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dual inhibitors

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1196

Inhibitors & Agonists

3

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4

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11

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4

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44

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31

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12

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-109108A
    Valemetostat tosylate
    4 Publications Verification

    DS-3201 tosylate

    Histone Methyltransferase Cancer
    Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC50 values <10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma .
    Valemetostat tosylate
  • HY-155195

    FLT3 Cancer
    FLT3/CHK-IN-1 (Compound 18) is a dual inhibitor of FLT3/CHK1. FLT3/CHK-IN-1 is more than 1700 times more selective to c-KI T and greatly reduces hERG affinity with an IC50 value of 58.4 μM. FLT3/CHK-IN-1 inhibits tumor growth in mouse xenotransplantation models inoculated with MV-4-11 cells .
    FLT3/CHK1-IN-1
  • HY-12652
    AZD3147
    1 Publications Verification

    mTOR Cancer
    AZD3147 is a potent, orally active, selective dual inhibitor of mTORC1 and mTORC2 with an IC50 value of 1.5 nM. AZD3147 also has a selective effect on PI3K .
    AZD3147
  • HY-119374
    BRM/BRG1 ATP Inhibitor-1
    30+ Cited Publications

    Epigenetic Reader Domain Cancer
    BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 µM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity .
    BRM/BRG1 ATP Inhibitor-1
  • HY-163787

    CDK Cancer
    YY173 is a dual inhibitor for CDK4 and CDK6 with IC50 of 7.7 and 88 nM. YY173 inhibits the proliferation of cell Jurkat with an IC50 of 1.46 μM. YY173 can be used for synthesis of PROTAC CDK4/6 degrader 1 (HY-163786) .
    YY173
  • HY-19373

    3DP-10017

    Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
    RWJ-445167
  • HY-101776

    Desmethyl-SB2343

    mTOR PI3K Cancer
    Desmethyl-VS-5584 is a dimethyl analog of VS-5584 which is an potent and selective mTOR/PI3K dual inhibitor with pyrido [2,3-d] pyrimidine structure .
    Desmethyl-VS-5584
  • HY-144824

    Cytochrome P450 Monoamine Oxidase Neurological Disease Cancer
    Monoamine oxidase/Aromatase-IN-1 (compound 2q) is a highly potent monoamine oxidase (MAO) and aromatase dual inhibitor with IC50s of 39 nM and 31 nM for MAO-B and aromatase, respectively. Monoamine oxidase/Aromatase-IN-1 can be used for researching neurological disorder and breast cancer .
    Monoamine oxidase/Aromatase-IN-1
  • HY-158763

    TG0205221

    SARS-CoV Cathepsin Virus Protease Infection
    MPI8 (TG0205221) is an inhibitor of the major protease of SARS-CoV-2 (MPro) with high antiviral activity. MPI8 exerts its antiviral effect by dual and selective inhibition of SARS-CoV-2 MPro and host cell cysteine protease L (cathepsin L). This dual inhibition enhanced the overall antiviral potency and effect of MPI8. MPI8 can be used in clinical studies of COVID-19 .
    MPI8
  • HY-158264

    Serotonin Transporter Endocrinology
    SNRI-IN-1 (Compound 7a) is a dual serotonin and noradrenaline monoamine reuptake inhibitor, P-glycoprotein Efflux Ratio is 20 .
    SNRI-IN-1
  • HY-174319

    Amylases Glycosidase Metabolic Disease
    α-Amylase/α-Glucosidase-IN-20 (Compound 6b) is a dual inhibitor of α-Amylase and α-Glucosidase with IC50s of 414.57 and 924.15 μM for α-Amylase and α-Glucosidase, respectively. α-Amylase/α-Glucosidase-IN-20 shows a potent anti-diabetic activity, promising for diabetes research .
    α-Amylase/α-Glucosidase-IN-20
  • HY-147922

    Carbonic Anhydrase Inflammation/Immunology
    hCAI/II-IN-2 (compound 2b) is a potent dual hCA I/II inhibitor with Ki values of 40.97, 15.15 and 61.88 nM for hCA I, hCA II and hCA Ⅸ. hCAI/II-IN-2 possesses anti-hypoxic activity against acute mountain sickness (AMS) and low cellular activity .
    hCAI/II-IN-2
  • HY-147923

    Carbonic Anhydrase Inflammation/Immunology
    hCAI/II-IN-3 (compound 5b) is a potent dual hCA I/II inhibitor with Ki values of 51.25, 13.15 and 42.18 nM for hCA I, hCA II and hCA Ⅸ. hCAI/II-IN-3 possesses anti-hypoxic activity against acute mountain sickness (AMS) and low cellular activity .
    hCAI/II-IN-3
  • HY-155161

