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Results for "

Reversible Inhibitors

" in MCE Product Catalog:

464

Inhibitors & Agonists

1

Screening Libraries

1

Fluorescent Dye

9

Peptides

34

Natural
Products

29

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-145373
    BMS-986143

    Btk Inflammation/Immunology
    BMS-986143 is an orally active, reversible BTK inhibitor with an IC50 of 0.26 nM. BMS-986143 also inhibits TEC, BLK, BMX, TXK FGR, YES1, ITK with IC50s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM,19 nM, 21 nM, respectively. BMS-986143 can be used for the research of autoimmune diseases.
  • HY-115902
    FGFR4-IN-7

    FGFR Apoptosis Cancer
    FGFR4-IN-7 (Compound C3) is a covalent reversible FGFR4 inhibitor with an IC50 value of 0.42 μM. FGFR4-IN-7 induces apoptosis via the FGFR4 signaling pathway blockage. FGFR4-IN-7 can be used for the research of hepatocellular carcinoma (HCC).
  • HY-124346
    T-3364366

    Others Metabolic Disease
    T-3364366 is a reversible, slow-binding, thienopyrimidinone delta-5 desaturase (D5D) inhibitor with IC50s of 1.9 nM and 2.1 nM in HepG2 and RLN-10 cells, respectively. T-3364366 exhibits potent D5D (IC500=19 nM) inhibitory activity and excellent selectivity away from delta-6 desaturase (D6D, IC50=6200 nM) and delta-9 desaturase (stearoyl-CoA desaturase, SCD,50 >10000 nM) in the enzymatic activity assay.
  • HY-143881
    FGFR4-IN-6

    FGFR Cancer
    FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC50 value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity.
  • HY-147862
    EGFR-IN-62

    EGFR Apoptosis Cancer
    EGFR-IN-62 (compound 9h) is a potent and reversible EGFR kinase inhibitor, with IC50 values of 10 nM (L858R/T790 M), 29 nM (WT), and 242 nM (L858R/T790 M/C797S), respectively. EGFR-IN-62 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.53 and 1.56 μM, respectively. EGFR-IN-62 induces dose-dependent apoptosis process, G1/G0-phase arrestation, and the inhibition of motility on A549 and/or H1975 cell lines.
  • HY-150587
    Anti-inflammatory agent 31

    ERK NF-κB Inflammation/Immunology
    Anti-inflammatory agent 31 (enone 17) is a kind of andrographolide derivatives, is a anti-inflammatory agent. Anti-inflammatory agent 31 inhibits NF-κB activation by upstream blockade of PI3K/Akt and ERK1/2 MAPK activation. Anti-inflammatory agent 31 shows recovery effective of the intracellular GSH levels and protective effect on liver.
  • HY-B0207A
    Pyridostigmine bromide

    Cholinesterase (ChE) Neurological Disease
    Pyridostigmine bromide is a parasympathomimetic and a reversible cholinesterase inhibitor.
  • HY-B1413
    Eprobemide

    LIS 630

    Monoamine Oxidase Neurological Disease
    Eprobemide is a non-competitive reversible inhibitor of monoamine oxidase A.
  • HY-B0884
    Minaprine

    Monoamine Oxidase Neurological Disease
    Minaprine is a reversible inhibitor of MAO-A; weakly inhibit acetylcholinesterase; an antidepressant for treatment of depression.
  • HY-B0884A
    Minaprine dihydrochloride

    Monoamine Oxidase Neurological Disease
    Minaprine dihydrochloride is a reversible inhibitor of MAO-A; weakly inhibit acetylcholinesterase; an antidepressant for treatment of depression.
  • HY-U00042
    SKF96067

    Proton Pump Inflammation/Immunology
    SKF96067 is a reversible inhibitor of the gastric H +/K +-ATPase.
  • HY-14260
    RS 8359

    Monoamine Oxidase Neurological Disease
    RS 8359 is a selective and reversible MAO-A inhibitor, with antidepressant activity.
  • HY-N1937
    Pristimerin

    Celastrol methyl ester

    Bacterial Cancer
    Pristimerin is a potent and reversible monoacylglycerol lipase (MGL) inhibitor with an IC50 of 93 nM.
  • HY-10836
    Cruzain-IN-1

    Parasite Others
    Cruzain-IN-1 is a covalent and reversible Cruzain inhibitor, with an IC50 of 10 nM.
  • HY-112465
    H-8 dihydrochloride

    PKA Cancer
    H-8 (dihydrochloride) is a cell-permeable, reversible and ATP-competitive PKA inhibitor.
  • HY-14196
    Toloxatone

    MD 69276

    Monoamine Oxidase Neurological Disease
    Toloxatone (MD 69276) is a reversible monoamine oxidase A (MAOA) inhibitor. Antidepressant.
  • HY-B1206
    Neostigmine methyl sulfate

    Cholinesterase (ChE) Neurological Disease
    Neostigmine methyl sulfate is a reversible inhibitor of acetylcholinesterase, can not cross the blood-brain barrier.
  • HY-70075
    CCG-63808

    RGS Protein Cancer
    CCG-63808 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins.
  • HY-103351
    Cathepsin G Inhibitor I

    Cathepsin Inflammation/Immunology
    Cathepsin G Inhibitor I is a potent, selective, reversible, competitive, non-peptide inhibitor of cathepsin G.
  • HY-14947
    Balamapimod

    MKI 833

    MEK Cancer
    Balamapimod (MKI 833) is a reversible Ras/Raf/MEK inhibitor with potential anti-tumor activity.
  • HY-100178
    CX-157

    Monoamine Oxidase Neurological Disease
    CX-157 is a reversible inhibitor of monoamine oxidase-A (MAO-A) with an EC50 of 19.3 ng/mL.
  • HY-B0207AS
    Pyridostigmine-d6 bromide

    Cholinesterase (ChE) Others
    Pyridostigmine D6 bromide is the deuterium labeled Pyridostigmine, which is a parasympathomimetic and a reversible cholinesterase inhibitor.
  • HY-15723
    NSC 23766

    Ras Cancer
    NSC 23766 is a cell-permeable, reversible and specific inhibitor of Rac GTPase, used for cancer treatment.
  • HY-101769
    UAMC00039 dihydrochloride

    Dipeptidyl Peptidase Cancer
    UAMC00039 dihydrochloride is a potent, reversible and competitive dipeptidyl peptidase II inhibitor with an IC50 of 0.48 nM.
  • HY-18690A
    Enasidenib mesylate

    AG-221 mesylate

    Isocitrate Dehydrogenase (IDH) Cancer
    Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes.
  • HY-103058
    GSK199

    Protein Arginine Deiminase Cancer Inflammation/Immunology Cardiovascular Disease
    GSK199 is a reversible and selective PAD4 inhibitor with an IC50 of 200 nM in the absence of calcium.
  • HY-108551
    MG-262

    Proteasome Cancer Inflammation/Immunology Cardiovascular Disease
    MG-262 is a reversible proteasome inhibitor with diverse biological activities.
  • HY-14984
    N6022

    GSNOR Inflammation/Immunology
    N6022 is a potent, selective, reversible, and efficacious S-Nitrosoglutathione reductase(GSNOR) inhibitor with IC50 of 8 nM.
  • HY-116533
    RMM-46

    MAPKAPK2 (MK2) Cancer
    RMM-46 is a selective and reversible covalent inhibitor for MSK/RSK-family kinases.
  • HY-B0882
    Edrophonium chloride

    Cholinesterase (ChE) Neurological Disease
    Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
  • 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-101793
    BMS-935177

    Btk Inflammation/Immunology
    BMS-935177 is a potent and selective reversible inhibitor of Bruton’s tyrosine kinase (Btk) with an IC50 of 3 nM.
  • HY-112411
    PD 174265

    EGFR Cancer
    PD 174265 is a potent, cell-permeable, reversible, and selective inhibitor of EGFR with an IC50 of 450 pM.
  • HY-N0918
    Desmethoxyyangonin

    Demethoxyyangonin; 5,6-Dehydrokavain

    Monoamine Oxidase Others
    Desmethoxyyangonin is one of the six major kavalactones found in the Piper methysticum (kava) plant; reversible inhibitor of MAO-B.
  • HY-15958
    VBY-825

    Cathepsin Cancer
    VBY-825 is a novel, reversible cathepsin inhibitor with high potency against cathepsins B, L, S and V.
  • HY-147860
    EGFR-IN-61

    EGFR Cancer
    EGFR-IN-61 (compound 22a) is a potent EGFR kinase inhibitor, with IC50 values of 42 nM (L858R/T790 M), 137 nM (L858R/T790 M/C797S), and 743 nM (WT), respectively. EGFR-IN-61 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.14 and 1.82 μM, respectively.
  • HY-16904
    RI-2

    RAD51 Cancer
    RI-2 is a reversible RAD51 inhibitor, with an IC50 of 44.17 μM, and specifically inhibits homologous recombination repair in human cells.
  • HY-15465A
    KN-93 hydrochloride

    CaMK Autophagy Cancer
    KN-93 hydrochloride is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.
  • HY-117226A
    GSK 690 Hydrochloride

    Histone Demethylase Others
    GSK 690 (Hydrochloride) is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a Kd value of 9 nM and a biochemical IC50 of 37 nM.
  • HY-117226
    GSK 690

    Histone Demethylase Cancer
    GSK 690 is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a Kd value of 9 nM and a biochemical IC50 of 37 nM.
  • HY-15465
    KN-93

    CaMK Autophagy Cancer
    KN-93 is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.
  • 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-19908
    BAY-85-8501

    Elastase Metabolic Disease
    BAY-85-8501 is a selective, reversible and potent inhibitor of Human Neutrophil Elastase (HNE), with an IC50 of 65 pM.
  • HY-18682
    Centrinone

    LCR-263

    Polo-like Kinase (PLK) Cancer
    Centrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 (PLK4) with a Ki of 0.16 nM.
  • HY-B0590A
    Tetrabenazine Racemate

    Ro 1-9569 Racemate

    Monoamine Transporter Neurological Disease
    Tetrabenazine Racemate (Ro 1-9569 Racemate) is a selective and reversible inhibitor of vesicular monoamine transporter-2 (VMAT-2).
  • HY-B0207AS1
    Pyridostigmine-d3 bromide

    Cholinesterase (ChE) Neurological Disease
    Pyridostigmine-d3 bromide is the deuterium labeled Pyridostigmine bromide. Pyridostigmine bromide is a parasympathomimetic and a reversible cholinesterase inhibitor.
  • HY-50877
    GSK461364

    GSK461364A

    Polo-like Kinase (PLK) Cancer
    GSK461364 is a selective, reversible and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with a Ki value of 2.2 nM.
  • HY-B0555B
    Nafcillin sodium

    Antibiotic Bacterial Infection
    Nafcillin sodium, an antibiotic, is a reversible inhibitor of β-lactamase. Nafcillin sodium can be used for the research of staphylococcal infections.
  • HY-B0590S1
    (+)-Tetrabenazine D6

    Monoamine Transporter
    (+)-Tetrabenazine D6 is the deuterium labeled (+)-Tetrabenazine. (+)-Tetrabenazine is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2).
  • HY-B0555A
    Nafcillin sodium monohydrate

    Bacterial Antibiotic Infection
    Nafcillin sodium monohydrate, an antibiotic, is a reversible inhibitor of β-lactamase. Nafcillin sodium monohydrate can be used for the research of staphylococcal infections.
  • HY-13867
    Bisindolylmaleimide I

    GF109203X; Go 6850

    PKC Metabolic Disease Cancer
    Bisindolylmaleimide I (GF109203X) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor with a Ki of 14 nM.
  • HY-120868
    TP-004

    Others Metabolic Disease
    TP-004 is a potent and reversible inhibitor of methionine aminopeptidase 2 (MetAP2), with an IC50 of 6 nM.
  • HY-101770
    BTB-1

    Microtubule/Tubulin Cancer
    BTB-1 is a potent, selective and reversible mitotic motor protein Kif18A inhibitor with an IC50 of 1.69 μM.
  • HY-100679
    Pirlindole

    Monoamine Oxidase Enterovirus Infection Neurological Disease
    Pirlindole is a selective and reversible MAO-A inhibitor. Pirlindole is also an inhibitor of enterovirus-D68 and coxsackievirus B3 (CV-B3).
  • HY-10270
    Flovagatran

    TGN 255

    Thrombin Cardiovascular Disease
    Flovagatran (TGN 255) is a potent and reversible thrombin inhibitor (Ki: 9 nM). Flovagatran can be used in the research of arterial and venous thrombosis.
  • HY-13447A
    PF429242 dihydrochloride

    Fatty Acid Synthase (FASN) Virus Protease Infection Metabolic Disease
    PF429242 dihydrochloride is a reversible and competitive SREBP site 1 protease (S1P) inhibitor with an IC50 of 175 nM.
  • HY-100244
    NS1652

    Chloride Channel Neurological Disease
    NS1652 is a reversible anion conductance inhibitor, blocks chloride channel, with an IC50 of 1.6 μM in human and mouse red blood cells.
  • HY-I0020
    Galanthaminone

    (-)-Narwedine; Narwedin

    Cholinesterase (ChE) Neurological Disease
    Galanthaminone (Narwedin) is a competitive and reversible cholinesterase (AChE) inhibitor; is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments.
  • HY-112166
    Rilzabrutinib

    PRN1008

    Btk Cancer Metabolic Disease
    Rilzabrutinib (PRN1008) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.
  • 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-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-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-100679A
    Pirlindole mesylate

    Monoamine Oxidase Enterovirus Infection Endocrinology
    Pirlindole mesylate is a selective and reversible MAO-A inhibitor. Pirlindole is also an inhibitor of enterovirus-D68 and coxsackievirus B3 (CV-B3) .
  • HY-112423
    CE-245677

    Trk Receptor Cancer Cardiovascular Disease
    CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50s of 4.7 and 1 nM.
  • HY-103391
    Qc1

    Others Metabolic Disease
    Qc1 is a reversible and noncompetitive threonine dehydrogenase (TDH) inhibitor. Qc1 can be used for the research of Metabolic disease.
  • HY-146649
    LmCPB-IN-1

    Parasite Cathepsin Infection
    LmCPB-IN-1 (compound 35) is a potent and reversible covalent Leishmania mexicana cysteine protease B (LmCPB) inhibitor with a pKi of 9.7.
  • HY-118994
    ARN19874

    Phospholipase Neurological Disease
    ARN19874 is a selective, reversible uncompetitive N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) activity inhibitor with an IC50 of ~34 μM.
  • HY-138630
    AG-270

