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Results for "A small molecule Inhibitors" in MCE Product Catalog:


Inhibitors & Agonists


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Dye Reagents



Cat. No. Product Name Target Research Areas
  • HY-17641
    Olumacostat glasaretil

    Acetyl-CoA Carboxylase Others
    Olumacostat glasaretil is a small molecule inhibitor of acetyl coenzyme A carboxylase (ACC).
  • HY-101091

    Apoptosis Cancer
    Importazole is a small molecule inhibitor of the nuclear transport receptor importin-β.
  • HY-12879

    Wnt Cancer
    IWP-4 is a small molecule Wnt inhibitor with an IC50 of 25 nM.
  • HY-111378
    Casein Kinase II Inhibitor IV

    Casein Kinase Others
    Casein Kinase II Inhibitor IV is a small-molecule inducer of epidermal keratinocyte differentiation.
  • HY-111378A
    Casein Kinase II Inhibitor IV Hydrochloride

    Casein Kinase Others
    Casein Kinase II Inhibitor IV Hydrochloride is a small-molecule inducer of epidermal keratinocyte differentiation.
  • HY-19959

    Others Cancer
    Mirin is a small-molecule inhibitor of MRN (Mre11, Rad50, and Nbs1) complex.
  • HY-13321

    HCV Infection
    Anguizole is a small molecule inhibitor of HCV replication and alters NS4B's subcellular distribution.
  • HY-19707

    IRE1 Inhibitor III

    IRE1 Metabolic Disease
    4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.
  • HY-16925

    Epigenetic Reader Domain Cancer
    MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.
  • HY-14987

    Bacterial Infection
    AX20017 is a small-molecule protein kinase G (PknG) inhibitor with an IC50 of 0.39 μM.
  • HY-19809

    Epigenetic Reader Domain Cancer
    MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.
  • HY-19748

    Bacterial Infection
    LED209 is a potent small molecule inhibitor of bacterial receptor QseC, is a potent prodrug that is highly selective for QseC.
  • HY-101865

    Bacterial Infection
    KKL-10 is a small-molecule ribosome rescue inhibitor with broad-spectrum antimicrobial activity against bacteria.
  • HY-19546

    Histone Methyltransferase Cancer
    BAY-598 is selective small molecule inhibitor of SMYD2 with an IC50 of 27 nM.
  • HY-100039

    HIV Infection
    YYA-021 is a small-molecule CD4 mimic that inhibits HIV entry, with high anti-HIV activity and low cytotoxicity.
  • HY-12796A
    Raxatrigine hydrochloride

    GSK-1014802 hydrochloride; CNV1014802 hydrochloride

    Sodium Channel Neurological Disease
    Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
  • HY-100493

    STAT Cancer
    BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC50 of 6.8 μM.
  • HY-12796

    GSK-1014802; CNV1014802

    Sodium Channel Neurological Disease
    Raxatrigine (GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
  • HY-50295

    PD 184352

    MEK Apoptosis Cancer
    CI-1040 (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.
  • HY-100735
    C 87

    TNF Receptor Inflammation/Immunology
    C87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC50 of 8.73 μM.
  • HY-16664

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    SJ-172550 is a small molecule inhibitor of MDMX; competes for the wild type p53 peptide binding to MDMX with an EC50 of 5 μM.
  • HY-15755

    ROCK Cancer
    RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 values of 14.5 nM and 6.2 nM, respectively.
  • HY-138617

    Others Cancer
    AI-10-47 is a small molecule inhibitor of CBFβ-RUNX binding, with an IC50 of 3.2 μM.
  • HY-10217
    Thrombin Inhibitor 2

    Thrombin Cardiovascular Disease
    Thrombin Inhibitor 2 is a small molecule direct thrombin inhibitor, extracted from US8541580B2. Thrombin Inhibitor 2 has antithrombotic activity.
  • HY-112167

    ARRY-575; RG7741

    Checkpoint Kinase (Chk) Cancer
    GDC-0575 (ARRY-575, RG7741) is a highly-selective oral small-molecule Chk1 inhibitor with an IC50 of 1.2 nM.
  • HY-133735

