuton

    ABT-761; VIA-2291

    Lipoxygenase Cardiovascular Disease
    Atreleuton (ABT-761) is a selective, reversible, and orally bioavailable 5-Lipoxygenase (5-LO) inhibitor. Atreleuton (ABT-761) exhibits potent and selective inhibition of leukotriene formation.
  • HY-111753A
    WDR5-IN-4 TFA

    Histone Methyltransferase Cancer
    WDR5-IN-4 TFA is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 TFA displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity.
  • HY-112698
    CA-5f

    Autophagy Apoptosis Cancer
    CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II (a marker to monitor autophagy) and SQSTM1 protein, and also increases ROS production. Anti-tumor activity.
  • HY-N0551
    Wedelolactone

    Caspase Lipoxygenase Apoptosis Cancer Inflammation/Immunology
    Wedelolactone, a natural product from Ecliptae herba, suppresses LPS-induced caspase-11 expression by directly inhibiting the IKK Complex. Wedelolactone inhibits 5-lipoxygenase (5-Lox) (IC50~2.5 μM) activity by an oxygen radical scavenging mechanism. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells via downregulation of PKCε without inhibiting Akt. Anti-cancer, anti-inflammatory, and antioxidant activities.
  • HY-N5011
    5,7-Dimethoxyflavone

    Cytochrome P450 Cancer Inflammation/Immunology
    5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor.
  • HY-N2008
    Luteolin 5-O-glucoside

    NO Synthase Reactive Oxygen Species Inflammation/Immunology
    Luteolin 5-O-glucoside, a major flavonoidfrom Cirsium maackii, possesses anti-inflammatory activity. Luteolin 5-O-glucoside inhibits LPS-induced NO production and t-BHP-induced ROS generation. Luteolin 5-O-glucoside suppresses the expression of iNOS and COX-2 in macrophages.
  • HY-15339
    CVT-313

    Cdk2 Inhibitor III

    CDK Cancer
    CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation.
  • HY-12220A
    MM-102 TFA

    HMTase Inhibitor IX TFA

    Histone Methyltransferase Cancer
    MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.
  • HY-14261
    Vilazodone Hydrochloride

    EMD 68843 Hydrochloride; SB659746A Hydrochloride

    5-HT Receptor Serotonin Transporter Neurological Disease
    Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
  • HY-B0407AS
    Chlorpromazine D6 hydrochloride

    Dopamine Receptor 5-HT Receptor Sodium Channel Potassium Channel Cancer Neurological Disease
    Chlorpromazine D6 hydrochloride is the deuterium labeled Chlorpromazine. Chlorpromazine is an inhibitor of dopamine receptor, 5-HT receptor, potassium channel, sodium channel.
  • HY-U00022
    RWJ 63556

    COX Lipoxygenase Inflammation/Immunology
    RWJ 63556 is an orally active COX-2 selective/5-lipoxygenase inhibitor, with anti-inflammatory activities.
  • HY-U00028
    T 82

    5-HT Receptor AChE Neurological Disease
    T 82 is a potent 5-HT3 antagonist and acetylcholinesterase (AChE) inhibitor, used for treatment of Alzheimer's Disease.
  • HY-14149
    Cisapride

    R 51619; (±)-Cisaprid

    5-HT Receptor Neurological Disease
    Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.
  • HY-B0141A
    Alpha-Estradiol

    Alfatradiol; Epiestradiol; Epiestrol

    5 alpha Reductase Endogenous Metabolite Inflammation/Immunology
    Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
  • HY-111931
    Indirubin-3'-monoxime-5-sulphonic acid

    CDK GSK-3 Cancer
    Indirubin-3'-monoxime-5-sulphonic acid is a potent and selective inhibitor of CDK1, CDK5, and GSK-3β with IC50s of 5 nM, 7 nM, and 80 nM, respectively.
  • HY-128342
    Complement C5-IN-1

    Complement System Inflammation/Immunology
    Complement C5-IN-1 (Compound 7) is a small-molecule inhibitor of complement component 5 protein (C5). Complement C5-IN-1 interacts with C5 to prevent its cleavage by the C5 convertase and blocks zymosan-induced the membrane-attack complex (MAC) deposition in 50% human whole blood with an IC50 of 0.77 µM.
  • HY-11018A
    Risperidone hydrochloride

    R 64 766 hydrochloride

    5-HT Receptor Dopamine Receptor P-glycoprotein Neurological Disease
    Risperidone hydrochloride (R 64 766 hydrochloride) 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-N2199
    Sotetsuflavone

    Others Cancer
    Sotetsuflavone is a potent inhibitor of DENV-NS5 RdRp (Dengue virus NS5 RNA-dependent RNA polymerase) with an IC50 of 0.16 uM, is the most active compound of this series .
  • HY-136774
    BCL6-IN-5

    Bcl-2 Family Cancer
    BCL6-IN-5 is a potent BCL6 inhibitor exacted from patent WO2018215801A1, example 1n, has a pIC50 of 5.82.
  • HY-100437
    HA15

    HSP Autophagy Apoptosis Cancer
    HA15 is a potent and specific inhibitor of ER chaperone BiP/GRP78/HSPA5, inhibits the ATPase activity of BiP, with anti-cancerous activity.
  • HY-13771
    Ursodiol

    Ursodeoxycholic acid; UDCA

    Endogenous Metabolite Metabolic Disease Cancer
    Ursodiol (Ursodeoxycholic acid; UDCA) is a potent liver-specific fatty acid transport protein 5 (FATP5) inhibitor. Ursodiol inhibit LCFA uptake by primary hepatocytes in a FATP5-dependent manner. Ursodiol reduces cholesterol absorption and is used to dissolve gallstones and has the potential for obesity-associated fatty liver disease research.
  • HY-14165
    Veliflapon

    BAY X 1005; DG-031

    FLAP Leukotriene Receptor Inflammation/Immunology Cardiovascular Disease
    Veliflapon (BAY X 1005; DG-031) is an orally active and selective 5-lipoxygenase activating protein (FLAP) inhibitor. Veliflapon inhibits the synthesis of the leukotrienes B4 and C4.
  • HY-N1942
    5-O-Demethylnobiletin

    5-Demethylnobiletin

    Lipoxygenase Leukotriene Receptor Inflammation/Immunology Neurological Disease Cancer
    5-O-Demethylnobiletin (5-Demethylnobiletin), a polymethoxyflavone isolated from Sideritis tragoriganum, is a direct inhibition of 5-LOX (IC50=0.1 μM), without affecting the expression of COX-2. 5-O-Demethylnobiletin (5-Demethylnobiletin) has anti-inflammatory activity, inhibits leukotriene B (4)(LTB4) formation in rat neutrophils and elastase release in human neutrophils with an IC50 of 0.35 μM.
  • HY-120400
    KDM5-C70

    Histone Demethylase Cancer
    KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels.
  • HY-15825
    IWP L6

    Porcn Inhibitor III

    Porcupine Cancer
    IWP L6 (Porcn Inhibitor III) is a Porcn inhibitor with an EC50 of 0.5 nM.
  • HY-112269
    Glutaminyl Cyclase Inhibitor 1

    Amyloid-β Neurological Disease
    Glutaminyl Cyclase Inhibitor 1 is a glutaminyl cyclase inhibitor with an IC50 of 0.5 μM.
  • HY-100235
    GSK591

    EPZ015866; GSK3203591

    Histone Methyltransferase Cancer
    GSK591 (EPZ015866) is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 4 nM.
  • HY-100130
    N-[(4-Aminophenyl)methyl]adenosine

    Adenosine Receptor Neurological Disease
    N-[(4-Aminophenyl)methyl]adenosine is a adenosine receptor inhibitor, with Ki of 29 nM for Rat ecto-5′-Nucleotidase.
  • HY-18625
    VEGFR-2-IN-5

    VEGFR Cancer
    VEGFR-2-IN-5 is a VEGFR2 inhibitor extracted from patent WO2013055780A1, Page 69.
  • HY-18625A
    VEGFR-2-IN-5 hydrochloride

    VEGFR Cancer
    VEGFR-2-IN-5 hydrochloride is a VEGFR2 inhibitor extracted from patent WO2013055780A1, Page 69.
  • HY-17357S
    Nepafenac D5

    AHR-9434 D5; AL-6515 D5

    COX Others
    Nepafenac D5 (AHR-9434 D5) is the deuterium labeled Nepafenac, which is a selective COX-2 inhibitor.
  • HY-13032B
    Molibresib besylate

    GSK 525762C; I-BET 762 besylate

    Epigenetic Reader Domain Cancer
    Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
  • HY-19956
    GI254023X

    GI4023; SRI028594

    MMP Cancer
    GI254023X is a potent MMP9 and ADAM10 inhibitor with IC50s of 2.5 and 5.3 nM, respectively.
  • HY-12983
    ALS-8112

    RSV Infection
    ALS-8112 is a potent and selective respiratory syncytial virus (RSV) polymerase inhibitor. The 5'-triphosphate form of ALS-8112 inhibits RSV polymerase with an IC50 of 0.02 μM.
  • HY-12632
    GNE 2861

    PAK Cancer
    GNE 2861 is a PAK inhibitor that displays group II selectivity. GNE 2861 inhibits PAK4, PAK5 and PAK6 with IC50s of 7.5, 36, 126 nM, respectively.
  • HY-100846
    JQEZ5

    Histone Methyltransferase Cancer
    JQEZ5 is a novel and potent EZH2 inhibitor.
  • HY-11018B
    Risperidone mesylate

    R 64 766 mesylate

    5-HT Receptor Dopamine Receptor P-glycoprotein Neurological Disease
    Risperidone mesylate(R 64 766 mesylate) is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-118283
    5-Hydroxylansoprazole

    AG1908

    Proton Pump Metabolic Disease
    5-Hydroxylansoprazole (AG1908) is an active metabolite of Lansoprazole in plasma. Lansoprazole is metabolized by CYP2C19 forming 5-Hydroxylansoprazole. Lansoprazole is a gastric proton-pump inhibitor and is effective in the treatment of various peptic diseases.
  • HY-108372
    Boc-C5-O-C5-O-C6-Cl

    PROTAC Linker 2

    PROTAC Linker Cancer
    Boc-C5-O-C5-O-C6-Cl (PROTAC Linker 2) is a PROTAC linker utilized to connect the respective tyrosine kinase inhibitor (TKI) to the E3 recruiting ligand.
  • HY-B0352S
    Mirtazapine D3

    Org3770 D3; 6-Azamianserin D3

    5-HT Receptor Neurological Disease
    Mirtazapine D3 (Org3770 D3; 6-Azamianserin D3) is a deuterium labeled Mirtazapine. Mirtazapine is a 5-HT receptor inhibitor. Mirtazapine is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent by blocking 5-HT2 and 5-HT3 receptors.
  • HY-19212
    S-2474

    COX Lipoxygenase Inflammation/Immunology
    S-2474 is an inhibitor of COX-2 and 5-lipoxygenase (5-LO), with IC50s of 11 nM and 27 μM for COX-2 and COX-1 in human intact cells, and used as a nonsteroidal anti-inflammatory drug.
  • HY-B0879A
    Suramin sodium salt

    Suramin hexasodium salt

    Phosphatase Sirtuin Reverse Transcriptase Topoisomerase Parasite Apoptosis Cancer Infection Cardiovascular Disease
    Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
  • HY-B0879
    Suramin

    Phosphatase Sirtuin Reverse Transcriptase Topoisomerase Parasite Apoptosis Cancer Infection Cardiovascular Disease
    Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
  • HY-P9949
    Reslizumab

    Sch 55700

    Interleukin Related Inflammation/Immunology
    Reslizumab (Sch 55700) is humanized monoclonal antibodies that target interleukin-5 (IL-5) for the treatment of eosinophilic asthma. Reslizumab is effective in neutralizing the function of IL-5. Reslizumab inhibits IL-5-dependent cell proliferation, with an IC50 value of approximately 91.1pM. Reslizumab has high binding affinity for human IL-5, with KD values of 109 pM and 4.3 pM in the the Biacore surface plasmon resonance and Kinetic Exclusion Assay, respectively.
  • HY-128341
    ERK5-IN-2

    ERK Cancer Cardiovascular Disease
    ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis.
  • HY-18305
    BMS-5

    LIMKi 3

    LIM Kinase (LIMK) Cancer
    BMS-5 (LIMKi 3) is a potent LIMK inhibitor with IC50s of 7 nM and 8 nM for LIMK1 and LIMK2, respectively.
  • HY-14443
    XMD8-92

    ERK Cancer
    XMD8-92 is a highly selective ERK5/BMK1 inhibitor with dissociation constant (Kd) value of 80 nM.
  • HY-136352
    Adenosine 5'-succinate

    Others Others
    Adenosine 5'-succinate is a chemically AMP-related compound and potently inhibits Denatonium benzoate/taste receptor activation of transducin.
  • HY-N2020
    Anacardic Acid

    Hydroginkgolic acid

    Histone Acetyltransferase Epigenetic Reader Domain Bacterial Cancer
    Anacardic Acid, extracted from cashew nut shell liquid, is a histone acetyltransferase inhibitor, inhibits HAT activity of p300 and PCAF, with IC50s of ∼8.5 μM and ∼5 μM, respectively.
  • 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-N7683
    Prunetin 5-O-β-D-glucopyranoside

    Glucosidase Metabolic Disease
    Prunetin 5-O-β-D-glucopyranoside is an isoflavone isolated from extracts of Potentilla astracanica. Prunetin 5-O-β-D-glucopyranoside is a potent and uncompetitive inhibitor of α-glucosidase, with an IC50 of 56.05 μg/mL. Prunetin 5-O-β-D-glucopyranoside can be used for the research of type-2 diabetes.
  • HY-N7514
    Strictosidinic acid

    5-HT Receptor Neurological Disease
    Strictosidinic acid, an orally active glycoside indole monoterpene alkaloid isolated from Psychotria myriantha leaves, inhibits precursor enzymes of 5-HT biosynthesis and reduces the 5-HT levels. Strictosidinic acid has peripheral analgesic and antipyretic activities in mice.
  • HY-B0215
    Acetylcysteine

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

    Reactive Oxygen Species Endogenous Metabolite Apoptosis Ferroptosis Influenza Virus Infection Neurological Disease
    Acetylcysteine (N-Acetylcysteine) is a mucolytic agent which reduces the thickness of the mucus. Acetylcysteine is a ROS inhibitor. Acetylcysteine is a cysteine precursor, prevents hemin-induced ferroptosis by neutralizing toxic lipids generated by arachidonate-dependent activity of 5-lipoxygenases. Acetylcysteine induces cell apoptosis. Acetylcysteine also has anti-influenza virus activities.
  • HY-N0451
    Acacetin

    5,7-Dihydroxy-4'-methoxyflavone

    Potassium Channel Cancer
    Acacetin (5,7-Dihydroxy-4'-methoxyflavone) was a 4.0-fold and 5.5-fold more potent inhibitor of BACE-1 than oleanolic acid and maslinic acid, respectively.
  • HY-112125
    KRN2

    Others Inflammation/Immunology
    KRN2 is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 100 nM. KRN2 has potential to treat NFAT5-mediated Chronic Arthritis.
  • HY-131284
    (S)-Dehydro Venlafaxine

    Others Others
    (S)-Dehydro Venlafaxine is an inactive S-enantiomer of Dehydro Venlafaxine. Dehydro Venlafaxine is an impurity of Venlafaxine hydrochloride. Venlafaxine hydrochloride (Wy 45030 hydrochloride) is a potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor.
  • HY-13746
    Sardomozide

    CGP 48664; SAM-486A

    Others Cancer
    Sardomozide is an S-adenosylmethionine decarboxylase (SAMDC) inhibitor with an IC50 of 5 nM.
  • HY-12495
    ISRIB (trans-isomer)

    PERK Autophagy Apoptosis Neurological Disease
    ISRIB (trans-isomer) is a potent inhibitor of PERK with an IC50 of 5 nM.
  • HY-19944
    Dimethylenastron

    Kinesin Cancer
    Dimethylenastron is a potent kinesin Eg5 inhibitor, with an IC50 of 200 nM.
  • HY-13746B
    Sardomozide dihydrochloride

    CGP 48664A

    Others Cancer
    Sardomozide dihydrochloride is an S-adenosylmethionine decarboxylase (SAMDC) inhibitor with an IC50 of 5 nM.
  • HY-B0196A
    Venlafaxine hydrochloride

    Wy 45030 hydrochloride

    Serotonin Transporter Neurological Disease
    Venlafaxine hydrochloride (Wy 45030 hydrochloride) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant.
  • HY-B1473
    Serotonin hydrochloride

    5-Hydroxytryptamine hydrochloride; 5-HT hydrochloride

    5-HT Receptor COMT Endogenous Metabolite Neurological Disease
    Serotonin hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.
  • HY-B0196
    Venlafaxine

    Wy 45030

    Serotonin Transporter Neurological Disease
    Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant.
  • HY-B1272
    Desipramine hydrochloride

    Dopamine Transporter Serotonin Transporter Neurological Disease Cancer
    Desipramine hydrochloride is an inhibitor of norepinephrine transporter (NET), 5-HT transporter (SERT) and dopamine transporter (DAT) with Kis of 4, 61 and 78,720 nM, respectively.
  • HY-W010791
    Adenosine 5'-diphosphate sodium salt

    Endogenous Metabolite Others
    Adenosine 5'-diphosphate (ADP) sodium salt is a nucleoside diphosphate, which is the product of ATP dephosphorylation by ATPases. Adenosine 5'-diphosphate sodium salt induces human platelet aggregation and inhibits stimulated adenylate cyclase by an action at P2T-purinoceptors.
  • HY-100014
    KDM5A-IN-1

    Histone Demethylase Cancer
    KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).
  • HY-117048
    PF-4191834

    PF-04191834

    Lipoxygenase Inflammation/Immunology
    PF-4191834 (PF-04191834) is an orally active, noniron chelating, and non-redox inhibitor of the 5-Lipoxygenase (5-LOX) (IC50=229 nM), displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes, and is effective in inflammation and pain.
  • HY-135194
    Risperidone E-oxime

    Others Others
    Risperidone E-oxime is an impurity of Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
  • HY-N0652
    2,3,5,4'-Tetrahydroxystilbene 2-O-β-D-glucoside

    2,3,4',5-Tetrahydroxystilbene 2-O-D-glucoside

    Others Others
    2,3,4',5-tetrahydroxystilbene 2-O-D-glucoside isolats from the roots of Polygonum species, inhibits the formation of 5-HETE, HHT and thromboxane B2, although less strongly.
  • HY-112390A
    Syk Inhibitor II

    Syk 5-HT Receptor Inflammation/Immunology
    Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect.
  • HY-111640
    3'-Azido-3'-deoxy-5-methylcytidine

    HIV Reverse Transcriptase Infection
    3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells.
  • HY-19205A
    CMI-392

    Lipoxygenase Inflammation/Immunology
    CMI-392 is a dual 5-lipoxygenese inhibitor and platelet-activating factor (PAF) receptor antagonist with IC50s of 100 and 10 nM, respectively.
  • HY-B0231AS
    Enalaprilat D5

    MK-422 D5

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Enalaprilat D5 (MK-422 D5) is the deuterium labeled Enalaprilat(MK-422), which is an angiotensin-converting enzyme (ACE) inhibitor.
  • HY-101563
    GSK3326595

    EPZ015938

    Histone Methyltransferase Cancer
    GSK3326595 (EPZ015938) is a potent, selective, reversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with an IC50 of 6.2 nM.
  • HY-B1122
    L-Cycloserine

    (S)-Cycloserine; (S)-4-Amino-3-isoxazolidone

    GABA Receptor HIV Neurological Disease Cancer
    L-Cycloserine ((S)-4-Amino-3-isoxazolidone) irreversibly inhibits GABA pyridoxal 5′-phosphate-dependent aminitransferase in E.
  • HY-19548A
    BEC hydrochloride

    Arginase Metabolic Disease
    BEC hydrochloride is a slow-binding and competitive Arginase II inhibitor with Ki of 0.31 μM and 30 nM at pH 7.5 and pH 9.5, respectively.
  • HY-124131
    DS-437

    Histone Methyltransferase Cancer Inflammation/Immunology
    DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC50s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3.
  • HY-128679
    TBK1/IKKε-IN-5

    IKK Cancer
    TBK1/IKKε-IN-5 (compound 1) is a dual TBK1 and IKKε inhibitor, with IC50 values of 1 nM and 5.6 nM for TBK1 and IKKε, respectively.
  • HY-13635A
    Finasteride acetate

    MK-906 acetate

    5 alpha Reductase Cancer
    Finasteride (MK-906) acetate is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride acetate has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride acetate can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia.
  • HY-13635
    Finasteride

    MK-906

    5 alpha Reductase Cancer
    Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia.
  • 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-10544
    Tegobuvir

    GS 333126; GS-9190

    HCV Infection
    Tegobuvir is a specific, covalent inhibitor of the HCV NS5B polymerase.
  • HY-103350
    CA-074

    Cathepsin Cancer Neurological Disease
    CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.
  • HY-19735
    KJ Pyr 9

    c-Myc Autophagy Cancer
    KJ Pyr 9 is an inhibitor of MYC with a Kd of 6.5 nM in in vitro assay.
  • HY-B0170
    Azatadine

    Histamine Receptor Inflammation/Immunology Endocrinology
    Azatadine is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.
  • HY-12176
    Aliskiren

    CGP 60536; CGP60536B; SPP 100

    Renin Autophagy Cardiovascular Disease Cancer
    Aliskiren(CGP 60536) is a direct renin inhibitor with IC50 of 1.5 nM.
  • HY-15971A
    AMD 3465

    GENZ-644494

    CXCR HIV Infection Endocrinology
    AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
  • HY-111540B
    (S)-IDO1-IN-5

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    (S)-IDO1-IN-5 (Example 1B) is an active S-isomer of IDO1-IN-5. (S)-IDO1-IN-5 binds to IDOL with an IC50 value less than 1.5 µΜ. IDO1-IN-5 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.
  • HY-133248
    Daclatasvir Impurity C

    Others Others
    Daclatasvir Impurity C is the impurity of Daclatasvir. Daclatasvir is a potent HCV NS5A protein inhibitor.
  • HY-133247
    Daclatasvir Impurity B

    Others Others
    Daclatasvir Impurity B is the impurity of Daclatasvir. Daclatasvir is a potent HCV NS5A protein inhibitor.
  • HY-100869A
    MM-589 TFA

    Histone Methyltransferase Cancer
    MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM.
  • HY-114189
    GW284543

    UNC10225170

    MEK Cancer
    GW284543 (UNC10225170) is a selective MEK5 inhibitor. GW284543 (UNC10225170) reduces pERK5, and decreases endogenous MYC protein.
  • HY-10431
    SB-431542

    TGF-β Receptor Cancer
    SB-431542 is a potent and selective inhibitor of ALK5/TGF-β type I Receptor with an IC50 value of 94 nM.
  • HY-15315
    Baricitinib

    LY3009104; INCB028050

    JAK Inflammation/Immunology
    Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
  • HY-N1957
    Gamma-Mangostin

    γ-Mangostin

    5-HT Receptor Metabolic Disease
    Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptors antagonist, purified from the fruit hull of the medicinal plant Garcinia mangostana. Gamma-Mangostin is a inhibitor of Transthyretin (TTR) fibrillization, it binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer. Gamma-Mangostin inhibits [3 H] spiperone binding to cultured rat aortic myocytes (IC50=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC50=0.32 µM) .
  • HY-121638A
    (5Z,2E)-CU-3

    Apoptosis Cancer
    (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.
  • HY-B0589C
    (3S,5S)-Atorvastatin

    Cytochrome P450 Metabolic Disease
    (3S,5S)-Atorvastatin is a inactive enantiomer of Atorvastatin. (3S,5S)-Atorvastatin can activate pregnane X receptor (PXR). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.
  • HY-15971
    AMD 3465 hexahydrobromide

    GENZ-644494 hexahydrobromide

    CXCR HIV Infection Endocrinology
    AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
  • HY-19807
    Indirubin-3'-monoxime

    Indirubin-3'-oxime

    GSK-3 Lipoxygenase Cancer
    Indirubin-3'-monoxime is a potent GSK-3β inhibitor, and weakly inhibits 5-Lipoxygenase, with IC50s of 22 nM and 7.8-10 µM, respectively; Indirubin-3'-monoxime also shows inhibitory activities against CDK5/p25 and CDK1/cyclin B, with IC50s of 100 and 180 nM.
  • 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-15315A
    Baricitinib phosphate

    LY3009104 phosphate; INCB028050 phosphate

    JAK Inflammation/Immunology
    Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) is a selective orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.
  • HY-15955
    CPI-360

    Histone Methyltransferase Apoptosis Cancer
    CPI-360 is a potent, selective EZH2inhibitor with IC50 of 0.5 nM and 2.5 nM nM for wt EZH2 and Y641N EZH2, respectively.
  • HY-A0061
    Trifluridine

    Trifluorothymidine; 5-Trifluorothymidine; TFT

    Thymidylate Synthase HSV Nucleoside Antimetabolite/Analog Cancer
    Trifluridine (Trifluorothymidine; 5-Trifluorothymidine; TFT) is an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral drug for herpes simplex virus (HSV) infection.
  • HY-15027
    5-Aminosalicylic Acid

    Mesalamine; 5-ASA; Mesalazine

    PPAR PAK NF-κB Endogenous Metabolite Inflammation/Immunology Cancer
    5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
  • HY-101298
    Paprotrain

    Kinesin Neurological Disease
    Paprotrain is a cell-permeable inhibitor of the kinesin MKLP-2, inhibits the ATPase activity of MKLP-2 with an IC50 of 1.35 μM and a Ki of 3.36 μM and shows a moderate inhibition activity on DYRK1A with an IC50 of 5.5 μM.
  • HY-13685
    Miltefosine

    HePC; Hexadecyl phosphocholine

    Akt HIV Infection Cancer
    Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity. Miltefosine is an inhibitor of CTP-phosphocholine cytidyltransferase (CCT).
  • HY-13817
    IU1

    Deubiquitinase Autophagy Cardiovascular Disease
    IU1 is a special Usp14 inhibitor with an IC50 of 4-5 μM.
  • HY-101846
    AX-15836

    ERK Cancer Inflammation/Immunology
    AX-15836 is a potent and selective ERK5 inhibitor with an IC50 of 8 nM.
  • HY-15984
    VER-50589

    HSP Apoptosis Cancer
    VER-50589 is a Hsp90 inhibitor, with an IC50 of 21 nM and a Kd of 4.5 nM.
  • HY-B0393
    Fudosteine

    Others Metabolic Disease
    Fudosteine is a novel mucoactive agent and a MUC5AC mucin hypersecretion inhibitor.
  • HY-B0170A
    Azatadine dimaleate