    Methionine Adenosyltransferase (MAT) Cancer
    AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC50 of 14 nM.
  • HY-132808
    Atuzabrutinib

    SAR 444727; PRN473

    Btk Inflammation/Immunology
    Atuzabrutinib (SAR 444727) is a potent, selective reversible inhibitor of Btk (Bruton's tyrosine kinase) inhibitor. Atuzabrutinib inhibits neutrophil recruitment via inhibition of macrophage antigen-1 signalling.
  • HY-100919
    Ambenonium chloride

    WIN 8077 chloride

    Cholinesterase (ChE) Others
    Ambenonium (WIN 8077) chloride is an orally active and reversible inhibitor of Acetyicholinesterase (AChE) with high affinity. Ambenonium chloride inhibits human AChE with an IC50 value of 0.7 nM (hAChE).
  • HY-13020
    GSK1838705A

    Anaplastic lymphoma kinase (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-23460A
    p-Ethynylphenylalanine hydrochloride

    4-Ethynyl-L-phenylalanine hydrochloride

    Tryptophan Hydroxylase Neurological Disease
    p-Ethynylphenylalanine hydrochloride (4-Ethynyl-L-phenylalanine hydrochloride) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a Ki of 32.6 μM.
  • HY-23460
    p-Ethynylphenylalanine

    4-Ethynyl-L-phenylalanine

    Tryptophan Hydroxylase Neurological Disease
    p-Ethynylphenylalanine (4-Ethynyl-L-phenylalanine) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a Ki of 32.6 μM.
  • HY-114503
    NSAH

    DNA/RNA Synthesis Cancer
    NSAH is a reversible and competitive nonnucleoside ribonucleotide reductase (RR) inhibitor, with cell-free IC50 of 32 μM and cell-based IC50 of ~250 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-150717
    RSK2-IN-3

    Ribosomal S6 Kinase (RSK) Cancer
    RSK2-IN-3 (Compound 26) is a reversible covalent inhibitor of the RPS6KA3 (RSK2) kinase.
  • HY-50887
    L-873724

    Cathepsin Metabolic Disease
    L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsin K inhibitor, with IC50s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively. L-873724 also exhibits an IC50 of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption.
  • HY-119721
    CP-424174

    NOD-like Receptor (NLR) Inflammation/Immunology
    CP-424174 is a reversible inhibitor against IL-1β processing with an IC50 of 210 nM.CP-424174 indirectly inhibits NLRP3.
  • HY-B0882S
    Edrophonium-d5 chloride

    Cholinesterase (ChE) Neurological Disease
    Edrophonium-d5 chloride is the deuterium labeled Edrophonium chloride. Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
  • 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-12631
    BMS-654457

    Factor Xa Cardiovascular Disease
    BMS-654457 is a small-molecule, reversible inhibitor of factor XIa (FXIa), binding with human and rabbit FXIa with Kis of 0.2 and 0.42 nM, respectively.
  • HY-10273
    Atecegatran metoxil

    AZD0837; Atecegatran fexenetil

    Thrombin Cardiovascular Disease
    Atecegatran metoxil is a oral anticoagulant, which inhibits thrombin factor II and is used in thromboembolic disorders. In vivo, Atecegatran metoxil is converted to AR-H067637, a selective and reversible direct thrombin inhibitor.
  • HY-129111
    EACC

    Autophagy Infection Neurological Disease
    EACC is a reversible autophagy inhibitor, which can block autophagic flux. EACC selectively inhibits the translocation of autophagosome-specific SNARE Stx17 thereby blocking autophagosome-lysosome fusion.
  • HY-146958
    MAO-B-IN-8

    Monoamine Oxidase Neurological Disease
    MAO-B-IN-8 is a potent reversible MAO-B inhibitor and an inhibitor of microglial production of neuroinflammatory mediator. MAO-B-IN-8 can be used for neurodegenerative disease research.
  • 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-121851
    Revaprazan

    SB 641257

    Proton Pump Inflammation/Immunology
    Revaprazan (SB 641257) is a reversible proton pump inhibitor with significant anti-inflammatory effects. Revaprazan can be used for chronic gastric inflammation research.
  • HY-112553
    HZ52

    Lipoxygenase Inflammation/Immunology
    HZ52 is a potent, reversible 5-lipoxygenase inhibitor, blocking leukotriene synthesis with an IC50 of 0.7 μM in intact human polymorphonuclear leukocytes.
  • HY-N9919
    Glyasperin C

    Others Others
    Glyasperin C is a potent and reversible noncompetitive inhibitor of neuraminidase with an IC50 of 20% at 200 μM. Glyasperin C is a polyphenol isolated from the roots of Glycyrrhiza uralensis.
  • 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-100526
    XMU-MP-1

    Hippo (MST) Cancer
    XMU-MP-1 is a reversible and selective MST1/2 inhibitor with IC50s of 71.1 and 38.1 nM, respectively.
  • HY-14574
    PF-03814735

    Aurora Kinase VEGFR Cancer
    PF-03814735 is a potent, orally available, ATP-competitive and reversible aurora A and aurora B inhibitor with IC50s of 0.8 and 0.5 nM, respectively.
  • HY-137573
    Trotabresib

    CC-90010

    Epigenetic Reader Domain Cancer
    CC-90010 (compound 1) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors.
  • HY-B0555
    Nafcillin

    Antibiotic Bacterial Infection
    Nafcillin, an antibiotic, is a reversible inhibitor of β-lactamase. Nafcillin exhibits bactericidal activity, and can be used for the research of staphylococcal infections.
  • HY-16709
    USP7-IN-1

    Deubiquitinase Cancer
    USP7-IN-1 is a selective and reversible inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 77 μM, and can be used for the research of cancer.
  • HY-N8533
    Sodium Camptothecin

    DNA/RNA Synthesis Cancer Infection
    Sodium Camptothecin is a plant alkaloid, with antitumor activity. Sodium Camptothecin is a reversible inhibitor of RNA synthesis. Sodium Camptothecin is an effective inhibitor of adenovirus replication. Sodium Camptothecin inhibits DNA synthesis and causes breaks in intracellular preformed viral DNA.
  • 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-135008
    J14

    Reactive Oxygen Species Cancer
    J14 is a reversible sulfiredoxin inhibitor with an IC50 of 8.1 μM. J14 induces oxidative stress (intracellular ROS accumulation) by inhibiting sulfiredoxin, leading to cytotoxicity and cancer cell death.
  • HY-100816
    Rbin-1

    Ribozinoindole-1

    Phosphatase Metabolic Disease
    Rbin-1 is a potent, reversible, and specific chemical inhibitor of eukaryotic ribosome biogenesis. Rbin-1 inhibits the ATPase with GI50 of 136 nM. Rbin-1 is a potent and selective chemical inhibitor of Midasin (Mdn1).
  • HY-116437
    Selatinib

    EGFR Cancer
    Selatinib is a reversible and orally active dual EGFR and ErbB2 inhibitor with IC50s of 13 nM and 22.5 nM, respectively. Selatinib has anticancer effects.
  • HY-139603
    MYF-01-37

    YAP Cancer
    MYF-01-37 is a covalent TEAD inhibitor targeting Cys380. MYF-01-37 has a reversible inhibition on YAP/TEAD interaction.
  • HY-114086
    ML359

    Others Cardiovascular Disease
    ML359 is a potent, selctive and reversible inhibitor of protein disulfide isomerase (PDI), with an IC50 of 250 nM. ML359 can prevent thrombus formation in vivo.
  • 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-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-13050
    Sapitinib

    AZD-8931

    EGFR Cancer
    Sapitinib (AZD-8931) is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.
  • 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-123863
    SSR411298

    FAAH Neurological Disease
    SSR411298 is an orally active, selective and reversible fatty acid amide hydrolase (FAAH) inhibitor. SSR411298 has the potential for post-traumatic stress disorder research.
  • HY-N0826
    Corynoline

    Cholinesterase (ChE) Keap1-Nrf2 Inflammation/Immunology Neurological Disease Cancer
    Corynoline is a reversible and noncompetitive acetylcholinesterase (AChE) inhibitor with an IC50 of 30.6 μM. Corynoline exhibits anti-inflammatory activity by activating Nrf2.
  • HY-118533A
    Ambenonium dichloride tetrahydrate

    WIN 8077 dichloride tetrahydrate

    Cholinesterase (ChE) Neurological Disease
    Ambenonium (WIN 8077) dichloride tetrahydrate is an orally active and reversible inhibitor of Acetyicholinesterase (AChE) with high affinity. Ambenonium dichloride tetrahydrate inhibits human AChE with an IC50 value of 0.7 nM (hAChE).
  • HY-103261
    SCH28080

    Proton Pump Endocrinology
    SCH28080 is a reversible, K +-competitive inhibitor of the gastric H,K-ATPase, with a Ki of 0.12 μM. SCH28080 is an effective inhibitor of acid secretion in vivo and with anti-gastric ulcer activity.
  • HY-N0457A
    L-Chicoric Acid

    (-)-Chicoric acid; trans-Caffeoyltartaric acid

    HIV Integrase HIV Endogenous Metabolite Infection Cancer
    L-Chicoric Acid ((-)-Chicoric acid) is a dicaffeoyltartaric acid and a potent, selective and reversible HIV-1 integrase inhibitor with an IC50 of ~100 nM. L-Chicoric Acid inhibits HIV-1 replication in tissue culture.
  • HY-144813
    Gü2602

    Cathepsin Cancer Inflammation/Immunology
    Gü2602 is a potent, reversible cathepsin K (CatK) inhibitor with a Ki of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsin K zymogen.
  • HY-137463
    AG-636

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Cancer
    AG-636 is a potent, reversible, selective and orally active dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 17 nM. AG-636 has strong anticancer effects.
  • HY-B1318
    Foscarnet sodium

    Trisodium phosphonoformate; Phosphonoformic acid trisodium salt

    DNA/RNA Synthesis Infection
    Foscarnet sodium (Trisodium phosphonoformate) is a viral DNA polymerase activity inhibitor, leading to reversible suppression of viral replication. Foscarnet sodium is an antiherpesvirus agent used in cytomegalovirus retinitis.
  • HY-10458
    PF-562271 besylate

    VS-6062 besylate

    FAK Pyk2 Cancer
    PF-562271 (VS-6062) 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-B0199A
    Mycophenolate mofetil hydrochloride

    RS 61443 hydrochloride; TM-MMF hydrochloride

    Endogenous Metabolite Bacterial Cancer
    Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.
  • HY-B0555BS
    Nafcillin-d5 sodium

    Antibiotic Infection
    Nafcillin-d5 sodium is the deuterium labeled Nafcillin sodium. Nafcillin sodium, an antibiotic, is a reversible inhibitor of β-lactamase. Nafcillin sodium can be used for the research of staphylococcal infections.
  • HY-18763
    Indobufen

    Ibustrin

    COX Cardiovascular Disease
    Indobufen is a platelet aggregation inhibitor. Indobufen is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes.
  • HY-P1081
    Acetyl-Calpastatin(184-210)(human)

    Proteasome Inflammation/Immunology
    Acetyl-Calpastatin(184-210)(human) is a potent, selective and reversible calpain inhibitor with Ki values of 0.2 nM and 6 μM for µ-calpain and cathepsin L, respectively.
  • HY-17388
    (±)-Huperzine A

    Cholinesterase (ChE) Neurological Disease
    (±)-Huperzine A, an active Lycopodium alkaloid extracted from traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD).
  • HY-20403
    PF-562271 hydrochloride

    VS-6062(hydrochloride)

    FAK Pyk2 Cancer
    PF-562271 (VS-6062) hydrochloride is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively.
  • HY-10459
    PF-562271

    VS-6062

    FAK Pyk2 Cancer
    PF-562271 (VS-6062) is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively.
  • HY-125856
    Milvexian

    BMS-986177; JNJ-70033093

    Factor Xa Cardiovascular Disease
    Milvexian (BMS-986177), an effective antithrombotic agent, is an orally-bioavailable, reversible and direct inhibitor of human and rabbit factor XIa (FXIa) with Ki of 0.11, and 0.38 nM, respectively.
  • 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-100736
    ML348

    GNF-Pf-1127

    Phospholipase Cancer
    ML348 (GNF-Pf-1127) is a selective and reversible acyl-protein thioesterase 1 (APT1)/lysophospholipase 1 (LYPLA1) inhibitor with an IC50 of 210 nM, and barely inhibits LYPLA2.
  • HY-104032
    Ac-CoA Synthase Inhibitor1

    RSV Infection Metabolic Disease
    Ac-CoA Synthase Inhibitor1 is a potent, reversible acetate-dependent acetyl-CoA synthetase 2 (ACSS2) inhibitor with an IC50 of 0.6 µM. Ac-CoA Synthase Inhibitor1 inhibits the respiratory syncytial virus (RSV).
  • HY-A0166A
    Cilastatin sodium

    MK0791 sodium

    Bacterial Antibiotic Infection
    Cilastatin sodium (MK0791 sodium) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin sodium inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin sodium is an antibacterial adjunct.
  • HY-133016A
    (R)-M8891

    Others Others
    (R)-M8891 (compound R-9) is a less active isomer of M8891. M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor.
  • HY-A0166
    Cilastatin

    MK0791

    Bacterial Antibiotic Infection
    Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct.
  • HY-133511
    MLS000544460

    Phosphatase Cancer
    MLS000544460 is a highly selective and reversible Eya2 phosphatase inhibitor with a Kd of 2.0 μM and an IC50 of 4 μM. MLS000544460 inhibit Eya2 phosphatase mediated cell migration and has anti-cancer activity.
  • HY-16373
    CP-609754

    LNK-754; OSI-754

    Farnesyl Transferase Cancer
    CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity.The IC50 for inhibiting farnesylation of recombinant human H-Ras is 0.57 ng/mL and recombinant K-Ras is 46 ng/mL.
  • HY-14838
    Etamicastat

    BIA 5-453

    Dopamine β-hydroxylase Cardiovascular Disease
    Etamicastat (BIA 5-453) 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-13917A
    PND-1186 hydrochloride

    VS-4718 hydrochloride; SR-2516 hydrochloride

    FAK Apoptosis Cancer
    PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis.
  • HY-144812
    Gü1303

    Cathepsin Cancer Inflammation/Immunology
    Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a Ki of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen.
  • HY-W018781
    Benzamidine hydrochloride

    Ser/Thr Protease Cancer
    Benzamidine hydrochloride is an reversible competitive inhibitor of trypsin-like serine proteases, with Kis of 97 µM, 21 µM, 20 µM and 110 µM for uPA, trypsin, tryptase and factor Xa, respectively.
  • HY-P1081A
    Acetyl-Calpastatin(184-210)(human) TFA