    Others Infection
    GRP-60367 is a first-in-class small-molecule rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains.
  • HY-12631

    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-15796

    LRRK2 Neurological Disease
    GNE0877 is a highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitor with an IC50 of 3 nM.
  • HY-100863

    PARP Cancer
    BRCA1-IN-1 is a novel small-molecule-like BRCA1 inhibitor with IC50 and Ki of 0.53 μM and 0.71 μM, respecrively.
  • HY-18696

    c-Met/HGFR Cancer
    AMG-337 is a potent and highly selective small molecule ATP-competitive MET kinase inhibitor. AMG 337 inhibits MET kinase activity with an IC50 of < 5nM in enzymatic assays.
  • HY-16999

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    RO8994 is a highly potent and selective series of spiroindolinone small-molecule MDM2 inhibitor, with IC50 of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays).
  • HY-12873

    Ras Cancer
    RBC8 is a novel small molecule inhibitor of Ral GTPase; has IC50 of 3.5 μM in H2122 cell and 3.4 μM in H358 cell.
  • HY-13809


    Smo Apoptosis Cancer
    BMS-833923 (XL-139) is an orally bioavailable small-molecule inhibitor of Smoothened with potential antineoplastic activity; inhibits BODIPY cyclopamine binding to SMO in a dose-dependent manner with an IC50 of 21 nM.
  • HY-15241

    LCQ-195; AT9311

    CDK Cancer
    NVP-LCQ195 (AT9311; LCQ195) is a small molecule heterocyclic inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM.
  • HY-107145A

    TAM Receptor VEGFR c-Met/HGFR Cancer
    Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.
  • HY-10527

    Bay 57-9352

    c-Kit PDGFR VEGFR Cancer
    Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit with IC50s of 6, 4, 15 and 1 nM, respectively.
  • HY-10530

    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-107145
    Ningetinib Tosylate

    TAM Receptor VEGFR c-Met/HGFR Cancer
    Ningetinib Tosylate is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.
  • HY-19708

    IRE1 Cancer Metabolic Disease Inflammation/Immunology
    KIRA6 is an advanced small-molecule IRE1α RNase kinase inhibitor with an IC50 of 0.6 µM. KIRA6 can trigger an apoptotic response.
  • HY-12521

    CRAC Channel Inflammation/Immunology
    GSK-5498A is a selective small molecule blocker of CARC (IC50, 1 μM); inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.
  • HY-15858


    Enolase Cancer
    ENOblock(AP-III-a4) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo.
  • HY-15858A
    AP-III-a4 hydrochloride

    ENOblock hydrochloride

    Enolase Cancer
    AP-III-a4 hydrochloride (ENOblock hydrochloride) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo.
  • HY-10398

    Ro 1130830; RS 130830

    MMP Cancer
    CTS-1027 is a potent small molecule inhibitor of MMPs, with IC50s of 0.3 nM, 0.5 nM for MMP2, MMP13, respectively, and has > 1,000 fold selectivity over MMP1.
  • HY-133735A
    GRP-60367 hydrochloride

    Others Infection
    GRP-60367 hydrochloride is a first-in-class small-molecule rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains. GRP-60367 hydrochloride specifically targets the RABV G protein.
  • HY-102034
    Complement factor D-IN-1

    Others 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-18741

    Proteasome Apoptosis Metabolic Disease Cancer
    VR23 is a small molecule that potently inhibits the activities of trypsin-like proteasomes (IC50=1 nM), chymotrypsin-like proteasomes (IC50=50-100 nM), and caspase-like proteasomes (IC50=3 μM).
  • HY-125017

    PLB-1001; CBT-101

    c-Met/HGFR Cancer
    Bozitinib (PLB-1001) is a highly selective c-MET kinase inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) is a ATP-competitive small-molecule inhibitor, binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily.
  • HY-106101