    Azatadine maleate

    Histamine Receptor Inflammation/Immunology Endocrinology
    Azatadine dimaleate is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.
  • HY-13502
    Mitoxantrone

    mitozantrone

    Topoisomerase PKC Cancer
    Mitoxantrone is a topoisomerase II inhibitor; also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM.
  • HY-A0116S
    Trandolaprilate D5

    Trandolaprilat D5; RU 44403 D5

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Trandolaprilate D5 is a deuterium labeled Trandolaprilate (Trandolaprilat). Trandolaprilate is an angiotensin-converting enzyme (ACE) inhibitor.
  • HY-13060
    ACHP Hydrochloride

    IKK-2 Inhibitor VIII

    IKK Inflammation/Immunology
    ACHP Hydrochloride (IKK-2 Inhibitor VIII) is a highly potent and selective IKK-β inhibitor with an IC50 of 8.5 nM.
  • HY-13502A
    Mitoxantrone dihydrochloride

    mitozantrone dihydrochloride

    Topoisomerase PKC Cancer
    Mitoxantrone dihydrochloride is a topoisomerase II inhibitor; also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM.
  • HY-122727
    STL127705

    DNA-PK Cancer
    STL127705 (Compound L) is a Ku 70/80 heterodimer protein inhibitor, inhibits Ku70/80-DNA interaction, with an IC50 of 3.5 μM. STL127705 also inhibits Ku-dependent activation of DNA-PKCS kinase (IC50, 2.5 μM).
  • HY-111540A
    (Rac)-IDO1-IN-5

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    (Rac)-IDO1-IN-5 (Example 1) is a racemate of IDO1-IN-5. IDO1-IN-5 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.
  • HY-N7656
    5,7,8-Trimethoxyflavone

    Norwogonin 5,7,8-trimethyl ether

    Others Inflammation/Immunology
    5,7,8-Trimethoxyflavone (Norwogonin 5,7,8-trimethyl ether), isolated from Andrographis echioides, inhibits NO with an IC50 of 39.1 μM. 5,7,8-Trimethoxyflavone has anti-inflammatory activity.
  • HY-10230S
    Midostaurin-D5

    PKC412-D5; CGP 41251-D5

    Others Cancer
    Midostaurin-D5 (PKC412-D5) is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM.
  • HY-16992A
    W-54011

    Complement System Reactive Oxygen Species Inflammation/Immunology
    W-54011 is a potent and orally active non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils with a Ki value of 2.2 nM. W-54011 also inhibits C5a-induced intracellular Ca 2+ mobilization, chemotaxis, and generation of ROS in human neutrophils with IC50s of 3.1 nM, 2.7 nM, and 1.6 nM, respectively.
  • HY-100943
    Cinanserin hydrochloride

    SQ 10643

    5-HT Receptor Influenza Virus Infection Inflammation/Immunology
    Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT2 receptor antagonist with a Ki of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT2 than for the 5-HT1 receptor (Ki of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro.
  • HY-14664C
    (3S,5R)-Fluvastatin sodium

    (3S,5R)-XU 62-320

    HMG-CoA Reductase (HMGCR) Cancer Cardiovascular Disease
    (3S,5R)-Fluvastatin sodium ((3S,5R)-XU 62-320) is the (3S,5R)-enantiomer of Fluvastatin. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway.
  • HY-102047B
    KDOAM-25 citrate

    Histone Demethylase Cancer
    KDOAM-25 citrate is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.
  • HY-10439
    HPGDS inhibitor 1

    PGE synthase Inflammation/Immunology
    HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX.
  • HY-15427
    GDC-0834

    Btk Inflammation/Immunology
    GDC-0834 is a potent and selective BTK inhibitor. GDC-0834 inhibits BTK with an in vitro IC50 of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC50 of 1.1 and 5.6 μM in mouse and rat, respectively.
  • HY-103687
    Abiraterone metabolite 1

    3β-OH-5α-Abi

    Drug Metabolite Cancer
    Abiraterone metabolite 1 is a 5β-reduced metabolite of abiraterone. Abiraterone, a steroidal drug, inhibits CYP17A1, blocks androgen synthesis and prolongs survival in prostate cancer.
  • HY-108045
    Lodenafil carbonate

    Phosphodiesterase (PDE) Endocrinology
    Lodenafil carbonate, a dimer that acts as a prodrug delivering Lodenafil in vivo, is an orally active phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).
  • HY-B0196B
    (S)-Venlafaxine

    Serotonin Transporter Cancer
    (S)-Venlafaxine is the (S)-configuration of Venlafaxine. Venlafaxine is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant agent.
  • HY-N3558
    Ceanothic acid

    Emmolic acid

    Others Cancer
    Ceanothic acid (Emmolic acid) is a ring-A homologue of betulinic acid. Ceanothic acid inhibits OVCAR-3, HeLa, and FS-5 cells with the cell survival of 68%, 65%, and 81%, respectively.
  • HY-111534
    SBI-115

    GPCR19 Others
    SBI-115 is a TGR5 (GPCR19) antagonist. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5.
  • HY-12318
    IBMX

    3-Isobutyl-1-methylxanthine; Isobutylmethylxanthine

    Phosphodiesterase (PDE) Inflammation/Immunology
    IBMX is a broad-spectrum phosphodiesterase (PDE) inhibitor, with IC50s of 6.5, 26.3 and 31.7 μM for PDE3, PDE4 and PDE5, respectively.
  • HY-N6256
    Ilexsaponin B2

    Phosphodiesterase (PDE) Cardiovascular Disease
    Ilexsaponin B2 is a saponin isolated from the root of Ilex pubescens Hook. et Arn. Ilexsaponin B2 is a potent phosphodiesterase 5 (PDE5) and PDEI inhibitor with IC50 values of 48.8 μM and 477.5 μM, respectively.
  • HY-111930
    5-Iodo-indirubin-3'-monoxime

    GSK-3 CDK Cancer
    5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively.
  • HY-13203
    NVP-TAE 226

    TAE226

    FAK Pyk2 IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    NVP-TAE 226 (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC50s of 5.5 nM and 140 nM, respectively. NVP-TAE 226 (TAE226) also effectively inhibits Pyk2 and insulin receptor (InsR) with IC50s of 3.5 nM and 44 nM, respectively.
  • HY-12814
    TH588

    DNA/RNA Synthesis Cancer
    TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM).
  • HY-18630A
    Ro 48-8071 fumarate

    Others Cancer
    Ro 48-8071 fumarate is an inhibitor of OSC (Oxidosqualene cyclase) with IC50 of appr 6.5 nM.
  • HY-101836
    DKM 2-93

    E1/E2/E3 Enzyme Cancer
    DKM 2-93 is a relatively selective inhibitor of UBA5 with an IC50 of 430 μM.
  • HY-17605
    Bictegravir

    GS-9883

    HIV HIV Integrase Infection
    Bictegravir is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.
  • HY-111472
    Porcn-IN-1

    Porcupine Cancer
    Porcn-IN-1 is potent porcupine inhibitor with an IC50 of 0.5±0.2 nM.
  • HY-12947
    GNE-3511

    MAP3K Cancer
    GNE-3511 is a dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM.
  • HY-13465
    VCH-916

    HCV Infection
    VCH-916 is a novel nonnucleoside HCV NS5B polymerase inhibitor.
  • HY-12177
    Aliskiren hemifumarate

    CGP 60536 hemifumarate; CGP60536B hemifumarate; SPP 100 hemifumarate

    Renin Autophagy Cardiovascular Disease Cancer
    Aliskiren hemifumarate(CGP 60536 hemifumarate) is a direct renin inhibitor with IC50 of 1.5 nM.
  • HY-W001179
    2,5-Dihydroxybenzoic acid

    Endogenous Metabolite FGFR Others
    2,5-Dihydroxybenzoic acid is a derivative of benzoic and a powerful inhibitor of fibroblast growth factors.
  • HY-101966
    NCT-503

    Others Cancer
    NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 2.5 µM.
  • HY-B0279
    Ramipril

    HOE-498

    Angiotensin-converting Enzyme (ACE) Apoptosis Cardiovascular Disease
    Ramipril (HOE-498) is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM.
  • HY-90009A
    Tadalafil

    IC-351

    Phosphodiesterase (PDE) Apoptosis Cardiovascular Disease
    Tadalafil (IC-351) is a PDE5 inhibitor with an IC50 value of 1.8 nM.
  • HY-12727
    EPZ015666

    GSK3235025

    Histone Methyltransferase Cancer
    EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 with an IC50 of 22 nM.
  • HY-15391
    Lucitanib

    E-3810

    VEGFR FGFR Cancer
    Lucitanib (E-3810) is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.
  • HY-12334
    HTH-01-015

    AMPK Cancer
    HTH-01-015 is a selective NUAK1/ARK5 inhibitor (IC50 is 100 nM). HTH-01-015 inhibits NUAK1 with >100-fold higher potency than NUAK2 (IC50 of >10 μM).
  • HY-18630
    Ro 48-8071

    Others Cancer
    Ro 48-8071 is an inhibitor of OSC (Oxidosqualene cyclase) with IC50 of appr 6.5 nM.
  • HY-117427
    D5D-IN-326

    Others Metabolic Disease
    D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC50s of 72 and 22 nM for rat and human D5D in enzymic and cell-based assays, respectively, has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in diet-induced obese C57BL/6J mice.
  • HY-109619
    D4-abiraterone

    Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite

    Androgen Receptor Cytochrome P450 Cancer
    D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
  • HY-14470
    Sibutramine hydrochloride monohydrate

    BTS 54-524 hydrochloride monohydrate

    Serotonin Transporter Potassium Channel Metabolic Disease Neurological Disease
    Sibutramine hydrochloride monohydrate is a novel 5-HT (serotonin) and noradrenaline reuptake inhibitor (SNRI). The IC50 for Sibutramine block of voltage-gated K + channel (KV)4.3 is 17.3 μM.
  • HY-100747
    PSB-12379

    CD73 Cancer
    PSB-12379, a nucleotide analogue, is a potent Ecto-5'-Nucleotidase (CD73) inhibitor with Kis of 9.03 nM (rat) and 2.21 nM (human).
  • HY-15982
    APY0201

    PIKfyve Interleukin Related Inflammation/Immunology
    APY0201 is a potent PIKfyve inhibitor, which inhibits the conversion of PtdIns3P to PtdIns(3,5)P2 in the presence of in the presence of [ 33P]ATP with an IC50 of 5.2 nM. APY0201 also inhibits IL-12/IL-23 production.
  • HY-111408
    EOAI3402143

    Deubiquitinase Cancer
    EOAI3402143 is a deubiquitinase (DUB) inhibitor, which inhibits dose-dependently inhibits Usp9x/Usp24 and Usp5.
  • HY-B1452
    Licofelone

    ML-3000

    COX Lipoxygenase Apoptosis Cancer Inflammation/Immunology
    Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins.
  • HY-32329
    Setiptiline

    Org-8282

    5-HT Receptor Adrenergic Receptor Neurological Disease
    Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
  • HY-108470
    Ro5-3335

    Others Cancer
    Ro5-3335, a benzodiazepine, acts as an inhibitor of core binding factor (CBF) leukemia. Ro5-3335 is a RUNX1-CBFβ interaction inhibitor that represses RUNX1/CBFB-dependent transactivation.
  • HY-10579
    Pluripotin

    SC1

    Ribosomal S6 Kinase (RSK) ERK Cancer
    Pluripotin is a dual inhibitor of ERK1 and RasGAP with KDs of 98 nM and 212 nM, respectively. Pluripotin also inhibits RSK1, RSK2, RSK3, and RSK4 with IC50s of 0.5, 2.5, 3.3, and 10.0 µM, respectively.
  • HY-10432A
    A 83-01 sodium salt

    TGF-β Receptor ALK Cancer
    A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
  • HY-15766A
    GNE-617 hydrochloride

    Nampt Cancer
    GNE-617 hydrochloride is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
  • HY-15766
    GNE-617

    Nampt Metabolic Disease Cancer
    GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
  • HY-17002
    Suplatast (Tosilate)

    IPD 1151T

    Interleukin Related Inflammation/Immunology
    Suplatast Tosilate (IPD 1151T) is a Th2 cytokine inhibitor that attenuates IL-2, IL-5 and IL-13 production and has no effect on IFN-γ production.
  • HY-N4289
    3-Epiursolic Acid

    Cathepsin Cancer
    3-Epiursolic Acid is a triterpenoid isolated from Myrtaceae, acts as a competitive inhibitor of cathepsin L (ICIC50, 6.5 μM; Ki, 19.5 μM), with no obvious effect on cathepsin B.
  • HY-125974
    HM03

    HSP Cancer
    HM03 is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 has anticancer activity.
  • HY-N1200
    Stigmasterol glucoside

    5 alpha Reductase Inflammation/Immunology
    Stigmasterol glucoside is a sterol isolated from P. urinaria with high antioxidant and anti-inflammatory activities, act as an inhibitor of 5α-reductase with an IC50 of 27.2 µM.
  • HY-18976
    UF010

    HDAC Cancer
    UF010 is a potent and selective HDAC inhibitor with IC50 ~0.06 μM, 0.1 μM, 0.5 μM and 1.5 μM for HDACs 3, 2, 1 and 8, respectively.
  • HY-111854
    SNIPER(ABL)-015

    SNIPER Bcr-Abl Cancer
    SNIPER(ABL)-015, conjugating GNF5 (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 5 μM .
  • HY-N0737
    Harmine hydrochloride

    Telepathine hydrochloride

    DYRK 5-HT Receptor Cancer Neurological Disease
    Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
  • HY-128067
    5-(N,N-Hexamethylene)-amiloride

    Hexamethylene amiloride; HMA

    Sodium Channel HIV Apoptosis Cancer Infection
    5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na +/H + exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively.
  • HY-10529
    Betulinic acid

    Lupatic acid; Betulic acid

    Apoptosis Topoisomerase HIV Autophagy Mitophagy NF-κB Endogenous Metabolite Cancer Infection Inflammation/Immunology
    Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties. Betulinic acid acts as a new activator of NF-kB.
  • HY-14768
    Favipiravir

    T-705

    DNA/RNA Synthesis Influenza Virus SARS-CoV Infection
    Favipiravir (T-705) is a potent viral RNA polymerase inhibitor, it is phosphoribosylated by cellular enzymes to its active form, Favipiravir-ribofuranosyl-5′-triphosphate (RTP). Favipiravir-RTP inhibits the influenza viral RNA-dependent RNA polymerase (RdRP) activity with an IC50 of 341 nM.
  • HY-A0006
    Pentostatin

    CI-825; Deoxycoformycin

    Adenosine Deaminase Cancer
    Pentostatin (CI-825; Deoxycoformycin) is an irreversible inhibitor of adenosine deaminase with Ki of 2.5 pM.
  • HY-13326
    ASP3026

    ALK Cancer
    ASP3026 is a novel and selective inhibitor for ALK (anaplastic lymphoma kinase) with IC50 of 3.5 nM.
  • HY-18253
    Udenafil

    DA8159

    Phosphodiesterase (PDE) Others
    Udenafil(DA8159) is a PDE5 inhibitor used in urology to treat erectile dysfunction.
  • HY-12069
    SB-743921

    Kinesin Cancer
    SB-743921 is a potent inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM.
  • HY-15683
    IDO5L

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO5L is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 67 nM.
  • HY-16699
    Nexturastat A

    HDAC Cancer
    Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM; no inhibition on other HDAC forms.
  • HY-13989
    b-AP15

    NSC 687852

    Deubiquitinase Apoptosis Cancer
    b-AP15 is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14.
  • HY-10455
    Carfilzomib

    PR-171

    Proteasome Autophagy Apoptosis Cancer
    Carfilzomib is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
  • HY-15317
    RI-1

    RAD51 Cancer
    RI-1 is a RAD51 inhibitor with IC50 ranging from 5 to 30 μM.
  • HY-101507
    Pico145

    HC-608

    TRP Channel Cancer
    Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.
  • HY-107139
    JNJ-10229570

    Melanocortin Receptor Endocrinology
    JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids. JNJ-10229570 inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC50 values of 270 nM and 200 nM, respectively.
  • HY-13613
    Dutasteride

    GG 745; GI 198745

    5 alpha Reductase Apoptosis Cancer
    Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT.
  • HY-12113
    Oprozomib

    ONX 0912; PR-047

    Proteasome Autophagy Cancer
    Oprozomib (ONX 0912; PR047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.
  • HY-16767
    Doravirine

    MK-1439

    HIV Reverse Transcriptase Infection
    Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively.
  • HY-12071
    LDN193189

    DM-3189

    TGF-β Receptor Cancer
    LDN193189 is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM).
  • HY-122243
    IU1-47

    Deubiquitinase Neurological Disease
    IU1-47 is a potent and specific USP14 inhibitor with an IC50 of 0.6 μM. IU1-47 inhibits IsoT/USP5 with an IC50 of 20 μM. IU1-47 induces tau elimination in cultured neurons.
  • HY-18353
    mTOR inhibitor-3

    mTOR Cancer
    mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
  • HY-19578B
    Isamoltane hemifumarate

    5-HT Receptor Adrenergic Receptor Neurological Disease
    Isamoltane hemifumarate is a selective antagonist of 5-HT1B receptor, with an IC50 of 39 nM for inhibits the binding of [ 125I]ICYP to 5-HT1B recognition sites in rat brain membranes. Isamoltane hemifumarate is also a β-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity.
  • HY-100421
    CPI-455

    Histone Demethylase Cancer
    CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents.
  • HY-P1453A
    CMD178 TFA

    STAT Inflammation/Immunology
    CMD178 (TFA) is a lead peptide that consistently reduces the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling. CMD178 (TFA) also is an inhibitor of STAT5 and inhibits Tregcells development.
  • HY-12071A
    LDN193189 Tetrahydrochloride

    TGF-β Receptor Cancer
    LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM).
  • HY-13998
    Dasabuvir

    ABT-333

    HCV Infection
    Dasabuvir (ABT-333) is a nonnucleoside inhibitor of the RNA-dependent RNA polymerase encoded by the HCV NS5B gene, inhibits recombinant NS5B polymerases derived from HCV genotype 1a and 1b clinical isolates, with IC50 between 2.2 and 10.7 nM.
  • HY-N0196
    Baicalein

    5,6,7-Trihydroxyflavone

    Xanthine Oxidase Influenza Virus Ferroptosis Cancer
    Baicalein (5,6,7-Trihydroxyflavone) is a xanthine oxidase inhibitor with an IC50 value of 3.12 mM.
  • HY-N0693
    Schisandrin A

    Schizandrin-A; Wuweizisu-A; Deoxyschizandrin

    Cytochrome P450 Autophagy Virus Protease Inflammation/Immunology Cancer
    Schisandrin A inhibits CYP3A activity with an IC50 of 6.60 μM and Ki of 5.83 μM, respectively.
  • HY-100285
    RD3-0028

    RSV Infection
    RD3-0028 is a potent and selective inhibitor of RSV replication with an EC50 of 4.5 μM.
  • HY-16902
    RO9021

    Syk Inflammation/Immunology
    RO9021 is an orally bioavailable, novel ATP-competitive inhibitor of SYK, with an average IC50 of 5.6 nM.
  • HY-100519
    NVS-PAK1-1

    PAK Cancer
    NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.
  • HY-14846A
    Litronesib Racemate

    LY2523355 Racemate

    Kinesin Others
    Litronesib Racemate (LY2523355 Racemate) is the racemate of litronesib. Litronesib is a selective, allosteric inhibitor of kinesin Eg5.
  • HY-101071A
    Monastrol

    (±)-Monastrol

    Kinesin Apoptosis Cancer
    Monastrol is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5 with an IC50 value of 14 μM.
  • HY-10818
    LY309887

    Antifolate Cancer
    LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 6.5 nM, and has antitumor activity.
  • HY-15333
    ZK-261991

    VEGFR Inflammation/Immunology
    ZK-261991 is an orally active VEGFR tyrosine kinase inhibitor with an IC50 of 5 nM for VEGFR2.
  • HY-19966
    K858 (Racemic)

    Kinesin Apoptosis Cancer
    K858 Racemic is an ATP-uncompetitive inhibitor of kinesin Eg5 with an IC50 of 1.3 μM.
  • HY-B0442
    Vardenafil

    Phosphodiesterase (PDE) Endocrinology
    Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction.
  • HY-B0442A
    Vardenafil hydrochloride

    Phosphodiesterase (PDE) Cardiovascular Disease
    Vardenafil hydrochloride is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride can be used for the research of erectile dysfunction.
  • HY-B0592S
    Trandolapril D5

    RU44570 D5

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Trandolapril D5 (RU44570 D5) is a deuterium labeled Trandolapril (RU44570). Trandolapril is an orally active angiotensin converting enzyme (ACE) inhibitor for hypertension and congestive heart failure (CHF).
  • HY-112468
    PNU112455A hydrochloride

    CDK Cancer
    PNU112455A hydrochloride is an ATP-competitive CDK2 and CDK5 inhibitor. PNU112455A hydrochloride binds to the ATP site of CDK2 and CDK5 with Kms of 3.6 and 3.2 μM, respectively.
  • HY-18770
    IDO-IN-5

    NLG-1489

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO-IN-5 (NLG-1489) is an indoleamine 2,3-dioxygenase (IDO) inhibitor extracted from patent WO WO2012142237A1, compound 1489, has an IC50 of 1-10 μM.
  • HY-13997
    Ombitasvir

    ABT-267

    HCV Infection
    Ombitasvir is a potent inhibitor of the hepatitis C virus protein NS5A, with EC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5, and 366 pM against genotype 6a.
  • HY-15789
    Elbasvir

    MK-8742

    HCV Infection
    Elbasvir (MK-8742) is a hepatitis C virus nonstructural protein 5A (HCV NS5A) inhibitor with EC50s of 4, 3 and 3 nM against genotype 1a, 1b, and 2a, respectively.
  • HY-15738
    GNF-5

    Bcr-Abl SARS-CoV Cancer
    GNF-5, an analogue of GNF-2 with improved pharmacokinetic properties, is a selective non-ATP competitive inhibitor of Bcr-Abl with an IC50 value of 0.22±0.1 uM (Wild type Abl).
  • HY-18931A
    NSC305787 hydrochloride

    Others Cancer
    NSC305787 hydrochloride is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, has antitumor activity.
  • HY-13067
    Tripterin

    Celastrol

    Proteasome Autophagy Mitophagy Apoptosis Inflammation/Immunology Cancer
    Tripterin (Celastrol) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
  • HY-15679
    PI4KIII beta inhibitor 3

    PI4K Cancer
    PI4KIII beta inhibitor 3 is a novel and high effective PI4KIIIβ inhibitor with IC50 of 5.7 nM.
  • HY-18931
    NSC305787

    Others Cancer
    NSC305787 is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, has antitumor activity.
  • HY-112164
    IACS-8968

    IDO/TDO Inhibitor

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IACS-8968 (IDO/TDO Inhibitor) is a dual IDO and TDO inhibitor, with pIC50s of 6.43 for IDO and <5 for TDO, respectively.
  • HY-100769
    YL0919

    5-HT Receptor Neurological Disease
    YL0919 is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective 5-HT1A receptor agonist (Ki=0.19 nM). YL0919 inhibits the uptake of [ 3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC50s of 1.78 nM and 1.93 nM, respectively. YL0919 shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder.
  • HY-10895
    SB-334867

    SB 334867A

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.
  • HY-111932
    Indirubin-5-sulfonate

    CDK GSK-3 Cancer
    Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively. Indirubin-5-sulfonate also shows inhibitory activity against GSK-3β.
  • HY-108256
    Melitracen hydrochloride

    5-HT Receptor Neurological Disease
    Melitracen hydrochloride is an orally active biphasic antidepressant and antianxiety agent. Melitracen hydrochloride can inhibit the uptake of Norepinephrine and 5-HT (serotonin) through the presynaptic membrane inducing the increase of monoamine transmitters in synaptic space.
  • HY-14882A
    Cenicriviroc Mesylate

    TAK-652 Mesylate; TBR-652 Mesylate

    CCR HIV Infection Inflammation/Immunology Endocrinology
    Cenicriviroc Mesylate (TAK-652 Mesylate) is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.
  • HY-12530
    Velpatasvir

    GS-5816

    HCV Cancer
    Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons.
  • HY-10792A
    Eplivanserin (mixture)

    SR-46349 (mixture)

    Serotonin Transporter 5-HT Receptor Neurological Disease
    Eplivanserin mixture (SR-46349 mixture) is a selective serotonin reuptake inhibitor and a 5-HT2A receptor antagonist, extracted from patent WO 2005/002578 A1.
  • HY-19981
    Derazantinib

    ARQ-087

    FGFR Cancer
    Derazantinib (ARQ-087) is an ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC50s of 4.5, 1.8, and 4.5 nM, respectively.
  • HY-10118
    Filibuvir

    HCV Infection
    Filibuvir is a potent, selective non-nucleoside inhibitor (NNI) of the HCV nonstructural 5B protein (NS5B) RNA-dependent RNA polymerase, and it binds noncovalently in the “Thumb 2” pocket of NS5B. In vitro, filibuvir is equipotent against genotype 1a and 1b replicons, with an EC50 of 59 nM.
  • HY-114205
    TP-238

    Epigenetic Reader Domain Cancer
    TP-238 is a potent and selective dual CECR2/BPTF probe with pIC50 values of 7.5 and 6.5, respectively. TP-238 also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases.
  • HY-12302
    Kenpaullone

    9-Bromopaullone; NSC-664704

    CDK GSK-3 Cancer
    Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively.
  • HY-10580
    GSK 3 Inhibitor IX

    6-Bromoindirubin-3'-oxime; BIO; MLS 2052

    GSK-3 CDK Apoptosis Cancer
    GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.
  • HY-17624
    Framycetin

    Neomycin B; Fradiomycin B

    Bacterial Infection
    Framycetin (Neomycin B), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections.
  • HY-111357
    Antifungal agent 2

    Fungal Infection
    Antifungal agent 2 is a broad-spectrum fungal inhibitor which inhibits growth of pertinent species of Candida, Cryptococcus, and Aspergillus at a concentration as low as 0.5 μg/mL.
  • HY-W018931
    DDR Inhibitor

    Discoidin Domain Receptor Cancer
    DDR Inhibitor is a potent discoidin domain receptor (DDR) inhibitor, with an IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM.
  • HY-10129
    Veliparib

    ABT-888

    PARP Autophagy Cancer
    Veliparib (ABT-888) is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively.
  • HY-133246
    Monodes(N-carboxymethyl)valine Daclatasvir

    Daclatasvir Impurity A

    HCV Infection
    Monodes(N-carboxymethyl)valine Daclatasvir (Daclatasvir Impurity A) is the main degradation product of Daclatasvir. Daclatasvir is a potent HCV NS5A protein inhibitor.
  • HY-12304
    IOX1