    Lipoxygenase COX Inflammation/Immunology
    COX-2/15-LOX-IN-4 (compound 5i) is a dual inhibitor of COX-2/15-LOX with IC50s of 0.075 μM and 1.97 μM, respectively. COX-2/15-LOX-IN-4 can inhibit LPS-induced cell production of promoting cytokines (IL-6, ROS) with specific anti-inflammatory activity .
    COX-2/15-LOX-IN-4
  • HY-155160

    Lipoxygenase COX Inflammation/Immunology
    COX-2/15-LOX-IN-3 (compound 5k) is a dual inhibitor of COX-2/15-LOX with IC50s of 0.075 μM and 1.97 μM, respectively. COX-2/15-LOX-IN-3 can inhibit LPS-induced cell production of promoting cytokines (IL-6, ROS, and NO), with specific anti-inflammatory activity .
    COX-2/15-LOX-IN-3
  • HY-151211

    Btk Inflammation/Immunology Cancer
    BTK-IN-16 is a dual inhibitor of BTK wild type and C481S mutant of Bruton’s tyrosine kinase (BTK) with IC50s of 5.1 and 4.1 μM. BTK-IN-16 can be used for the research of autoimmune diseases and chronic lymphocytic leukemia .
    BTK-IN-16
  • HY-155493

    Cytochrome P450 Cancer
    CYP19A1/CYP11B2-IN-1 (Compound X21) is a potent and selective aromatase and aldosterone synthase dual inhibitor with IC50s of 2.3 nM and 29 nM for aromatase (CYP19A1) and aldosterone synthase (CYP11B2), respectively. CYP19A1/CYP11B2-IN-1 has excellent antiproliferative and pro-apoptotic activity against the cancer cell. CYP19A1/CYP11B2-IN-1 can be used for research of breast cancer .
    CYP19A1/CYP11B2-IN-1
  • HY-168088

    HDAC DNA Methyltransferase Cancer
    DNMT1/HDAC-IN-1 (compound (R)-23a) is a DNMT1/HDAC dual inhibitor (HDAC1:IC50=0.05 μM), HDAC1 is a major HDAC isoform that interacts with DNMT1 in multiple protein complexes for transcriptional silencing of TSGs. DNMT1/HDAC-IN-1 can reshape the tumor immune microenvironment and induce tumor regression, and effectively reverse cancer-specific epigenetic abnormalities .
    DNMT1/HDAC-IN-1
  • HY-115904

    CDK FLT3 Cancer
    FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo .
    FLT3/CDK4-IN-1
  • HY-156094

    HDAC Histone Demethylase Apoptosis Cancer
    JMJD3/HDAC-IN-1 (compound A5b) is a dual inhibitor targeting Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylase (HDAC1, IC50=16 nM). JMJD3/HDAC-IN-1 promotes hypermethylation of histone H3K27 and hyperacetylation of H3K9, and also cleaves caspase-7 and PARP to induce apoptosis. JMJD3/HDAC-IN-1 effectively inhibits cancer cell cloning, migration, and invasion .
    JMJD3/HDAC-IN-1
  • HY-150774

    HDAC HSP Apoptosis Cancer
    HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor of HDAC6 and Hsp90, with IC50s of 105.7 and 61 nM, respectively. HDAC6/HSP90-IN-2 can be used for the research of cancer .
    HDAC6/HSP90-IN-2
  • HY-15496

    ER-806201

    MEK FLT3 Cancer
    E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC50 value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC50 value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC50 value of 19 nM. Anti-tumor and anti-psoriasis efficacy .
    E6201
  • HY-149016

    Microtubule/Tubulin Farnesyl Transferase Cancer
    Tubulin polymerization-IN-25 (compound 17f) is a dual inhibitor of tubulin polymerization and farnesyl transferase (FTase) with IC50s of 1.11 μM and 0.39 μM, respectively. Tubulin polymerization-IN-25 displays cytotoxicity and excellent antitumor activity .
    Tubulin polymerization-IN-25
  • HY-144806
    PI3K/AKT-IN-1
    10+ Cited Publications

    PI3K Akt Apoptosis Cancer
    PI3K/AKT-IN-1 is an effective PI3K/AKT dual inhibitor (IC50 of 6.99, 4.01 and 3.36 μM for PI3Kγ, PI3Kδ and AKT, respectively). PI3K/AKT-IN-1 has anticancer activity and acts by inhibiting PI3K/AKT axis and inducing caspase 3 dependent apoptosis .
    PI3K/AKT-IN-1
  • HY-143402

    Topoisomerase Cancer
    Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer .
    Topoisomerase I/II inhibitor 2
  • HY-162061