    Quinomycin A; NSC-13502

    HIF/HIF Prolyl-Hydroxylase Cancer
    Echinomycin (Quinomycin A) is potent small-molecule and cell-permeable inhibitor of hypoxia-inducible factor-1 (HIF-1) DNA-binding activity. Echinomycin selectively inhibits the cancer stem cells (CSCs) with an IC50 of 29.4 pM.
  • HY-124700

    Others Metabolic Disease
    LYPLAL1-IN-1 (Compound 11) is an selective covalent small-molecule inhibitor of Lysophospholipase-like 1 (LYPLAL1) with an IC50 of 0.006 μM. LYPLAL1-IN-1 increases glucose production.
  • HY-17493

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    MI-773 is a new small molecule inhibitor of the MDM2-p53 interaction, binds to MDM2 with high affinity (Ki=0.88 nM) and blocks the p53-MDM2 interaction.
  • HY-115467

    Others Metabolic Disease
    MitoBloCK-10 (MB-10) is the first small molecule modulator to attenuate protein-associated motor (PAM) complex activity. MitoBloCK-10 (MB-10) inhibits Tim44 (C-terminal domain) binding to the precursor and to Hsp70.
  • HY-14454
    TPh A

    Triphenyl Compound A

    Others Cancer
    TPh A (Triphenyl Compound A) is a potent inhibitor of the nuclear protein pirin and binds specifically to pirin with a Ki of 0.6 uM. TPh A disrupts the formation of the bcl3–pirin complex. TPh A can be used as a novel small molecule tool to regulate pirin in cells.
  • HY-15827
    NSC 405020

    MMP Cancer
    NSC 405020 is a novel small molecule inhibitor of MT1-MMP that specifically targets PEX domain rather than the catalytic domain of MT1-MMP with IC50 >100 μM and does not inhibit the catalytic activity of MT1-MMP or MMP-2.
  • HY-125286

    CD73 Cancer
    AB-680 is highly potent, reversible and selective small molecule 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-16661
    Skp2 Inhibitor C1

    SKPin C1

    E1/E2/E3 Enzyme Cancer
    Skp2 Inhibitor C1(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation, selectively inhibited Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts.
  • HY-125176

    Bacterial Infection
    G907 is a selective small-molecule antagonist of ATP-binding cassette (ABC) transporter, MsbA. It inhibits purified E. coli MsbA in amphipols with an IC50 of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket. Bactericidal activity.
  • HY-124771

    Others Metabolic Disease
    RH01386 is a small molecule that can prevent ER stress-induced β cell dysfunction and death, and inhibits proapoptotic gene expression. RH01386 restores ER stress-impaired glucose-stimulated insulin secretion responses. RH01386 has the potential for type 2 diabetes treatment.
  • HY-12185

    Ribosomal S6 Kinase (RSK) Cancer Metabolic Disease
    BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells.
  • HY-129039
    Butyrolactone 3

    Histone Acetyltransferase Cancer
    Butyrolactone 3 is a specifical small-molecule inhibitor of the histone acetyltransferase Gcn5 (IC50=100 μM), which has a high affinity to the Gcn5 enzyme comparable to that of its natural substrate, histone H3. Butyrolactone 3 shows weak inhibitory on CBP (IC50=0.5 mM)
  • HY-128338

    CETP Cardiovascular Disease
    CETP-IN-3 (Compound 13) is an small molecule inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP. CETP-IN-3 for the CETP inhibitory activity in the scintillation proximity (SPA) and whole plasma assay (WPA) with IC50s of 0.002 μM and 0.06 μM, respectively.
  • HY-113965

    Hedgehog Smo Apoptosis Inflammation/Immunology
    CUR61414 is a novel, potent and cell permeable Hedgehog signaling pathway inhibitor (IC50 =100-200 nM). CUR61414 is a small-molecule aminoproline class compound and selectively binds to smoothened (Smo) with a Ki  value of 44 nM. CUR-61414 can induce apoptosis in cancer cells without affecting neighboring non-tumor cells.
  • HY-117259

    Amyloid-β Neurological Disease
    ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated prodrug of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound. ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease.
  • HY-117930