    Histone Demethylase Cancer
    IOX1, 5-Carboxy-8-hydroxyquinoline, is a potent broad‐spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 inhibits KDM4C, KDM4E, KDM2A, KDM3A and KDM6B with IC50 values of 0.6 μM, 2.3 μM, 1.8 μM, 0.1 μM and 1.4 μM, respectively. IOX1 also inhibits ALKBH5.
  • HY-N0401A
    (Z)-Ligustilide

    Bacterial Infection Metabolic Disease
    (Z)-Ligustilide is extracted from Ligusticum chuanxiong Hort, has antimicrobial and antifungal activity, exhibits an average antifungal score of 5.6. (Z)-Ligustilide inhibits the expression of FATP5 and DGAT, inhibits fatty acid uptake and esterification in mice and has potential as therapeutics for nonalcoholic fatty liver disease (NAFLD) .
  • HY-100975
    TB5

    Monoamine Oxidase Neurological Disease
    TB5 is a potent, selective and reversible inhibitor of hMAO-B with a Ki value of 0.11±0.01 μM.
  • HY-14846
    Litronesib

    LY2523355

    Kinesin Cancer
    Litronesib (LY2523355) is a selective mitosis-specific kinesin Eg5 inhibitor, with antitumor activity.
  • HY-10992
    AZD-7762

    Checkpoint Kinase (Chk) Cancer
    AZD-7762 is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
  • HY-10997A
    Ibrutinib Racemate

    PCI-32765 Racemate

    Btk Cancer
    Ibrutinib Racemate (PCI-32765 Racemate) is the racemate of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with IC50 value of 0.5 nM.
  • HY-128561
    AM12

    TRP Channel Cardiovascular Disease
    AM12 inhibits Lanthanide-evoked TRPC5 activity with an IC50 of 0.28 μM.
  • HY-10993
    Adavosertib

    AZD1775; MK-1775

    Wee1 Cancer
    Adavosertib (AZD-1775; MK-1775) is a potent Wee1 inhibitor with an IC50 of 5.2 nM.
  • HY-10550A
    Tariquidar methanesulfonate, hydrate

    XR9576 methanesulfonate, hydrate

    P-glycoprotein Cancer
    Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) is a potent and specific inhibitor of P-glycoprotein (P-gp) with a Kd of 5.1 nM.
  • HY-19328
    ACY-775

    HDAC Neurological Disease Cardiovascular Disease
    ACY-775 is a potent and selective inhibitor of the of histone deacetylase 6 (HDAC6) with an IC50 of 7.5 nM.
  • HY-17399
    Racecadotril

    Acetorphan

    Neprilysin Neurological Disease
    Racecadotril (acetorphan), a potent enkephalinase inhibitor (IC50= 4.5 uM), protects endogenous enkephalins from degradation.
  • HY-16691
    AK-7

    Sirtuin Neurological Disease
    AK-7 is a selective cell- and brain-permeable SIRT2 inhibitor, with an IC50 of 15.5 μM.
  • HY-16937
    ISA-2011B

    Others Cancer
    ISA-2011B is a PIP5K1α inhibitor with promising anticancer effects .
  • HY-12082A
    GSK369796 Dihydrochloride

    Potassium Channel Parasite Infection
    GSK369796 Dihydrochloride is an affordable and effective antimalarial and inhibits hERG potassium ion channel repolarization with an IC50 of 7.5 μM.
  • HY-N1201
    Apigenin

    4',5,7-Trihydroxyflavone; Apigenol; C.I. Natural Yellow 1

    Autophagy Cytochrome P450 Inflammation/Immunology Cancer
    Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a Ki of 2 μM.
  • HY-19994
    ML264

    KLF Cancer
    ML264 is an antitumor agent that potently and selectively inhibits Krüppel-like factor five (KLF5) expression.
  • HY-101465
    AK-1

    Sirtuin Neurological Disease
    AK-1 is a potent, specific and cell-permeable SIRT2 inhibitor, with an IC50 of 12.5 μM.
  • HY-135385
    Dihydro Dutasteride

    Drug Metabolite Inflammation/Immunology
    Dihydro Dutasteride is a metabolite of Dutasteride. Dutasteride is a potent inhibitor of both 5 alpha-reductase isozymes.
  • HY-101774
    CSF1R-IN-1

    c-Fms Cancer
    CSF1R-IN-1 is a CSF1R inhibitor with an with an IC50 of 0.5 nM.
  • HY-10997
    Ibrutinib

    PCI-32765

    Btk Ligand for Target Protein for PROTAC Cancer
    Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
  • HY-B0165A
    Pravastatin sodium

    CS-514 sodium

    HMG-CoA Reductase (HMGCR) Autophagy Ferroptosis Cardiovascular Disease Cancer
    Pravastatin sodium (CS-514 sodium) is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
  • HY-W015422
    1,5-Isoquinolinediol

    PARP Metabolic Disease
    1,5-Isoquinolinediol is a potent PARP inhibitor, with an IC50 of 0.18-0.37 µM. 1,5-Isoquinolinediol attenuates diabetes-induced NADPH oxidase-derived oxidative stress in retina.
  • HY-15745
    PSI-7409

    HCV Cancer
    PSI-7409 is the active 5'-triphosphate metabolite of Sofosbuvir (PSI-7977). Sofosbuvir (PSI-7977) is a selective and highly active nucleotide analog inhibitor of HCV.
  • HY-15802
    WZ4003

    AMPK Cancer
    WZ4003 is the first potent and highly specific NUAK kinase inhibitor with IC50 of 20 nM/100 nM for NUAK1 (ARK5)/NUAK2, without significant inhibition on other 139 kinases.
  • HY-107790
    5-Methoxyflavone

    DNA/RNA Synthesis Neurological Disease
    5-Methoxyflavone, belonged to Flavonoid family, is a DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. possess central nervous system (CNS) depressant effect mediated through the ionotropic GABAA receptors.
  • HY-119819
    Psicofuranine

    Bacterial Parasite Antibiotic Infection
    Psicofuramine a nucleoside antibiotic and has the inhibition of xanthosine 5'-phosphate aminase. Psicofuranine also specifically inhibits GMP synthase, and interrupts parasite growth. Psicofuranine exhibits a dose-dependent inhibition of P. falciparum growth.
  • HY-101564
    JNJ-64619178

    Histone Methyltransferase Cancer
    JNJ-64619178 is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.14 nM. JNJ-64619178 has potent activity In lung cancer.
  • HY-111540
    IDO1-IN-5

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO1-IN-5 is a potent, selective and brain penetrated inhibitor of IDO1 activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.
  • HY-76948
    5-R-Rivaroxaban

    Factor Xa Cardiovascular Disease
    5-R-Rivaroxaban is (R)-enantiomer of Rivaroxaban. Rivaroxaban (BAY 59-7939) is a highly potent and selective, direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).
  • HY-13962
    SGI-1027

    DNA Methyltransferase Apoptosis Cancer
    SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.
  • HY-15463
    Imatinib

    STI571; CGP-57148B

    Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy Cancer
    Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
  • HY-14664DS
    (3S,5R)-Fluvastatin D6

    (3S,5R)-XU 62-320 free acid D6

    Autophagy Cancer Cardiovascular Disease
    (3S,5R)-Fluvastatin D6 is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway.
  • HY-14664B
    (3R,5S)-Fluvastatin

    (3R,5S)-XU 62-320 free acid

    HMG-CoA Reductase (HMGCR) Autophagy Cancer Cardiovascular Disease
    (3R,5S)-Fluvastatin is the 3R,5S-isomer Fluvastatin. Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway.
  • HY-14664CS
    (3S,5R)-Fluvastatin D6 sodium

    (3S,5R)-XU 62-320 D6

    HMG-CoA Reductase (HMGCR) Cancer Cardiovascular Disease
    (3S,5R)-Fluvastatin D6 sodium is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway.
  • HY-13521
    SB-505124

    TGF-β Receptor Cancer
    SB-505124 is a selective inhibitor of TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
  • HY-15945
    DBeQ

    JRF 12

    p97 Autophagy Apoptosis Cancer
    DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC50 value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC50 of 11.5 μM.
  • HY-17624A
    Framycetin sulfate

    Neomycin B sulfate; Fradiomycin B sulfate

    Bacterial Infection
    Framycetin sulfate (Neomycin B sulfate), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin sulfate competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin sulfate inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin sulfate, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections.
  • HY-10895A
    SB-334867 free base

    SB334867A free base

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.
  • HY-129039
    Butyrolactone 3

    Histone Acetyltransferase Cancer
    Butyrolactone 3 is a specifical small-molecule inhibitor of the histone acetyltransferase Gcn5 (IC50=100 μM), which has a high affinity to the Gcn5 enzyme comparable to that of its natural substrate, histone H3. Butyrolactone 3 shows weak inhibitory on CBP (IC50=0.5 mM)
  • HY-10432
    A 83-01

    ALK TGF-β Receptor Cancer
    A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
  • HY-15769A
    WHI-P180 hydrochloride

    Janex 3 hydrochloride

    RET VEGFR EGFR Cancer
    WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively.
  • HY-70035
    Otamixaban

    FXV673

    Factor Xa Cardiovascular Disease
    Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.
  • HY-15769
    WHI-P180

    Janex 3

    VEGFR EGFR Cancer
    WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively.
  • HY-10165
    PSI-6130

    R 1656

    HCV Infection
    PSI-6130 is a potent and selective inhibitor of HCV NS5B polymerase, and inhibits HCV replication with a mean IC50 of 0.6 μM. 
  • HY-75800
    Lomibuvir

    VX-222

    DNA/RNA Synthesis HCV Infection
    Lomibuvir (VX-222), a selective, non-nucleoside polymerase inhibitor, targets thumb pocket 2 of the HCV NS5B polymerase (RdRp) with a Kd of 17 nM. Lomibuvir inhibits the 1b/Con1 HCV subgenomic replicon with an EC50 of 5.2 nM. Lomibuvir preferentially inhibits elongative RNA synthesis rather than de novo-initiated RNA synthesis.
  • HY-125801
    3-Oxo-5β-cholanoic acid

    Dehydrolithocholic acid; 3-oxoLCA

    ROR Inflammation/Immunology
    3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid), a bile acid metabolite, inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd=1.13 μM).
  • HY-15874A
    Fiboflapon sodium

    GSK2190915 sodium salt; AM-803 sodium

    FLAP Leukotriene Receptor Inflammation/Immunology
    Fiboflapon sodium (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
  • HY-N0737A
    Harmine

    Telepathine

    DYRK 5-HT Receptor Cancer Neurological Disease
    Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
  • HY-N1549
    Prunin

    Naringenin 7-0-glucoside

    Enterovirus Phosphatase Infection Metabolic Disease
    Prunin is a potent inhibitor of human enterovirus A71 (HEVA71). Prunin shows strong inhibitory activity against protein tyrosine phosphatase 1B (PTP1B), with an IC50 of 5.5 µM.
  • HY-N1673
    2,5-Dihydroxybenzaldehyde

    Gentisaldehyde

    Bacterial Infection
    2,5-Dihydroxybenzaldehyde (Gentisaldehyde) is a naturally occurring antimicrobial that inhibits the growth of Mycobacterium avium subsp. paratuberculosis. 2,5-Dihydroxybenzaldehyde is active against S. aureus strains with a MIC50 of 500 mg/L.
  • HY-12036
    GSK1059615

    PI3K mTOR Apoptosis Cancer
    GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.
  • HY-15874
    Fiboflapon

    GSK2190915; AM-803

    FLAP Leukotriene Receptor Inflammation/Immunology
    Fiboflapon (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
  • HY-B1902
    Diaveridine

    EGIS-5645

    Antifolate Bacterial Infection
    Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.
  • HY-122524
    7-Methylguanosine

    Nucleoside Antimetabolite/Analog Endogenous Metabolite Inflammation/Immunology
    7-Methylguanosine is a novel cNIIIB nucleotidase inhibitor with IC50 value of 87.8 ± 7.5 µM.
  • HY-13804
    PP1

    AGL 1872; EI 275

    Src Apoptosis Cancer
    PP1 is a potent, and Src family-selective tyrosine kinase inhibitor with IC50 of 5 and 6 nM for Lck and Fyn, respectively.
  • HY-B0331AS
    Enalapril D5 maleate

    MK-421 D5 maleate

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Enalapril (MK-421) D5 maleate is deuterium labeled Enalapril, which is an angiotensin converting enzyme (ACE) inhibitor.
  • HY-101856
    BMS-986142

    Btk Inflammation/Immunology
    BMS-986142 is a potent and highly selective reversible inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 0.5 nM.
  • HY-13282
    GANT 58

    NSC 75503

    Gli Cancer
    GANT 58 is a potent Gli antagonist that inhibits GLI1-induced transcription with IC50 of 5 μM.
  • HY-N0002
    (-)-Epicatechin gallate

    Epicatechin gallate; ECG; (-)-Epicatechin 3-O-gallate

    COX Autophagy Virus Protease Cancer
    (-)-Epicatechin gallate (Epicatechin gallate) inhibits cyclooxygenase-1 (COX-1) with an IC50 of 7.5 μM.
  • HY-16975
    SH-4-54

    STAT Cancer
    SH-4-54 is a STAT inhibitor that binds to STAT3 and STAT5 with KDs of 300, 464 nM, respectively.
  • HY-50703
    MK-2461

    c-Met/HGFR Cancer
    MK-2461 is a novel ATP-competitive multitargeted inhibitor of activated c-Met with a mean IC50 of 2.5 nM.
  • HY-13980
    UNC0642

    Histone Methyltransferase Cancer
    UNC0642 is a potent and selective lysine methyltransferases G9a and GLP inhibitor, with an IC50 of <2.5 nM for G9a.
  • HY-10110
    IC-87114

    PI3K Cancer
    IC-87114 is a potent and selective PI3Kδ inhibitor with IC50 of 0.5 μM.
  • HY-N1970
    5,7-Dihydroxychromone

    Keap1-Nrf2 Arenavirus Caspase PARP Neurological Disease
    5,7-Dihydroxychromone, the extract of Cudrania tricuspidata, activates Nrf2/ARE signal and exerts neuroprotective effects against 6-hydroxydopamine (6-OHDA)-induced oxidative stress and apoptosis. 5,7-Dihydroxychromone inhibits the expression of activated caspase-3 and caspase-9 and cleaved PARP in 6-OHDA-induced SH-SY5Y cells.
  • HY-108400
    SCH-23390 maleate

    R-(+)-SCH-23390 maleate

    Dopamine Receptor 5-HT Receptor Potassium Channel Neurological Disease
    SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 maleate is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 maleate also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
  • HY-19545A
    SCH-23390 hydrochloride

    R-(+)-SCH-23390 hydrochloride

    Dopamine Receptor 5-HT Receptor Potassium Channel Neurological Disease
    SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
  • HY-19928A
    Vactosertib Hydrochloride

    EW-7197 Hydrochloride; TEW-7197 Hydrochloride

    TGF-β Receptor Cancer
    Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect.
  • HY-18998
    LMK-235

    HDAC Cancer
    LMK-235 is a potent and selective HDAC4/5 inhibitor, inhibits HDAC5, HDAC4, HDAC6, HDAC1, HDAC2, HDAC11 and HDAC8, with IC50s of 4.22 nM, 11.9 nM, 55.7 nM, 320 nM, 881 nM, 852 nM and 1278 nM, respectively, and is used in cancer research.
  • HY-135374
    (3R,5S)-Atorvastatin sodium

    Others Metabolic Disease Inflammation/Immunology
    (3R,5S)-Atorvastatin sodium is an impurity of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively.
  • HY-19026
    Siguazodan

    SKF 94836

    Phosphodiesterase (PDE) Cardiovascular Disease
    Siguazodan (SKF 94836) is a potent, selective and orally active phosphodiesterase III (PDE-III) inhibitor with an IC50 of 117 nM. Siguazodan increases cAMP accumulation in intact platelets with an EC50 of 18.88 μM. Siguazodan also inhibits phenylephrine-induced 5-HT release with an IC50 value of 4.2 μM.
  • HY-19928
    Vactosertib

    EW-7197; TEW-7197

    TGF-β Receptor Cancer
    Vactosertib (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib has potently antimetastatic activity and anticancer effect.
  • HY-12686
    5Z-7-Oxozeaenol

    FR148083; L783279; LL-Z 1640-2

    MAP3K VEGFR Antibiotic 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-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-135878
    2',5'-Dideoxyadenosine

    Adenylate Cyclase Adrenergic Receptor Metabolic Disease
    2',5'-Dideoxyadenosine is a potent and non-competitive adenylyl cyclase inhibitor via binding the P-site with an IC50 of 3 µM . 2',5'-Dideoxyadenosine is a nucleoside analog and exerts a potent antiadrenergic action in heart.
  • HY-100111
    GLX351322

    NADPH Oxidase Metabolic Disease
    GLX351322 is an inhibitor of NADPH oxidase 4 (Nox4), and inhibits hydrogen peroxide production from NOX4-overexpressing cells with an IC50 of 5 μM.
  • HY-B0856
    Validamycin A

    Fungal Tyrosinase Infection
    Validamycin A is an aminoglycoside agricultural antibiotic. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL. Validamycin A is a reversible tyrosinase inhibitor, with a Ki of 5.893 mM.
  • HY-112443
    AZD3458

    PI3K Cancer Metabolic Disease Inflammation/Immunology
    AZD3458 is a potent and remarkably selective PI3Kγ inhibitor with pIC50s of 9.1, 5.1, <4.5, and 6.5 for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively.
  • HY-108938
    SDZ285428

    Cytochrome P450 Fungal Parasite Infection
    SDZ285428 is a CYP51 inhibitor. SDZ285428 inhibits Trypanosoma cruzi (TC) CYP51 with I/E2 <1 (5 min) and I/E2=9 (1 h). SDZ285428 inhibits Trypanosoma brucei (TB) CYP51 with I/E2 <1 (5 min) and I/E2=35 (1 h).
  • HY-15745A
    PSI-7409 tetrasodium

    HCV Infection
    PSI-7409 tetrasodium is an active 5'-triphosphate metabolite of sofosbuvir (PSI-7977), inhibiting HCV NS5B polymerases, with IC50s of 1.6, 2.8, 0.7 and 2.6 μM for GT 1b_Con1, GT 2a_JFH1, GT 3a, and GT 4a NS5B polymerases, respectively.
  • HY-N2056
    11-​Keto-​beta-​boswellic acid

    11-Keto-β-boswellic acid

    Lipoxygenase Leukotriene Receptor NF-κB Cancer
    11-Keto-beta-boswellic acid (11-Keto-β-boswellic acid) is a pentacyclic triterpenic acid of the oleogum resin from the bark of the Boswellia serrate tree, popularly known as Indian Frankincense. 11-Keto-beta-boswellic acid has the anti-inflammatory activity is primarily due to inhibit 5-lipoxygenase (5-LOX) and subsequent leukotriene and nuclear factor-kappa B (NF-κB) activation and tumor necrosis factor alpha generation production.
  • HY-131275
    Imatinib Impurity E

    Others Others
    Imatinib Impurity E is the impurity of Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
  • HY-124738
    BI 01383298

    Sodium Channel Metabolic Disease
    BI 01383298 is a potent inhibitor of the sodium-citrate co-transporter (SLC13A5) that is highly expressed in the liver.
  • HY-116100A
    HA155

    Phosphodiesterase (PDE) Inflammation/Immunology
    HA-155 is a potent and selective autotaxin (ATX) inhibitor with an IC50 of 5.7 nM.
  • HY-P1034
    DAPTA

    D-Ala-peptide T-amide; Adaptavir

    CCR HIV Infection Endocrinology
    DAPTA is a synthetic peptide, functions as a viral entry inhibitor by targeting selectively CCR5, and shows potent anti-HIV activities.
  • HY-112125A
    KRN2 bromide

    Others Inflammation/Immunology
    KRN2 (bromide) is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 0.1 μM.
  • HY-101634
    ABT-072

    HCV Infection
    ABT-072 is a nonnucleoside NS5B polymerase inhibitor and a candidate drug evaluated for treatment of hepatitis C virus.
  • HY-18304
    BMS-3

    LIM Kinase (LIMK) Cancer
    BMS-3 is a potent LIMK inhibitor with IC50s of 5 nM and 6 nM for LIMK1 and LIMK2, respectively.
  • HY-14882
    Cenicriviroc

    TAK-652; TBR-652

    CCR HIV Infection Endocrinology
    Cenicriviroc (TAK-652) is an orally active, dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective 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-B0578
    Loxoprofen

    COX Inflammation/Immunology
    Loxoprofen is a non-steroidal anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively.
  • HY-112205A
    RR-11a analog

    Parasite Infection
    RR-11a analog is a potent and selective inhibitors of asparaginyl endopeptidases (AE) (Legumain), with IC50 values of 4.5 nM, 4.5 nM and 31 nM for AE1 in Trichomonas Vaginalis, AE in Ixodes ricinus and AE in Schistosoma mansoni, respectively.
  • HY-B0578A
    Loxoprofen sodium

    COX Inflammation/Immunology
    Loxoprofen sodium is a non-steroidal anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively.
  • HY-10326
    GW788388

    TGF-β Receptor Cancer
    GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
  • HY-18696
    AMG-337

    c-Met/HGFR Cancer
    AMG-337 is a potent and highly selective small molecule ATP-competitive MET kinase inhibitor. AMG 337 inhibits MET kinase activity with an IC50 of < 5nM in enzymatic assays.
  • HY-B1490
    Imipramine hydrochloride

    Serotonin Transporter Neurological Disease
    Imipramine hydrochloride inhibits serotonin transporter with an IC50 value of 32 nM in vitro. Imipramine hydrochloride is reported to prevent the translocation of aSMase, inhibiting MV and exosomes secretion.
  • HY-11102
    RO4929097

    RG-4733

    γ-secretase Notch Neurological Disease Cancer
    RO4929097 (RG-4733) is a γ secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively.
  • HY-16712
    LDN-214117

    TGF-β Receptor Cancer
    LDN-214117 is a potent and selective ALK2 inhibitor with IC50 of 22 nM; > 100 fold selectivity for ALK5; also inhibits BMP6(IC50=100 nM).
  • HY-101840
    EIPA

    L593754; MH 12-43

    TRP Channel Sodium Channel Cancer Inflammation/Immunology
    EIPA (L593754) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also inhibits Na +/H +-exchanger (NHE) and macropinocytosis.
  • HY-19712
    LJH685

    Ribosomal S6 Kinase (RSK) Apoptosis Cancer
    LJH685 is a potent, specific and selective RSK inhibitor, inhibits RSK1, 2, and 3 biochemical activities with IC50s of 6, 5, 4 nM, respectively.
  • HY-101840A
    EIPA hydrochloride

    L593754 hydrochloride; MH 12-43 hydrochloride

    TRP Channel Sodium Channel Cancer Inflammation/Immunology
    EIPA hydrochloride (L593754 hydrochloride) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA hydrochloride also inhibits Na +/H +-exchanger (NHE) and macropinocytosis.
  • HY-13020
    GSK1838705A

    ALK IGF-1R Insulin Receptor Cancer Endocrinology
    GSK1838705A is a potent and reversible IGF-IR and the insulin receptor inhibitor with IC50s of 2.0 and 1.6 nM, respectively. It also inhibits ALK with an IC50 of 0.5 nM.
  • HY-P1189
    Echistatin

    Integrin Metabolic Disease Inflammation/Immunology
    Echistatin, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
  • HY-116364
    AZT triphosphate

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

    HIV DNA/RNA Synthesis HBV Reactive Oxygen Species Apoptosis Infection
    AZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate also inhibits the DNA polymerase of HBV. AZT triphosphate activates the mitochondria-mediated apoptosis pathway.
  • HY-107613
    R 59-022

    DKGI-I; Diacylglycerol kinase inhibitor I

    PKC 5-HT Receptor Inflammation/Immunology
    R 59-022 (DKGI-I) is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 is a 5-HTR antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
  • HY-15768
    Ilomastat

    GM6001; Galardin

    MMP Cancer
    Ilomastat (GM6001) is a potent and broad spectrum matrix metalloprotease (MMP) inhibitor, inhibits MMPs (IC50s, 1.5 nM for MMP-1; 1.1 nM for MMP-2; 1.9 nM for MMP-3; 0.5 nM for MMP-9), with a Ki of 0.4 nM for human skin fibroblast collagenase (MMP-1).
  • HY-A0077
    Perphenazine

    5-HT Receptor Adrenergic Receptor Dopamine Receptor Histamine Receptor Neurological Disease Endocrinology
    Perphenazine is a typical antipsychotic drug, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.
  • HY-N0587
    Demethylzeylasteral

    Apoptosis Cancer Inflammation/Immunology
    Demethylzeylasteral is a triterpene compound isolated from Tripterygium wilfordii Hook F, with anti-inflammatory, immunosuppressive and anti-tumor activities. Demethylzeylasteral can significantly alleviates atherosclerosis (AS). Demethylzeylasteral inhibits triple-negative breast cancer invasion by blocking the canonical and non-canonical TGF-β signaling pathways.
  • HY-107427
    PF-3644022

    MAPKAPK2 (MK2) p38 MAPK Inflammation/Immunology
    PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect.
  • HY-136573
    5-Hydroxytoluene-2,4-disulphonic acid diammonium

    Virus Protease Infection
    5-Hydroxytoluene-2,4-disulphonic acid diammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability.
  • HY-135680
    I-OMe-Tyrphostin AG 538

    I-OMe-AG 538

    IGF-1R Cancer Metabolic Disease
    I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50 of 1 µM.
  • HY-12047
    Ponatinib

    AP24534

    Bcr-Abl PDGFR VEGFR FGFR Src Autophagy Cancer
    Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
  • HY-13561
    AZM475271

    M475271

    Src Cancer
    AZM475271 is a potent and selective Src kinase inhibitor with IC50 of 5 nM; no inhibitory activity on Flt3, KDR, Tie-2.
  • HY-N0083
    Betulin

    Trochol

    Fatty Acid Synthase (FASN) Apoptosis Endogenous Metabolite Cancer
    Betulin (Trochol), is a sterol regulatory element-binding protein (SREBP) inhibitor with an IC50 of 14.5 μM in K562 cell line.
  • HY-U00426
    BF738735

    PI4K Reverse Transcriptase Infection
    BF738735 is a phosphatidylinositol 4-kinase III beta (PI4KIIIβ) inhibitor with an IC50 of 5.7 nM.
  • HY-101408
    Docosatrienoic Acid

    cis-13,16,19-docosatrienoic acid; (13Z,16Z,19Z)-13,16,19-Docosatrienoic acid

    Endogenous Metabolite Cardiovascular Disease
    Docosatrienoic acid is a rare ω-3 fatty acid; inhibits LTB4 binding to pig neutrophil membranes with an Ki of 5 μM.
  • HY-18977
    KML29

    MAGL Metabolic Disease
    KML29 is a potent and selective MAGL inhibitor with IC50 = 5.9, 15, and 43 nM in human, mouse, and rat brain proteomes, respectively.
  • HY-10974
    MK-0752