    Proteasome Inflammation/Immunology
    Acetyl-Calpastatin(184-210)(human) TFA is a potent, selective and reversible calpain inhibitor with Ki values of 0.2 nM and 6 μM for µ-calpain and cathepsin L, respectively.
  • 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-10530
    Varlitinib

    ASLAN001; ARRY-334543

    EGFR Cancer
    Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC50s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively.
  • HY-12293
    LY2857785

    CDK Apoptosis Cancer
    LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9 (IC50 11 nM) and other transcription kinases CDK8 (IC50 16 nM), and CDK7 (IC50 246 nM).
  • HY-139032
    CM121

    Aldehyde Dehydrogenase (ALDH) Others
    CM121 is an active site-directed reversible ALDH1A2 inhibitor (IC50=0.54 μM;Kd=1.1 μM) with a variety of hydrophobic interactions.
  • HY-13917
    PND-1186

    VS-4718; SR-2516

    FAK Apoptosis Cancer
    PND-1186 (VS-4718) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis.
  • HY-119307
    Apratastat

    TMI-005

    MMP TNF Receptor Cancer
    Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α. Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC).
  • HY-18336
    GlyH-101

    CFTR Cardiovascular Disease
    GlyH-101 is a potent CFTR inhibitor. GlyH-101 also is a potent and reversible inhibitor of the VSORC conductance. GlyH-101 shows antiproliferative activity. GlyH-101 inhibits CFTR-like current and VSORC current.
  • HY-109079A
    Abeprazan hydrochloride

    DWP14012 hydrochloride; Fexuprazan hydrochloride

    Proton Pump Metabolic Disease
    Abeprazan hydrochloride (DWP14012 hydrochloride) is a potassium-competitive acid blocker. Abeprazan hydrochloride inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan hydrochloride is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases.
  • HY-109079
    Abeprazan

    DWP14012; Fexuprazan

    Proton Pump Metabolic Disease
    Abeprazan (DWP14012) is a potassium-competitive acid blocker. Abeprazan inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases.
  • HY-122632
    Ciliobrevin D

    Hedgehog Cancer
    Ciliobrevin D is a cell-permeable, reversible and specific inhibitor of AAA+ ATPase motor cytoplasmic dynein. Ciliobrevin D inhibits Hedgehog (Hh) signaling and primary cilia formation. Ciliobrevin D inhibits dynein-dependent microtubule gliding and ATPase activity in vitro.
  • HY-N3474
    Isolicoflavonol

    Others Others
    Isolicoflavonol potently inhibits hCES2A(Human carboxylesterase 2)-mediated fluorescein diacetate hydrolysis in a reversible and mixed inhibition manner, with Ki values less than 1.0 μM.
  • HY-146305
    α-Glucosidase-IN-4

    Glucosidase Cancer Infection Endocrinology Metabolic Disease Inflammation/Immunology Neurological Disease Cardiovascular Disease Others
    α-Glucosidase-IN-4 is a reversible and mixed type α-glucosidase inhibitor with an IC50 of 12.98 μM, a KI of 27.02 μM, and a KIS of 13.65 μM, respectively.
  • HY-100655
    O-Desmethyl apixaban

    Drug Metabolite Cardiovascular Disease
    O-Desmethyl apixaban is a metabolite of Apixaban (BMS-562247-01). Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.
  • HY-145339
    ARN19702

    Others Inflammation/Immunology Neurological Disease
    ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 230 nM for human NAAA. ARN19702 has pain relief effects.
  • HY-120337
    V-11-0711

    Others Cancer
    V-11-0711 is a potent and selective choline kinase alpha (ChoKα) inhibitor with an IC50 of 20 nM. V-11-0711 causes a reversible growth arrest in HeLa cells.
  • HY-146318
    MIF-IN-5

    Others Cancer Metabolic Disease Inflammation/Immunology
    MIF-IN-5 (compound 1d) is a potent and reversible macrophage migration inhibitory factor (MIF) competitive inhibitor with an IC50 of 4.8 μM and a Ki value of 3.3 μM, respectively.
  • HY-121422
    JZP-361

    MAGL Histamine Receptor Inflammation/Immunology
    JZP-361 is a potent, reversible and selective inhibitor of human recombinant MAGL (hMAGL) with an IC50 of 46 nM. JZP-361 also shows antihistaminergic activities and can be used for asthma research.
  • HY-12853
    Mesotrione

    Reactive Oxygen Species Others
    Mesotrione is a herbicide belongs to the benzoylcyclohexanedione family. Mesotrione is a potent and competitive and reversible inhibitor of HPPD enzyme. Mesotrione is selective to maize due to rapid metabolism and relative high tolerance by the susceptible crop plant.
  • HY-16446
    SAR125844

    c-Met/HGFR Apoptosis Cancer
    SAR125844 is a potent, highly selective, reversible and ATP-competitive MET receptor tyrosine kinase (RTK) inhibitor, with an IC50 of 4.2 nM. Shows inhibition of MET autophosphorylation in cell-based assays.
  • HY-101945
    A-69412

    Lipoxygenase Inflammation/Immunology
    A-69412 is a reversible, specific inhibitor of the 5-lipoxygenase (5-LO). A-69412 has the potential to treat asthma and ulcerative colitis, and possibly other inflammatory and allergic conditions.
  • HY-144323
    YF135

    PROTACs PERK Cancer
    YF135 is an efficient and reversible-covalent KRAS G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway.
  • HY-13520
    Nocodazole

    Oncodazole; R17934

    Microtubule/Tubulin Bcr-Abl CRISPR/Cas9 Autophagy Apoptosis Cancer
    Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, and activates CRISPR/Cas9.
  • HY-110067
    VO-OHPic

    PTEN Apoptosis Autophagy Cancer Metabolic Disease Inflammation/Immunology Cardiovascular Disease
    VO-OHPic is a reversible, noncompetitive and selective PTEN inhibitor with an IC50 of 46 nM. VO-OHPic attenuates apoptosis, adverse cardiac remodeling, and pro-inflammatory M1 macrophages in doxorubicin-induced cardiomyopathy. VO-OHPic inhibits autophagy.
  • 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-17543
    ML-323

    Deubiquitinase Cancer
    ML-323 is a reversible, potent USP1-UAF1 inhibitor with IC50 of 76 nM in a Ub-Rho assay. The measured inhibition constants of ML-323 for the free enzyme (Ki) is 68 nM.
  • HY-18690
    Enasidenib

    AG-221

    Isocitrate Dehydrogenase (IDH) Cancer
    Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2 R140Q and IDH2 R172K, respectively.
  • HY-W016645
    4-Diethylaminobenzaldehyde

    Aldehyde Dehydrogenase (ALDH) Cancer
    4-Diethylaminobenzaldehyde is a reversible aldehyde dehydrogenases (ALDHs) inhibitor, with a Ki of 4 nM for ALDH1. 4-Diethylaminobenzaldehyde displays potent anti-androgenic effect (IC50= 1.71μM).
  • HY-101456
    PCPA methyl ester hydrochloride

    4-Chloro-DL-phenylalanine methyl ester hydrochloride

    Tryptophan Hydroxylase 5-HT Receptor Neurological Disease
    PCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride), a reversible tryptophan hydroxylase inhibitor, is a serotonin (5-HT) synthesis inhibitor. PCPA methyl ester hydrochloride crosses the blood brain barrier and reduces 5-HT central availability.
  • HY-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-14879B
    Avibactam sodium hydrate

    NXL-104 hydrate

    Bacterial Antibiotic Infection
    Avibactam sodium (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-150643
    RSK2-IN-2

    Ribosomal S6 Kinase (RSK) Cancer
    RSK2-IN-2 (Compound 25) is a reversible covalent inhibitor of the RPS6KA3 (RSK2) kinase. RSK2-IN-2 is also described to inhibit MSK1, MSK2 and RSK3.
  • HY-144689
    BChE-IN-3

    Cholinesterase (ChE) Neurological Disease
    BChE-IN-3 (compound 45a) is a potent, selective, time-dependent and pseudoirreversible BChE inhibitor, with an IC50 of 56.9 nM. BChE-IN-3 also shows marginal and reversible (not time-dependent) inhibition of AChE.
  • HY-W013256
    Foscarnet trisodium hexahydrate

    Trisodium phosphonoformate hexahydrate; Phosphonoformic acid trisodium salt hexahydrate

    DNA/RNA Synthesis Infection
    Foscarnet trisodium hexahydrate (Trisodium phosphonatoformate hexahydrate) is a viral DNA polymerase activity inhibitor, leading to reversible suppression of viral replication. Foscarnet trisodium hexahydrate is an antiherpesvirus agent used in cytomegalovirus retinitis.
  • HY-B0534
    Moclobemide

    Ro111163

    Monoamine Oxidase Neurological Disease
    Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A.Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
  • HY-118795
    SC-22716

    Aminopeptidase Inflammation/Immunology
    SC-22716 is a potent, competitive, reversible inhibitor of human LTA4 hydrolase, with an IC50 of 0.20 µM. SC-22716 has potential for the research of inflammatory bowel disease (IBD) and psoriasis.
  • HY-12041
    SP600125

    JNK Autophagy Apoptosis Ferroptosis Cancer
    SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 inhibits autophagy and activates apoptosis.
  • HY-124366
    Slingshot inhibitor D3

    Others Cancer Infection
    Slingshot inhibitor D3 is a potent, selective, reversible and competitive inhibitor of Slingshot. The IC50 value for Slingshot 1 is 3 μM and the Ki value for Slingshot 2 is 3.9 μM. Slingshot inhibitor D3 has similar inhibitory activities toward both Slingshot 1 and Slingshot 2.
  • HY-14179
    PPQ-102

    CFTR Inhibitor

    CFTR Others
    PPQ-102 (CFTR Inhibitor) is a reversible CFTR inhibitor that completely inhibits CFTR chloride currents (IC50 ~90 nM). PPQ-102 is not affected by membrane potential-dependent cell allocation or blocking efficiency (uncharged at physiological pH) and effectively prevents cyst enlargement in polycystic kidney disease.
  • HY-14879C
    Avibactam sodium dihydrate

    NXL-104 dihydrate

    Bacterial Antibiotic Infection
    Avibactam sodium (NXL-104) dihydrate 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-100817
    Rbin-2

    Phosphatase Others
    Rbin-2 is a potent, reversible and selective inhibitor of Midasin (Mdn1), an enzyme belonging to the AAA+ (ATPases associated with diverse cellular activities) protein family. Rbin-2 inhibits eukaryotic ribosome biogenesis and is a powerful probe for the eukaryotic ribosome assembly.
  • HY-14879
    Avibactam free acid

    NXL-104 free acid

    Bacterial Antibiotic Infection
    Avibactam (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-18780
    RR6

    Others Cancer
    RR6 is a potent, selective, reversible, competitive and orally active vanin inhibitor with an IC50 of 540 nM for recombinant vanin-1. RR6 also potently inhibits human, bovine and rat serum pantetheinase with IC50 values of 40 nM, 41 nM and 87 nM, respectively.
  • HY-19651
    Zanapezil free base

    TAK-147 free base

    Cholinesterase (ChE) Neurological Disease
    Zanapezil (TAK-147) free base is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil free base shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil free base shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil free base can be used for the research of early stages of Alzheimer's disease (AD).
  • HY-10227
    Bortezomib

    PS-341; LDP-341; NSC 681239

    Proteasome NF-κB Apoptosis Autophagy Cancer
    Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity.
  • HY-W013571
    4-Isopropylbenzoic acid

    Fungal Infection
    4-Isopropylbenzoic acid, an aromatic monoterpenoid, is isolated from the stem bark of Bridelia retusa. 4-Isopropylbenzoic acid exhibits antifungal activities. 4-Isopropylbenzoic acid is also a reversible and uncompetitive inhibitor of mushroom tyrosinase.
  • HY-B0590
    Tetrabenazine

    Ro 1-9569

    Monoamine Transporter Neurological Disease
    Tetrabenazine (Ro 1-9569) is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease.
  • HY-115062
    MJ33 lithium salt

    Phospholipase Metabolic Disease
    MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6.
  • HY-B0590E
    Tetrabenazine mesylate

    Ro 1-9569 mesylate

    Monoamine Transporter Neurological Disease
    Tetrabenazine (Ro 1-9569) mesylate is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine mesylate can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease.
  • HY-10716A
    PF-03463275

    GlyT Neurological Disease
    PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research.
  • HY-102034
    Complement factor D-IN-1

    Complement System Inflammation/Immunology
    Complement factor D-IN-1 is a potent and selective small-molecule reversible factor d inhibitor, with IC50s of 0.006 and 0.05 μM in FD Thioesterolytic Fluorescent Assay and a MAC Deposition Assay, respectively.
  • HY-151875
    MurA-IN-3

    Bacterial Infection Inflammation/Immunology
    MurA-IN-3 is a reversible pyrrolidinedione-based MurA inhibitor. MurA-IN-3 has inhibitory activity for MurA with an IC50 value of 4.5 μM. MurA-IN-3 also has antibacterial activity.
  • 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-16420
    R112

    Syk Inflammation/Immunology
    R112 is a fast and reversible inhibitor of spleen tyrosine kinase (Syk) kinase. R112 inhibits Syk kinase activity with an IC50 value of 226 nM and a Ki value of 96 nM. R112 inhibits IgE-FcεRI signaling pathway. R112 can be used for the research of allergic rhinitis.
  • HY-108341
    PF-06424439

    Acyltransferase Metabolic Disease
    PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.
  • HY-120394
    TVB-3166

    Fatty Acid Synthase (FASN) Apoptosis Cancer
    TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC50s of 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth.
  • HY-18763S
    Indobufen-d5

    Ibustrin-d5

    COX Cardiovascular Disease
    Indobufen-d5 is deuterium labeled Indobufen. Indobufen is a platelet aggregation inhibitor. Indobufen is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes.
  • HY-16946
    CP-610431

    Acetyl-CoA Carboxylase Metabolic Disease
    CP-610431 is a reversible, ATP-uncompetitive, isozyme-nonselective acetyl-CoA carboxylase (ACC) inhibitor. CP-610431 inhibits ACC1 and ACC2 with IC50s of ~50 nM. CP-610431 can be used for the research of metabolic syndrome.
  • HY-141513
    NH-3

    Thyroid Hormone Receptor Neurological Disease
    NH-3 is an orally active, reversible thyroid hormone receptor (THR) antagonist with an IC50 of 55 nM. NH-3, a derivative of the selective thyromi-metic GC-1, inhibits binding of thyroid hormones to their receptor and that inhibits cofactor recruitment.
  • HY-106405
    Nebicapone