    Monoamine Oxidase Neurological Disease
    ChEs/MAOs-IN-1 (Compound 4i) is a dual inhibitor of cholinesterases (ChEs) and monoamine oxidases (MAOs).ChEs/MAOs-IN-1 has IC50 values of 0.048 μM, 0.89 μM, 3.58 μM, and 0.095 μM for AChE, BChE, MAO-B and MAO-B respectively. ChEs/MAOs-IN-1 can be used in the study of neurodegenerative diseases .
    ChEs/MAOs-IN-1
  • HY-B0703

    BIA 2-093

    Beta-secretase Sodium Channel Neurological Disease
    Eslicarbazepine acetate (BIA 2-093), an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
    Eslicarbazepine acetate
  • HY-175292

    EGFR Microtubule/Tubulin Cancer
    EGFR WT/T790M-IN-3 is an irreversible covalent EGFR WT and EGFR T790M inhibitor with IC50s value of 28.1 and 24.6 nM. EGFR WT/T790M-IN-3 hampers tubulin polymerization through IC50 value of 5.1 μM. EGFR WT/T790M-IN-3 shows significant anti-proliferative effects on HCT116 and T47D cells, with IC50 values of 3.12 and 4.12 μM, respectively. EGFR WT/T790M-IN-3 can be used for the study of cancers such as non-small cell lung cancer, colon cancer and breast cancer .
    EGFR WT/T790M-IN-3
  • HY-169400

    HDAC Histone Methyltransferase Apoptosis Cancer
    HDACs/EZH2-IN-1 (Compound 22a) is a HDACs/EZH2 inhibitor (EZH2 Y641N inhibition rate at 50 nM: 98%), with selective inhibition against HDAC1 and HDAC6 (IC50: 0.23 μM and 0.07 μM, respectively). HDACs/EZH2-IN-1 exerts a antiproliferative effect on diffuse large B-cell lymphoma cells harboring an EZH2 mutation and on various acute myeloid leukemia cells. HDACs/EZH2-IN-1 has the ability to induce cell differentiation and Apoptosis .
    HDACs/EZH2-IN-1
  • HY-151885

    Cholinesterase (ChE) Monoamine Oxidase Neurological Disease
    Dual AChE-MAO B-IN-3 (compound C10) is a potent dual AChE/MAO-B inhibitior, with IC50 values of 0.58 and 0.41 μM, respectively. Dual AChE-MAO B-IN-3 is a dual-binding inhibitor bound to both the catalytic anionic site and peripheral anionic site of AChE. Dual AChE-MAO B-IN-3 can be used for Alzheimer’s disease (AD) research .
    Dual AChE-MAO B-IN-3
  • HY-139950
    Rasarfin
    1 Publications Verification

    Ras Cancer
    Rasarfin is a dual Ras and ARF6 inhibitor .
    Rasarfin
  • HY-129426

    Akt Cancer
    PDK1/Akt/Flt dual pathway inhibitor is one of a component of KP372-1 (HY-15673 ), and inhibits PDK1/Akt/Flt dual pathway .
    PDK1/Akt/Flt dual pathway inhibitor
  • HY-144738

    Epoxide Hydrolase FAAH Inflammation/Immunology
    Dual FAAH/sEH-IN-1 (compound 3) is a high affinity dual sEH (soluble epoxide hydrolase) and FAAH (fatty acid amide hydrolase) inhibitor, with IC50 values of 9.6 and 7 nM, respectively. Dual FAAH/sEH-IN-1 shows antinociception against the inflammatory phase .
    Dual FAAH/sEH-IN-1
  • HY-173326

    STING Inflammation/Immunology
    STING-IN-14 is an inhibitor of STING (IC50: 0.6 nM). STING-IN-14 inhibits the activation of the IRF pathway in THP1-Dual TM cells. STING-IN-14 can be used in autoimmune diseases research .
    STING-IN-14
  • HY-114937

    BIA 2-059; (R)-Licarbazepine acetate

    Beta-secretase Sodium Channel Neurological Disease
    (R)-Eslicarbazepine acetate (BIA 2-059) is the R-enantiomer of Eslicarbazepine acetate (HY-B0703). Eslicarbazepine acetate is an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel .
    (R)-Eslicarbazepine acetate
  • HY-101017R

    Reference Standards Endogenous Metabolite Akt Calcium Channel Inflammation/Immunology Cancer
    Eslicarbazepine acetate (Standard) is the analytical standard of Eslicarbazepine acetate. This product is intended for research and analytical applications. Eslicarbazepine acetate (BIA 2-093), an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
    Palmitoylcarnitine chloride (Standard)
  • HY-B0703R

    BIA 2-093 (Standard)