    γ-secretase Neurological Disease Cancer
    MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM.
  • HY-15698A
    CRT0066101 dihydrochloride

    PKD Cancer
    CRT0066101 dihydrochloride is a potent and specific PKD inhibitor with IC50 values of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively.
  • HY-17604
    Bexagliflozin

    EGT1442; EGT0001442; THR-1442

    SGLT Metabolic Disease
    Bexagliflozin is a potent and selective SGLT2 inhibitor with IC50 value of 5.6 μM /2 nM in SGLT1 /SGLT2 respectively.
  • HY-112096
    eCF506

    Src Cancer
    eCF506 is a highly potent and orally bioavailable inhibitor of the non-receptor tyrosine kinase Src with an IC50 of less than 0.5 nM.
  • HY-12043
    SB 525334

    TGF-β Receptor Cancer
    SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.
  • HY-14654
    Aspirin

    Acetylsalicylic Acid; ASA

    COX Autophagy Mitophagy Virus Protease Inflammation/Immunology Cancer
    Aspirin is a non-selective and irreversible inhibitor of COX-1 and COX-2 with IC50s of 5 and 210 μg/mL.
  • HY-100494
    SH5-07

    STAT Cancer
    SH5-07 is a hydroxamic acid based Stat3 inhibitor with an IC50 of 3.9 μM in in vitro assay.
  • HY-101578
    2614W94

    Monoamine Oxidase Neurological Disease
    2614W94 is a selective, reversible inhibitor of monoamine oxidase-A with a competitive mechanism of inhibition and IC50 of 5 nM and Ki of 1.6 nM with serotonin as substrate.
  • HY-B0165
    Pravastatin

    CS-514

    HMG-CoA Reductase (HMGCR) Autophagy Cardiovascular Disease
    Pravastatin (CS-514) is a competitive HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
  • HY-U00125
    CGP-53153

    5 alpha Reductase Endocrinology
    CGP-53153 is a steroidal inhibitor of 5 alpha reductase with IC50s of 36 and 262 nM in rat and human prostatic tissue, respectively.
  • HY-15991
    Tenapanor

    AZD1722; RDX5791

    Sodium Channel Cardiovascular Disease
    Tenapanor is an inhibitor of the Na +/H + exchanger NHE3 with IC50 values of 5 and 10 nM against human and Rat NHE3, respectively.
  • HY-13253
    AMG 900

    Aurora Kinase Cancer
    AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor with IC50 of 5 nM, 4 nM and 1 nM for Aurora A, B and C, respectively.
  • HY-13805
    PP2

    AGL 1879

    Src Cancer
    PP2 is a reversible and ATP-competitive Src family kinases inhibitor with IC50s of 4 and 5 nM for Lck and Fyn, respectively.
  • HY-100578
    AGK2

    Sirtuin Apoptosis Cancer
    AGK2 is a selective SIRT2 inhibitor with IC50 of 3.5 μM. AGK2 can also inhibit SIRT1 and SIRT3 with IC50 of 30 and 91 μM, respectively.
  • HY-12558
    LY3009120

    DP-4978

    Raf Autophagy Cancer
    LY3009120 is a pan RAF inhibitor which inhibits BRAF V600E, BRAF WT and CRAF WT with IC50s of 5.8, 9.1 and 15 nM, respectively.
  • HY-100625
    BVT948

    Phosphatase Cytochrome P450 Histone Methyltransferase Cancer
    BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8 (KMT5A).
  • HY-12063
    PHT-427

    Akt Apoptosis Cancer
    PHT-247 is an inhibitor of the pleckstrin homology (PH) domain of Akt, and it is also an inhibitor of PDPK1 with Kis of 2.7 µM and 5.2 µM and for Akt and PDPK1, respectively.
  • 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-12057
    Vemurafenib

    PLX4032; RG7204; RO5185426

    Raf Autophagy Cancer
    Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAF V600E and c-RAF-1, respectively. Vemurafenib induces cell autophagy.
  • HY-110398
    5,6,7-Trimethoxyflavone

    Baicalein trimethyl ether

    p38 MAPK Inflammation/Immunology Cancer
    5,6,7-Trimethoxyflavone is a novel p38-α MAPK inhibitor with an anti-inflammatory effect. 5,6,7-Trimethoxyflavone is isolated from several plants including Zeyhera tuberculosa, Callicarpa japonica, and Kickxia lanigera.
  • HY-131265
    Mesalamine impurity P

    PPAR PAK NF-κB Cancer Inflammation/Immunology
    Mesalamine impurity P is an impurity of Mesalamine (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
  • HY-17542
    PLpro inhibitor

    SARS-CoV Infection
    PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with an IC50 of 2.6 µM. PLpro inhibitor inhibits SARS-CoV-2 PLpro with an IC50 of 5.0 µM and an EC50 of 21.0 µM.
  • HY-18299A
    Purvalanol A

    NG-60

    CDK Autophagy Apoptosis Cancer
    Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.
  • HY-10985
    Marizomib

    Salinosporamide A; NPI-0052

    Proteasome Cancer
    Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC50=3.5, 28, and 430 nM, respectively).
  • HY-106161
    Rupintrivir

    AG7088

    Virus Protease Enterovirus Infection Inflammation/Immunology
    Rupintrivirvr (AG7088), an antiviral drug, is a potent, selective and irreversible inhibitor of human rhinovirus (HRV) 3C protease. Rupintrivirvr inhibits replication of a panel of 48 different HRV serotypes in H1-HeLA and MRC-5 cell protection assays, with a mean EC50 of 0.023 μM. Rupintrivirvr shows immune-modulatory effect.
  • HY-P1189A
    Echistatin TFA

    Integrin Metabolic Disease Inflammation/Immunology
    Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
  • HY-111745
    Tyk2-IN-5

    JAK Inflammation/Immunology
    Tyk2-IN-5 (compound 6) is a highly potent, selective and orally active Tyk2 inhibitor and targets the JH2 domain, with a Ki of 0.086 nM for Tyk2 JH2 and an IC50 of 25 nM for IFNα. Highly effective in inhibiting IFNγ production in a rat pharmacodynamics model and fully efficacious in a rat adjuvant arthritis model.
  • HY-17447SA
    (rel)-Tranylcypromine D5 hydrochloride

    2-Phenylcyclopropylamine D5 hydrochloride

    Monoamine Oxidase Histone Demethylase Neurological Disease
    (rel)-Tranylcypromine D5 hydrochloride (2-Phenylcyclopropylamine D5 hydrochloride) is a deuterium labeled (rel)-Tranylcypromine hydrochloride. (rel)-Tranylcypromine hydrochloride is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. (rel)-Tranylcypromine hydrochloride is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis.
  • HY-116175
    BIBB 515

    Others Metabolic Disease
    BIBB 515 is a potent, selective and orally active 2,3-oxidosqualene cyclase (OSC) inhibitor with ED50 values of 0.2-0.5 mg/kg and 0.36-33.3 mg/kg in rats and mice (1-5 hours), respectively. BIBB 515 exerts lipid-lowering effect mainly by inhibiting the production of low-density lipoprotein (LDL).
  • HY-100556
    Tie2 kinase inhibitor 1

    Others Cancer
    Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC50 of 250 nM. Tie2 kinase inhibitor 1 has anti-cancer activity.
  • HY-108601A
    Ro 32-0432 hydrochloride

    PKC Inflammation/Immunology Neurological Disease
    Ro 32-0432 hydrochloride is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of Ro 32-0432 hydrochloride for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. Ro 32-0432 hydrochloride is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. Ro 32-0432 hydrochloride prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research.
  • HY-126750
    GNF362

    Phosphatase Inflammation/Immunology
    GNF362 is a selective, potent, and orally bioavailable inhibitor of inositol trisphosphate 3’ kinase B (Itpkb) with an IC50 of 9 nM. GNF362 also inhibits Itpka and Itpkc with IC50 values of 20 nM and 19 nM, respectively. Inositol trisphosphate 3’ kinase B (Itpkb) is a Ca 2+-dependent kinase, which phosphorylates the 3’ position of Ins (1,4,5) P3 to generate inositol 1,3,4,5-tetrakisphosphate [Ins (1,3,4,5) P4].
  • HY-101257B
    YKL-5-124 TFA

    CDK Cancer
    YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.
  • HY-101257
    YKL-5-124

    CDK Cancer
    YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.
  • HY-112885B
    nor-NOHA monoacetate

    Nω-Hydroxy-nor-L-arginine monoacetate

    Arginase Metabolic Disease
    nor-NOHA (Nω-Hydroxy-nor-L-arginine) monoacetate is a potent and selective arginase inhibitor. nor-NOHA monoacetate inhibits rat liver arginase with a Ki of 0.5 µM.
  • HY-10453
    Ixazomib

    MLN2238

    Proteasome Autophagy Cancer
    Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM).
  • HY-15704
    LH846

    Casein Kinase Cancer
    LH846 is a selective inhibitor of CKIδ, with an IC50 of 290 nM, and less potently inhibits CKIα and CKIε, with IC50s of 2.5 μM and 1.3 μM, respectively.
  • HY-131246
    DM-01

    Histone Methyltransferase Cancer
    DM-01 is a powerful and selective EZH2 inhibitor for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 genetically defined solid tumors.
  • HY-13308
    Regorafenib Hydrochloride

    BAY 73-4506 hydrochloride

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  • HY-101483
    Dihydromunduletone

    DHM

    Others Cancer Neurological Disease
    Dihydromunduletone (DHM) is a rotenoid derivative and a selective, potent adhesion G protein-coupled receptor (aGPCR) (GPR56 and GPR114/ADGRG5) antagonist with an IC 50 of 20.9 μM for GPR56, but not inhibit GPR110 or class A GPCRs.
  • HY-10331A
    Regorafenib monohydrate

    BAY 73-4506 monohydrate

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib monohydrate (BAY 73-4506 monohydrate) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  • HY-103061
    Dehydro-ZINC39395747

    Others Cardiovascular Disease
    Dehydro-ZINC39395747 is a derivative of ZINC39395747. ZINC39395747 is a potent cytochrome b5 reductase 3 (CYB5R3) inhibitor with an IC50 of 9.14 μM and a Kd of 1.11 μM. ZINC39395747 can increase NO bioavailability in vascular cells.
  • HY-15873
    FTI 276

    Farnesyl Transferase Cancer
    FTI-276 is a protein farnesyl transferase (PFT) inhibitor with IC50s of 0.9 and 0.5 nM for Plasmodium falciparum and human.
  • HY-16785
    Veledimex

    INXN-1001; RG-115932

    Cytochrome P450 Interleukin Related Cancer Inflammation/Immunology
    Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5.
  • HY-112719
    BRD 4354

    HDAC Cancer
    BRD 4354 is a moderately potent inhibitor of HDAC5 and HDAC9, with IC50s of 0.85 and 1.88 μM, respectively.
  • HY-B0575
    Triamterene

    Sodium Channel GPCR19 Metabolic Disease
    Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner, which used as a mild diuretic. Triamterene as an inhibitor of the TGR5 receptor.
  • HY-10268
    Betrixaban

    PRT054021

    Factor Xa Cardiovascular Disease
    Betrixaban (PRT054021) is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with IC50 of 1.5 nM.
  • HY-111510
    IPI-3063

    PI3K Inflammation/Immunology
    IPI-3063 is a potent and selective PI3K p110δ inhibitor with an IC50 of 2.5 ± 1.2 nM.
  • HY-U00003
    ICAM-1-IN-1

    Integrin Inflammation/Immunology
    ICAM-1-IN-1 is a potent and selective inhibitor of E-selectin and ICAM-1 with IC50 values of 7 and 5 nM, respectively.
  • HY-13783
    BIBF0775

    TGF-β Receptor Cancer
    BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM.
  • HY-16664
    SJ-172550

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    SJ-172550 is a small molecule inhibitor of MDMX; competes for the wild type p53 peptide binding to MDMX with an EC50 of 5 μM.
  • HY-76251
    Etodolac

    AY-24236

    COX Inflammation/Immunology Cancer
    Etodolac (AY-24236) is a non-steroidal anti-inflammatory compound that is a non-selective inhibitor of COX (IC50=53.5 nM)
  • HY-100744
    AS8351

    NSC51355

    Histone Demethylase Cardiovascular Disease
    AS8351 is a KDM5B inhibitor, which can induce and sustain active chromatin marks to facilitate the induction of cardiomyocyte-like cells.
  • HY-18997
    PLX7904

    Raf Cancer
    PLX7904 is a potent and selective BRAF inhibitor, with IC50 of appr 5 nM against BRAF V600E in mutant RAS expressing cells.
  • HY-13917
    PND-1186

    VS-4718; SR-2516

    FAK Apoptosis Cancer
    PND-1186 (VS-4718; SR-2516) is a potent and reversible inhibitor of FAK with an IC50 of 1.5 nM in cell assay.
  • HY-101126
    TP-3654

    Pim Cancer
    TP-3654 is a second-generation Pim kinase inhibitor with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively.
  • HY-12624
    ON123300

    CDK Cancer
    ON123300 is a potent inhibitor of CDK4, with an IC50 of 3.8 nM, with little inhibitory activity against CDKs 1,2,5 and 8.
  • HY-17634
    Glecaprevir

    ABT-493

    HCV HCV Protease Infection
    Glecaprevir is a novel HCV NS3/4A protease inhibitor, with IC50 values ranging from 3.5 to 11.3 nM.
  • HY-15755
    RKI-1447

    ROCK Cancer
    RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 values of 14.5 nM and 6.2 nM, respectively.
  • HY-B0231BS
    Enalaprilat D5 Sodium Salt

    MK-422 D5 Sodium Salt

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Enalaprilat (MK-422) D5 Sodium Salt is the deuterium labeled Enalaprilat(MK-422), which is an angiotensin-converting enzyme (ACE) inhibitor.
  • 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-N6796
    Manumycin A

    Farnesyl Transferase Ras Apoptosis Phospholipase Cancer Infection
    Manumycin A is an antibiotic. Manumycin A acts as a selective, competitive inhibitor of protein farnesyltransferase (FTase) with respect to farnesylpyrophosphate (Ki =1.2 μM), and as a noncompetitive inhibitor with respect to the Ras protein. Manumycin A induces apoptosis and exerts antitumor activity . Manumycin A suppresses exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling. Manumycin A is a nSMase inhibitor (EC50=0.25 μM).
  • HY-122502
    Pyrazofurin

    DNA/RNA Synthesis Cancer
    Pyrazofurin, a pyrimidine nucleoside analogue with antineoplastic activity, inhibits cell proliferation and DNA synthesis in cells by inhibiting uridine 5'-phosphate (UMP) synthase. Pyrazofurin is an active, sensitive orotate-phosphoribosyltransferase inhibitor with IC50s between 0.06-0.37 µM in the three squamous cell carcinoma (SCC) cell lines Hep-2, HNSCC-14B and HNSCC-14C.
  • HY-12270
    T-5224

    MMP Others
    T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription.
  • HY-116364A
    AZT triphosphate TEA

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

    HIV DNA/RNA Synthesis HBV Reactive Oxygen Species Apoptosis Infection
    AZT triphosphate TFA (3'-Azido-3'-deoxythymidine-5'-triphosphate TFA) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TFA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TFA also inhibits the DNA polymerase of HBV. AZT triphosphate TFA activates the mitochondria-mediated apoptosis pathway.
  • HY-12949
    ML204

    TRP Channel Neurological Disease
    ML204 is a potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca 2+ channels.
  • HY-N0908
    Ginsenoside Rg5

    IGF-1R NF-κB COX Cancer Inflammation/Immunology Cardiovascular Disease Endocrinology
    Ginsenoside Rg5 is the main component of Red ginseng. Ginsenoside blocks binding of IGF-1 to its receptor with an IC50 of ~90 nM. Ginsenoside Rg5 also inhibits the mRNA expression of COX-2 via suppression of the DNA binding activities of NF-κB p65.
  • HY-12987
    Pimozide

    R6238

    Dopamine Receptor Adrenergic Receptor STAT Cancer Neurological Disease Endocrinology
    Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
  • HY-10331
    Regorafenib

    BAY 73-4506

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
  • HY-19306
    SB-267268

    Integrin Cancer
    SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression.
  • HY-N1750
    3-(2,4-Dihydroxyphenyl)propanoic acid

    Tyrosinase Others
    3-(2,4-Dihydroxyphenyl)propanoic acid (DPPacid) is a potent and competitive tyrosinase inhibitor, inhibits L-Tyrosine and DL-DOPA with an IC50 and a Ki of 3.02 μM and 11.5 μM, respectively.
  • HY-100339
    GSK583

    RIP kinase Endocrinology
    GSK583 is a highly potent, orally active and selective inhibitor of RIP2 Kinase, with IC50 of 5 nM. GSK583 inhibits both TNF-α and IL-6 production with an IC50 value of 200 nM.
  • HY-15515
    SEA0400

    Na+/Ca2+ Exchanger Cardiovascular Disease
    SEA0400 is a novel and selective inhibitor of the Na +-Ca 2+ exchanger (NCX), inhibiting Na +-dependent Ca 2+ uptake in cultured neurons, astrocytes, and microglia with IC50s of from 5 to 33 nM.
  • HY-N2021A
    Phosphoramidon Disodium

    Angiotensin-converting Enzyme (ACE) Neprilysin Inflammation/Immunology Cardiovascular Disease Cancer
    Phosphoramidon Disodium is a metalloprotease inhibitor. Phosphoramidon inhibits endothelin-converting enzyme (ECE), neutral endopeptidase (NEP), and angiotensin-converting enzyme (ACE) with IC50 values of 3.5, 0.034, and 78 μM, respectively.
  • HY-16961
    Sitravatinib

    MGCD516; MG-516

    VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Cancer Inflammation/Immunology
    Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
  • HY-103430
    SKF-83566 hydrobromide

    Dopamine Receptor 5-HT Receptor Adenylate Cyclase Neurological Disease
    SKF-83566 hydrobromide is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM). SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta. SKF-83566 can be used for the research of parkinson’s disease and nicotine craving alleviation.
  • HY-103430A
    SKF-83566

    Dopamine Receptor 5-HT Receptor Adenylate Cyclase Neurological Disease
    SKF-83566 is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM). SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta. SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation.
  • HY-115502
    BCI

    (E)-BCI

    Phosphatase Cancer Inflammation/Immunology
    BCI is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI does not inhibit DUSP5.
  • HY-15557
    AZ20

    ATM/ATR Cancer
    AZ20 is a potent and selective inhibitor of ATR with an IC50 of 5 nM, and has 8-fold selectivity against mTOR (IC50=38 nM).
  • HY-17385
    Atomoxetine hydrochloride

    Tomoxetine hydrochloride; LY 139603; (R)-Tomoxetine hydrochloride

    Others Neurological Disease
    Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively).
  • HY-112082
    BAY885

    ERK Cancer
    BAY885 is a highly potent and selective ERK5 inhibitor with an IC50 of 35 nM. BAY885 shows weak inhibition on others kinases.
  • HY-125833
    Alpha-Naphthoflavone

    Aromatase Cancer
    Alpha-Naphthoflavone is a synthetic flavonoid, acts as a potent and competitive aromatase inhibitor with an IC50 and a Ki of 0.5 and 0.2 μM, respectively.
  • HY-10614
    A-966492

    PARP Cancer
    A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
  • HY-78727
    Ibrutinib deacryloylpiperidine

    IBT4A

    Btk Cancer
    Ibrutinib deacryloylpiperidine (IBT4A) is an impurity of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
  • HY-N2300
    Kuwanon A

    NO Synthase Metabolic Disease Inflammation/Immunology
    Kuwanon A is a flavone derivative isolated from the root barks of the mulberry tree (Morus alba L.); inhibits nitric oxide production with an IC50 of 10.5 μM.
  • HY-N0430
    Coptisine

    Coptisin

    Indoleamine 2,3-Dioxygenase (IDO) Cancer Metabolic Disease
    Coptisine is an alkaloid from Chinese goldthread, and acts as an efficient uncompetitive IDO inhibitor with a Ki value of 5.8 μM and an IC50 value of 6.3 μM.
  • HY-14719
    RO4987655

    CH4987655

    MEK Cancer
    RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM for inhibition of MEK1/MEK2.
  • HY-18030A
    CEP-28122 mesylate salt

    ALK Cancer
    CEP-28122 mesylate salt is a highly potent and selective orally active ALK inhibitor with IC50 of 1.9 ± 0.5 nM in an enzyme-based TRF assay.
  • HY-15407
    Sacubitril

    AHU-377

    Neprilysin Cardiovascular Disease
    Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril (AHU-377) is a component of the heart failure medicine LCZ696.
  • HY-16276
    Osilodrostat

    LCI699

    Mineralocorticoid Receptor Inflammation/Immunology Cancer
    Osilodrostat (LCI699) is a potent inhibitor of human 11β-hydroxylase and aldosterone synthase with IC50 values of 2.5 and 0.7 nM, respectively.
  • 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-10163AS
    Dabigatran D4 hydrochloride

    BIBR-953 D4 hydrochloride

    Thrombin Cardiovascular Disease
    Dabigatran (BIBR-953) D4 hydrochloride is deuterium labeled Dabigatran, which is a reversible and selective, direct thrombin inhibitor (DTI) with a Ki value of 4.5 nM.
  • HY-15407A
    Sacubitril hemicalcium salt

    AHU-377 hemicalcium salt

    Neprilysin Cardiovascular Disease
    Sacubitril hemicalcium salt (AHU-377 hemicalcium salt) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696.
  • HY-15030A
    Naproxen sodium

    Autophagy COX Inflammation/Immunology Cancer
    Naproxen sodium is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
  • HY-16143
    Cilengitide TFA

    EMD 121974 TFA

    Integrin Autophagy Cancer
    Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50 values of 4 nM and 79 nM, respectively.
  • HY-16690
    BTS

    N-Benzyl-p-toluenesulfonamide; N-Tosylbenzylamine

    Myosin Cancer
    BTS is a potent inhibitor of Ca2+-stimulated myosin S1 ATPase (IC50 ~ 5 μM) and reversibly blocks the gliding motility.
  • HY-15485
    Zardaverine

    Phosphodiesterase (PDE) Inflammation/Immunology
    Zardaverine is a newly developed dual-selective PDE3/4 inhibitor with IC50 values of 0.5 uM and 0.8 uM respectively.
  • HY-101055
    Kinetin riboside

    N6-Furfuryladenosine

    Apoptosis Cancer
    Kinetin riboside, a cytokinin analog, can induce apoptosis in cancer cells. It inhibits the proliferation of HCT-15 cells with an IC50 of 2.5 μM.
  • HY-15617
    JNK-IN-7

    JNK inhibitor

    JNK Cancer
    JNK-IN-7 is a potent JNK inhibitor with IC50 of 1.5, 2 and 0.7 nM for JNK1, JNK2 and JNK3, respectively.
  • HY-13535A
    ATN-161 trifluoroacetate salt

    ATN-161 TFA salt

    Integrin Cancer
    ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
  • HY-15030
    Naproxen

    (S)-Naproxen

    COX Autophagy Inflammation/Immunology Cancer
    Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
  • HY-10550
    Tariquidar

    XR9576

    P-glycoprotein Cancer
    Tariquidar (XR9576) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM).
  • HY-U00231
    KF 13218

    Prostaglandin Receptor Cardiovascular Disease Endocrinology
    KF 13218 is a potent, selective and long lasting thromboxane B2 (TXB2) synthase inhibitor with an IC50 value of 5.3±1.3 nM.
  • HY-100697
    TPOP146

    Epigenetic Reader Domain Histone Acetyltransferase Cancer
    TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
  • HY-100005A
    Fumarate hydratase-IN-2 sodium salt

    Mitochondrial Metabolism Cancer
    Fumarate hydratase-IN-2 sodium salt (compound 3) is a cell-permeable and competitive fumarate hydratase inhibitor (Ki=4.5 μM) with nutrient-dependent cytotoxicity .
  • HY-13536
    AZD-2461

    PARP Cancer
    AZD-2461 is a potent PARP inhibitor, with IC50s of 5 nM, 2 nM and 200 nM for PARP1, PARP2 and PARP3, respectively.
  • HY-117506B
    SBFI-26

    FABP Inflammation/Immunology Neurological Disease
    SBFI-26 is a selective and competitive inhibitor of fatty acid binding proteins FABP5 and FABP7, with Kis of 0.9 µM and 0.4 µM for FABP5 and FABP7, respectively. SBFI-26 produces anti-nociceptive and anti-inflammatory effects.
  • HY-12949A
    ML204 hydrochloride

    TRP Channel Neurological Disease
    ML204 hydrochloride is a novel, potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca 2+ channels.
  • HY-130293
    Propargyl-PEG4-CH2CH2-Boc

    ADC Linker Cancer
    Propargyl-PEG4-CH2CH2-Boc is a PEG- and Alkyl/ether-based non-cleavable ADC linker. Propargyl-PEG5-Boc can used to synthesize ADC inhibitors of Galectin-3.
  • HY-21141
    Cysteine protease inhibitor-2

    Cathepsin Cancer
    Cysteine protease inhibitor-2 is a cysteine protease inhibitor extracted from patent US20070032499A1, compound 12. Cysteine protease inhibitor-2 inhibits the cells growth of DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.
  • HY-100018
    BAY1125976

    Akt Cancer
    BAY1125976 is a selective allosteric Akt1/Akt2 inhibitor; inhibits Akt1 and Akt2 activity with IC50 values of 5.2 nM and 18 nM at 10 μM ATP, respectively.
  • HY-B0579
    Cyclosporin A

    Cyclosporine; Ciclosporin

    Phosphatase Complement System Inflammation/Immunology Cancer
    Cyclosporin A is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of calcineurin with an IC50 of 5 nM. Cyclosporin A also inhibits CD11a/CD18 adhesion.
  • HY-13862
    AZD1080

    GSK-3 Neurological Disease
    AZD1080 is a potent and selective GSK3 inhibitor. AZD1080 inhibits recombinant human GSK3α and GSK3β with pKi (IC50) of 8.2 (6.9 nM) and 7.5 (31 nM), respectively.
  • HY-135902A
    Synucleozid hydrochloride

    NSC 377363 hydrochloride

    DNA/RNA Synthesis Neurological Disease
    Synucleozid hydrochloride (NSC 377363 hydrochloride) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein (IC50=1.5 μM). Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease.
  • HY-10185
    TG 100572 Hydrochloride

    Src VEGFR FGFR PDGFR Inflammation/Immunology
    TG 100572 Hydrochloride is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-B0151
    Pregnenolone

    3β-Hydroxy-5-pregnen-20-one

    Cannabinoid Receptor Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication.
  • HY-100734
    Histone Acetyltransferase Inhibitor II

    Histone Acetyltransferase Cancer
    Histone Acetyltransferase Inhibitor II (compound 2c) is a potent, selective and cell permeable p300 histone acetyltransferase inhibitor, with an IC50 of 5 µM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.
  • HY-102058
    WM-1119