    BIA 3-202

    COMT Metabolic Disease
    Nebicapone (BIA 3-202), a reversible catechol-O-methyltransferase (COMT) inhibitor, is mainly metabolized by glucuronidation. Nebicapone is mainly peripherally acting inhibitor that decreases the biotransformation of L-DOPA to 3-O-methyl-DOPA by inhibition of COMT, and it is potential for the treatment of Parkinson's disease.
  • HY-117421A
    CM-579 trihydrochloride

    Histone Methyltransferase DNA Methyltransferase Cancer
    CM-579 trihydrochloride is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells.
  • HY-117421
    CM-579

    Histone Methyltransferase DNA Methyltransferase Cancer
    CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells.
  • HY-100642
    3-O-Methyltolcapone

    Ro 40-7591

    COMT Neurological Disease
    3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease.
  • HY-N4143
    Cyanidin 3-arabinoside

    Phosphatase Metabolic Disease
    Cyanidin 3-arabinoside is a selective and reversible protein tyrosine phosphatase 1B (PTP1B) inhibitor, with an IC50 of 8.91 μM. Cyanidin 3-arabinoside is potential for the research of type 2 diabetes.
  • 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-13945
    NVP 231

    Apoptosis Cancer
    NVP 231 is a potent, specific, and reversible ceramide kinase (CerK) inhibitor(IC50=12 nM) that competitively inhibits binding of ceramide to CerK. NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage.
  • HY-127105A
    Iptacopan hydrochloride

    LNP023 hydrochloride

    Complement System Metabolic Disease Inflammation/Immunology
    LNP023 hydrochloride is an orally bioavailable, highly potent and highly selective factor B inhibitor. LNP023 shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. LNP023 inhibits factor B with an IC50 value of 10 nM.
  • HY-126075A
    WS-383

    E1/E2/E3 Enzyme Cancer
    WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
  • HY-108552
    MG-115

    Proteasome Apoptosis Cancer
    MG-115 is a potent and reversible proteasome inhibitor, with Kis of 21 nM and 35 nM for 20S and 26S proteasome, respectively. MG-115 specifically inhibit the chymotrypsin-like activity of the proteasome, induces p53-dependent apoptosis.
  • HY-16693
    LDN-27219

    Others Others
    LDN-27219 is a reversible, slow-binding inhibitor of TGase. LDN-27219 inhibits human TGase with an IC50 value of 0.6 μM. LDN-27219 effectively decreases blood pressure and induces vasodilation, it can be used for the research of cardiovascular disease.
  • HY-108341A
    PF-06424439 methanesulfonate

    Acyltransferase Metabolic Disease
    PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.
  • HY-10715
    SSR504734

    GlyT Neurological Disease
    SSR504734 is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 (IC50=18, 15, and 38 nM, respectively). SSR504734 shows anti-schizophrenia, anti-anxiety and anti-depression activities.
  • HY-103462
    TC-F2

    FAAH Cancer Inflammation/Immunology Metabolic Disease
    TC-F2 is a reversible non-covalent binding inhibitor of fatty acid amide hydrolase (FAAH) with an IC50 of 28 nM. FAAH is involved in many human diseases, particularly cancer, pain and inflammation as well as neurological, metabolic and cardiovascular disorders.
  • HY-B0034
    Donepezil Hydrochloride

    E2020

    Cholinesterase (ChE) Neurological Disease
    Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity.
  • HY-N1581
    Quassin

    Nigakilactone D

    Parasite Infection Endocrinology
    Quassin (Nigakilactone D) is a bioactive triterpenoid from stem bark extract of Quassia amara. Quassin inhibits P. falciparum with an IC50 of 0.15 μM. Quassin possesses reversible antifertility, anti-estrogenic and anti-plasmodial activity.
  • HY-50667
    Apixaban

    BMS-562247-01

    Factor Xa Cardiovascular Disease
    Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively. Apixaban is in development for the prevention and treatment of various thromboembolic diseases.
  • HY-139031
    ALDH1A2-IN-1

    Aldehyde Dehydrogenase (ALDH) Endocrinology
    ALDH1A2-IN-1 is an active site-directed reversible ALDH1A2 inhibitor (IC50=0.91 μM; Kd=0.26 μM) with several hydrophobic interactions.
  • HY-15497
    AZD7687

    Acyltransferase Metabolic Disease
    AZD7687 is a potent, selective, reversible and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor with an IC50 of 80 nM for human DGAT1. AZD7687 can be used for type 2 diabetes mellitus and obesity research.
  • HY-70074
    CCG-63802

    RGS Protein Cancer Inflammation/Immunology
    CCG-63802 is a selective, reversible and allosteric RGS4 inhibitor. CCG-63802 specifically binds to RGS4 and blocks the RGS4-Gαo interaction, with an IC50 value of 1.9 μM.
  • HY-11002
    CP-466722

    ATM/ATR Cancer
    CP-466722 is a rapidly reversible inhibitor of ATM, with an IC50 of 4.1 μM, and has no effects on PI3K or closely related PI3K-like protein kinase (PIKK) family members.
  • HY-P0322
    GRGDSPK

    EMD 56574

    Integrin Metabolic Disease Cardiovascular Disease
    GRGDSPK (EMD 56574) is a peptide incluing Arg-Gly-Asp (RGD). GRGDSPK (EMD 56574) is an competitive and reversible inhibitory peptide for inhibiting integrin-fibronectin binding. GRGDSPK is used to study the role of integrins in bone formation and resorption.
  • HY-118628
    N-(p-amylcinnamoyl) Anthranilic Acid

    ACA

    Phospholipase TRP Channel Cardiovascular Disease
    N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker. N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia.
  • HY-P1346
    APETx2

    Sodium Channel Inflammation/Immunology Neurological Disease
    APETx2, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain.
  • HY-P1346A
    APETx2 TFA

    Sodium Channel Inflammation/Immunology Neurological Disease
    APETx2 TFA, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain.
  • HY-10253
    AG1024

    Tyrphostin AG 1024

    IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selective IGF-1R inhibitor with an IC50 of 7 μM. AG1024 inhibits phosphorylation of IR (IC50=57 μM). AG1024 induces apoptosis and has anti-cancer activity.
  • HY-N6722
    Swainsonine

    Tridolgosir

    Apoptosis Antibiotic Cancer Infection
    Swainsonine (Tridolgosir) is an natural indolizidine alkaloid, a potent and reversible α-mannosidase inhibitor. Swainsonine induces apoptosis and cell cycle arrest at G2/M phase. Swainsonine shows anti-tumor activity.
  • HY-100514
    GSK484 hydrochloride

    Protein Arginine Deiminase Cancer Inflammation/Immunology Cardiovascular Disease
    GSK484 hydrochloride is a selective and reversible peptidylarginine deiminase 4 (PAD4) inhibitor. GSK484 hydrochloride demonstrates high affinity binding to PAD4 with IC50s of 50 nM in the absence of Calcium. In the presence of 2 mM Calcium, notably lower potency (250 nM) is observed.
  • HY-112215
    ARQ 531

    MK-1026

    Btk Cancer Inflammation/Immunology
    ARQ 531 (MK-1026) is a reversible non-covalent and orally active inhibitor of Bruton’s Tyrosine Kinase (BTK), with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.
  • HY-115537
    NAE-IN-M22

    Apoptosis Cancer
    NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo.
  • HY-144452
    Immunoproteasome inhibitor 1

    Proteasome Cancer
    Immunoproteasome inhibitor 1 is a potent, reversible, time-independent immunoproteasome and proteasome inhibitor (Kis of 1.18, 0.27, 1.91 μM in β5c, β1i, β5i submits, respectively). Immunoproteasome inhibitor 1 can be used for the treatment of certain neoplastic diseases.
  • 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-10163S
    Dabigatran-d4

    BIBR 953-d4; BIBR 953ZW-d4

    Thrombin Cardiovascular Disease
    Dabigatran-d4 is deuterium labeled Dabigatran. 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-146313
    BChE-IN-7

    Cholinesterase (ChE) Neurological Disease
    BChE-IN-7 (compound 13) is a potent, selective, BBB-penetrated and reversible AChE and BChE inhibitor, with an IC50 of 0.06 μM (BChE). BChE-IN-7 can protect neuronal-like cells from toxic Aβ-species.
  • HY-13030
    (+)-JQ-1

    JQ1

    Epigenetic Reader Domain Autophagy Ligands for Target Protein for PROTAC Cancer
    (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy.
  • HY-151591
    SPAA-52

    Phosphatase Metabolic Disease
    SPAA-52 is an orally active, competitive and reversible low-molecular-weight protein tyrosine phosphatase (LMW-PTP) inhibitor (IC50=4 nM, Ki=1.2 nM). SPAA-52 can be used in diabete research.
  • HY-112885A
    nor-NOHA acetate

    Nω-Hydroxy-nor-L-arginine acetate

    Arginase Apoptosis Cancer Metabolic Disease Inflammation/Immunology
    nor-NOHA acetate (Nω-Hydroxy-nor-L-arginine acetate) is a specific and reversible arginase inhibitor, induces apoptosis in ARG2-expressing cells under hypoxia but not normoxia. Anti-leukemic activity, effective in endothelial dysfunction, immunosuppression and metabolism.
  • HY-P0322A
    GRGDSPK TFA

    EMD 56574 TFA

    Integrin Metabolic Disease Cardiovascular Disease
    GRGDSPK TFA (EMD 56574 TFA) is a peptide incluing Arg-Gly-Asp (RGD). GRGDSPK TFA is an competitive and reversible inhibitory peptide for inhibiting integrin-fibronectin binding. GRGDSPK TFA is used to study the role of integrins in bone formation and resorption.
  • HY-B0590B
    (+)-Tetrabenazine

    (+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine

    Monoamine Transporter Cancer
    (+)-Tetrabenazine ((+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine) is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2), inhibits transport by VMAT2 with 10-fold greater potency than transport by VMAT1.
  • HY-15517A
    KN-92 phosphate

    Others Cancer
    KN-92 phosphate is an inactive derivative of KN-93, without CaM kinase inhibitory activity. KN-92 phosphate is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 is a cell-permeable, reversible and competitive CaMKII inhibitor.
  • HY-15517
    KN-92

    Others Cancer
    KN-92 is an inactive derivative of KN-93, without CaM kinase inhibitory activity. KN-92 is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 is a cell-permeable, reversible and competitive CaMKII inhibitor.
  • 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-125286
    AB-680

    CD73 Cancer
    AB-680 is a highly potent, reversible and selective inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity.
  • HY-10285A
    Saxagliptin hydrate

    BMS-477118 hydrate

    Dipeptidyl Peptidase Metabolic Disease
    Saxagliptin hydrate (BMS-477118 hydrate) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrate has the peotential for type 2 diabetes mellitus research.
  • HY-131342
    BIIB068

    Btk Inflammation/Immunology
    BIIB068 is a potent, selective, reversible and orally active BTK inhibitor with an IC50 of 1 nM and a Kd of 0.3 nM. BIIB068 shows more >400-fold selective for BTK than other kinases. BIIB068 has the potential for autoimmune diseases research.
  • HY-15185
    Nirogacestat

    PF-3084014; PF-03084014

    γ-secretase Apoptosis Cancer
    Nirogacestat (PF-3084014) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers.
  • HY-126125
    CHIR-98023

    GSK-3 Metabolic Disease Neurological Disease
    CHIR-98023 is a potent, selective and reversible inhibitor of GSK3, with IC50s of 10 nM and 6.7 nM for GSK3α and GSK3β, respectively. CHIR-98023 can improve insulin action and glucose metabolism.
  • HY-10285
    Saxagliptin

    BMS-477118

    Dipeptidyl Peptidase Metabolic Disease
    Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research.
  • HY-139984
    BIIB091

    Btk Inflammation/Immunology Neurological Disease
    BIIB091 is a potent, selective, orally active and reversible BTK inhibitor, with an IC50 of <0.5 nM. BIIB091 binds the BTK protein to sequester TYR-551 into an inactive conformation with excellent affinity. BIIB091 can be used for the research of multiple sclerosis.
  • HY-16448
    Saxagliptin hydrochloride

    BMS-477118 hydrochloride

    Dipeptidyl Peptidase Metabolic Disease
    Saxagliptin hydrochloride (BMS-477118 hydrochloride) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrochloride has the peotential for type 2 diabetes mellitus research.
  • HY-143245
    Monoamine Oxidase B inhibitor 2

    Monoamine Oxidase Neurological Disease
    Monoamine Oxidase B inhibitor 2 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 1.33 nM. Monoamine Oxidase B inhibitor 2 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 2 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study.
  • HY-143244
    Monoamine Oxidase B inhibitor 1

    Monoamine Oxidase Neurological Disease
    Monoamine Oxidase B inhibitor 1 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 0.02 nM. Monoamine Oxidase B inhibitor 1 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 1 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study.
  • HY-135396
    (1S,2S)-Bortezomib

    Proteasome Apoptosis Cancer
    (1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans.
  • HY-N6608
    Physostigmine

    Eserine

    Cholinesterase (ChE) Neurological Disease
    Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning.
  • HY-107367
    Epertinib

    S-22611

    EGFR Cancer
    Epertinib (S-22611) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER4 and HER2, with IC50s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib shows potent antitumor activity.
  • HY-143438
    2-PAT

    Monoamine Oxidase Neurological Disease
    2-PAT, an analogue of Rasagiline and Selegiline, a reversible MAO-A inhibitor with an IC50 of 0.721 µM. 2-PAT is an inactivator of MAO-B with an IC50 of 14.6 µM. 2-PAT has the potential for Parkinson’s disease and depression research.
  • HY-125286A
    AB-680 ammonium

    CD73 Cancer
    AB-680 ammonium is a highly potent, reversible and selective inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity.
  • HY-B0534S1
    Moclobemide-d4

    Ro111163-d4

    Monoamine Oxidase Neurological Disease
    Moclobemide-d4 is deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A.Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
  • HY-107367A
    Epertinib hydrochloride

    S-22611 hydrochloride

    EGFR Cancer
    Epertinib (S-22611) hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER4 and HER2, with IC50s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib hydrochloride shows potent antitumor activity.
  • HY-103353A
    SID 26681509 quarterhydrate

    Cathepsin Parasite Cancer Infection
    SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 quarterhydrate 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 quarterhydrate shows no inhibitory activity against cathepsin G.
  • HY-108466
    Ro 08-2750