    Complement System Inflammation/Immunology
    Danicopan (ACH-4471), a selective and orally active small-molecule factor D inhibitor, shows high binding affinity to human Factor D with Kd value of 0.54 nM. Danicopan (ACH-4471) inhibits alternative pathway of complement (APC) activity, has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS).
  • HY-103046

    E1/E2/E3 Enzyme Inflammation/Immunology
    UbcH5c-IN-1 (compound 6d) is a potent and selective small-molecule inhibitor of Ubiquitin-conjugating enzyme UbcH5c, with a Kd of 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85. A promising lead compound for the development of new antirheumatoid arthritis (RA) agent.
  • HY-122611

    Androgen Receptor Apoptosis Cancer
    CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
  • HY-135813

    Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-128342
    Complement C5-IN-1

    Complement System Inflammation/Immunology
    Complement C5-IN-1 (Compound 7) is a small-molecule inhibitor of complement component 5 protein (C5). Complement C5-IN-1 interacts with C5 to prevent its cleavage by the C5 convertase and blocks zymosan-induced the membrane-attack complex (MAC) deposition in 50% human whole blood with an IC50 of 0.77 µM.
  • HY-16438

    Apoptosis Parasite Cancer Infection Inflammation/Immunology
    RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes drug resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity. RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α. RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity.
  • HY-19824

    Others Cancer
    3PO is a novel small-molecule inhibitor of the PFKFB3 isozyme, 3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μM) IC50 value Target: PFKFB3 isozyme in vitro: 3PO inhibits recombinant PFKFB3 activity, suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.
  • HY-16291

    LOR-253; LT-253

    c-Myc KLF Apoptosis Cancer Inflammation/Immunology
    APTO-253 (LOR-253) is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through induction of the Krüppel-like factor 4 (KLF4) tumor suppressor. APTO-253 has antiarthritic activity.
  • HY-120836

    DNA/RNA Synthesis Apoptosis Cancer
    AOH1160 is a potent, first-in-class, orally available small molecule proliferating cell nuclear antigen (PCNA) inhibitor, interferes with DNA replication, blocks homologous recombination-mediated DNA repair, causes cell-cycle arrest and induces apoptosis. AOH1160 selectively kills many types of cancer cells (mean GI50=330 nM) without causing significant toxicity to a broad range of nonmalignant cells.
  • HY-136348

    Bacterial Infection
    ML338 is a selective small molecule inhibitor probe of non-replicating Mycobacterium tuberculosis bacilli and is against the non-replicating M. tuberculosis with IC90 and IC99 values of 1 μM and 4 μM, respectively by CFU. ML338 is a invaluable tool for identifying both essential functions and vulnerabilities of the M. tuberculosis bacilli in the nutrient deprivation states. ML338 can be used for the study of M. tuberculosis chemotherapy.
  • HY-103045

    PKC ROCK Cardiovascular Disease
    CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure.
  • HY-12302

    9-Bromopaullone; NSC-664704

    CDK GSK-3 Cancer
    Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively. Kenpaullone, a small molecule inhibitor of KLF4, reduces self-renewal of breast cancer stem cells and cell motility in vitro.
  • 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-100513A

    Apoptosis DNA/RNA Synthesis Antibiotic Cancer
    Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM). Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis. Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo.
  • HY-N6800A
    Netropsin dihydrochloride

    DNA/RNA Synthesis Bacterial Influenza Virus Antibiotic Infection Inflammation/Immunology
    Netropsin (dihydrochloride) is a small-molecule MGB (minor-groove binder), inhibits the catalytic activity of isolated topoisomerase and interferes with the stabilization of the cleavable complexes of topoisomerase II and I in nuclei. Netropsin (dihydrochloride) has potential antibiotic and antiviral properties by binding to dsDNA in a non-intercalative manner, it improves survival from murine endotoxaemia by attenuating NOS2 induction through interference with HMGA1 DNA binding to the core NOS2 promoter. Netropsin (dihydrochloride) in solutions of DNA has radioprotective ability against radiation-induced damage due to its high binding affinity and high structural stabilization, hydroxyl radical (OH*) generated by ionizing radiation cannot radiolyse the netropsin-DNA complex.