    Histone Acetyltransferase Cancer
    WM-1119 is a highly potent and selective KAT6A inhibitor, with an IC50 of 0.25 μM for KAT6A in lymphoma cells, the binding KD values of WM-1119 with KAT6A, KAT5 and KAT7 are 2 nM, 2.2 μM, 0.5 μM , respectively.
  • HY-119944
    JND3229

    EGFR Cancer
    JND3229 is a highly potent and fourth-generation EGFR C797S reversible inhibitor with IC50 value of 5.8 nM, and also potently suppressed EGFR L858R/T790M and EGFR WT with IC50 values of 30.5 and 6.8 nM.
  • HY-I0678
    Regorafénib N-oxyde (M2)

    Drug Metabolite Cancer
    Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  • HY-16115
    BPH-652

    Others Metabolic Disease
    BPH-652 is a S. aureus dehydrosqualene synthase (CrtM) inhibitor, with a Ki of 1.5 nM and an IC50 of 100-300 nM (S. aureus pigment formation).
  • HY-N0159
    Paeonol

    Monoamine Oxidase Autophagy Neurological Disease Cancer
    Paeonol is an active extraction from the root of Paeonia suffruticosa, Paeonol inhibits MAO-A and MAO-B with IC50 of 54.6 μM and 42.5 μM, respectively.
  • HY-112719B
    BRD 4354 ditrifluoroacetate

    HDAC Cancer
    BRD 4354 (ditrifluoroacetate) is a moderately potent inhibitor of HDAC5 and HDAC9, with IC50s of 0.85 and 1.88 μM, respectively.
  • HY-N3943
    Glabrene

    Tyrosinase Neurological Disease
    Glabrene, an isoflavene derived from licorice root, shows estrogen-like activity. Glabrene is a tyrosinase inhibitor with an IC50 of 3.5 μM.
  • HY-10458
    PF-562271 besylate

    PF562271 besylate; PF 562271 besylate

    FAK Pyk2 Cancer
    PF-562271 besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively.
  • HY-112113
    SLV-2436

    SEL201-88; SEL-201

    MNK Cancer
    SLV-2436 is a highly potent and ATP-competitive inhibitor of MNK1 and MNK2 with IC50s of 10.8  nM and 5.4 nM, respectively.
  • HY-100230A
    ML133 hydrochloride

    Potassium Channel Others
    ML133 hydrochloride is a selective Kir2 family channels inhibitor, with an IC50 of 1.8 μM at pH 7.4 and 290 nM at pH 8.5.
  • HY-N1470
    Plantagoside

    Others Metabolic Disease
    Plantagoside, isolated from the seeds of Plantago asiatica, is a specific and non-competitive inhibitor for jack bean α-mannosidase, with an IC50 of 5 μM.
  • HY-100733
    4E2RCat

    Eukaryotic Initiation Factor (eIF) Autophagy Virus Protease Neurological Disease
    4E2RCat is an inhibitor of eIF4E-eIF4G interaction with an IC50 of 13.5 μM.
  • HY-14660A
    Dabrafenib Mesylate

    GSK2118436 Mesylate; GSK 2118436B

    Raf Cancer
    Dabrafenib Mesylate is a potent and selective Raf kinase inhibitor with IC50s of 0.6 and 5.0 nM for Raf V600E and c-Raf, respectively.
  • HY-101243
    XMD16-5

    Tyrosinase Cancer
    XMD16-5 is a potent TNK2 inhibitor with IC50 values of 16 and 77 nM for the D163E and R806Q mutations, respectively.
  • HY-14818
    Laninamivir

    R 125489

    Influenza Virus Infection
    Laninamivir (R 125489) is a potent influenza neuraminidase (NA) inhibitor with IC50s of 0.90 nM, 1.83 nM and 3.12 nM for avian H12N5 NA (N5), pH1N1 N1 NA (p09N1) and A/RI/5+/1957 H2N2 N2 (p57N2), respectively.
  • HY-115502A
    BCI hydrochloride

    (E)-BCI hydrochloride

    Phosphatase Cancer Inflammation/Immunology
    BCI hydrochloride ((E)-BCI hydrochloride) is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI hydrochloride specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI hydrochloride does not inhibit DUSP5.
  • 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-12235
    PI-3065

    PI3K Inflammation/Immunology Cancer
    PI-3065 is a potent inhibitor of PI3K p110δ, with IC50 and Ki values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM.
  • HY-14874
    Topiroxostat

    FYX-051

    Xanthine Oxidase Cytochrome P450 Metabolic Disease
    Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment.
  • HY-10037
    Quiflapon

    MK-591

    FLAP Apoptosis Inflammation/Immunology
    Quiflapon (MK-591) is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.6 nM in a FLAP binding assay. Quiflapon is also a potent and orally active Leukotriene biosynthesis (LT) inhibitor, shows IC50 values of 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively. Quiflapon induces cell apoptosis.
  • HY-10466
    Daclatasvir

    BMS-790052; EBP 883

    HCV Infection
    Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively.
  • HY-B0097
    Floxuridine

    5-Fluorouracil 2'-deoxyriboside

    Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Bacterial CMV HSV Cancer Infection
    Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis. Floxuridine has antiviral effects against HSV and CMV.
  • HY-10465
    Daclatasvir dihydrochloride

    BMS-790052 dihydrochloride; EBP 883 dihydrochloride

    HCV Infection
    Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir dihydrochloride is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively.
  • HY-112457
    MK-2 Inhibitor III

    MAPKAPK2 (MK2) Inflammation/Immunology
    MK-2 Inhibitor III (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 0.85 nM, and is exceptional selectivity against MK-3 (IC50=0.21 μM), MK-5 (IC50=0.081 μM), ERK2 (IC50=3.44 μM), MNK1(IC50=5.7 μM) as well as CDK2, JNK2, IKK2, MSK1, and MSK2.
  • HY-B0166
    L-Ascorbic acid

    L-Ascorbate; Vitamin C

    Calcium Channel Reactive Oxygen Species Apoptosis Metabolic Disease
    L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor.
  • HY-B0166A
    L-Ascorbic acid sodium salt

    Sodium L-ascorbate; Vitamin C sodium salt

    Calcium Channel Reactive Oxygen Species Apoptosis Cancer
    L-Ascorbic acid sodium salt (Sodium L-ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid sodium salt is also a collagen deposition enhancer and an elastogenesis inhibitor.
  • HY-10452
    Ixazomib citrate

    MLN9708

    Proteasome Autophagy Cancer
    Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM.
  • HY-136259
    ML188

    SARS-CoV Virus Protease Infection
    ML188, a first in class probe, is a selective non-covalent SARS-CoV 3CLpro inhibitor with an IC50 of 1.5 μM. Antiviral activity.
  • HY-10130
    Veliparib dihydrochloride

    ABT-888 dihydrochloride

    PARP Autophagy Cancer
    Veliparib (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Kis of 5.2 nM and 2.9 nM in cell-free assays, respectively.
  • HY-101977
    Selitrectinib

    LOXO-195

    Trk Receptor Cancer
    Selitrectinib (LOXO-195) is a next-generation TRK kinase inhibitor, with IC50s of 0.6 nM and <2.5 nM for TRKA and TRKC, respectively.
  • HY-115466
    MLT-748

    MALT1 Inflammation/Immunology
    MLT-748 is a potent, selective and allosteric inhibitor of MALT1, binds MALT1 in the allosteric Trp580 pocket, with an IC50 of 5 nM.
  • HY-14894
    Ipragliflozin

    ASP1941

    SGLT Metabolic Disease
    Ipragliflozin (ASP1941) is a highly potent and selective SGLT2 inhibitor with IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6.
  • HY-15602
    Ledipasvir

    GS-5885

    HCV Infection
    Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively.
  • HY-15873A
    FTI 276 TFA

    Farnesyl Transferase Cancer
    FTI-276 is a protein farnesyl transferase (PFT) inhibitor with IC50s of 0.9 nM and 0.5 nM for Plasmodium falciparum and human, respectively.
  • HY-12032
    AG14361

    PARP Cancer
    AG14361 is a potent PARP-1 inhibitor, with a Ki of < 5 nM, and in permeabilized SW620 and intact SW620 cells, the IC50s are 29 nM and 14 nM, respectively.
  • HY-16999
    RO8994

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    RO8994 is a highly potent and selective series of spiroindolinone small-molecule MDM2 inhibitor, with IC50 of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays).
  • HY-15591A
    TMC647055 Choline salt

    HCV Infection
    TMC647055 choline salt is a cell-permeating, selective HCV NS5B inhibitor, eliciting a mean IC50 of 34 nM, as assessed in the RdRp primer-dependent transcription assay.
  • HY-108325
    Brequinar

    DUP785; NSC 368390

    Dihydroorotate Dehydrogenase Virus Protease DNA/RNA Synthesis Cancer Infection Inflammation/Immunology
    Brequinar (DUP785) is a potent inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of 5.2 nM for human DHODH. Brequinar has potent activities against a broad spectrum of viruses.
  • HY-10459
    PF-562271

    FAK Pyk2 Cancer
    PF-562271 is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively.
  • HY-108277
    Ginsenoside F5

    Apoptosis Cancer
    Ginsenoside F5, from crude extracts of flower buds of Panax ginseng, remarkably inhibits the growth of HL-60 cells by the apoptosis pathway.
  • HY-133012
    GFB-8438

    TRP Channel Neurological Disease
    GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model.
  • HY-14248
    Letrozole

    CGS 20267

    Aromatase Autophagy Cancer
    Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer.
  • 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-12511
    SKF-86002

    p38 MAPK Autophagy Apoptosis Inflammation/Immunology
    SKF-86002 is a potent inhibitor of p38 MAP kinase wit IC50 of 0.5-1 uM; inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50 = 1 μM).
  • HY-32718
    Pelitinib

    EKB-569; WAY-EKB 569

    EGFR Src Cancer
    Pelitinib (EKB-569;WAY-EKB 569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively.
  • HY-16026
    Ricolinostat

    ACY-1215; Rocilinostat

    HDAC Apoptosis Cancer
    Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC50 of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively.
  • HY-14471
    Cetilistat

    ATL-962

    Others Metabolic Disease
    Cetilistat (ATL-962), an inhibitor of pancreatic lipase, acts as an effective anti-obesity agent. Cetilistat inhibits rat and human pancreatic lipase activity with IC50s of 54.8 nM, and 5.95 nM, respectively.
  • 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-125851
    TGFβRI-IN-2

    ALK Inflammation/Immunology
    TGFβRI-IN-2 (compound 18) is a potent, selective and orally active (Activin-Like Kinase 5) ALK 5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose.
  • HY-14262
    Vilazodone

    EMD 68843; SB659746A

    5-HT Receptor Serotonin Transporter Neurological Disease
    Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders.
  • HY-N2435
    [8]-Shogaol

    COX Apoptosis Cancer
    [8]-Shogaol, one of the pungent phenolic compounds in ginger, exhibits anti-platelet activity (IC50=5 μM) and inhibits COX-2 (IC50=17.5 μM). [8]-Shogaol induces apoptosis in human leukemia cells.
  • HY-N0643
    Carnosol

    Ribosomal S6 Kinase (RSK) Keap1-Nrf2 Cancer
    Carnosol is a potent Ribosomal S6 Kinase (RSK2) inhibitor that could be useful for treating gastric cancer, with an IC50 of ~5.5 μM. Carnosol, a Nrf2 activator, increases the nuclear levels of Nrf2 and can promote the expression of heme oxygenase 1 (HMOX1).
  • HY-B1739
    Pregnenolone monosulfate

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

    Cannabinoid Receptor Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate can protect the brain from cannabis intoxication.
  • HY-110189
    Pregnenolone monosulfate sodium salt

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

    Cannabinoid Receptor Endogenous Metabolite Autophagy Neurological Disease
    Pregnenolone monosulfate sodium salt (3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication.
  • HY-17504C
    (3R,5R)-Rosuvastatin

    HMG-CoA Reductase (HMGCR) Potassium Channel Autophagy Metabolic Disease Cardiovascular Disease
    (3R,5R)-Rosuvastatin is the (3R,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
  • HY-17504D
    (3S,5R)-Rosuvastatin

    HMG-CoA Reductase (HMGCR) Potassium Channel Autophagy Metabolic Disease Cardiovascular Disease
    (3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
  • HY-118532
    Tyrphostin AG30

    AG30

    EGFR Cancer
    Tyrphostin AG30 (AG30) is a potent and selective EGFR tyrosine kinase inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts.
  • HY-U00369
    FCE 28654

    Acyltransferase Cardiovascular Disease
    FCE 28654 is a water soluble inhibitor of acylCoA: cholesterol acyltransferase (ACAT), weakly inhibiting ACAT in microsomes from rabbit aorta and intestine, and monkey liver, with IC50s of 2.55, 1.08 and 5.69 μM, respcetively.
  • HY-N3032
    Xanthatin

    Apoptosis VEGFR Lipoxygenase Bacterial Cancer Infection Inflammation/Immunology
    Xanthatin is isolated from Xanthium strumarium leaves. Xanthatin exhibits strong antitumor activities against a variety of cancer cells through apoptosis persuasion and shows anti-inflammatory activities by inhibiting PGE2 synthesis and 5-lipoxygenase activity. Xanthatin is a potent and orally active inhibitor of VEGFR2 kinase activity with an IC50 of 3.8 μM and prominently blocks the phosphorylation of VEGFR2 at Tyr951 site. Xanthatin inhibits angiogenesis and has the potential for the investigation of breast cancer.
  • HY-12815A
    MCC950 sodium

    CP-456773 sodium; CRID3 sodium salt

    NOD-like Receptor (NLR) Inflammation/Immunology
    MCC950 sodium (CP-456773 sodium; CRID3 sodium salt) is a potent, selective NLRP3 inhibitor with IC50s of 7.5 and 8.1 nM in BMDMs and HMDMs, respectively.
  • HY-13424
    RITA

    NSC 652287

    MDM-2/p53 Autophagy DNA Alkylator/Crosslinker Cancer
    RITA is an inhibitor of p53-HDM-2 interaction, binds to p53dN, with a Kd of 1.5 nM, and also induces DNA-DNA cross-links.
  • HY-P0273
    Histatin 5

    MMP Inflammation/Immunology
    Histatin 5 inhibits the activity of the host matrix metalloproteinases MMP-2 and MMP-9 with IC50s of 0.57 and 0.25 μM, respectively.
  • HY-15313B
    CBB1007 hydrochloride

    Histone Demethylase Cancer
    CBB1007 Hcl is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
  • HY-B1324
    Oxiconazole nitrate

    Ro 13-8996

    Fungal Antibiotic Infection
    Oxiconazole nitrate is a broad spectrum antifungal which can inhibit the growth of T. tonsurans and T. rubrum with MIC90s of 0.25 and 0.5 μg/mL, respectively.
  • HY-15312
    WP1066

    STAT JAK Apoptosis Cancer
    WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.
  • HY-12090
    Anacetrapib

    MK-0859

    CETP Cardiovascular Disease
    Anacetrapib is a potent CETP inhibitor, with IC50s of 7.9±2.5 nM and 11.8±1.9 nM for rhCETP and C13S CETP mutant, respectively.
  • HY-100015
    Mivebresib

    ABBV-075

    Epigenetic Reader Domain Apoptosis Cancer
    Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a Ki of 1.5 nM.
  • HY-15313C
    CBB1007 trihydrochloride

    Histone Demethylase Cancer
    CBB1007 trihydrochloride is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
  • HY-12469
    Decernotinib

    VX-509; VRT-831509

    JAK Inflammation/Immunology
    Decernotinib is a potent, orally active JAK3 inhibitor, with Kis of 2.5, 11, 13 and 11 nM for JAK3, JAK1, JAK2, and TYK2, respectively.
  • HY-12873
    RBC8

    Ras Cancer
    RBC8 is a novel small molecule inhibitor of Ral GTPase; has IC50 of 3.5 μM in H2122 cell and 3.4 μM in H358 cell.
  • HY-15313
    CBB1007

    Histone Demethylase Cancer
    CBB1007 is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
  • HY-15663
    IPA-3

    PAK Cancer
    IPA-3 is a selective non-ATP competitive PAK1 inhibitor with IC50 of 2.5 μM, and shows no inhibition to group II PAKs (PAKs 4-6).
  • HY-117109
    Amino Tadalafil

    Others
    Amino Tadalafil is an analog of tadalafil. Tadalafil is a potent inhibitor of phosphodiesterase 5 with applications in several conditions, including erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction.
  • HY-100791
    NSC23005 sodium

    Others Cancer
    NSC23005 sodium is a novel and effective p18 inhibitor (ED50=5.21 nM) in promoting Hematopoietic stem cells (HSCs) expansion in both murine and human models.
  • HY-18983
    Calyculin A

    (-)-Calyculin A

    Phosphatase Cancer
    Calyculin A is a potent and cell-permeable protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A) inhibitor with IC50s of 2 nM and 0.5-1 nM.
  • HY-N0430A
    Coptisine Sulfate

    Indoleamine 2,3-Dioxygenase (IDO) Cancer Metabolic Disease
    Coptisine Sulfate is an alkaloid from Chinese goldthread, and acts as an efficient uncompetitive IDO inhibitor with a Ki value of 5.8 μM and an IC50 value of 6.3 μM.
  • HY-12815
    MCC950

    CP-456773; CRID3

    NOD-like Receptor (NLR) Inflammation/Immunology
    MCC950 (CP-456773; CRID3) is a potent and selective NLRP3 inhibitor with IC50s of 7.5 and 8.1 nM in BMDMs and HMDMs, respectively.
  • HY-10333
    BMS-690514

    EGFR VEGFR Cardiovascular Disease Cancer
    BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR; has IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.
  • HY-100675
    JTE-013

    LPL Receptor Apoptosis Cancer
    JTE-013 is a potent and specific S1P2 (Sphingosine-1-Phosphate 2; EDG-5) antagonist. JTE-013 inhibits the specific binding of radiolabeled S1P to human and rat S1P2 with IC50s of 17 nM and 22 nM, respectively.
  • HY-128694
    Foropafant

    SR27417

    Others Cardiovascular Disease
    Foropafant (SR27417) highly potent, competitive, selective and orally active antagonist of platelet-activating factor (PAF) receptor, with a Ki value of 57 pM for [ 3H]PAF binding, at least 5-fold lower than that of unlabeled PAF itself. Foropafant potently inhibits PAF-induced aggregation of rabbit and human platelets.
  • HY-15893
    DMOG

    Dimethyloxallyl Glycine

    HIF/HIF Prolyl-Hydroxylase Autophagy Cancer
    DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo. DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal. DMOG induces cell autophagy.
  • HY-14879A
    Avibactam sodium

    NXL-104

    Bacterial Antibiotic Infection
    Avibactam sodium (NXL-104) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
  • HY-B0486
    Lonidamine

    AF-1890; Diclondazolic Acid; DICA

    Hexokinase Mitochondrial Metabolism Apoptosis Cancer
    Lonidamine (AF-1890), an antitumor agent, is a hexokinase, mitochondrial pyruvate carrier (Ki 2.5 μM in isolated rat liver mitochondria) and plasma membrane monocarboxylate transporters inhibitor, which also inhibits mitochondrial complex II.
  • HY-15999
    Cerdulatinib

    PRT062070; PRT2070

    JAK Syk Cancer
    Cerdulatinib (PRT062070) is a selective Tyk2 inhibitor with an IC50 of 0.5 nM. Cerdulatinib (PRT062070) also is a dual JAK and SYK inhibitor with IC50s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively.
  • HY-P2233
    Globomycin

    Bacterial Infection
    Globomycin is a lipopeptide antibiotic and a signal peptidase II (LspA) inhibitor. Globomycin inhibits processing of the prolipoprotein by binding irreversibly to the peptidase. Globomycin has toxic for the mollicute Spiroplasma melliferum with a MIC in the range 6.25-12.5 μM.
  • HY-14879B
    Avibactam sodium hydrate

    NXL-104 hydrate

    Bacterial Antibiotic Infection
    Avibactam sodium hydrate (NXL-104 hydrate) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
  • HY-136124
    Cetilistat impurity 1

    Others Others
    Cetilistat impurity 1 is an impurity of Cetilistat. Cetilistat, an inhibitor of pancreatic lipase, acts as an effective anti-obesity agent. Cetilistat inhibits rat and human pancreatic lipase activity with IC50s of 54.8 nM, and 5.95 nM, respectively.
  • HY-N7603
    Rubrofusarin triglucoside

    Monoamine Oxidase Neurological Disease
    Rubrofusarin triglucoside is a glycoside compound isolated from Cassia obtusifolia Linn seeds. Rubrofusarin triglucoside inhibits human monoamine oxidase A (hMAO-A) with an IC50 of 85.5 μM.
  • HY-N0014
    Icariin

    Ieariline

    Phosphodiesterase (PDE) PPAR Autophagy Inflammation/Immunology Cardiovascular Disease Cancer
    Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC50s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator.
  • HY-N0060
    Ferulic acid

    Coniferic acid

    FGFR Endogenous Metabolite Cancer
    Ferulic acid is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC50s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively.
  • HY-100510
    RAF709

    Raf Cancer
    RAF709 is a potent, selective, and efficacious RAF inhibitor with IC50s of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively. Antitumor efficacy.
  • HY-14660
    Dabrafenib

    GSK2118436A; GSK2118436

    Raf Cancer
    Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-Raf V600E, respectively.
  • HY-10240
    Mericitabine

    RG 7128; R-7128; PSI 6130 diisobutyrate

    HCV Infection
    Mericitabine (RG 7128; R-7128) is a nucleoside inhibitor of the HCV NS5B polymerase that acts as an RNA chain terminator and prevents elongation of RNA transcripts during replication.
  • HY-136534
    RET V804M-IN-1

    RET Cancer
    RET V804M-IN-1 (compound 5) is a wt-RET -selective inhibitors of RETV804M kinase, with an IC50 of 20 nM.
  • HY-B1388
    Homatropine methylbromide

    Homatropine methobromide

    mAChR Neurological Disease
    Homatropine methylbromide (Homatropine methobromide) is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.
  • HY-18361
    TMP195

    HDAC Cancer
    TMP195 is a selective class IIa histone deacetylase (HDAC) inhibitor with Kis of 59, 60, 26, 15 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.
  • HY-12869
    AZD-8835

    PI3K Cancer
    AZD8835 is a potent and selective inhibitor of PI3Kα and PI3Kδ with IC50s of 6.2 and 5.7 nM, respectively.
  • HY-N0060A
    Ferulic acid sodium

    Coniferic acid sodium

    FGFR Endogenous Metabolite Reactive Oxygen Species Cardiovascular Disease Cancer
    Ferulic acid sodium is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC50s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively.
  • HY-12335
    UNC0379

    Histone Methyltransferase Cancer
    UNC0379 is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM; selective over 15 other methyltransferases.
  • HY-124330
    Tripolin A

    (E)-Tripolin A

    Aurora Kinase Others
    Tripolin A ((E)-Tripolin A) is a specific non-ATP competitive Aurora A kinase inhibitor, with IC50 values of 1.5 μM and 7 μM for Aurora A and Aurora B, respectively.
  • HY-70044
    GSK-1070916

    GSK-1070916A

    Aurora Kinase Apoptosis Cancer
    GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with Kis of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.
  • HY-15602B
    Ledipasvir D-tartrate

    GS-5885 D-tartrate

    HCV Infection
    Ledipasvir D-tartrate is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
  • HY-50861
    AZD3988

    Acyltransferase Metabolic Disease
    AZD3988 is a diacylglycerol acyl transferase-1 (DGAT-1) inhibitor with IC50s of 6, 5, 11 nM for human, rat, mouse, respectively.
  • HY-78349
    A 77-01

    TGF-β Receptor Cancer
    A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC50 of 25 nM.
  • HY-12437
    BDP5290

    ROCK Cancer
    BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.
  • HY-112066
    SHIN1

    RZ-2994

    Others Cancer
    SHIN1 (RZ-2994) is a human serine hydroxymethyltransferse 1 and 2 (SHMT1/2) inhibitor with IC50s of 5 and 13 nM, respectively, in an in vitro assay.
  • HY-15241
    NVP-LCQ195

    LCQ-195; AT9311

    CDK Cancer
    NVP-LCQ195 (AT9311; LCQ195) is a small molecule heterocyclic inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM.
  • HY-P0273A
    Histatin 5 TFA

    MMP Inflammation/Immunology
    Histatin 5 TFA inhibits the activity of the host matrix metalloproteinases MMP-2 and MMP-9 with IC50s of 0.57 and 0.25 μM, 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-13264
    Degrasyn

    WP1130

    Deubiquitinase Bcr-Abl Autophagy Apoptosis Cancer
    Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. Degrasyn has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.
  • HY-101873S
    Atorvastatin lactone D5

    HMG-CoA Reductase (HMGCR) Metabolic Disease Inflammation/Immunology
    Atorvastatin lactone D5 is a deuterated form of Atorvastatin lactone (HY-101873). Atorvastatin lactone is a prodrug form of atorvastatin. Atorvastatin is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor.
  • HY-10163
    Dabigatran

    BIBR 953; BIBR 953ZW

    Thrombin Cardiovascular Disease
    Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM).
  • HY-N0447
    8-Gingerol

    TRP Channel Infection Inflammation/Immunology Cancer
    8-Gingerol, found in the rhizomes of ginger (Z. officinale) with oral bioavailability, activates TRPV1, with an EC50 of 5.0 µM. 8-Gingerol inhibits COX-2, and inhibits the growth of H. pylori in vitro.
  • HY-12048
    Chelerythrine chloride

    PKC Bcl-2 Family Apoptosis Autophagy Cancer Metabolic Disease Inflammation/Immunology
    Chelerythrine chloride is a potent, cell-permeable inhibitor of protein kinase C, with an IC50 of 660 nM. Chelerythrine chloride inhibits the Bcl-XL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from Bcl-XL. Chelerythrine chloride induces apoptosis and autophagy.
  • HY-108333
    SB-633825

    Others Cancer Cardiovascular Disease
    SB-633825 is a potent and ATP-competitive inhibitor of TIE2, LOK (STK10) and BRK with IC50s of 3.5 nM, 66 nM, 150 nM, respectively. SB-633825 can inhibit cancer cell growth and angiogenesis.
  • HY-125108
    PHPS1 sodium

    Phosphatase Cancer Cardiovascular Disease
    PHPS1 sodium is a potent and selective Shp2 inhibitor with Kis of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively.
  • HY-14374
    GPP78

    CAY10618

    Nampt Autophagy Cancer Inflammation/Immunology
    GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects.
  • HY-79256
    MMAF-OMe