    Apoptosis Cancer Neurological Disease
    Ro 08-2750 is a non-peptide and reversible nerve growth factor (NGF) inhibitor which binds to NGF, and with an IC50 of ~ 1 µM. Ro 08-2750 inhibits NGF binding to p75 NTR selectively over TRKA. Ro 08-2750 is a selective MSI RNA-binding activity inhibitor, with an IC50 of 2.7 μM.
  • HY-130126
    SCO-792

    Others Others
    SCO-792 is a potent, orally active and reversible enteropeptidase inhibitor with IC50s of 4.6 nM and 5.4 nM for rat enteropeptidase and human enteropeptidase. SCO-792 can slowly dissociate from enteropeptidase in vitro and inhibit protein digestion in vivo. SCO-792 can be used for researching the effects of inhibiting enteropeptidase on biological actions.
  • HY-N2554
    Osthenol

    Ostenol

    Monoamine Oxidase Neurological Disease
    Osthenol (Ostenol), a prenylated coumarin isolated from the dried roots of Angelica pubescens, is selective, reversible, and competitive human monoamine oxidase-A (hMAO-A) inhibitor (Ki=0.26 µM). Osthenol potently inhibits recombinant hMAO-A with an IC50 of 0.74 µM and shows a high selectivity index for hMAO-A versus hMAO-B.
  • HY-14248S
    Letrozole-d4

    Aromatase Autophagy Cancer
    Letrozole-d4 (CGS 20267-d4) is the deuterium labeled Letrozole. 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-15816A
    Ulixertinib hydrochloride

    BVD-523 hydrochloride; VRT752271 hydrochloride

    ERK Cancer
    Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line.
  • HY-123517
    DC07090 dihydrochloride

    Enterovirus Infection
    DC07090 dihydrochloride is a low toxicity, potent, reversible and competitive non-peptidyl human enterovirus 71 3C protease inhibitor with an IC50 and a Ki value for 21.72 μM and 23.29 μM. DC07090 dihydrochloride could also inhibit coxsackievirus A16 (CVA16) replication with an EC50 value of 27.76 μM.
  • HY-102046
    FM-381

    JAK Inflammation/Immunology
    FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
  • HY-W013636
    2-Ketoglutaric acid

    Alpha-Ketoglutaric acid

    Tyrosinase Endogenous Metabolite Others
    2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM).
  • HY-133130
    JNJ-42226314

    MAGL Neurological Disease
    JNJ-42226314 is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain.
  • HY-139664
    GSK-3685032

    DNA Methyltransferase Cancer
    GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition.
  • HY-139535
    Luxeptinib

    CG-806

    FLT3 Btk Apoptosis Cancer
    Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells.
  • HY-120062
    TVB-3664

    Fatty Acid Synthase (FASN) Cancer
    TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC50 values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression.
  • HY-100540
    Golgicide A

    GCA

    Enterovirus Cancer Infection
    Golgicide A (GCA) is a potent, highly specific, and reversible inhibitor of the cis-Golgi ADP-ribosylation factor guanine nucleotide exchange factors (ArfGEF) GBF1. Golgicide A drastically reduced replication of coxsackievirus B3 (CVB3) and other human enterovirus species.
  • HY-120019
    Ac-YVAD-CHO

    L-709049

    Interleukin Related Inflammation/Immunology
    Ac-YVAD-CHO (L-709049) is a potent, reversible, specific tetrapeptide interleukin-lβ converting enzyme (ICE) inhibitor with mouse and human Ki values of 3.0 and 0.76 nM. Ac-YVAD-CHO can suppress the production of mature IL-lβ.
  • HY-133016
    M8891

    Others Cancer Cardiovascular Disease
    M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 54 nM and a Ki of 4.33 nM. M8891 does not inhibit MetAP-1 (IC50>10 µM). M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity.
  • HY-111538
    MAGL-IN-1

    MAGL Cancer
    MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC50 of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays.
  • HY-121467
    Acotiamide

    Z-338 free base; YM443 free base

    Cholinesterase (ChE) Metabolic Disease Inflammation/Immunology
    Acotiamide is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC50 of 1.79 μM. Acotiamide can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory.
  • 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-W013636B
    Calcium 2-oxoglutarate

    Tyrosinase Endogenous Metabolite Metabolic Disease
    Calcium 2-oxoglutarate is an intermediate in the production of ATP or GTP in the Krebs cycle. Calcium 2-oxoglutarate also acts as the major carbon skeleton for nitrogen-assimilatory reactions. Calcium 2-oxoglutarate is a reversible inhibitor of tyrosinase (IC50=15 mM).
  • HY-W013636A
    2-Ketoglutaric acid Sodium

    Alpha-Ketoglutaric acid Sodium

    Tyrosinase Endogenous Metabolite Metabolic Disease
    2-Ketoglutaric acid Sodium (Alpha-Ketoglutaric acid Sodium) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid Sodium also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid Sodium is a reversible inhibitor of tyrosinase (IC50=15 mM).
  • HY-121467A
    Acotiamide hydrochloride

    Z-338; YM443

    Cholinesterase (ChE) Metabolic Disease Inflammation/Immunology Others
    Acotiamide hydrochloride is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC50 of 1.79 μM. Acotiamide hydrochloride can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide hydrochloride has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory.
  • HY-15185B
    Nirogacestat dihydrobromide

    PF-3084014 dihydrobromide; PF-03084014 dihydrobromide

    γ-secretase Apoptosis Cancer
    Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat dihydrobromide while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers.
  • HY-129944
    MJ33-OH

    Phospholipase Inflammation/Immunology
    MJ33-OH is a metabolite of MJ33. MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6.
  • HY-120139
    KMH-233

    Others Cancer
    KMH-233, a potent, reversible and selective l-type amino acid transporter 1 (LAT1) inhibitor, inhibits the uptake of LAT1 substrate, l-leucin (IC50=18 μM) as well as cell growth. KMH-233 significantly potentiates the efficacy of Bestatin and Cisplatin even at low concentrations (25 μM).
  • HY-126075
    WS-383 free base

    E1/E2/E3 Enzyme Cancer
    WS-383 free base is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 free base inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
  • HY-B0856
    Validamycin A

    Fungal Tyrosinase Antibiotic Infection
    Validamycin A, a fungicidal, is an agricultural antibiotic. Validamycin A is originally isolated from Streptomyces hygroscopicus var. limoneus. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL. Validamycin A shows potent inhibitory activity against trehalase of Rhizoctonia solani, with an IC50 of 72 μM. Validamycin A is a reversible tyrosinase inhibitor, with a Ki of 5.893 mM.
  • HY-117596
    UNC569

    TAM Receptor Cancer
    UNC569 is a potent, reversible, ATP-competitive and orally active Mer kinase inhibitor with an IC50 of 2.9 nM and a Ki of 4.3 nM. UNC569 also inhibits Axl and Tyro3 with IC50s of 37 nM and 48 nM, respectively. UNC569 can be used for acute lymphoblastic leukemia (ALL) and atypical teratoid/rhabdoid tumors research
  • HY-A0166S
    Cilastatin-15N,d3

    MK0791-15N,d3

    Bacterial Antibiotic Infection
    Cilastatin-15N,d3 is a 15N-labeled and deuterium labeled Cilastatin. Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct.
  • HY-13007A
    PF-3758309 hydrochloride

    PF-03758309 hydrochloride

    PAK Apoptosis Cancer
    PF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
  • HY-13007
    PF-3758309

    PF-03758309

    PAK Apoptosis Cancer
    PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
  • HY-13007B
    PF-3758309 dihydrochloride

    PF-03758309 dihydrochloride

    PAK Apoptosis Cancer
    PF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
  • HY-10163S1
    Dabigatran-d3

    BIBR 953-d3; BIBR 953ZW-d3

    Thrombin Cardiovascular Disease
    Dabigatran-d3 (BIBR 953-d3) is the deuterium labeled Dabigatran. 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-10163S3
    Dabigatran-13C,d3

    BIBR 953-13C,d3; BIBR 953ZW-13C,d3

    Thrombin Cardiovascular Disease
    Dabigatran-13C,d3 is the 13C- and deuterium labeled Dabigatran. 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-100859
    LSD1-IN-5

    Histone Demethylase Cancer
    LSD1-IN-5 (Compound 4e) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 121 nM. LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1.
  • HY-N1919
    Ajmalicine

    Raubasine

    Adrenergic Receptor Cholinesterase (ChE) Endocrinology Neurological Disease
    Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity.
  • HY-B0034S
    Donepezil-d5 hydrochloride

    E2020-d5

    Cholinesterase (ChE) Neurological Disease
    Donepezil-d5 (hydrochloride) is deuterium labeled Donepezil (Hydrochloride). Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity.
  • HY-120824
    Mofezolac

    COX Inflammation/Immunology
    Mofezolac, a non-steroidal anti-inflammatory drug (NSAID), is a selective, reversible and orally active COX-1 inhibitor with an IC50 of 1.44 nM. Mofezolac shows weak inhibitory activity on COX-2 (IC50 of 447 nM). Mofezolac can relieve pain and has anti-inflammatory activities.
  • HY-129944A
    MJ33-OH lithium

    Phospholipase Inflammation/Immunology
    MJ33-OH lithium is a metabolite of MJ33. MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6.
  • HY-100860
    LSD1-IN-6

    Histone Demethylase Cancer
    LSD1-IN-6 (Compound 4m) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 123 nM. LSD1-IN-6 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1.
  • HY-111163
    NSC49652

    Apoptosis Cancer
    NSC49652 is a reversible, orally active p75 neurotrophin receptor (p75 NTR, also known as NGFR, TNFRSF16, and CD271) inhibitor. NSC49652 targets the transmembrane domain of p75 NTR. NSC49652 induces apoptosis and affects the viability of melanoma cells.
  • HY-N1919A
    Ajmalicine hydrochloride

    Raubasine hydrochloride

    Adrenergic Receptor Cholinesterase (ChE) Endocrinology Neurological Disease
    Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity.
  • HY-18637
    LDN-57444

    Deubiquitinase Apoptosis Neurological Disease
    LDN-57444 is a reversible, competitive and site-directed inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1), with an IC50 of 0.88 μM and a Ki of 0.40 μM; LDN-57444 also suppresses UCH-L3 activity, with an IC50 of 25 μM.
  • HY-117825
    RU-TRAAK-2

    Potassium Channel Neurological Disease
    RU-TRAAK-2 is a completely reversible TRAAK (TWIK-related arachidonic acid-stimulated K + channel) inhibitor. RU-TRAAK-2 exerts no activity for non-K2P channels (Kv1.2, Slo1 and GIRK2).
  • HY-117822
    BRD0209

    GSK-3 Neurological Disease
    BRD0209 is a potent, selective and dual inhibitor of GSK3α/β inhibitor (GSK3α IC50 = 19 nM; GSK3β IC50 = 5 nM). BRD0209 is also a reversible ATP-competitive inhibitor with fast-off kinetics (Ki = 4.2 nM, respectively). BRD0209 is a tricyclic pyrazolotetrahydroquinolinone compound. BRD0209 has the potential for the research of mood disorder diseases.
  • HY-15237
    SL 0101-1

    SL0101

    Ribosomal S6 Kinase (RSK) Cancer
    SL 0101-1 (SL0101), a kaempferol glycoside, isolated from the tropical plant F. refracta, is a cell-permeable, selective, reversible, ATP-competitive p90 Ribosomal S6 Kinase (RSK) inhibitor, with an IC50 of 89 nM. SL 0101-1 (SL0101) is a selective RSK1/2 inhibitor, with a Ki of 1 μM.
  • HY-118567
    Bis(maltolato)oxovanadium(IV)

    BMOV

    SHP2 Phosphatase Metabolic Disease
    Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive and orally active pan-PTP (protein tyrosine phosphatases) inhibitor. Bis(maltolato)oxovanadium(IV) inhibits HCPTPA, PTP1B, HPTPβ and SHP2 with IC50s of 126 nM, 109 nM, 26 nM and 201 nM, respectively. Bis(maltolato)oxovanadium(IV) is a potent insulin sensitizer.
  • HY-130173
    Bafilomycin C1

    Bacterial Fungal Na+/K+ ATPase Apoptosis Antibiotic Cancer Infection
    Bafilomycin C1 is a macrolide antibiotic isolated from Streptomyces sp. Bafilomycin C1 is a potent, specific and reversible inhibitor of vacuolar-type H +-ATPases (V-ATPases). Bafilomycin C1 inhibits growth of gram-positive bacteria and fungi. Bafilomycin C1 induces cell apoptosis and can be used for the study of hepatocellular carcinoma (HCC).
  • HY-115747
    Namoline

    Histone Demethylase Cancer
    Namoline, a γ-pyrone, is a selective and reversible Lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 51 μM in a HRP-coupled enzymatic assay. Namoline impairs LSD1 demethylase activity and blocks cell proliferation. Namoline has the potential for androgen-dependent prostate cancer research.
  • HY-50667S
    Apixaban-13C,d3

    BMS-562247-01-13C,d3

    Factor Xa Cardiovascular Disease
    Apixaban-13C,d3 (BMS-562247-01-13C,d3) is a deuterium and 13C labeled Apixaban. Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.
  • HY-118424
    JNJ-55511118

    iGluR Neurological Disease
    JNJ-55511118 is a highly potent, reversible, and selective AMPA receptor inhibitor selective for TARP-γ8. JNJ-55511118 fully displaces the radioligand (20 nM) with the Ki of 26 nM in competition binding experiments. JNJ-55511118 is a tool molecule with potential therapeutic utility as an anticonvulsant or neuroprotectant.
  • HY-143264
    FAAH/MAGL-IN-2

    FAAH MAGL Neurological Disease
    FAAH/MAGL-IN-2 is a potent, reversible, orally active, and cross the blood-brain barrier FAAH and MAGL inhibitor with IC50s of 11 nM and 36 nM (Kis of 28 nM and 60 nM), respectively . FAAH/MAGL-IN-2 has the potential to treat neuropathic pain without causing locomotion impairment.
  • HY-B1266
    Physostigmine salicylate

    Eserine salicylate

    Cholinesterase (ChE) Neurological Disease
    Physostigmine salicylate (Eserine salicylate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine salicylate crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine salicylate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine salicylate is also an antidote for anticholinergic poisoning.
  • HY-116171
    (Rac)-Calpain Inhibitor XII