    Reference Standards Beta-secretase Sodium Channel Neurological Disease
    Eslicarbazepine acetate (Standard) is the analytical standard of Eslicarbazepine acetate. This product is intended for research and analytical applications. Eslicarbazepine acetate (BIA 2-093), an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
    Eslicarbazepine acetate (Standard)
  • HY-145708

    Cholinesterase (ChE) Monoamine Oxidase Neurological Disease
    Dual AChE-MAO B-IN-2 is a potent AChE and MAO B dual inhibitor with IC50s of 0.12 µM and 0.01 µM for b>AChE and MAO B, respectively. Dual AChE-MAO B-IN-2 has the potential for the research of Alzheimer’s disease .
    Dual AChE-MAO B-IN-2
  • HY-170543

    Galectin EGFR Apoptosis Inflammation/Immunology
    Dual Galectin-3/EGFR-IN-1 (Compound 29) is the dual inhibitor for Galectin-3 and EGFR with the KD of 52.29 μM and 3.31 μM. Dual Galectin-3/EGFR-IN-1 inhibits TGF-β-induced hepatic stellate cell (HSCs) activation, induces apoptosis in LX-2 cell, and exhibits anti-liver fibrotic efficacy .
    Dual Galectin-3/EGFR-IN-1
  • HY-B0703S

    BIA 2-093-d4

    Beta-secretase Sodium Channel Isotope-Labeled Compounds Neurological Disease
    Eslicarbazepine acetate-d4 is deuterated labeled Eslicarbazepine acetate (HY-B0703). Eslicarbazepine acetate (BIA 2-093), an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
    Eslicarbazepine acetate-d4
  • HY-W744263

    Isotope-Labeled Compounds Beta-secretase Sodium Channel Neurological Disease
    Eslicarbazepine Acetate-d3 is the deuterium labeled Eslicarbazepine acetate (HY-B0703). Eslicarbazepine acetate (BIA 2-093), an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
    Eslicarbazepine Acetate-d3
  • HY-158695

    Cholinesterase (ChE) Monoamine Oxidase Neurological Disease
    Dual AChE-MAO B-IN-4 (compound 7) is a dual AChE/MAO-B inhibitor, with IC50 values ​​of 261 nM and 15 nM, respectively. Dual AChE-MAO B-IN-4 protects against oxidative damage induced by H2O2 and 6-OHDA in SH-SY5Y cells. Dual AChE-MAO B-IN-4 can penetrate the central nervous system in a cell model that mimics the blood-brain barrier. Dual AChE-MAO B-IN-4 can be used in the study of neurological diseases such as Alzheimer's disease (AD) .
    Dual AChE-MAO B-IN-4
  • HY-115875

    Lactate Dehydrogenase Metabolic Disease
    LDHA-IN-5 is a novel, potent, dual GO/LDHA inhibitor for primary hyperoxaluria.
    LDHA-IN-5
  • HY-18208
    Omapatrilat
    2 Publications Verification

    BMS-186716

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Omapatrilat is a dual inhibitor of the metalloproteases ACE and NEP with Ki values of 0.64 and 0.45 nM, respectively.
    Omapatrilat
  • HY-114332

    MAP3K Neurological Disease
    GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK) .
    GNE-8505
  • HY-13758

    BMS-247615

    Topoisomerase Cancer
    TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
    TAS-103
  • HY-13758A
    TAS-103 dihydrochloride
    1 Publications Verification

    BMS-247615 dihydrochloride

    Topoisomerase Cancer
    TAS-103 dihydrochloride is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
    TAS-103 dihydrochloride
  • HY-115851

    Endogenous Metabolite Neurological Disease
    Demethyl PL265 is an enduring dual ENKephalinase inhibitor (DENKi) that holds promise for pain relief.
    Demethyl PL265
  • HY-175294

    PD-1/PD-L1 NAMPT Cancer
    PD-L1/Nampt-IN-1 is an orally active inhibitor that simultaneously target PD-L1 and NAMPT (nicotinamide phosphoribosyltransferase) with IC50s value of 63 nM and 582 nM. PD-L1/Nampt-IN-1 demonstrates cross-species affinity with comparable KD values for hPD-L1 (52.6 nM) and mPD-L1 (49.1 nM), respectively. PD-L1/Nampt-IN-1 effectively inhibits tumor growth by activating the tumor immune microenvironment. PD-L1/Nampt-IN-1 can be used for the study of melanoma .
    PD-L1/Nampt-IN-1
  • HY-16273A
    L-778123 hydrochloride
    4 Publications Verification

    Farnesyl Transferase Cancer
    L-778123 hydrochloride is a dual inhibitor of FPTase and GGPTase-I, with IC50 values of 2 nM and 98 nM respectively.
    L-778123 hydrochloride

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