    Monomethyl auristatin F methyl ester

    ADC Cytotoxin Cancer
    MMAF-Ome, an antitubulin agent, belongs to ADC. MMAF-Ome inhibits several tumor cell lines with IC50s of 0.056 nM, 0.166 nM, 0.183 nM, and 0.449 nM for MDAMB435/5T4, MDAMB361DYT2, MDAMB468, and Raji (5T4 -) cell lines, respectively.
  • HY-114372
    Lycopodine

    Lipoxygenase Caspase Apoptosis Cancer
    Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity. Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation.
  • HY-17377
    Vicriviroc maleate

    SCH-417690 maleate; SCH-D maleate

    CCR HIV Infection Endocrinology
    Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC90s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU 570).
  • HY-N0232
    Psoralidin

    COX Lipoxygenase Notch Reactive Oxygen Species Bacterial Cancer
    Psoralidin, isolated from the seed of Psoralea corylifolia, is a dual inhibitor of COX-2 and 5-LOX, regulates ionizing radiation (IR)-induced pulmonary inflammation.Anti-cancer, anti-bacterial, and anti-inflammatory properties. Psoralidin significantly downregulates NOTCH1 signaling. Psoralidin also greatly induces ROS generation.
  • HY-19322C
    (1S,3R,5R)-PIM447 dihydrochloride

    (1S,3R,5R)-LGH447 dihydrochloride

    Pim Cancer
    (1S,3R,5R)-PIM447 (dihydrochloride) an PIM inhibitor extracted from patent US 20100056576 A1, compound example 72, has IC50 values of 0.095 μM for Pim1, 0.522 μM for Pim2 and 0.369 μM for Pim3.
  • HY-111422
    PLX51107

    Epigenetic Reader Domain Cancer
    PLX51107 is a potent and selective BET inhibitor, with Kds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range).
  • HY-N6682
    Cytochalasin D

    Zygosporin A; NSC 209835

    Arp2/3 Complex Bacterial Antibiotic YAP Infection
    Cytochalasin D (Zygosporin A; NSC 209835) is a potent and cell-permeable inhibitor of actin polymerization derived from fungus, inhibits the G-actin–cofilin interaction by binding to G-actin. Cytochalasin D (Zygosporin A; NSC 209835) also inhibits the binding of cofilin to F-actin and decreases the rate of both actin polymerization and depolymerization in living cells.Cytochalasin D can reduce exosome release, in turn reducing the amount of survivin present in the tumour environment. Cytochalasin D induces phosphorylation and cytoplasmic retention of YAP.
  • HY-14362
    GSK-25

    ROCK Ribosomal S6 Kinase (RSK) Cardiovascular Disease
    GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively).
  • HY-N0043
    Ginsenoside Rd

    Gypenoside VIII

    NF-κB COX Calcium Channel Cytochrome P450 Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease Cancer
    Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca 2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
  • HY-U00179
    CDC801

    Phosphodiesterase (PDE) TNF Receptor Cancer
    CDC801 is a potent and orally active phosphodiesterase 4 (PDE4) and tumor necrosis factor-α (TNF-α) inhibitor with IC50 of 1.1 μM and 2.5 μM, respectively.
  • HY-101842
    ND-646

    Acetyl-CoA Carboxylase Cancer
    ND-646 is an orally bioavailable and steric inhibitor of acetyl-CoA carboxylase (ACC) with IC50s of 3.5 nM and 4.1 nM for recombinant hACC1 and hACC2, respectively.
  • HY-N6770
    Curvularin

    (S)-Curvularin

    NO Synthase Inflammation/Immunology Infection
    Curvularin, a fungal metabolite and a potent mycotoxin naturally isolated from Curvularia lunata, inhibits cytokine-induced nitric oxide synthase (iNOS), with an IC50 of 9.5 µM.
  • HY-N0481
    Roburic acid

    COX Inflammation/Immunology
    Roburic acid, a tetracyclic triterpenoid found in Gentiana macrophylla, acts as an inhibitor of COX, with IC50s of 5 and 9 μM for COX-1 and COX-2, respectively.
  • HY-19568
    Peficitinib

    ASP015K; JNJ-54781532

    JAK Inflammation/Immunology Cancer
    Peficitinib is an oral JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
  • HY-112164B
    IACS-8968 S-enantiomer

    IDO/TDO Inhibitor (S-enantiomer)

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IACS-8968 (S-enantiomer) is the S-enantiomer of IACS-8968. IACS-8968 is a dual IDO and TDO inhibitor, with pIC50s of 6.43 for IDO and <5 for TDO, respectively.
  • HY-112164A
    IACS-8968 R-enantiomer

    IDO/TDO Inhibitor (R-enantiomer)

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IACS-8968 (R-enantiomer) is the R-enantiomer of IACS-8968. IACS-8968 is a dual IDO and TDO inhibitor, with pIC50s of 6.43 for IDO and <5 for TDO, respectively.
  • HY-15186
    Ipatasertib

    GDC-0068; RG7440

    Akt Cancer
    Ipatasertib (GDC-0068) is a highly selective and ATP-competitive pan-Akt inhibitor with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively.
  • HY-16965
    TH287

    DNA/RNA Synthesis Cancer
    TH287 is a potent inhibitor of MTH1 (NUDT1) with an IC50 value of 0.8 nM, less potent for MTH2, NUDT5, NUDT12, NUDT14, and NUDT16.
  • HY-16141
    Cilengitide

    EMD 121974

    Integrin Autophagy Cancer
    Cilengitide, a cyclic RGD-containing peptide, is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50s of 4 and 79 nM, respectively.
  • HY-90009
    Nortadalafil

    Demethyl Tadalafil

    Phosphodiesterase (PDE) Cardiovascular Disease
    Nortadalafil is demethyl Tadalafil, which is a PDE5 inhibitor, currently marketed in pill form for treating erectile dysfunction (ED) under the name Cialis; and under the name Adcirca for the treatment of pulmonary arterial hypertension.
  • HY-12335A
    UNC0379 TFA

    Histone Methyltransferase Cancer
    UNC0379 TFA is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM; selective over 15 other methyltransferases.
  • HY-13263
    CHIR-124

    Checkpoint Kinase (Chk) FLT3 PDGFR Apoptosis Cancer
    CHIR-124 is a potent and selective Chk1 inhibitor with IC50 of 0.3 nM, and also potently targets PDGFR and FLT3 with IC50s of 6.6 nM and 5.8 nM.
  • HY-15186A
    Ipatasertib dihydrochloride

    GDC-0068 dihydrochloride; RG-7440 dihydrochloride

    Akt Cancer
    Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive pan-Akt inhibitor with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively.
  • HY-111860
    SNIPER(ABL)-013

    SNIPER Bcr-Abl Cancer
    SNIPER(ABL)-013, conjugating GNF5 (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 20 μM.
  • HY-15230
    Geldanamycin

    HSP Bacterial Influenza Virus Antibiotic Cancer Infection Inflammation/Immunology
    Geldanamycin is a Hsp90 inhibitor with antimicrobial activity against many Gram-positive and some Gram-negative bacteria. Geldanamycin has anti-influenza virus H5N1 activities.
  • HY-114368
    Kira8

    AMG-18

    IRE1 Inflammation/Immunology
    Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
  • HY-19749
    PD 151746

    Proteasome Cardiovascular Disease
    PD151746 is a calpain inhibitor, shows a 20-fold selectivity for u-calpain (Ki = 0.26 ± 0.03 μM) over m-calpain (Ki = 5.33 ± 0.77 μM).
  • HY-N4185
    Licoflavone A

    Phosphatase Neurological Disease
    Licoflavone A is a flavonoid isolated from the roots of Glycyrrhiza uralensis, inhibits protein tyrosine phosphatase-1B (PTP1B), with an IC50 of 54.5 μM.
  • HY-P1104A
    FC131 TFA

    CXCR HIV Infection
    FC131 TFA is a CXCR4 antagonist, inhibits [ 125I]-SDF-1 binding to CXCR4, with an IC50 of 4.5 nM. Anti-HIV activity.
  • HY-13266A
    BS-181 hydrochloride

    CDK Cancer
    BS-181 hydrochloride is a highly selective CDK7 inhibitor with IC50 of 21 nM, and > 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
  • HY-15427A
    GDC-0834 Racemate

    Btk Inflammation/Immunology
    GDC-0834 Racemate is the racemate form of GDC-0834, which is a potent and selective BTK inhibitor with in vitro IC50s of 5.9 and 6.4 nM in biochemical and cellular assays, respectively.
  • HY-16965A
    TH287 hydrochloride

    DNA/RNA Synthesis Cancer
    TH287 hydrochloride is a potent inhibitor of MTH1 (NUDT1) with an IC50 value of 0.8 nM, less potent for MTH2, NUDT5, NUDT12, NUDT14, and NUDT16.
  • HY-10492
    Dinaciclib

    SCH 727965

    CDK Apoptosis Cancer
    Dinaciclib (SCH 727965) is a potent inhibitor of CDK, with IC50s of 1 nM, 1 nM, 3 nM, and 4 nM for CDK2, CDK5, CDK1, and CDK9, respectively.
  • HY-19706
    ARS-853

    Ras Apoptosis Cancer
    ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation.
  • HY-14879
    Avibactam free acid

    NXL-104 free acid

    Bacterial Antibiotic Infection
    Avibactam free acid (NXL-104 free acid) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
  • HY-15438
    SB 415286

    GSK-3 Apoptosis Metabolic Disease
    SB 415286 is a potent and selective cell permeable inhibitor of GSK-3α, with an IC50 of 77.5 nM, and a Ki of 30.75 nM; SB 415286 is equally effective at inhibiting human GSK-3α and GSK-3β.
  • HY-17468S
    Bumetanide D5

    NKCC Cardiovascular Disease
    Bumetanide D5 is a deuterium labeled Bumetanide. Bumetanide is a selective Na +-K +-Cl - (NKCC1) inhibitor, weakly inhibits NKCC2, with  IC50s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively.
  • HY-116716
    PIN1 inhibitor API-1

    MicroRNA Cancer
    PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development.
  • HY-50673
    Dactolisib

    BEZ235; NVP-BEZ235

    PI3K mTOR Autophagy Cancer
    Dactolisib (BEZ235) is a dual pan-class I PI3K and mTOR kinase inhibitor with IC50s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. Dactolisib (BEZ235) inhibits both mTORC1 and mTORC2.
  • HY-B0132S
    Norfloxacin-d5

    Bacterial Antibiotic
    Norfloxacin-d5 is a deuterium labeled Norfloxacin. Norfloxacin is a fluoroquinolone antibiotic that inhibits the growth of Gram-positive and Gram-negative bacteria (MICs = 4 μg/mL and 1 μg/mL for S. aureus and P. aeruginosa, respectively). Norfloxacin also inhibits the growth S. pseudintermedius, S. aureus, E. coli, Pasturella, and S. canis isolates from dogs (mean MIC50s = 0.25 μg/mL, 1 μg/mL, 0.03 μg/mL, 1 μg/mL, and 1 μg/mL, respectively).
  • HY-101676
    RG-12525

    NID 525

    Leukotriene Receptor PPAR Cytochrome P450 Metabolic Disease
    RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 µM.
  • HY-100349
    SU4312

    PDGFR VEGFR Cancer
    SU4312 is the racemate of (Z)-SU4312 and (E)-SU4312. (Z)-SU4312 inhibits PDGFR and FLK-1 with IC50s of 19.4 and 0.8 μM, respectively. (E)-SU4312 inhibits PDGFR, FLK-1, EGFR, HER-2, and IGF-1R with IC50s of 24.2, 5.2, 18.5, 16.9 and 10.0 μM, respectively.
  • HY-N7510
    12-O-Methylcarnosic acid

    12-Methoxycarnosic acid

    5 alpha Reductase Cancer Infection
    12-O-Methylcarnosic acid (12-Methoxycarnosic acid), a diterpene carnosic acid isolated from the acetone extract of Salvia microphylla, is an active constituent of 5α-reductase inhibition with an IC50 value of 61.7 μM. 12-O-Methylcarnosic acid inhibits proliferation in LNCaP cells. 12-O-Methylcarnosic acid has antioxidant, anti-cancer and antimicrobial activity.
  • HY-B0602
    Desvenlafaxine

    O-Desmethylvenlafaxine

    Serotonin Transporter Neurological Disease
    Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter.
  • HY-12333
    G-749

    FLT3 Apoptosis Cancer
    G-749 is a novel FLT3 inhibitor that showed potent and sustained inhibition of the FLT3 wild type and mutants with IC50s of 0.4/0.6/3.5/7.5 nM for Wt Flt3/D835Y/MV4-11/Molm-14 respectively.
  • HY-122942
    Moracin M

    Phosphodiesterase (PDE) Endogenous Metabolite Inflammation/Immunology
    Moracin M, a phenolic component in the skin of Morus alba L., is a potent phosphodiesterase-4 (PDE4) inhibitor with IC50 values of 2.9, 4.5, >40, and >100 μM for PDE4D2, PDE4B2, PDE5A1, and PDE9A2, respectively. Moracin M has anti-inflammatory activity.
  • HY-18085S
    Quercetin D5

    PI3K Autophagy Mitophagy Apoptosis Cancer
    Quercetin D5 is a deuterium labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.
  • HY-13768
    Topotecan

    SKF 104864A; NSC 609669

    Topoisomerase Autophagy Cancer
    Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95±0.24 μM of GSCs-U87.
  • HY-11006
    KU-57788

    NU7441

    DNA-PK CRISPR/Cas9 Cancer
    KU-57788 (NU7441) is a highly potent and selective DNA-PK inhibitor with an IC50 of 14 nM. KU-57788 is an NHEJ pathway inhibitor. KU-57788 also inhibits PI3K and mTOR with IC50s of 5.0 and 1.7 μM, respectively.
  • HY-136199
    SIRT1-IN-1

    Sirtuin CMV Infection
    SIRT1-IN-1 is a selective SIRT1 inhibitor with an IC50 of 0.205 μM. SIRT1-IN-1 inhibits SIRT2 with an IC50 of 11.5 μM. SIRT1-IN-1, a indole, is a cytomegalovirus (CMV) inhibitors and has antiviral activity.
  • HY-110150
    UNC3230

    Others Cancer Inflammation/Immunology
    UNC3230 is a potent, selective and ATP-competitive PIP5K1C inhibitor with an IC50 of ~41 nM. UNC3230 also inhibits PIP4K2C and does not inhibit any of the other lipid kinases that regulate phosphoinositide levels. UNC3230 has antinociceptive and anticancer effects.
  • HY-15174
    Dactolisib Tosylate

    BEZ235 Tosylate; NVP-BEZ 235 Tosylate

    PI3K mTOR Autophagy Cancer
    Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.
  • HY-70013
    Abiraterone

    CB-7598

    Cytochrome P450 Cancer
    Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
  • HY-125402
    GSK-843

    GSK'843

    RIP kinase Inflammation/Immunology
    GSK-843 (GSK'843) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 8.6 nM, and inhibits kinase activity with an IC50 of 6.5 nM.
  • 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-14434
    Asunaprevir

    BMS-650032

    HCV HCV Protease Infection
    Asunaprevir (BMS-650032) is a potent and orally bioavailable hepatitis C virus (HCV) NS3 protease inhibitor, with IC50 of 0.2 nM-3.5 nM.
  • HY-15651
    Alvelestat

    AZD9668

    Elastase Inflammation/Immunology
    Alvelestat (AZD9668) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM.
  • HY-50862
    Akt1 and Akt2-IN-1

    Akt Cancer
    Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity.
  • HY-14838A
    Etamicastat hydrochloride

    BIA 5-453 hydrochloride

    Dopamine β-hydroxylase Cardiovascular Disease
    Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a potent and reversible dopamine-β-hydroxylase (DBH) inhibitor with an IC50 value of 107 nM. Etamicastat can be used in the research of cardiovascular diseases.
  • HY-13330
    AZD4547

    FGFR Cancer
    AZD4547 is a potent inhibitor of the FGFR family with IC50s of 0.2 nM, 2.5 nM, 1.8 nM, and 165 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
  • HY-10572
    Efavirenz

    DMP 266; EFV; L-743726

    Reverse Transcriptase HIV Autophagy Infection Cancer
    Efavirenz is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture.
  • HY-108518
    SB-772077B dihydrochloride

    ROCK Cardiovascular Disease
    SB-772077B dihydrochloride is an aminofurazan-based Rho kinase (ROCK) inhibitor with IC50s of 5.6 nM and 6 nM toward ROCK1 and ROCK2, respevtively.
  • HY-N0121
    Sesamin

    Others Neurological Disease
    Sesamin, abundant lignan found in sesame oil, is a potent and selective delta 5 desaturase inhibitor in polyunsaturated fatty acid biosynthesis. Sesamin exerts effective neuroprotection against cerbral ischemia.
  • HY-100691
    NOD-IN-1

    NOD-like Receptor (NLR) Inflammation/Immunology
    NOD-IN-1 is a potent mixed inhibitor of nucleotide-binding oligomerization domain (NOD)-like receptors, NOD1 and NOD2, with IC50 of 5.74 μM and 6.45 μM, respectively.
  • HY-N4206
    Leptomerine

    AChE Neurological Disease
    Leptomerine, an alkaloid from stems of Esenbeckia leiocarpa Engl. (Rutaceae) as potential treatment for Alzheimer Disease. Leptomerine inhibits acetyl cholinesterase (AChE) with an IC50 of 2.5 μM. Anticholinesterasic activity.
  • HY-122575
    Aurintricarboxylic acid

    P2X Receptor Influenza Virus Topoisomerase Infection Inflammation/Immunology Neurological Disease
    Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway.Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM.
  • HY-13600
    Clobetasol propionate

    Cytochrome P450 Inflammation/Immunology Endocrinology
    Clobetasol propionate is a potent and selective CYP3A5 inhibitor with an IC50 of 0.206 μM. Clobetasol propionate has no inhibiting on CYP3A4 or other major CYPs. Clobetasol propionate is a corticosteroid and has the potential for psoriasis and other dermatoses research.
  • HY-103021
    LY3200882

    TGF-β Receptor Cancer Inflammation/Immunology
    LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC50 of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent.
  • HY-112711
    LV-320

    Autophagy Cathepsin Cancer
    LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC50 of 24.5 µM and a Kd of 16 µM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo.
  • HY-N0749
    Jatrorrhizine

    AChE 5-HT Receptor Bacterial Neurological Disease
    Jatrorrhizine is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.
  • HY-14600
    Rosiglitazone maleate

    BRL 49653C

    PPAR TRP Channel Autophagy Ferroptosis Cancer Metabolic Disease Inflammation/Immunology
    Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
  • HY-N2009
    3-O-Methylgallic acid

    3,4-Dihydroxy-5-methoxybenzoic acid

    Apoptosis Cancer
    3-O-Methylgallic acid (3,4-Dihydroxy-5-methoxybenzoic acid) is an anthocyanin metabolite and has potent antioxidant capacity. 3-O-methylgallic acid inhibits Caco-2 cell proliferation with an IC50 value of 24.1 μM. 3-O-methylgallic acid also induces cell apoptosis and has anti-cancer effects.
  • HY-B0602A
    Desvenlafaxine succinate hydrate

    O-Desmethylvenlafaxine succinate hydrate

    Serotonin Transporter Neurological Disease
    Desvenlafaxine succinate hydrate, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine succinate hydrate shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter.
  • HY-N0740
    Jatrorrhizine chloride

    AChE 5-HT Receptor Bacterial Inflammation/Immunology Neurological Disease
    Jatrorrhizine chloride is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine chloride is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine chloride reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.
  • HY-N2284
    Sophoflavescenol

    AChE Beta-secretase Phosphodiesterase (PDE) Cancer
    Sophoflavescenol is a prenylated flavonol, which shows great inhibitory activity with IC50 of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC50s of 0.30 µM, 0.17 µM, 17.89 µg/mL, 10.98 µM, 8.37 µM and 8.21 µM, respectively.
  • HY-18299
    Purvalanol B

    NG 95

    CDK Cancer
    Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitor with IC50 values of 6, 6, 9, > 10,000, and 6 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively.
  • HY-122198
    ML367

    Others Cancer
    ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation.
  • HY-111415
    EGFR-IN-5

    EGFR Cancer
    EGFR-IN-5 is a EGFR inhibitor with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFR L858R, EGFR L858R/T790M, and EGFR L858R/T790M/C797S, respectively.
  • HY-114424A
    H-Ile-Pro-Pro-OH hydrochloride

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    H-Ile-Pro-Pro-OH hydrochloride, a milk-derived peptide, inhibits angiotensin-converting enzyme (ACE) with an IC50 of 5 μM. Antihypertensive tripeptides.
  • HY-18360
    TMP269

    HDAC Cancer
    TMP269 is a novel and selective class IIa histone deacetylase (HDAC) inhibitor with IC50s of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.
  • HY-17044
    Duvelisib

    IPI-145; INK1197

    PI3K Cancer
    Duvelisib is a selectivite p100δ inhibitor with IC50 of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively.
  • HY-15190
    NVP-HSP990

    HSP-990

    HSP Apoptosis Cancer
    NVP-HSP990 is a potent and selective Hsp90 inhibitor, with IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively.
  • HY-30237
    Seliciclib

    Roscovitine; CYC202; R-roscovitine

    CDK Cancer
    Seliciclib (Roscovitine) is an orally bioavailable and selective CDKs inhibitor with IC50s of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5, Cdc2, and CDK2, respectively.
  • HY-N0493
    Pectolinarigenin

    COX Lipoxygenase Inflammation/Immunology
    Pectolinarigenin, isolated from Cirsium chanroenicum, is a dual inhibitor of COX-2/5-LOX. Anti-inflammatory activity. Pectolinarigenin has potent inhibitory activities on melanogenesis.
  • HY-135407S
    N-Desethyl Oxybutynin D5 hydrochloride

    Drug Metabolite Neurological Disease
    N-Desethyl Oxybutynin D5 hydrochloride is deuterium labeled N-Desethyl Oxybutynin hydrochloride. N-Desethyl Oxybutynin is the the active metabolite Oxybutynin. Oxybutynin is an anticholinergic agent that inhibits voltage-dependent K + channels.
  • HY-114424
    H-Ile-Pro-Pro-OH

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    H-Ile-Pro-Pro-OH, a milk-derived peptide, inhibits angiotensin-converting enzyme (ACE) with an IC50 of 5 μM. Antihypertensive tripeptides.
  • HY-13914
    Roniciclib

    BAY 1000394

    CDK Cancer
    Roniciclib is an orally bioavailable pan-cyclin dependent kinase (CDK) inhibitor, with IC50s of 5-25 nM for CDK1, CDK2, CDK3, CDK4, CDK7 and CDK9.
  • HY-W001174
    2,5-Dihydroxyacetophenone

    ERK NF-κB Inflammation/Immunology
    2,5-Dihydroxyacetophenone, isolated from Rehmanniae Radix Preparata, inhibits the production of inflammatory mediators in activated macrophages by blocking the ERK1/2 and NF-κB signaling pathways.
  • HY-16425
    RG2833

    RGFP109

    HDAC Cancer
    RG2833 is a brain-penetrant HDAC inhibitor with IC50s of 60 nM and 50 nM for HDAC1 and HDAC3, respectively. The Ki values for HDAC1 and HDAC3 are 32 and 5 nM, respectively.
  • HY-103353
    SID 26681509

    Cathepsin Parasite Cancer Infection
    SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G.
  • HY-10585A
    Valproic acid sodium salt

    Sodium Valproate

    HDAC Autophagy Mitophagy HIV Notch Cancer
    Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
  • HY-12034
    WYE-354

    mTOR Autophagy Apoptosis Cancer
    WYE-354 is an ATP-competitive mTOR inhibitor with an IC50 of 5 nM. WYE-354 also inhibits PI3Kα and PI3Kγ with IC50s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits both mTORC1 and mTORC2.
  • HY-15164A
    Icotinib

    BPI-2009

    EGFR Cancer
    Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q.
  • HY-B0144A
    Pitavastatin

    NK-104

    HMG-CoA Reductase (HMGCR) Autophagy Mitophagy Apoptosis Cancer Metabolic Disease
    Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity.
  • HY-15164
    Icotinib Hydrochloride

    BPI-2009H

    EGFR Cancer
    Icotinib Hydrochloride (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q.
  • HY-14435
    Pyridone 6

    JAK Cancer
    Pyridone 6 is a pan-JAK inhibitor, which potently inhibits the JAK kinase family, with IC50s of 1 nM for JAK2 and TYK2, 5 nM for JAK3, and 15 nM for JAK1, while displaying significantly weaker affinities (130 nM to >10 mM) for other protein tyrosine kinases.
  • HY-19615B
    MS023 dihydrochloride

    Histone Methyltransferase Cancer
    MS023 dihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.
  • HY-19615
    MS023

    Histone Methyltransferase Cancer
    MS023 is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.
  • HY-107371
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde

    NSC95682

    IRE1 Cancer
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) is an IRE-1α inhibitor with an IC50 of 0.08 μM, extracted from patent WO 2008154484 A1, IRE-lα inhibitor compound 3-5.
  • HY-D0143
    Quinine

    Parasite Potassium Channel Infection
    Quinine is an alkaloid derived from the bark of the cinchona tree, acts as an anti-malaria agent. Quinine is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM.
  • HY-112163
    Zotatifin

    eFT226

    Eukaryotic Initiation Factor (eIF) SARS-CoV Apoptosis Cancer
    Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM) and interferes with the assembly of the eIF4F initiation complex. Zotatifin shows robust antiviral effects, it effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis (IC90=37 nM). Zotatifin induces cell apoptosis.
  • HY-10186
    TG 100801

    VEGFR FGFR PDGFR Src Cancer
    TG 100801 is a prodrug that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-111388A
    SEL120-34A monohydrochloride

    CDK Cancer
    SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50s of 4.4 nM and 10.4 nM, respectively, with a Kd of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC50=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726. Has anti-tumor activity.
  • 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-15762
    Valdecoxib

    SC 65872

    COX Inflammation/Immunology
    Valdecoxib is a highly potent and selective inhibitor of COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, respeceively. Valdecoxib can be used in the research of arthritis and pain.
  • HY-15790
    Elobixibat

    A 3309; AZD 7806

    Others Metabolic Disease
    Elobixibat is a potent ileal bile acid transporter (IBAT) inhibitor with IC50 values of 0.53 ± 0.17 nM, 0.13 ± 0.03 nM, and 5.8 ± 1.6 nM for human IBAT, mouse IBAT, and canine IBAT.
  • HY-109049
    Adavivint

    SM04690; Lorecivivint

    Wnt Inflammation/Immunology Cancer
    Adavivint (SM04690; Lorecivivint) is a potent and selective inhibitor of canonical Wnt signaling, with an EC50 of 19.5 nM via a high-throughput TCF/LEF-reporter assay in SW480 colon cancer cells.
  • HY-U00448
    ADDA 5 hydrochloride