    Proteasome Neurological Disease Cardiovascular Disease
    (Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I (μ-calpain, Ki=19 nM). (Rac)-Calpain Inhibitor XII has lower affinities for calpain II (m-calpain, Ki=120 nM) and cathepsin B (Ki=750 nM). (Rac)-Calpain Inhibitor XII has the potential for studying the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury.
  • HY-10227S
    Bortezomib-d8

    PS-341-d8; LDP-341-d8; NSC 681239-d8

    Proteasome NF-κB Apoptosis Autophagy Cancer
    Bortezomib-d8 (PS-341-d8) is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity.
  • HY-100558
    Bafilomycin A1

    BafA1

    Proton Pump Autophagy Antibiotic Bacterial Apoptosis Cancer Infection
    Bafilomycin A1 (BafA1) is a specific and reversible inhibitor of vacuolar H +-ATPase (V-ATPase) with IC50 values of 4-400 nmol/mg. Bafilomycin A1, a macrolide antibiotic, is also used as an autophagy inhibitor at the late stage. Bafilomycin A1 blocks autophagosome-lysosome fusion and inhibits acidification and protein degradation in lysosomes of cultured cells. Bafilomycin A1 induces apoptosis.
  • HY-P1259
    PR-39

    Proteasome Bacterial Inflammation/Immunology
    PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
  • HY-B0986
    Hexylresorcinol

    4-Hexylresorcinol

    Parasite Bacterial Apoptosis Glucosidase Endogenous Metabolite Cancer Infection Metabolic Disease
    Hexylresorcinol (4-Hexylresorcinol) is a natural compound found in plants with antimicrobial, anthelmintic, antiseptic and antitumor activities. Hexylresorcinol can induce apoptosis in squamous carcinoma cells. Hexylresorcinol is a reversible and noncompetitive inhibitor of α-glucosidase. Hexylresorcinol has protective effects against oxidative DNA damage.
  • HY-147953
    MAO-B-IN-13

    Monoamine Oxidase Neurological Disease
    MAO-B-IN-13 (compound 12a) is a highly potent, reversible and blood-brain barrier (BBB) penetrant MAO-B inhibitor with an IC50 value of 10 nM. MAO-B-IN-13 has neuroprotective and antioxidant activity. MAO-B-IN-13 can be used for researching Parkinson’s disease.
  • HY-147328
    LCS3

    Apoptosis Cancer
    LCS3 is a reversible and uncompetitive glutathione disulfide reductase (GSR) and thioredoxin reductase 1 (TXNRD1) inhibitor (IC50=3.3 µM and 3.8 µM, respectively). LCS3 shows anti-tumor activity, and induces apoptosis. LCS3 can be used in lung adenocarcinoma (LUAD) research.
  • HY-115944
    BTK-IN-9

    Btk Apoptosis Cancer Inflammation/Immunology
    BTK-IN-9 is a reversible BTK inhibitors with potent antiproliferative activity in mantle cell lymphoma. BTK-IN-9 specifically disturbs mitochondrial membrane potential and increases reactive oxygen species level in Z138 cells. BTK-IN-9 also induces cell apoptosis in Z138 cells.
  • HY-117290
    BMS-962212

    Factor Xa Cardiovascular Disease
    BMS-962212 is a direct, reversible, selective factor XIa (FXIa) inhibitor . BMS-962212 is well tolerated, with fast onset of pharmacodynamic (PD) responses and rapid elimination. BMS-962212 increases exposure dependently in activated partial thromboplastin time, and decreases exposure dependently in FXI clotting activity.
  • HY-15695
    Puromycin aminonucleoside

    NSC 3056

    Bacterial Apoptosis Dipeptidyl Peptidase Aminopeptidase Antibiotic Cancer
    Puromycin aminonucleoside (NSC 3056) is the aminonucleoside portion of the antibiotic puromycin, and used in nephrosis animal models. Puromycin aminonucleoside induces apoptosis. Puromycin aminonucleoside is a reversible inhibitor of dipeptidyl peptidase II and cytosol alanyl aminopeptidase. Puromycin aminonucleoside induces secretion of cell migrasome.
  • HY-N2320
    Physostigmine hemisulfate

    Eserine hemisulfate

    Cholinesterase (ChE) Neurological Disease
    Physostigmine hemisulfate (Eserine hemisulfate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine hemisulfate can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine hemisulfate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine hemisulfate is also an antidote for anticholinergic poisoning.
  • HY-N0063
    Punicalagin

    SARS-CoV HBV Cancer Infection Metabolic Disease
    Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CL pro inhibitor and inhibits SARS-CoV-2 replication in vitro. Punicalagin is an anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects. Punicalagin has the potential for the research of COVID-19.
  • HY-103713
    Seclidemstat

    SP-2577

    Histone Demethylase Cancer
    Seclidemstat is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat can be used for the research of Ewing Sarcoma.
  • HY-107794
    Clodronate disodium tetrahydrate

    Disodium clodronate tetrahydrate

    Others Inflammation/Immunology Neurological Disease
    Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl - competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC50 of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain.
  • HY-18010
    PCI 29732

    Btk BCRP Inflammation/Immunology
    PCI 29732 is a potent, orally active, reversible BTK inhibitor with Ki app values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2.
  • HY-125039
    N-Acetyl lysyltyrosylcysteine amide

    Glutathione Peroxidase Neurological Disease Cardiovascular Disease
    N-Acetyl lysyltyrosylcysteine amide is a potent, reversible, specific, and non-toxic tripeptide inhibitor of myeloperoxidase (MPO). N-Acetyl lysyltyrosylcysteine amide effectively inhibits MPO generation of toxic oxidants in vivo. N-Acetyl lysyltyrosylcysteine amide reduces neuronal damage and preserves brain tissue and neurological function in the stroked brain. N-Acetyl lysyltyrosylcysteine amide inhibits MPO-dependent hypochlorous acid (HOCl) generation, protein nitration, and LDL oxidation.
  • HY-19840
    Voxilaprevir

    GS-9857

    HCV Protease Infection
    Voxilaprevir (GS-9857) is a noncovalent, reversible inhibitor of HCV NS3/4A protease inhibitor (PI) with pangenotypic antiviral activity. Voxilaprevir inhibits genotype 1b and 3a wild-type NS3 proteases with Ki values of 0.038 nM and 0.066 nM, respectively. Voxilaprevir is an orally active direct-acting antiviral agent (DAA) and can be used for HCV infection research.
  • HY-124704
    Chst15-IN-1

    Others Neurological Disease
    Chst15-IN-1 is a potent reversible covalent Chst15 inhibitor. Chst15-IN-1 effectively inhibits chondroitin sulfate-E (CS-E) sulfation levels and other closely related glycosaminoglycans (GAG) sulfotransferases. Chst15-IN-1, as a selective sulfotransferase inhibitor, can diminish the inhibitory effects of chondroitin sulfate proteoglycans (CSPGs), and can be used for the stimulation of neuronal repair.
  • HY-P1259A
    PR-39 TFA

    Proteasome Bacterial Inflammation/Immunology
    PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
  • HY-132310
    MAGL-IN-4

    MAGL Neurological Disease
    MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain.
  • HY-15999A
    Cerdulatinib hydrochloride

    PRT062070 hydrochloride; PRT2070 hydrochloride

    Syk JAK Cancer
    Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC50s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies.
  • HY-B0607
    Nitisinone

    NTBC; Nitisone; SC0735

    Others Metabolic Disease
    Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism.
  • HY-B2155
    Acotiamide monohydrochloride trihydrate

    Cholinesterase (ChE) Metabolic Disease Inflammation/Immunology
    Acotiamide monohydrochloride trihydrate is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC50 of 1.79 μM. Acotiamide monohydrochloride trihydrate can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide monohydrochloride trihydrate has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .
  • HY-100540A
    (Rac)-Golgicide A

    (Rac)-GCA

    Enterovirus Infection
    (Rac)-Golgicide A ((Rac)-GCA) is a racemate of Golgicide A. Golgicide A (GCA) is a potent, highly specific, and reversible inhibitor of the cis-Golgi ADP-ribosylation factor guanine nucleotide exchange factors (ArfGEF) GBF1.Golgicide A drastically reduced replication of coxsackievirus B3 (CVB3) and other human enterovirus species.
  • HY-N0313
    Euphol

    Endogenous Metabolite MAGL Inflammation/Immunology
    Euphol is a tetracyclic triterpene alcohol isolated from the sap of Euphorbia tirucalli with anti-mutagenic, anti-inflammatory and immunomodulatory effects, orally active. Euphol inhibits the monoacylglycerol lipase (MGL) activity via a reversible mechanism (IC50=315 nM). MGL inhibition in the periphery modulates the endocannabinoid system to block the development of inflammatory pain.
  • HY-B0534S
    Moclobemide-d8

    Ro111163-d8

    Monoamine Oxidase Neurological Disease
    Moclobemide-d8 (Ro111163-d8) is the deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A.Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
  • HY-125365
    Rifamycin S

    Bacterial Reactive Oxygen Species Antibiotic Infection
    Rifamycin S, a quinone, is an antibiotic against Gram-positive bacteria (including MRSA). Rifamycin S is the oxidized forms of a reversible oxidation-reduction system involving two electrons. Rifamycin S generates reactive oxygen species (ROS) and inhibits microsomal lipid peroxidation. Rifamycin S can be used for tuberculosis and leprosy.
  • HY-W040468
    2-Phenyl-2-(1-piperidinyl)propane

    Cytochrome P450 Metabolic Disease
    2-Phenyl-2-(1-piperidinyl)propane is a selective and reversible human CYP2B6 inhibitor with an IC50 of 5.1 μM and a Ki of 5.6. 2-Phenyl-2-(1-piperidinyl)propane inhibits CYP2D6 (IC50=74 μM), CYP3A (IC50=200 μM).
  • HY-15816
    Ulixertinib

    BVD-523; VRT752271

    ERK Cancer
    Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line.
  • HY-144396
    SHP2-IN-8

    SHP2 Phosphatase Akt Apoptosis Cancer
    SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC50 value of 23 nM and Ki of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 ℃. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells.
  • HY-12248A
    Telaglenastat hydrochloride

    CB-839 hydrochloride

    Glutaminase Autophagy Cancer
    Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity.
  • HY-103713A
    Seclidemstat mesylate

    SP-2577 mesylate

    Histone Demethylase Cancer
    Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma.
  • HY-12248
    Telaglenastat

    CB-839

    Glutaminase Autophagy Cancer
    Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat inuduces autophagy and has antitumor activity.
  • HY-100671
    L002

    Histone Acetyltransferase STAT Cancer Inflammation/Immunology
    L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment.
  • HY-100707
    IC 86621

    DNA-PK Apoptosis Cancer Inflammation/Immunology
    IC 86621 is a potent DNA-dependent protein kinase (DNA-PK) inhibitor, with an IC50 of 120 nM. IC 86621 also acts as a selective and reversible ATP-competitive inhibitor.IC 86621 inhibits DNA-PK mediated cellular DNA double-strand break (DSB) repair (EC50=68 µM). IC 86621 increases DSB-induced antitumor activity without cytotoxic effects. IC 86621 can protects rheumatoid arthritis (RA) T cells from apoptosis.
  • HY-14292
    NVP-DPP728

    Dipeptidyl Peptidase Metabolic Disease
    NVP-DPP728 is a potent, reversible and nitrile-dependent dipeptidyl peptidase IV (DPP-IV) inhibitor. NVP-DPP728 can inhibit human DPP-IV amidolytic activity with a Ki of 11 nM. NVP-DPP728 inhibits degradation of glucagon-like peptide-1 (GLP-1) and thereby potentiates insulin release in response to glucose intake. NVP-DPP728 can be used for researching diabetes.
  • HY-10235
    Telaprevir

    VX-950

    HCV Protease HCV SARS-CoV Infection
    Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide. Telaprevir inhibits SARS-CoV-2 3CL pro activity.
  • HY-106934
    Peldesine

    BCX 34

    Nucleoside Antimetabolite/Analog HIV Cancer Infection Inflammation/Immunology
    Peldesine (BCX 34) is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research.
  • HY-106934A
    Peldesine dihydrochloride

    BCX 34 dihydrochloride

    Nucleoside Antimetabolite/Analog HIV Cancer Infection Inflammation/Immunology
    Peldesine (BCX 34) dihydrochloride is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine dihydrochloride is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine dihydrochloride has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research.
  • HY-117884
    (Rac)-CCT 250863

    Apoptosis Cancer
    (Rac)-CCT 250863 (compound rac-21) is a selective and reversible NEK 2 inhibitor with an IC50 of 0.073 µM. (Rac)-CCT 250863 shows good effects of inducing cell cycle arrest and also can antiproliferative in cells (Pomalidomide sensitive/resistant). (Rac)-CCT 250863 induces apoptosis when combines with Pomalidomide.
  • HY-100642S
    3-O-Methyltolcapone D7

    Ro 40-7591 D7

    COMT Neurological Disease
    3-O-Methyltolcapone D7 (Ro 40-7591 D7) is a deuterium labeled 3-O-Methyltolcapone. 3-O-Methyltolcapone is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease.
  • HY-114237
    GDC-0276

    Sodium Channel Neurological Disease
    GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects.
  • HY-18962
    AMI-1

    Histone Methyltransferase Cancer
    AMI-1 is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 exerts PRMTs inhibitory effects by blocking peptide-substrate binding.
  • HY-18620
    DZ2002

    Others Inflammation/Immunology
    DZ2002 is an orally active, reversible and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), with good immunosuppressive activity. DZ2002 prevents the development of experimental dermal fibrosis by reversing the profibrotic phenotype of various cell types. DZ2002 can be used in studies of autoimmune diseases such as lupus syndrome and systemic sclerosis.
  • HY-16482
    Teglicar

    Endogenous Metabolite Metabolic Disease Neurological Disease
    Teglicar is a selective and reversible orally active liver isoform of carnitine palmitoyl-transferase 1 (L-CPT1) inhibitor with an IC50 value of 0.68 μM and a Ki value of 0.36 μM. Teglicar has a potential antihyperglycemic propert. Teglicar can be used for the research of diabetes and neurodegenerative disease including Huntington's disease (HD).
  • HY-139664A
    (R)-GSK-3685032

    DNA Methyltransferase Cancer
    (R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition.
  • HY-127105
    Iptacopan

    LNP023

    Complement System Metabolic Disease Inflammation/Immunology
    Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G).
  • HY-115750
    Nω-allyl-L-arginine

    NO Synthase Neurological Disease
    Nω-allyl-L-arginine is a competitive and reversible inhibitor of bovine brain nitric oxide synthase (nNOS). Nω-allyl-L-arginine can inactivate nNOS in a time-dependent manner. Nω-allyl-L-arginine also is a substrate, producing L-arginine, acrolein, and H2O.
  • HY-B0034S1
    Donepezil-d4 hydrochloride

    E2020-d4

    Cholinesterase (ChE) Neurological Disease
    Donepezil-d4 hydrochloride (E2020-d4) is the deuterium labeled Donepezil hydrochloride. Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity.
  • HY-146039
    AChE-IN-15

    Cholinesterase (ChE) Neurological Disease
    AChE-IN-15 (Compound 3d) is a reversible human acetylcholinesterase (huAChE) (IC50=6.8 μM) and human butyrylcholinesterase (huBChE) (IC50=16.1 μM) inhibitor. AChE-IN-15 shows significant antioxidant potency, AChE-IN-15 can be used for the research of Alzheimer’s disease.
  • HY-135457
    JMS-053

    Phosphatase Cancer
    JMS-053 is a potent, selective and reversible PTP4A inhibitor, with IC50s of 29.1 nM, 48.0 nM, 34.7 nM, 92.6 nM, and 207.6 nM for PTP4A1, PTP4A2, PTP4A3, CDC25B, and DUSP3, respectively. JMS-053 can inhibit cancer cell migration and spheroid growth in vitro, attenuate in vivo ovarian tumor growth.
  • 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-N6608S
    Physostigmine-d3

    Eserine-d3

    Cholinesterase (ChE) Neurological Disease
    Physostigmine-d3 (Eserine-d3) is the deuterium labeled Physostigmine. Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning.
  • HY-18962A
    AMI-1 free acid

    Histone Methyltransferase Cancer
    AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding.
  • HY-109124
    Taniborbactam

    VNRX-5133

    Bacterial Infection
    Taniborbactam (VNRX-5133) is a reversible and selective boronic acid-containing pan-spectrum β-lactamase inhibitor with IC50s of 8-530 nM. Taniborbactam has IC50s of 30 nM, 32 nM, 42 nM, 20 nM for KPC-2, AmpC, OXA-48, and VIM-2. Taniborbactam is against Gram-negative bacteria.
  • HY-14892
    Gemigliptin

    LC15-0444

    Dipeptidyl Peptidase Metabolic Disease
    Gemigliptin (LC15-0444 ) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin exhibits potent anti-glycation properties. Gemigliptin can be used for the research of advanced glycation end products (AGE)-related diabetic complications.
  • HY-14930A
    Mirodenafil dihydrochloride

    SK-3530 dihydrochloride

    Phosphodiesterase (PDE) Glucocorticoid Receptor Wnt β-catenin Apoptosis Endocrinology Inflammation/Immunology Neurological Disease
    Mirodenafil (SK3530) dihydrochloride is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil dihydrochloride is a glucocorticoid receptor (GR) modulator Mirodenafil dihydrochloride activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil dihydrochloride can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).
  • HY-14930
    Mirodenafil

    SK3530

    Phosphodiesterase (PDE) Glucocorticoid Receptor Wnt β-catenin Apoptosis Endocrinology Inflammation/Immunology Neurological Disease
    Mirodenafil (SK3530) is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil is a glucocorticoid receptor (GR) modulator Mirodenafil activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).
  • HY-19801
    CVT-10216

    Aldehyde Dehydrogenase (ALDH) Neurological Disease
    CVT-10216 is a highly selective, reversible aldehyde dehydrogenase-2 (ALDH-2) inhibitor with an IC50 of 29 nM. CVT-10216 also has inhibitory effect of ALDH-1 with an IC50 of 1.3 μM. CVT-10216 can reduce excessive alcohol drinking in alcohol-preferring rats and exhibit anxiolytic effects.
  • HY-146312
    AChE/BChE/MAO-B-IN-1

    Cholinesterase (ChE) Monoamine Oxidase Neurological Disease
    AChE/BChE/MAO-B-IN-1 (Compound 10) is a reversible and non-time-dependent AChE, BChE and MAO-B inhibitor with IC50 values of 7.31, 0.56 and 26.1 μM for hAChE, hBChE and hMAO-B, respectively. AChE/BChE/MAO-B-IN-1 can cross the BBB and shows neuroprotective effects without cytotoxicity.
  • HY-N10096
    Epoxyazadiradione

    Parasite Infection
    Epoxyazadiradione is a limonoid purified from neem (Azadirachta indica) fruits. Epoxyazadiradione inhibits the tautomerase activity of MIF of both human (huMIF) and malaria parasites (Plasmodium falciparum (PfMIF) and Plasmodium yoelii (PyMIF)) non-competitively in a reversible fashion (Ki, 2.11-5.23 μM). Epoxyazadiradione has the potential against proinflammatory reactions induced by MIF of both malaria parasites and human.
  • HY-109124A
    Taniborbactam hydrochloride

    VNRX-5133 hydrochloride

    Bacterial Infection
    Taniborbactam hydrochloride (VNRX-5133 hydrochloride) is a reversible and selective boronic acid-containing pan-spectrum β-lactamase inhibitor with IC50s of 8-530 nM. Taniborbactam hydrochloride has IC50s of 30 nM, 32 nM, 42 nM, 20 nM for KPC-2, AmpC, OXA-48, and VIM-2. Taniborbactam hydrochloride is against Gram-negative bacteria.
  • HY-101925
    CM-272

    Histone Methyltransferase DNA Methyltransferase Apoptosis Cancer
    CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death.
  • HY-13281
    PIK-75 hydrochloride

    DNA-PK PI3K Apoptosis Cancer
    PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 hydrochloride induces apoptosis.
  • HY-15425
    PF-543

    Sphingosine Kinase 1 Inhibitor II

    SphK LPL Receptor Apoptosis Autophagy Cancer Inflammation/Immunology Cardiovascular Disease
    PF-543 (Sphingosine Kinase 1 Inhibitor II) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy.
  • HY-15425B
    PF-543 hydrochloride

    Sphingosine Kinase 1 Inhibitor II hydrochloride

    SphK LPL Receptor Apoptosis Autophagy Cancer Inflammation/Immunology Cardiovascular Disease
    PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy.
  • HY-107834
    PIK-75

    DNA-PK PI3K Apoptosis Cancer
    PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 induces apoptosis.
  • HY-123872
    MSC1094308

    p97 Cancer
    MSC1094308 is a non-competitive and reversible VPS4B/p97 (VCP) (I/II type AAA ATPase) allosteric inhibitor, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively. MSC1094308 inhibits the D2 ATPase activity by binding to a drugable hotspot of p97. MSC1094308 can be used in study of cancer.
  • HY-14202
    Lazabemide hydrochloride

    Ro 19-6327 hydrochloride

    Monoamine Oxidase Neurological Disease
    Lazabemide hydrochloride (Ro 19-6327 hydrochloride) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide  inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease.
  • HY-14201
    Lazabemide

    Ro 19-6327

    Monoamine Oxidase Neurological Disease
    Lazabemide (Ro 19-6327) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide  inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease.
  • HY-13814
    PR-619

    Deubiquitinase Autophagy Apoptosis Cancer
    PR-619 is a broad-range and reversible DUB inhibitor with EC50s of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively. PR-619 induces ER Stress and ER-Stress related apoptosis.
  • HY-100414
    Soraprazan

    BYK61359

    Proton Pump Metabolic Disease
    Soraprazan (BYK61359) is a selective, reversible K-competitive inhibitor of the H,K-ATPase (Ki=6.4 nM), with an IC50 of 0.19 μM in gastric glands. Soraprazan binds to the H,K-ATPase with a Kd of 28.27 nM. Soraprazan shows immediate inhibition of acid secretion and is more than 2000-fold selective for H,K-ATPase over Na,K- and Ca-ATPases.
  • HY-146691
    hMAO-B-IN-2

    Monoamine Oxidase Neurological Disease
    hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research.
  • HY-129388A
    Pulrodemstat

    CC-90011; LSD1-IN-7

    Histone Demethylase Cancer
    Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
  • HY-10200
    BMS-754807

    IGF-1R Insulin Receptor Cancer Endocrinology
    BMS-754807 is a potent and reversible IGF-1R/IR inhibitor (IC50=1.8 and 1.7 nM, respectively; Ki=<2 nM for both). BMS-754807 also shows potent activities against Met, RON, TrkA, TrkB, AurA, and AurB with IC50 values of 6, 44, 7, 4, 9, and 25 nM, respectively.
  • HY-18263C
    Elubrixin tosylate

    SB-656933 tosylate

    CXCR Interleukin Related Inflammation/Immunology
    Elubrixin tosylate (SB-656933 tosylate) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin tosylate inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin tosylate has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation.
  • HY-D0004
    Azure B

    Azure B chloride

    Monoamine Oxidase Neurological Disease
    Azure B is a cationic dye and the major metabolite of Methylene blue. Azure B is used in making Azure eosin stains for blood smear staining. Azure B is a high-potency, selective and reversible inhibitor of monoamine oxidases (MAO)-A, with IC50s of 11 and 968 nM for recombinant human MAO-A and MAO-B, respectively. Azure B possesses significant antidepressant-like effects.
  • HY-13290
    KN-62

    CaMK P2X Receptor Metabolic Disease Cancer
    KN-62 is a selective and reversible inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with a Ki of 0.9 μM for rat brain CaMK-II. KN-62 directly binds to the calmodulin binding site of CaMK-II. KN-62 displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
  • HY-118700
    2-Iminobiotin

    Guanidinobiotin

    NO Synthase Neurological Disease
    2-Iminobiotin (Guanidinobiotin) is a biotin (vitamin H or B7) analog. 2-Iminobiotin is a reversible nitric oxide synthases inhibitor with Kis of 21.8 and 37.5μM for murine iNOS and rat n-cNOS, respectively. 2-Iminobiotin superimposes on hypothermia protects human neuronal cells from hypoxia-induced cell damage.
  • HY-18263A
    Elubrixin

    SB-656933

    CXCR Interleukin Related Inflammation/Immunology
    Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation.
  • HY-136813
    Multitarget AD inhibitor-1

    Beta-secretase Amyloid-β Neurological Disease
    Multitarget AD inhibitor-1 is a selective and reversible butyrylcholinesterase (BuChE) inhibitor with IC50s of 7.22 μM and 1.55 μM for hBuChE and eqBuChE (BuChE from equine serum), respectively. Multitarget AD inhibitor-1 inhibits β-secretase (IC50hBACE-1=41.60 μM), amyloid β aggregation (IC50Aβ=3.09 μM), tau aggregation. Multitarget AD inhibitor-1, a diphenylpropylamine derivative, has the potential for multifunctional disease-modifying anti-Alzheimer’s research.
  • HY-145015
    HM43239

    FLT3 Apoptosis Cancer
    HM43239 is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. HM43239 inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. HM43239 inhibits the proliferation and induces the apoptosis of leukemic cells.
  • HY-135396S
    (1S,2S)-Bortezomib-d5

    Proteasome Apoptosis Cancer
    (1S,2S)-Bortezomib-d5 is the deuterium labeled (1S,2S)-Bortezomib. (1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans.
  • HY-113952
    Actinonin

    (-)-Actinonin

    Aminopeptidase Bacterial MMP Apoptosis Antibiotic Cancer Infection
    Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities.
  • HY-15425A
    PF-543 Citrate

    Sphingosine Kinase 1 Inhibitor II Citrate

    SphK LPL Receptor Apoptosis Autophagy Cancer Inflammation/Immunology Cardiovascular Disease
    PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy.
  • HY-10683
    PKI-402

    PI3K mTOR Cancer
    PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC50=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).
  • 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-17387
    (-)-Huperzine A

    Huperzine A

    Cholinesterase (ChE) Apoptosis iGluR Neurological Disease
    (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease.
  • HY-16718
    Dagrocorat

    PF-00251802

    Glucocorticoid Receptor Cytochrome P450 Endocrinology Inflammation/Immunology
    Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis.
  • HY-17369B
    Tirofiban

    L700462; MK383

    Integrin Cardiovascular Disease
    Tirofiban (L700462) is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area.
  • HY-A0009
    Galanthamine hydrobromide

    Galantamine hydrobromide

    Cholinesterase (ChE) nAChR Neurological Disease
    Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD).
  • HY-150702
    MAGLi 432

    MAGL Inflammation/Immunology Neurological Disease
    MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. MAGLi 432 binds with high affinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease.
  • HY-B0563
    Ropivacaine

    Sodium Channel Potassium Channel Neurological Disease Cardiovascular Disease
    Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine is used for the research of neuropathic pain management.
  • HY-144677
    pan-HER-IN-2

    EGFR Apoptosis Cancer
    pan-HER-IN-2 (Compound C6) is a reversible, orally active pan-HER inhibitor with IC50 values of 0.72, 2.0, 8.2 and 75.1 nM against EGFR, HER4, EGFR T790M/L858R and HER2, respectively. pan-HER-IN-2 induces apoptosis and shows antitumor activities.
  • HY-17369A
    Tirofiban hydrochloride

    L700462 hydrochloride; MK383 hydrochloride

    Integrin Cardiovascular Disease
    Tirofiban (L700462) hydrochloride is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban hydrochloride induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area.
  • HY-123319A
    Antofloxacin

    Bacterial Antibiotic Infection
    Antofloxacin is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin is a weak, reversible inhibitor of CYP1A2 for the treatment of infections caused by a diverse group of bacterial species.
  • HY-16718A
    Dagrocorat hydrochloride

    PF-00251802 hydrochloride

    Glucocorticoid Receptor Cytochrome P450 Endocrinology Inflammation/Immunology
    Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis.
  • HY-123319
    Antofloxacin hydrochloride

    Bacterial Antibiotic Infection
    Antofloxacin hydrochloride is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin hydrochloride shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin hydrochloride is a weak, reversible inhibitor of CYP1A2 for the treatment of infections caused by a diverse group of bacterial species.
  • HY-B0563B
    Ropivacaine hydrochloride

    Sodium Channel Potassium Channel Neurological Disease Cardiovascular Disease
    Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine is widely used for neuropathic pain management in vivo.
  • HY-14892A
    Gemigliptin tartrate

    LC15-0444 tartrate

    Dipeptidyl Peptidase Metabolic Disease
    Gemigliptin tartrate (LC15-0444 tartrate) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin tartrate exhibits potent anti-glycation properties. Gemigliptin tartrate can be used for the research of advanced glycation end products (AGE)-related diabetic complications.
  • HY-100642S1
    3-O-Methyltolcapone-d4

    Ro 40-7591-d4

    COMT Neurological Disease
    3-O-Methyltolcapone-d4 (Ro 40-7591-d4) is the deuterium labeled 3-O-Methyltolcapone. 3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease.
  • HY-17369
    Tirofiban hydrochloride monohydrate