    Others Cancer
    ADDA 5 hydrochloride is a partial non-competitive inhibitor of cytochrome c oxidase (CcO), with IC50s of 18.93 μM and 31.82 μM for purified CcO from human glioma and bovine heart, respectively.
  • HY-116649
    CB1 antagonist 2

    Cannabinoid Receptor Neurological Disease
    CB1 antagonist 2 is caimabinoid 1 (CB1) antagonist extracted from patent WO2016184310A1, compound 3, inhibits CB1 in vivo with an IC50 of 25.5 nM.
  • HY-16478
    Trifluridine/tipiracil hydrochloride mixture

    TAS-102

    Nucleoside Antimetabolite/Analog Thymidylate Synthase Cancer
    Trifluridine-tipiracil hydrochloride mixture (TAS-102) is a novel oral combination drug that consists of an antineoplastic thymidine-based nucleoside analog, trifluorothymidine, and a potent thymidine phosphorylase inhibitor, tipiracil, in a 1:0.5 molar ratio.
  • HY-100302
    FR183998 free base

    Sodium Channel Inflammation/Immunology Cardiovascular Disease
    FR183998 free base is a potent Na +/H +-exchange inhibitor, with IC50s of 0.3 nM, 3.1 nM and 6.5 nM by measurement of pHi change in rat lymphocytes, rat and human platelets, respectively.
  • HY-16903
    PKC-IN-1

    PKC Inflammation/Immunology
    PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.
  • HY-12987S
    Pimozide D4

    R6238 D4

    Dopamine Receptor Adrenergic Receptor STAT Cancer Endocrinology Neurological Disease
    Pimozide D4 (R6238 D4) is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
  • HY-N0749A
    Jatrorrhizine hydroxide

    AChE 5-HT Receptor Bacterial Inflammation/Immunology Neurological Disease
    Jatrorrhizine hydroxide is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine hydroxide is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine hydroxide reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.
  • HY-122537A
    Arotinolol

    Adrenergic Receptor 5-HT Receptor Cardiovascular Disease
    Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.
  • HY-15236
    PSI-6206

    RO 2433; GS-331007

    HCV Infection
    PSI-6206 (RO 2433) is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM.
  • HY-13816
    NU6027

    CDK ATM/ATR Cancer
    NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with Kis of 2.5 µM and 1.3 µM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner.
  • HY-12930
    SPR719

    VXc-486

    Topoisomerase Bacterial Infection
    SPR719 (VXc-486) is a gyrase B inhibitor, with bactericidal activity. SPR719 potently inhibits multiple drug-sensitive isolates and drug-resistant isolates of Mycobacterium tuberculosis, with MICs of 0.03 to 0.30 μg/ml and 0.08 to 5.48 μg/ml, respectively.
  • HY-101111
    PF-06840003

    EOS200271

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    PF-06840003 is a highly selective orally bioavailable IDO-1 inhibitor with IC50s of 0.41 μM, 0.59 μM, and 1.5 μM for hIDO-1, dIDO-1, and mIDO-1, respectively.
  • HY-100521
    GKI-1

    Others Cancer
    GKI-1 is a Greatwall (GWL) kinase inhibitor with IC50s of 4.9 and 2.5 µM against hGWL FL and hGWL-KinDom, respectively. GKI-1 robustly inhibits ROCK1 with an IC50 of 11 µM, but only weakly affected PKA.
  • HY-13427
    Allitinib tosylate

    AST-1306 (TsOH)

    EGFR Cancer
    Allitinib tosylate (AST-1306 (TsOH)) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. Allitinib tosylate also inhibits ErbB4 with an IC50 of 0.8 nM. Allitinib tosylate is an anilino-quinazoline compound and has anti-cancer activity
  • HY-135652
    Hexyl gallate

    Hexyl 3,4,5-trihydroxybenzoate

    Bacterial Parasite Infection
    Hexyl gallates (Hexyl 3,4,5-trihydroxybenzoate) shows antibacterial activity and inhibits the production of rhamnolipid and pyocyanin by inhibiting RhlR. Hexyl gallate, a alkyl ester derivative of gallic acid, exhibits potent antimalarial activity against Plasmodium falciparum, with IC50 of 0.11 mM.
  • HY-13002
    Torin 2

    mTOR DNA-PK Autophagy Apoptosis Cancer
    Torin 2 is an mTOR inhibitor with EC50 of 0.25 nM for inhibiting cellular mTOR activity, and exhibits 800-fold selectivity over PI3K (EC50: 200 nM). Torin 2 also inhibits DNA-PK with an IC50 of 0.5 nM in the cell free assay. Torin 2 can suppress both mTORC1 and mTORC2.
  • HY-18095A
    CX-6258 hydrochloride hydrate

    Pim Cancer
    CX-6258 hydrochloride hydrate is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively.
  • HY-18095
    CX-6258

    Pim Cancer
    CX-6258 is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively.
  • HY-B0580S
    Ketorolac D5

    COX Inflammation/Immunology
    Ketorolac D5 is a deuterium labeled Ketorolac. Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2.
  • HY-100626
    WNK463

    Ser/Thr Protease Cancer
    WNK463 is an orally bioavailable pan-With-No-Lysine (K) (WNK)-kinase inhibitor with IC50s of 5 nM, 1 nM, 6 nM, and 9 nM for WNK1, WNK2, WNK3, and WNK4, respectively.
  • HY-109080
    Belvarafenib

    HM95573; GDC-5573; RG6185

    Raf Cancer
    Belvarafenib (HM95573) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAF v600E and C-RAF respectively.
  • HY-100870
    ABX464

    HIV Infection
    ABX464 is a potent anti-HIV agent. ABX464 inhibits HIV-1 replication in stimulated peripheral blood mononuclear cells (PBMCs) with an IC50 ranging between 0.1 μM and 0.5 μM.
  • HY-15064
    HC-030031

    TRP Channel Neurological Disease
    HC-030031 is a potent and selective TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively.
  • HY-10398
    CTS-1027

    Ro 1130830; RS 130830

    MMP Cancer
    CTS-1027 is a potent small molecule inhibitor of MMPs, with IC50s of 0.3 nM, 0.5 nM for MMP2, MMP13, respectively, and has > 1,000 fold selectivity over MMP1.
  • HY-103178
    MRE3008F20

    Adenosine Receptor Cancer
    MRE3008F20 is a highly potent and selective antagonist of adenosine A3 receptor (AA3R), inhibiting agonist-induced cAMP elevation in resting T lymphocytes with an IC50 of 5 nM.
  • HY-18095B
    CX-6258 hydrochloride

    Pim Cancer
    CX-6258 hydrochloride is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively.
  • HY-100270
    Rho-Kinase-IN-1

    ROCK Cancer
    Rho-Kinase-IN-1 is a Rho kinase (ROCK) inhibitor (Ki values of 30.5 and 3.9 nM for ROCK1 and ROCK2, respectively) extracted from US20090325960A1, compound 1.008.
  • HY-12137
    Volasertib

    BI 6727

    Polo-like Kinase (PLK) Apoptosis Cancer
    Volasertib is a highly potent Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM, as well as the two closely related kinases PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively.
  • HY-14718A
    Resminostat hydrochloride

    RAS2410 hydrochloride; 4SC-201 hydrochloride

    HDAC Cancer
    Resminostat hydrochloride is a potent inhibitor of HDAC1, HDAC3 and HDAC6, with mean IC50 values of 42.5, 50.1, 71.8 nM, respectively, and shows less potent activities against HDAC8, with an IC50 of 877 nM.
  • HY-100742A
    (R)-GNE-140

    Lactate Dehydrogenase Cancer
    (R)-GNE-140 is a potent lactate dehydrogenase A (LDHA) inhibitor, with IC50s of 3 nM and 5 nM for LDHA and LDHB, respectively; (R)-GNE-140 is 18-fold more potent than S enantiomer.
  • HY-117661
    SPHINX31

    SRPK Cancer
    SPHINX31 is a potent and selective inhibitor of serine/arginine-rich protein kinase 1 (SRPK1), with an IC50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 is a potential topical therapeutic for neovascular eye disease.
  • HY-10403
    PH-797804

    p38 MAPK Autophagy Inflammation/Immunology Cancer
    PH-797804 is a ATP-competitive, selective p38α/p38β inhibitor (IC50=26 nM and Ki=5.8 nM for p38α; Ki=40 nM for p38β) and does not inhibit JNK2.
  • HY-136427
    KRM-III

    Others Inflammation/Immunology
    KRM-III is a potent and orally active T-cell antigen receptor (TCR) inhibitor. KRM-III inhibits TCR- and phorbol myristate acetate/ionomycin-induced activation of nuclear factor of activated T cells (NFAT) and T-cell proliferation with an IC50 of ~5 μM. Anti-inflammatory activity.
  • HY-P0018
    Pepstatin

    Pepstatin A

    Proteasome HIV Protease Autophagy Infection Cancer
    Pepstatin (Pepstatin A) is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
  • HY-D0143B
    Quinine hemisulfate hydrate

    Parasite Potassium Channel Infection
    Quinine hemisulfate hydrate is an alkaloid derived from the bark of the cinchona tree, acts as an anti-malaria agent. Quinine hemisulfate hydrate is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM.
  • HY-14134
    BMS-378806

    BMS-806

    HIV Infection
    BMS-378806 is a potent HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions. BMS-378806 selectively inhibits the binding of HIV-1 gp120 to the CD4 receptor with EC50 of 0.85-26.5 nM in virus.
  • HY-P0018A
    Pepstatin Trifluoroacetate

    Pepstatin A Trifluoroacetate

    Proteasome HIV Protease Infection
    Pepstatin Trifluoroacetate (Pepstatin A Trifluoroacetate) is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
  • HY-P0018B
    Pepstatin Ammonium

    Pepstatin A Ammonium

    Proteasome HIV Protease Cancer Infection
    Pepstatin Ammonium is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
  • HY-N0822
    Shikonin

    C.I. 75535; Isoarnebin 4

    Chloride Channel Pyruvate Kinase NF-κB TNF Receptor HIV Cancer
    Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis.
  • HY-N6818
    5,​7,​4'-​Trimethoxyflavone

    Apoptosis Caspase PARP Cancer
    5,7,4'-Trimethoxyflavone is isolated from Kaempferia parviflora (KP) that is a famous medicinal plant from Thailand. 5,7,4'-Trimethoxyflavone induces apoptosis, as evidenced by increments of sub-G1 phase, DNA fragmentation, annexin-V/PI staining, the Bax/Bcl-xL ratio, proteolytic activation of caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein.5,7,4'-Trimethoxyflavone is significantly effective at inhibiting proliferation of SNU-16 human gastric cancer cells in a concentration dependent manner.
  • HY-N2038
    3,​5,​6,​7,​8,​3',​4'-​Heptemthoxyflavone

    Others Cancer Neurological Disease
    3,5,6,7,8,3',4'-heptamethoxyflavone, a flavonoid in C. unshiu peels, exhibits anti-tumor-initiating effect and Anti-neuroinflammatory activity. 3,5,6,7,8,3',4'-heptamethoxyflavone inhibits collagenase activity and increased type I procollagen content in HDFn cells. 3,5,6,7,8,3',4'-heptamethoxyflavone induces brain-derived neurotrophic factor (BDNF) expression via cAMP/ERK/CREB signaling and reduces phosphodiesterase activity in C6 cells.
  • HY-108464A
    Phenamil methanesulfonate

    Sodium Channel TRP Channel Metabolic Disease Inflammation/Immunology
    Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM. Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca 2+ transport with an IC50 of 140 nM in a Ca 2+ uptake assay. Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease.
  • HY-16561
    Resveratrol

    trans-Resveratrol; SRT501

    IKK Autophagy Mitophagy Sirtuin Apoptosis Bacterial Fungal Antibiotic Keap1-Nrf2 Cancer Infection Inflammation/Immunology
    Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model.
  • 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-15178
    Oglemilast

    GRC 3886

    Phosphodiesterase (PDE) Inflammation/Immunology
    Oglemilast (GRC 3886) is a potent and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 0.5 nM for PDE4D3. Oglemilast inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast has the potential for inflammatory airway diseases.
  • HY-17470
    Mizoribine

    NSC 289637; HE 69

    HCV SARS-CoV Inflammation/Immunology
    Mizoribine (NSC 289637), an imidazole nucleoside, inhibits HCV RNA replication with IC50 of approximately 100 μM for anti-HCV activity. Immunosuppressant. Mizoribine, an IMPDH inhibitor, inhibits replication of SARS-CoV with IC50s of 3.5 μg/mL and 16 μg/mL for SARS-CoV Frankfurt-1 and SARS-CoV HKU39849, respectively.
  • HY-101813
    Laflunimus

    HR325

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Prostaglandin Receptor Inflammation/Immunology
    Laflunimus (HR325) is an immunosuppressive agent and an analogue of the Leflunomide-active metabolite A77 1726. Laflunimus is an orally active inhibitor of dihydroorotate dehydrogenase (DHODH). Laflunimus suppresses immunoglobulin (Ig) secretion, with IC50 values of 2.5 and 2 µM for IgM and IgG, respectively. Laflunimus also is a prostaglandin endoperoxide H synthase (PGHS) -1 and -2 inhibitor.
  • HY-10585
    Valproic acid

    VPA; 2-Propylpentanoic Acid

    HDAC Autophagy Mitophagy HIV Notch Cancer
    Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
  • HY-101451
    PBIT

    Histone Demethylase Cancer
    PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1) histone demethylase with an IC50 of about 3 μM . PBIT also inhibits JARID1A and JARID1C with IC50s of 6 μM and 4.9 μM, respectively.
  • HY-10468
    NM107

    2'-C-Methylcytidine; NM-107

    HCV Infection
    NM107 (2'-C-Methylcytidine) is an nucleoside inhibitor of the hepatitis C virus (HCV) NS5B polymerase, the EC50 of NM107 in the wild-type replicon cells is 1.85 μM.
  • HY-18748
    BQR-695

    NVP-BQR695

    PI4K Parasite Infection
    BQR-695 is a PI4KIIIβ inhibitor with IC50s of 80 and 3.5 nM for human PI4KIIIβ and Plasmodium variant of PI4KIIIβ, respectively.
  • HY-16294
    LY2090314

    GSK-3 Cancer
    LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.
  • HY-N1374
    Magnolin

    ERK Inflammation/Immunology
    Magnolin, a major component of Magnolia flos (Shin-Yi), inhibits the Ras/ERKs/RSK2 signaling axis by targeting the active pocket of ERK1 and ERK2 with IC50s of 87 nM and 16.5 nM, respectively.
  • HY-109080A
    Belvarafenib TFA

    HM95573 TFA; GDC-5573 TFA; RG6185 TFA

    Raf Cancer
    Belvarafenib TFA (HM95573 TFA) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv 600E and C-RAF respectively.
  • HY-15749
    XL228

    Aurora Kinase Bcr-Abl IGF-1R Src Cancer Endocrinology
    XL228 is a multi-targeted tyrosine kinase inhibitor with IC50s of 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src and Lyn, respectively.
  • HY-129150
    Ganoderic acid TR

    Influenza Virus Infection
    Ganoderic acid TR is a broad-spectrum inhibitor against influenza neuraminidases (NAs), particularly H5N1 and H1N1 neuraminidases. The IC50 values of 10.9 and 4.6 μM, respectively.
  • HY-10162
    Olaparib

    AZD2281; KU0059436

    PARP Autophagy Mitophagy Cancer
    Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.
  • HY-101653
    MHP 133

    AChE mAChR 5-HT Receptor Neurological Disease
    MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
  • HY-110100
    CPYPP

    Others Inflammation/Immunology
    CPYPP is a DOCK2-Rac1 interaction inhibitor. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2 DHR-2 for Rac1 in a dose-dependent manner with an IC50 of 22.8 µM. CPYPP also inhibits DOCK180 and DOCK5 and less inhibits DOCK9.
  • HY-10211
    Tanespimycin

    17-AAG; NSC 330507; CP 127374

    HSP Autophagy Mitophagy Bacterial Apoptosis Antibiotic Cancer Infection
    Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression.
  • HY-N6972
    Cepharanthine

    HIV Autophagy Apoptosis Cancer Infection Inflammation/Immunology
    Cepharanthine, an alkaloid derived from Stephania cepharantha Hayata, with possesses anti-inflammatory and antioxidative activities. Cepharanthine attenuates muscle and kidney injuries induced by limb ischemia/reperfusion (I/R). Cepharanthine induces autophagy, apoptosis and cell cycle arrest in breast cancer cells. Cepharanthine inhibits the HIV-1 entry process by reducing plasma membrane fluidity.
  • HY-15844
    AG-825

    Tyrphostin AG-825

    EGFR Apoptosis Cancer Inflammation/Immunology Neurological Disease
    AG-825 (Tyrphostin AG-825) is a selective and ATP-competitive ErbB2 inhibitor which suppresses tyrosine phosphorylation, with an IC50 of 0.35 μM. AG-825 displays anti-cancer activity. AG825 significantly accelerates apoptosis of human neutrophils. AG-825 is a potential agent for overcoming Mn-induced neurotoxicity or AD development.
  • HY-N0319
    Salvianolic acid C

    Cytochrome P450 Cancer
    Salvianolic acid C is a noncompetitive Cytochrome P4502C8 (CYP2C8) inhibitor and a moderate mixed inhibitor of Cytochrome P45022J2 (CYP2J2), with Kis of 4.82 μM and 5.75 μM for CYP2C8 and CYP2J2, respectively.
  • HY-10044
    WYE-132

    WYE-125132

    mTOR Apoptosis Cancer
    WYE-132 (WYE-125132) is a highly potent, ATP-competitive, and specific mTOR kinase inhibitor (IC50: 0.19±0.07 nM; >5,000-fold selective versus PI3Ks). WYE-132 (WYE-125132) inhibits mTORC1 and mTORC2.
  • HY-110195
    Smurf1-IN-A01

    A01

    Others Others
    Smurf1-IN-A01 (A01) is an ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) inhibitor with a kd of 3.664 nM, which increases BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation.
  • HY-16952A
    Bepridil hydrochloride hydrate

    (±)-Bepridil hydrochloride hydrate; Org 5730 hydrochloride hydrate

    Calcium Channel Cardiovascular Disease
    Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) is a non-selective, long-acting Ca + channel antagonist and Na +, K + channel inhibitor, with antianginal and type I antiarrhythmic effects. Bepridil hydrochloride hydrate also acts as a cardiac Na +/Ca2 + exchange (NCX1) inhibitor. Bepridil hydrochloride hydrate can be used for the research of cardiovascular disorders.
  • HY-18666
    D77

    HIV Infection
    D77 is anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75. D77 inhibits HIV-1(IIIB) replication by EC50 value of 23.8 μg/ml in MT-4 cell (5.03 μg/ml for C8166 cells).
  • HY-101494
    LY3214996

    ERK Cancer
    LY3214996 is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. LY3214996 potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. LY3214996 shows potent antitumor activities in cancer models with MAPK pathway alterations.
  • HY-106198
    Lidorestat

    IDD-676

    Aldose Reductase Metabolic Disease
    Lidorestat (IDD-676) is a potent, selective and orally active aldose reductase inhibitor with an IC50 of 5 nM. Lidorestat can be used for chronic diabetes complications. Lidorestat also improves nerve conduction and reduces cataract formation.
  • HY-10941
    VER-155008

    HSP Autophagy Neurological Disease Cancer
    VER-155008 is an inhibitor of Hsp70, with IC50s of 0.5 μM, 2.6 μM, and 2.6 μM for Hsp70, Hsc70 and Grp7, respectively, and with a Kd of 0.3 μM for Hsp70.
  • HY-13814
    PR-619

    Deubiquitinase Autophagy Cancer
    PR-619 is a broad-range DUB inhibitor with EC50 of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively.
  • HY-12494
    LDC1267

    TAM Receptor Inflammation/Immunology Cancer
    LDC1267 is a highly selective TAM (Tyro3, Axl and Mer) kinase inhibitor with IC50s of <5 nM/8 nM/29 nM for Tyro3,Axl and Mer respectively.
  • HY-103504
    (S)-SNAP5114

    GABA Receptor Neurological Disease
    (S)-SNAP5114 is a selective GABA transport inhibitor, with IC50 values of 5 μM and 21 μM for hGAT-3 and rGAT-2, respectively. (S)-SNAP5114 is an anticonvulsant drug.
  • HY-15761
    AZD2858

    GSK-3 Neurological Disease
    AZD2858 is a potent, orally active GSK-3 inhibitor, with IC50s of 0.9 and 5 nM for GSK-3α and GSK-3β, respectively, used in the research of fracture healing.
  • HY-10721
    PF-AKT400

    AKT protein kinase inhibitor

    Akt Cancer
    PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).
  • HY-14609
    MPEP Hydrochloride

    mGluR Neurological Disease
    MPEP Hydrochloride is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP Hydrochloride has anxiolytic-or antidepressant-like effects.
  • HY-14291
    Vildagliptin

    LAF237; NVP-LAF 237

    Dipeptidyl Peptidase Ferroptosis Apoptosis Metabolic Disease
    Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity.
  • HY-B0825A
    Fenpyroximate

    Parasite Infection
    Fenpyroximate is an acaricide and insecticide against many mites and insect pests of agricultural crops and ornamentals. Fenpyroximate is also a strong inhibitor of bovine heart mitochondrial NADH-ubiquinone oxidoreductase (complex I), binds to the ND5 subunit.
  • HY-14609A
    MPEP

    mGluR Neurological Disease
    MPEP is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP has anxiolytic-or antidepressant-like effects.
  • HY-15602A
    Ledipasvir (acetone)

    GS-5885 acetone

    HCV Infection
    Ledipasvir acetone (GS-5885 acetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
  • HY-15136
    Lonafarnib

    Sch66336

    Farnesyl Transferase Autophagy Influenza Virus Cancer Infection
    Lonafarnib is an orally bioavailable farnesyl protein transferase (FPTase) inhibitor for H-ras, K-ras and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib has anti-hepatitis delta virus (HDV) activities.
  • HY-15141
    Staurosporine

    Antibiotic AM-2282; STS; AM-2282

    PKC PKA Apoptosis Bacterial Fungal Antibiotic Cancer Infection
    Staurosporine is a potent and non-selective inhibitor of protein kinases with IC50s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively. Staurosporine is an apoptosis inducer.
  • HY-103241
    Ro 90-7501

    Amyloid-β ATM/ATR Phosphatase Apoptosis Cancer Neurological Disease
    Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces 42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells.
  • HY-103045
    CMPD101

    PKC ROCK Cardiovascular Disease
    CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure.
  • HY-10626
    T0901317

    LXR FXR ROR Apoptosis Cancer Metabolic Disease Cardiovascular Disease
    T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα. T0901317 activates FXR with an EC50 of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.
  • HY-111787
    CSF1R-IN-2

    Src c-Met/HGFR c-Fms Cancer
    CSF1R-IN-2 (compound 5) is an oral-active inhibitor of SRC, MET and c-FMS, with IC50 values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively.
  • HY-101257A
    CDK7-IN-1

    CDK Cancer
    CDK7-IN-1, an analog of YKL-5-124, is a cyclin-dependent kinase 7 (cdk7) inhibitor, with an IC50 of less than 100 nM, extracted from patent WO 2016105528 A2, Compound 215.
  • HY-123979
    ζ-Stat

    NSC37044

    PKC Apoptosis Cancer
    ζ-Stat (NSC37044) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro.
  • HY-12681
    CCT251545

    Wnt Cancer
    CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with an IC50 of 5 nM in 7dF3 cells. CCT251545 is a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
  • HY-N2434
    [10]-Shogaol

    COX Cancer
    [10]-Shogaol is an antioxidant from Zingiber officinale for human skin cell growth and a migration enhancer. [10]-Shogaol inhibits COX-2 with an IC50 of 7.5 μM and has antiproliferation activity.
  • HY-10858
    WAY 316606

    sFRP-1 Cancer
    WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM.
  • HY-80012
    SJB3-019A

    Deubiquitinase Cancer
    SJB3-019A is a potent and novel USP1 inhibitor, 5 times more potent than SJB2-043 in promoting ID1 degradation and cytoxicity in K562 cells with IC50 of 0.0781 μM.
  • HY-P1045
    187-1, N-WASP inhibitor

    Arp2/3 Complex Others
    187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
  • HY-P1045A
    187-1, N-WASP inhibitor TFA

    Arp2/3 Complex Others
    187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
  • HY-112144
    TP0463518

    HIF/HIF Prolyl-Hydroxylase Metabolic Disease
    TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with a Ki value of 5.3 nM for human PHD2. TP0463518 also inhibits human PHD1/PHD3 with IC50s of 18 and 63 nM as well as monkey PHD2 with an IC50 value of 22 nM.
  • HY-18009
    LFM-A13

    Btk Polo-like Kinase (PLK) JAK Cancer
    LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.
  • HY-W013857
    Lavendustin C

    CaMK EGFR Src Cancer
    Lavendustin C is a potent Ca 2+ calmodulin-dependent kinase II (CaMK II) inhibitor with an IC50 of 0.2 µM. Lavendustin C inhibits EGFR-associated tyrosine kinase (IC50=0.012 µM) and pp60 c-src(+) kinase (IC50=0.5 µM) .
  • HY-B0006A
    Carvedilol phosphate hemihydrate

    BM 14190 phosphate hemihydrate

    Adrenergic Receptor Autophagy Cancer Inflammation/Immunology Cardiovascular Disease
    Carvedilol phosphate hemihydrate (BM 14190 phosphate hemihydrate) is a non-selective β/α-1 blocker. Carvedilol phosphate hemihydrate inhibits lipid peroxidation with an IC50 of 5 μM. Carvedilol phosphate hemihydrate is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol phosphate hemihydrate is an autophagy inducer that inhibits the NLRP3 inflammasome.
  • HY-10330
    Toceranib

    SU11654; PHA 291639E

    PDGFR VEGFR c-Kit Cancer
    Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors.
  • HY-10197
    Wortmannin

    SL-2052; KY-12420

    PI3K Polo-like Kinase (PLK) Autophagy Cancer
    Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC50s of 5.8 and 48 nM, respectively.
  • HY-109091
    Lanraplenib

    GS-9876

    Syk Inflammation/Immunology
    Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib (GS-9876) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.
  • HY-B0422S
    Nateglinide D5

    A4166 D5; Senaglinide D5

    Potassium Channel Dipeptidyl Peptidase Metabolic Disease
    Nateglinide D5 is a deuterium labeled Nateglinide. Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K + channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus[1] [2] .
  • HY-10330A
    Toceranib phosphate

    SU11654 phosphate; PHA 291639E phosphate

    PDGFR VEGFR c-Kit Cancer
    Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors .
  • HY-N0736
    Coptisine chloride