    L700462 hydrochloride monohydrate; MK383 hydrochloride monohydrate

    Integrin Cardiovascular Disease
    Tirofiban (L700462) hydrochloride monohydrate is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban hydrochloride monohydrate induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride monohydrate can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area.
  • HY-144680
    BLU-945

    EGFR Cancer
    BLU-945 is a potent, highly selective, reversible and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKIs). BLU-945 can effectively inhibit EGFR with L858R and/or exon 19 deletion mutation, T790M mutation and C797S mutation. BLU-945 can be used for the research of lung cancer including non-small cell lung cancer (NSCLC).
  • HY-W008566
    Norharmane

    Norharman; β-Carboline

    Monoamine Oxidase Endogenous Metabolite Cancer Infection Neurological Disease
    Norharmane (Norharman), a β-carboline alkaloid, is a potent and reversible monoamine oxidase inhibitor, with IC50 values of 6.5 and 4.7 μM for MAO-A and MAO-B, respectively. Norharmane causes antidepressant responses. Norharmane is also a prospective anti-cancer photosensitizer. Norharmane alters polar auxin transport (PAT) by inhibiting PIN2, PIN3 and PIN7 transport proteins, thus causing a significant inhibitory effect on the growth of Arabidopsis thaliana seedlings.
  • HY-115669
    Pentachloropseudilin

    Antibiotic A 15104 Y; PClP

    Myosin TGF-β Receptor Cancer
    Pentachloropseudilin (Antibiotic A 15104 Y; PClP) is a reversible and allosteric potent inhibitor of Myo1s (class 1 myosins) with IC50s range from 1 to 5 μM for mammalian class-1 myosins and greater than 90 μM for class-2 and class-5 myosins. Pentachloropseudilin is a potent inhibitor of transforming growth factor-β (TGF-β)-stimulated signaling, with an IC50 of 0.1 to 0.2 μM for TGF-β.
  • HY-103371
    DCPIB

    Chloride Channel Potassium Channel Neurological Disease
    DCPIB is a selective, reversible and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB voltage-dependently activates potassium channels TREK1 and TRAAK, and inhibits TRESK, TASK1 and TASK3 (IC50s: 0.14, 0.95, 50.72 μM, respectively). DCPIB is also a selective blocker of swelling-induced chloride current (ICl,swell), with an IC50 of 4.1 μM. DCPIB is a useful tool for investigating structure-function studies of K2P channels.
  • HY-129388B
    Pulrodemstat benzenesulfonate

    CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate

    Histone Demethylase Cancer
    CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
  • HY-100867
    TAK-659

    Syk FLT3 Cancer
    TAK-659 is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL).
  • HY-146165
    Metallo-β-lactamase-IN-8

    Bacterial Infection
    Metallo-β-lactamase-IN-8 (compound 17) is a potent, reversible and competitive broad-spectrum inhibitor of metallo-β-lactamases (MβLs), with IC50s of 1.3 μM, 5.7 μM, 9.8 μM, and 9.9 μM for L1, ImiS, IMP-1 and VIM-2, respectively. Metallo-β-lactamase-IN-8 exhibits antibacterial activity.
  • HY-16214
    FX-11

    LDHA Inhibitor FX11

    Lactate Dehydrogenase Pyruvate Kinase Apoptosis Reactive Oxygen Species Cancer
    FX-11 is a potent, selective, reversible and competitive lactate dehydrogenase A (LDHA) specific inhibitor, with a Ki of 8 μM. FX-11 can effectively activate PKM2 (pyruvate kinase M2). FX-11 reduces ATP levels and induces oxidative stress, ROS production and cell death. FX-11 shows antitumor activity in lymphoma and pancreatic cancer xenografts.
  • HY-118700A
    2-Iminobiotin hydrobromide

    Guanidinobiotin hydrobromide

    NO Synthase Neurological Disease
    2-Iminobiotin hydrobromide (Guanidinobiotin hydrobromide) is a biotin (vitamin H or B7) analog. 2-Iminobiotin hydrobromide is a reversible nitric oxide synthases inhibitor with Kis of 21.8 and 37.5 μM for murine iNOS and rat n-cNOS, respectively. 2-Iminobiotin hydrobromide superimposes on hypothermia protects human neuronal cells from hypoxia-induced cell damage.
  • HY-100867A
    TAK-659 hydrochloride

    Syk FLT3 Cancer
    TAK-659 hydrochloride is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 hydrochloride induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL).
  • HY-B0563A
    Ropivacaine hydrochloride monohydrate

    Sodium Channel Potassium Channel Neurological Disease Cardiovascular Disease
    Ropivacaine hydrochloride monohydrate is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine is widely used for regional anesthesia and neuropathic pain management in vivo.
  • HY-W107464
    G6PDi-1

    Others Metabolic Disease Inflammation/Immunology
    G6PDi-1 is a reversible and non-competitive glucose-6-phosphate dehydrogenase (G6PD) inhibitor with an IC50 of 0.07 μM. G6PDi-1 depletes NADPH most strongly in lymphocytes. G6PDi-1 markedly decreases inflammatory cytokine production in T cells.
  • HY-B0879A
    Suramin sodium salt

    Suramin hexasodium salt

    Phosphatase Sirtuin Reverse Transcriptase Topoisomerase SARS-CoV 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 is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor. Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
  • HY-B0879
    Suramin

    Phosphatase Sirtuin Reverse Transcriptase Topoisomerase SARS-CoV 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 is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor.Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
  • HY-B0563C
    Ropivacaine mesylate

    Sodium Channel Potassium Channel Neurological Disease Cardiovascular Disease
    Ropivacaine mesylate is a long-acting amide local anaesthetic agent for a spinal block and effectively blocks neuropathic pain. Ropivacaine blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibressup>[1]. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane.
  • HY-129388
    Pulrodemstat Methylbenzenesulfonate

    CC-90011 Methylbenzenesulfonate; LSD1-IN-7 Methylbenzenesulfonate

    Histone Demethylase Cancer
    CC-90011 Methylbenzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 Methylbenzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 Methylbenzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
  • HY-12755
    ML141

    CID-2950007

    Ras Apoptosis Cancer
    ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines.
  • HY-10235S
    Telaprevir-d4

    VX-950-d4

    HCV Protease HCV SARS-CoV Infection
    Telaprevir-d4 (VX-950-d4) is the deuterium labeled Telaprevir. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide. Telaprevir inhibits SARS-CoV-2 3CL pro activity.
  • HY-103312
    Xestospongin C

    (-)-Xestospongin C

    Calcium Channel Apoptosis Neurological Disease
    Xestospongin C ((-)-Xestospongin C) is a selective, reversible inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor. Xestospongin C acts as an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca 2+ ATPase (SERCA) pump of internal stores. Xestospongin C blocks IP3-induced Ca 2+ release from cerebellar microsomes with an IC50 of 358 nM. Xestospongin C is a valuable tool for investigating the structure and function of IP3Rs and Ca 2+ signaling in neuronal and nonneuronal cells.
  • HY-B0563S1
    Ropivacaine-d7

    Sodium Channel Potassium Channel Neurological Disease Cardiovascular Disease
    Ropivacaine-d7 is deuterium labeled Ropivacaine. Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine is used for the research of neuropathic pain management.
  • HY-128717A
    GSK3368715 dihydrochloride

    EPZ019997 dihydrochloride

    Histone Methyltransferase Cancer
    GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.
  • HY-117026
    LKY-047

    Cytochrome P450 Metabolic Disease Inflammation/Immunology
    LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A.
  • HY-103352
    L-006235

    L-235

    Cathepsin Metabolic Disease
    L-006235 (L-235) is a potent, selective, reversible and orally active inhibitor of cathepsin K, with an IC50 of 5 nM in bone resorption assay. L-006235 shows selectivity for cathepsin K (Ki=0.2 nM) over cathepsin B, cathepsin L, and cathepsin S (Ki=1, 6, and 47 μM, respectively). L-006235 can reduce collagen degradation and prevent bone loss.
  • HY-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-128717
    GSK3368715

    EPZ019997

    Histone Methyltransferase Cancer
    GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.
  • HY-130983
    N-piperidine Ibrutinib hydrochloride

    Btk Ligands for Target Protein for PROTAC Cancer
    N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively. N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.
  • HY-44062
    G9a-IN-1

    Histone Methyltransferase Inflammation/Immunology Cancer
    G9a-IN-1 (Compound 113) is a G9a protein inhibitor. G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes histone H3 lysine 9 dimethylation (H3K9me2), which is a reversible modification generally associated with transcriptional gene silencing. G9a-IN-1 can be used for the research of autoimmune disorders or cancer.
  • HY-10230
    Midostaurin

    PKC412; CGP 41251

    PKC VEGFR c-Kit NO Synthase Apoptosis Cancer
    Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin 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. Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects.
  • 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-18299
    Purvalanol B

    NG 95

    CDK Parasite Cancer Infection
    Purvalanol B (NG 95) is a potent, selective, reversible and ATP-competitive inhibitor CDK, with IC50s of 6 nM, 6 nM, 9 nM, 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. Purvalanol B shows selectivity for CDK over a range of other protein kinases (IC50>1000 nM). Purvalanol B inhibits the growth a chloroquine-resistant strain of P. falciparum.
  • HY-14280A
    Entacapone sodium salt

    COMT Neurological Disease
    Entacapone sodium salt is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone sodium salt inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone sodium salt can be used for the research of Parkinson's disease. Entacapone sodium salt serves as as a inhibit of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.
  • HY-14280
    Entacapone

    COMT Neurological Disease
    Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.
  • HY-A0009S
    Galanthamine-d3 hydrobromide

    Galantamine-d3 hydrobromide

    Cholinesterase (ChE) nAChR Neurological Disease
    Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD).
  • HY-76474
    BAY 61-3606

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

    Syk Apoptosis Inflammation/Immunology Cancer
    BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM. BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
  • HY-D0976
    NF279

    P2X Receptor HIV Infection
    NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC50 of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC50=1.62 μM), P2X4 (IC50>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env.
  • HY-131014
    FM-479

    JAK Inflammation/Immunology
    FM-479 is the negative control of FM-381 (HY-102046) and has no activity on JAK3 or other kinases. FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
  • HY-110137A
    Furamidine

    DB75; NSC 305831

    Histone Methyltransferase Phosphodiesterase (PDE) Parasite Cancer Infection Inflammation/Immunology
    Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent.
  • HY-119944
    JND3229

    EGFR Cancer
    JND3229 is a reversible EGFR C797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFR L858R/T790M/C797S, EGFR WT and EGFR L858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma.
  • HY-110137
    Furamidine dihydrochloride

    DB75 dihydrochloride; NSC 305831 dihydrochloride

    Histone Methyltransferase Phosphodiesterase (PDE) Parasite Cancer Infection Inflammation/Immunology
    Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent.
  • HY-14280S2
    (E)-Entacapone-d10

    COMT Neurological Disease
    Entacapone-d10 is the deuterium labeled Entacapone. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.
  • HY-14280S
    Entacapone-d10

    COMT Neurological Disease
    Entacapone-d10 is the deuterium labeled Entacapone. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.
  • HY-B0653
    Levobupivacaine

    (S)-(-)-Bupivacaine

    Sodium Channel Ferroptosis Cancer Neurological Disease
    Levobupivacaine ((S)-(-)-Bupivacaine) is a long-acting amide local anaesthetic. Levobupivacaine exerts anaesthetic and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer.
  • HY-B0653A
    Levobupivacaine hydrochloride

    (S)-(-)-Bupivacaine monohydrochloride

    Sodium Channel Ferroptosis Neurological Disease Cancer
    Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local anaesthetic. Levobupivacaine hydrochloride exerts anaesthetic and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer.
  • HY-130612
    PROTAC BRD2/BRD4 degrader-1

    Epigenetic Reader Domain PROTACs Cancer
    PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A.
  • HY-108239
    BIX-01294 trihydrochloride

    Histone Methyltransferase Autophagy Cancer
    BIX-01294 trihydrochloride is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 trihydrochloride inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294 trihydrochloride, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 trihydrochloride has antitumor activity in recurrent tumor cells.
  • HY-10587
    BIX-01294

    Histone Methyltransferase Autophagy Cancer
    BIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells.
  • HY-70057
    Safinamide

    FCE 26743; EMD 1195686

    Monoamine Oxidase Neurological Disease
    Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM). Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al.
  • HY-B1033
    Metergoline

    5-HT Receptor Dopamine Receptor Sodium Channel Neurological Disease
    Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na + channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation.
  • HY-111790
    M3258

    Proteasome Apoptosis Cancer
    M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells.
  • HY-N6789
    KT5720

    PKA Cancer Neurological Disease
    KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 µM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2 + concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases.
  • HY-70057A
    Safinamide mesylate

    FCE 26743 mesylate; EMD 1195686 mesylate

    Monoamine Oxidase Neurological Disease Cardiovascular Disease
    Safinamide (FCE 26743; EMD 1195686) mesylate is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 nM). Safinamide mesylate also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide mesylate has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke et.al.
  • HY-110137AS
    Furamidine-d8

    Histone Methyltransferase Phosphodiesterase (PDE) Parasite Cancer Infection Inflammation/Immunology
    Furamidine-d8 (DB75-d8) is the deuterium labeled Furamidine. Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent.
  • HY-B1033S
    Metergoline-d5

    5-HT Receptor Dopamine Receptor Sodium Channel Neurological Disease
    Metergoline-d5 is the deuterium labeled Metergoline. Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na + channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation.
  • HY-70057S1
    Safinamide-d4-1

    FCE 26743-d4-1; EMD 1195686-d4-1

    Monoamine Oxidase Neurological Disease
    Safinamide-d4-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM). Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al.
  • HY-70057S
    Safinamide-d4

    Monoamine Oxidase Neurological Disease
    Safinamide-d4 (FCE 26743-d4) is the deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM). Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al.
  • HY-147100
    α1A-AR Degrader 9c

    PROTACs Adrenergic Receptor Cancer
    α1A-AR Degrader 9c (compound 9c) is a potent, selective and reversible α1A-AR (Adrenergic receptor) PROTAC degrader, with a DC50 of 2.86 μM. α1A-AR Degrader 9c induces α1A-AR degradation can be attributed to proteasomal degradation. α1A-AR Degrader 9c inhibits the proliferation of PC-3 cells, with an IC50 of 6.12 μM. α1A-AR Degrader 9c shows antitumor activity, and can be used for prostate cancer research.