    Indoleamine 2,3-Dioxygenase (IDO) Bacterial Influenza Virus Cancer Infection Metabolic Disease
    Coptisine chloride is an alkaloid from Chinese goldthread, and acts as an efficient uncompetitive IDO inhibitor with a Ki value of 5.8 μM and an IC50 value of 6.3 μM. Coptisine chloride is a potent H1N1 neuraminidase (NA-1) inhibitor with an IC50 of 104.6 μg/mL and can be used for influenza A (H1N1) infection.
  • HY-115510
    SPR inhibitor 3

    SPRi3

    Others Inflammation/Immunology
    SPR inhibitor 3 (SPRi3) is a potent sepiapterin reductase (SPR) inhibitor. SPR inhibitor 3 (SPRi3) displays high binding affinity to human SPR in a cell-free assay (IC50=74 nM) and efficiently reduces biopterin levels in a cell-based assay (IC50=5.2 μM). SPR inhibitor 3 (SPRi3) reduces neuropathic and inflammatory pain through a reduction of BH4 levels.
  • HY-12276
    MALT1 inhibitor MI-2

    MALT1 Cancer
    MALT1 inhibitor MI-2 is a MALT1 inhibitor (IC50=5.84 μM). MALT1 inhibitor MI-2 binds directly to MALT1, irreversibly suppresses protease function and is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MALT1 inhibitor MI-2 shows nontoxic to animals.
  • HY-123604A
    TH1834 dihydrochloride

    Histone Acetyltransferase Apoptosis Cancer
    TH1834 dihydrochloride is a specific Tip60 (KAT5) histone acetyltransferase inhibitor. TH1834 dihydrochloride induces apoptosis and increases DNA damage in breast cancer. TH1834 dihydrochloride does not affect the activity of related histone acetyltransferase MOF. Anticancer activity.
  • HY-N2463
    Kushenol E

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    Kushenol E is a class of flavonoids isolated from Sophora flavescens and is a non-competitive indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 of 7.7 µM and a Ki of 9.5 µM, has anti-tumor activity.
  • HY-10358
    MK-2206 dihydrochloride

    MK-2206 (2HCl)

    Akt Autophagy Apoptosis Cancer
    MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy.
  • HY-111532
    (3R,4R)-A2-32-01

    Bacterial Infection
    (3R,4R)-A2-32-01 (compound 2), an anti-virulence drug, is a specific caseinolytic protein proteases (ClpP) inhibitor with an EC50 of 4.5 μM, and shows a tolerable cytotoxicity.
  • HY-103018
    Gusacitinib

    ASN-002

    JAK Syk Cancer
    Gusacitinib (ASN-002) is an orally active and potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM. Gusacitinib has anti-cancer activity in both solid and hematological tumor types.
  • HY-N0505
    Rosiridin

    Monoamine Oxidase Neurological Disease
    Rosiridin, which is isolated from Rhodiola rosea L., inhibits MAO A and MAO B with potential beneficial effect in depression and senile dementia. Rosiridin shows an inhibition of 83.8% against MAO B at 10 μM (pIC50=5.38).
  • HY-129701
    MCL-1/BCL-2-IN-3

    Bcl-2 Family Cancer
    MCL-1/BCL-2-IN-3 (Compound 2) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor with IC50s of 5.95 and 4.78 μM, respectively.
  • HY-12273
    DMH-1

    Autophagy TGF-β Receptor Cancer
    DMH-1 is a potent and selective BMP inhibitor with IC50s of 27/107.9/<5/47.6 nM for ALK1/ALK2/ALK3/ALK6, respectively.
  • HY-16694
    BAMB-4

    ITPKA-IN-C14

    Others Cancer
    BAMB-4(ITPKA-IN-C14) is a new membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A((ITPKA) with IC50 of 37 μM in ADP-Glo Assay.
  • HY-122605
    TRPM4-IN-1

    CBA

    TRP Channel Cancer Cardiovascular Disease
    TRPM4-IN-1 (CBA) is a potent and selective inhibitor of the cation channel TRPM4, with an IC50 of 1.5 μM. TRPM4-IN-1 can be used for the research of cardiac diseases and prostate cancer.
  • 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-107522
    DL-TBOA

    EAAT2 Neurological Disease
    DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA inhibits the uptake of [ 14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively.
  • HY-10238
    Danoprevir

    ITMN-191; R7227; RO5190591; RG7227

    HCV Protease HCV Infection
    Danoprevir (ITMN-191) is an orally active NS3/4A protease inhibitor for hepatitis C virus (HCV) with an IC50 of 0.29 nM and is selective for NS3/4A over a panel of 53 proteases (IC50 higher than 10 μM). Danoprevir (ITMN-191) inhibits HCV genotypes 1a, 1b, 4, 5, and 6 (IC50s=0.2-0.4 nM) as well as 2b and 3a (IC50s=1.6, 3.5 nM).
  • HY-15730
    Poziotinib

    HM781-36B; NOV120101

    EGFR Apoptosis Cancer
    Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFR wt, HER-2 and HER-4 with IC50s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFR T790M and EGFR L858R/T790M, with IC50s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity.
  • HY-P1717B
    AMY-101 acetate

    Cp40 acetate

    Complement System SARS-CoV Inflammation/Immunology
    AMY-101 acetate (Cp40 acetate), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 acetate (Cp40 acetate) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation.
  • HY-119757
    Tyrphostin AG1433

    SU1433; AG1433

    PDGFR VEGFR Cancer
    Tyrphostin AG1433 (SU1433) is a tyrosine kinases inhibitor. AG1433 is also a selective PDGFRβ and VEGFR-2 (Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively. Tyrphostin AG1433 prevents blood vessel formation.
  • HY-U00364
    CI-949

    Histamine Receptor Prostaglandin Receptor Leukotriene Receptor Inflammation/Immunology Endocrinology
    CI-949 is an allergic mediator release inhibitor, which inhibits histamine, leukotriene C4/D4 (LTC4/LTD4), and thromboxane B2 (TXB2) release with IC50s of 11.4 μM, 0.5 μM and 0.1 μM, respectively.
  • HY-12481
    SAR405

    PI3K Autophagy Cancer
    SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity.
  • HY-101903
    BMS-309403

    FABP Metabolic Disease Cardiovascular Disease
    BMS-309403 is a potent, selective and cell-permeable inhibitor of adipocyte fatty acid binding protein (FABP4) with a Ki of less than 2 nM, which exhibits Ki values of 250 nM for FABP3 and 350 nM for FABP5. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids .
  • HY-B0006
    Carvedilol

    BM 14190

    Adrenergic Receptor Autophagy Cancer Inflammation/Immunology Cardiovascular Disease
    Carvedilol (BM 14190) is a non-selective β/α-1 blocker. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome.
  • HY-W013274
    CPTH2

    Histone Acetyltransferase Apoptosis Cancer
    CPTH2 is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B).
  • HY-128773A
    MRL-494 hydrochloride

    Bacterial Infection
    MRL-494 hydrochloride, an antibacterial agent, is a inhibitor of β-barrel assembly machine A (BamA) impervious to efflux and the outer membrane permeability barrier. MRL-494 hydrochloride can inhibits Gram-positive (MIC of 12.5 μM for Staphylococcus aureus COL) and Gram-negative (MIC of 25 μM for E. coli JCM158) bacterias.
  • HY-15959
    Savolitinib

    Volitinib; HMPL-504; AZD-6094

    c-Met/HGFR Cancer
    Savolitinib (AZD-6094) is a potent, highly selective, and orally bioavailable c-Met inhibitor with IC50 s of 5 nM and 3 nM for c-Met and p-Met, respectively. Savolitinib (AZD-6094) selectively binds to and inhibits the activation of c-Met in an ATP-competitive manner, and disrupts c-Met signal transduction pathways. Antineoplastic activity.
  • HY-15486
    Salubrinal

    Phosphatase HSV Autophagy Apoptosis Cancer Infection Inflammation/Immunology
    Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation. Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis. Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5.
  • HY-123604
    TH1834

    Histone Acetyltransferase Apoptosis Cancer
    TH1834 is a specific Tip60 (KAT5) histone acetyltransferase (HAT) inhibitor. TH1834 induces apoptosis and increases DNA damage in breast cancer. TH1834 does not affect the activity of related histone acetyltransferase MOF. Anticancer activity.
  • HY-114153
    PLX5622

    c-Fms Neurological Disease
    PLX5622 is a highly selective brain penetrant and oral active CSF1R inhibitor with an Ki of 5.9 nM, for extended and specific microglial elimination, preceding and during pathology development. PLX5622 demonstrates desirable PK properties in varies animals.
  • HY-124047
    RX 67668

    AChE Neurological Disease
    RX 67668 is a potent cholinesterase inhibitor with an IC50 of 5 μM for both acetylcholinesterase (AChE) and butyrylcholinesterase. RX 67668 can reverse the neuromuscular blockade induced by D-tubocurarine. RX 67668 is a muscle relaxant used to relieve skeletal muscle fatigue.
  • HY-14872
    Tideglusib

    NP031112

    GSK-3 Neurological Disease
    Tideglusib (NP031112) is an irreversible GSK-3 inhibitor with IC50s of 5 nM and 60 nM for GSK-3β WT (1 h preincubation) and GSK-3β C199A (1 h preincubation), respectively.
  • HY-120056
    YKL-06-061

    Salt-inducible Kinase (SIK) Inflammation/Immunology
    YKL-06-061 is a potent, selective, second-generation salt-inducible kinase (SIK) inhibitor with IC50 values of 6.56 nM/1.77 nM/20.5 nM for SIK1/2/3, respectively.
  • HY-U00235
    SR121566A

    Integrin Inflammation/Immunology
    SR121566A is a novel non-peptide Glycoprotein IIb/IIIa (GP IIb-IIIa) antagonist, which can inhibit ADP-, arachidonic acid- and collagen-induced human platelet aggregation with IC50s of 46±7.5, 56±6 and 42±3 nM, respectively.
  • HY-100738
    Ubiquitin Isopeptidase Inhibitor I, G5

    NSC144303

    Apoptosis Cancer
    Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively.
  • HY-18932
    DEL-22379

    ERK Apoptosis Cancer
    DEL-22379 is an ERK dimerization Inhibitor. DEL-22379 readily binds to ERK2 with a Kd estimated in the low micromolar range, though binding is detectable even at low nanomolar concentrations. ERK2 dimerization is progressively inhibited with an IC50 of ~0.5 μM.
  • HY-14291A
    Vildagliptin dihydrate

    LAF237 dihydrate; NVP-LAF 237 dihydrate

    Dipeptidyl Peptidase Ferroptosis Apoptosis Metabolic Disease
    Vildagliptin dihydrate (LAF237 dihydrate) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin dihydrate possesses excellent oral bioavailability and potent antihyperglycemic activity.
  • HY-19675
    Naproxen etemesil

    LT-NS 001; MX 1094

    COX Inflammation/Immunology
    Naproxen etemesil is a lipophilic, non-acidic, inactive prodrug of naproxen that is hydrolysed to pharmacologically active Naproxen once absorbed. Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
  • HY-18991
    CCG215022

    PKA Cancer
    CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, GRK5 and GRK1, respectively.
  • 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-B0075
    Melatonin

    N-Acetyl-5-methoxytryptamine

    Melatonin Receptor Autophagy Mitophagy Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress.
  • HY-18944
    FIT-039

    CDK HSV CMV DNA/RNA Synthesis Infection
    FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.
  • HY-19356A
    Didesmethylrocaglamide

    Eukaryotic Initiation Factor (eIF) Apoptosis Cancer
    Didesmethylrocaglamide, a derivative of Rocaglamide, is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. Didesmethylrocaglamide has potent growth-inhibitory activity with an IC50 of 5 nM. Didesmethylrocaglamide suppresses multiple growth-promoting signaling pathways and induces apoptosis in tumor cells. Antitumor activity.
  • HY-15729
    Rociletinib

    CO-1686; AVL-301; CNX-419

    EGFR Cancer
    Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
  • HY-117407
    ALLO-2

    Smo Cancer
    ALLO-2 is a potent drug-resistant Smoothened (Smo) mutant antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM.
  • HY-18644
    CWHM-12

    Integrin Cancer
    CWHM-12 is a potent inhibitor of αV integrins with IC50s of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1.
  • HY-12942
    PF-05175157

    Acetyl-CoA Carboxylase Metabolic Disease
    PF-05175157 is broad spectrum acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 27.0, 33.0, 23.5 and 50.4 nM for ACC1 (human), ACC2 (human), ACC1 (rat), ACC2 (rat), respectively.
  • HY-U00186
    K134

    OPC33509

    Phosphodiesterase (PDE) Cardiovascular Disease
    K134 is a phosphodiesterase 3 (PDE3) inhibitor. The IC50s of K134 toward PDE3A, PDE3B, PDE5, PDE2 and PDE4 are 0.1, 0.28, 12.1, >300 and >300 µM, respectively.
  • HY-110086
    RWJ 50271

    Integrin Inflammation/Immunology
    RWJ 50271 is an selective inhibitor of lymphocyte function-associated antigen-1/intercellular adhesion molecule-1(LFA-1/ICAM-1) interaction with an IC50 of 5.0 μM (HL60 cells).
  • HY-123979A
    ζ-Stat trisodium

    NSC37044 trisodium

    PKC Apoptosis Cancer
    ζ-Stat trisodium (NSC37044 trisodium) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat trisodium can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro.
  • HY-13513
    U-104

    SLC-0111

    Carbonic Anhydrase Cancer
    U-104 (SLC-0111) is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki values of 45.1 nM and 4.5 nM, respectively. U-104 shows a significant delay in tumor growth in mice model.
  • HY-109099
    Pemigatinib

    INCB054828

    FGFR Cancer
    Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma.
  • HY-12830
    M-110

    Pim Cancer
    M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM.
  • HY-N4327
    Eurycomalactone

    NF-κB Infection Inflammation/Immunology
    Eurycomalactone is a natural product found in Eurycoma longifolia Jack., acts as a potent NF-κB inhibitor, with an IC50 of 0.5 μM. Eurycomalactone inhibits protein synthesis, depletes cyclin D1, but does not affect TNFα-induced degradation of IκBα or the phosphorylation of IKKα/β and IκBα.
  • HY-109091B
    Lanraplenib succinate

    GS-9876 succinate

    Syk Inflammation/Immunology
    Lanraplenib succinate (GS-9876 succinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib succinate (GS-9876 succinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.
  • HY-133779
    Gefitinib impurity 5

    Others Others
    Gefitinib impurity 5 is the impurity of Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
  • HY-100036
    MK-4101

    Smo Apoptosis Hedgehog Cancer
    MK-4101 is a Smoothened (SMO) antagonist (IC50 of 1.1 µM for 293 cells ) and also a potent inhibitor of the hedgehog pathway (IC50 of 1.5 µM for mouse cells; IC50 of 1 µM for KYSE180 oesophageal cancer cells). MK-4101 has robust antitumor activity that inhibits tumor cell proliferation and induces extensive apoptosis.
  • HY-N6778
    Paxilline

    Potassium Channel Calcium Channel Neurological Disease
    Paxilline is an indole alkaloid mycotoxin from Penicillium paxilli, acts as a potent BK channels inhibitor by an almost exclusively closed-channel block mechanism. Paxilline also inhibits the sarco/endoplasmic reticulum Ca 2+ ATPase (SERCA) with IC50s between 5 μM and 50 μM for differing isoforms. Paxilline possesses significant anticonvulsant activity.
  • HY-16231
    GGTI-2418

    Others Cancer
    GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors.
  • HY-P1717A
    AMY-101 TFA

    Cp40 TFA

    Complement System SARS-CoV Inflammation/Immunology
    AMY-101 TFA (Cp40 TFA), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 (Cp40) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation.
  • HY-126246
    CDC25B-IN-1

    Phosphatase Cancer
    CDC25B-IN-1 (compound 4a) is a potent inhibitor of cell division cycle 25B (CDC25B) phosphatase, with a Ki of 8.5 μM. CDC25B-IN-1 potently inhibits cell proliferation and colony formation, causes an increase of the G2/M phase.
  • 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-N1074
    Warangalone

    Scandenolone

    Parasite PKA Infection Inflammation/Immunology
    Warangalone is an anti-malarial compound which can inhibit the growth of both strains of parasite 3D7 (chloroquine sensitive) and K1 (chloroquine resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively. Warangalone can also inhibit cyclic AMP-dependent protein kinase catalytic subunit (cAK) with an IC50 of 3.5 μM.
  • HY-19983
    ASP5878

    FGFR Cancer
    ASP5878 is an oral active inhibitor of FGFR 1, 2, 3, and 4, with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM and 3.5 nM for FGFR 1, 2, 3, and 4 kinase activity. ASP5878 has potential antineoplastic activity.
  • HY-107443
    I-BET762 carboxylic acid

    Molibresib carboxylic acid; GSK525762A carboxylic acid; PROTAC BRD4-binding moiety 2

    Ligand for Target Protein for PROTAC Epigenetic Reader Domain Cancer
    I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1.
  • HY-10261A
    Afatinib dimaleate

    BIBW 2992MA2

    EGFR Autophagy Cancer
    Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively.
  • HY-114153A
    PLX5622 hemifumarate

    c-Fms Neurological Disease
    PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor with an Ki of 5.9 nM, for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals.
  • HY-B1464
    Cetylpyridinium chloride

    Bacterial HBV Infection Inflammation/Immunology
    Cetylpyridinium chloride, a cationic quaternary ammonium compound, is an anti-bacterial agent with broad-spectrum activity. Cetylpyridinium chloride is an effective anti-HBV capsid assembly inhibitor with an IC50 of 2.5 μM. Cetylpyridinium chloride is used in pesticides and various types of mouthwashes, and other personal care products.
  • HY-10596
    BMS-688521

    Integrin Inflammation/Immunology
    BMS-688521 is a highly potent, orally active inhibitor of the LFA-1/ICAM interaction, with an IC50 of 2.5 nM in the adhesion assay and an IC50 of 60 nM in the MLR assay. BMS-688521 is efficacious in a mouse allergic eosinophilic lung inflammation model.
  • HY-B1856
    Haloxyfop

    Others Metabolic Disease
    Haloxyfop is an aryloxyphenoxypropionic acid herbicide and is widely used in grass weeds in broad-leaf crops. Haloxyfop inhibits the acetyl coenzyme A carboxylase (EC 6.4.1.2) from corn seedling chloroplasts with an IC50 of 0.5 μM, but has no effect on this enzyme in pea.
  • HY-116761
    GSK467

    Histone Demethylase Cancer
    GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a Ki of 10 nM, shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members.
  • HY-101567
    BMS-986158

    Epigenetic Reader Domain Cancer
    BMS-986158 is a potent BET inhibitor with IC50s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively.
  • HY-104008
    ACY-957

    HDAC Others
    ACY-957 is an orally active and selective inhibitor of HDAC1 and HDAC2, with IC50s of 7 nM, 18 nM, and 1300 nM against HDAC1/2/3, respectively, and shows no inhibition on HDAC4/5/6/7/8/9.
  • HY-100591
    SirReal2

    Sirtuin Cancer Inflammation/Immunology Neurological Disease
    SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1.
  • HY-18686
    AS1949490

    Phosphatase Metabolic Disease
    AS1949490 is a potent and selective SHIP-2 (SH2 domain-containing inositol 5′ phosphatase 2) inhibitor, with an IC50 of 620 nM. AS1949490 activated glucose metabolism via up-regulation of GLUT1 gene in L6 myotubes.
  • HY-136063
    Mefentrifluconazole

    Fungal Cytochrome P450 Infection
    Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent. Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on human aromatase (IC50=0.92 μM).
  • HY-108538
    Ethacrynic acid D5

    Gutathione S-transferase NF-κB Calcium Channel Inflammation/Immunology
    Ethacrynic acid D5 is a deuterium labeled Ethacrynic acid. Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
  • HY-13335
    PKCβ inhibitor 1

    PKC Apoptosis Cancer
    PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε).
  • HY-100574A
    Cl-amidine hydrochloride

    Protein Arginine Deiminase Apoptosis MicroRNA Cancer Inflammation/Immunology
    Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR)-16 expression and causes cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.
  • HY-18340
    (R)​-​CR8

    CR8, (R)-Isomer

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

    CR8, (R)-Isomer trihydrochloride

    CDK Apoptosis Cancer Neurological Disease
    (R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect. (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K.
  • HY-W011391
    GPNA hydrochloride

    Apoptosis Cancer
    GPNA hydrochloride is a well known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride is a specific glutamine (Gln) transporter ASCT2 inhibitor. GPNA hydrochloride also inhibit Na +-dependent carriers, such as SNAT family (SNAT1/2/4/5), and the Na +-independent leucine transporters LAT1/2. GPNA reversibly induces apoptosis in A549 cells.
  • HY-18161
    CCT241736

    FLT3 Aurora Kinase Cancer
    CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM; Aurora-B Kd, 48 nM), FLT3 kinase (Kd, 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd, 38 nM) and FLT3(D835Y) (Kd, 14 nM).
  • HY-13241
    Ralimetinib dimesylate

    LY2228820 dimesylate

    p38 MAPK Autophagy Apoptosis Cancer Inflammation/Immunology
    Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
  • HY-122614
    S29434

    NMDPEF

    Autophagy Neurological Disease
    S29434 (NMDPEF) is a potent, competitive, selective and cell-permeable inhibitor of quinone reductase 2 (QR2), with IC50s ranging from 5 to 16 nM for human QR2 at different organizational levels, and has good selectivity for QR2 over QR1. S29434 (NMDPEF) induces autophagy and inhibits QR2-mediated ROS production.
  • HY-B0144
    Pitavastatin Calcium

    NK-104 hemicalcium; Pitavastatin hemicalcium

    HMG-CoA Reductase (HMGCR) Autophagy Mitophagy Apoptosis Metabolic Disease Cancer
    Pitavastatin Calcium (NK-104 hemicalcium) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin Calcium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity.
  • HY-114459
    Mutant IDH1-IN-4

    Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ≤ 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells.
  • HY-19826
    Isofistularin-3

    DNA Methyltransferase ADC Cytotoxin Autophagy Apoptosis Cancer
    Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM. Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin.
  • HY-15729A
    Rociletinib hydrobromide

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

    EGFR Cancer
    Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
  • HY-13036
    (Rac)-IBT6A

    Btk Cancer
    (Rac)-IBT6A is a racemate of IBT6A. IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
  • HY-107515
    LY367385

    mGluR Neurological Disease
    LY367385 is a highly potent and selective mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with > 100 μM for mGlu5a. LY367385 has neuroprotective, anticonvulsant and antiepileptic effects.
  • HY-100492
    Fisogatinib

    BLU-554

    FGFR Cancer
    Fisogatinib (BLU-554) is a potent, highly selective and orally active fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 5 nM. Fisogatinib has significant anti-tumor activity in models of hepatocellular carcinoma (HCC) that are dependent on FGFR4 signalling.
  • HY-N3513
    Mulberrin

    Kuwanon C

    Others Cardiovascular Disease
    Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.
  • HY-13026
    Idelalisib

    CAL-101; GS-1101

    PI3K Autophagy Cancer
    Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.
  • HY-10261
    Afatinib

    BIBW 2992

    EGFR Autophagy Cancer
    Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively.
  • HY-100246
    CI-1044

    PD-189659

    Phosphodiesterase (PDE) Inflammation/Immunology
    CI-1044 is an orally active PDE4 inhibitor with IC50s of 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3, respectively.
  • HY-B0258
    Gemfibrozil

    CI-719

    PPAR Cytochrome P450 Metabolic Disease Cardiovascular Disease
    Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering drug; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
  • HY-15415
    KB-R7943 mesylate

    Na+/Ca2+ Exchanger Autophagy Cancer
    KB-R7943 mesylate is a widely used inhibitor of the reverse Na +/Ca 2+ exchanger (NCXrev) with IC50 of 5.7±2.1 µM. KB-R7943 mesylate induces cancer cell death via activating the JNK pathway and blocking autophagic flux.
  • HY-123931
    ZLDI-8

    Notch Phosphatase Apoptosis Cancer
    ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC50 of 31.6 μM and a Ki of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC50 of 5.32 μM.
  • HY-10012
    AZD-5438

    CDK Cancer
    AZD-5438 is a potent CDK1, CDK2, and CDK9 inhibitor, with IC50s of 16 nM, 6 nM, and 20 nM in cell-free assays, respectively. AZD-5438 shows less inhibition activity against GSK3β, CDK5 and CDK6 .
  • HY-13267
    Droxinostat

    NS 41080

    HDAC Apoptosis Cancer
    Droxinostat(NS41080) is a selective inhibitor of HDAC3, HDAC6, and HDAC8 with IC50 of 16.9, 2.47 and 1.46 μM, respectively; > 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10.
  • HY-100027A
    Ro 41-1049 hydrochloride

    Monoamine Oxidase Neurological Disease
    Ro 41-1049 hydrochloride is a reversible and selective inhibitor of monoamine oxidase-A (MAO-A). An homogeneous population of high affinity binding sites for [ 3H]Ro 41-1049 is found in membrane preparations from human frontal cortex and placenta (Kd values of 16.5 and 64.4 nM, respectively).
  • HY-N0877
    Bufalin

    Na+/K+ ATPase Cancer
    Bufalin is an active component isolated from Chan Su, acts as a potent Na +/K +-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively. Anti-cancer activity.
  • HY-N1390
    Syringaldehyde

    COX Metabolic Disease Inflammation/Immunology
    Syringaldehyde is a polyphenolic compound belonging to the group of flavonoids and is found in different plant species like Manihot esculenta and Magnolia officinalis. Syringaldehyde moderately inhibits COX-2 activity with an IC50 of 3.5 μg/mL. Anti-hyperglycemic and anti-inflammatory activities.
  • HY-N7715
    Ferulic acid acyl-β-D-glucoside

    Ferulic acid glucoside

    Drug Metabolite Others
    Ferulic acid acyl-β-D-glucoside is a metabolite of Ferulic Acid (HY-N0060). Ferulic acid is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC50s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively.
  • HY-136128
    H3B-120

    Potassium Channel Cancer
    H3B-120 is a highly selective, competitive and allosteric carbamoyl phosphate synthetase 1 (CPS1) inhibitor with an IC50 of 1.5 μM and a Ki of 1.4 μM. H3B-120 has anti-cancer activity.
  • HY-136530
    SR18662

    KLF Cancer
    SR18662 is a potent inhibitor of Krüppel-like factor five (KLF5) with an IC50 of 4.4 nM and an analogue of ML264 (HY-19994) with improved inhibitory potency against colorectal cancer cells. SR18662 can be used for the study of colorectal cancer.
  • 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-15147
    XAV-939

    β-catenin PARP Cancer
    XAV-939 is a potent tankyrase inhibitor that targets Wnt/β-catenin signaling. XAV-939 stabilizes axin by inhibiting tankyrase 1 and tankyrase 2 (IC50s of 5 and 2 nM, respectively), thereby stimulating β-catenin degradation. XAV939 binds tightly to the catalytic (PARP) domains of TNKS1 and TNKS2 (Kds of 99 and 93 nM, respectively).
  • 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 inh