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Selective inhibition

" in MedChemExpress (MCE) Product Catalog:

692

Inhibitors & Agonists

5

Screening Libraries

5

Fluorescent Dyes

3

Biochemical Assay Reagents

11

Peptides

5

Inhibitory Antibodies

39

Natural
Products

33

Isotope-Labeled Compounds

7

Click Chemistry

5

Oligonucleotides

1

GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15979
    H-89
    175+ Cited Publications

    PKA Autophagy Neurological Disease
    H-89 is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase, and others kinases.
    H-89
  • HY-15979A
    H-89 dihydrochloride
    175+ Cited Publications

    PKA Autophagy Others
    H-89 dihydrochloride is a potent and selective inhibitor of protein kinase A (PKA) with an IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase.
    H-89 dihydrochloride
  • HY-15418
    RS 504393
    25+ Cited Publications

    CCR Inflammation/Immunology Endocrinology
    RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively).
    RS 504393
  • HY-139664
    GSK-3685032
    10+ Cited Publications

    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 .
    GSK-3685032
  • HY-13909
    RGFP966
    50+ Cited Publications

    HDAC Cancer
    RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM. RGFP966 can penetrate the blood brain barrier (BBB).
    RGFP966
  • HY-107361
    Golidocitinib
    2 Publications Verification

    AZD4205

    JAK Cancer
    Golidocitinib (AZD4205) is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2 (IC50>14.7 μM), and shows little inhibition on JAK3 (IC50>30 μM) .
    Golidocitinib
  • HY-15663
    IPA-3
    15+ Cited Publications

    PAK Cancer
    IPA-3 is a selective non-ATP competitive PAK1 inhibitor with IC50 of 2.5 μM, and shows no inhibition to group II PAKs (PAKs 4-6).
    IPA-3
  • HY-12299
    WH-4-023
    5 Publications Verification

    Dual LCK/SRC inhibitor

    Src Cancer
    WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38α and KDR.
    WH-4-023
  • HY-131922

    Tetraisopropyl pyrophosphoramide

    Cholinesterase (ChE) Neurological Disease
    Iso-OMPA (Tetraisopropyl pyrophosphoramide) is a selective inhibitor of the irreversible butyrylcholinesterase (BuChE). Iso-OMPA enhances soman toxicity in rats associated with the inhibition of plasma carboxylesterase (CarbE) .
    Iso-OMPA
  • HY-108431
    MN58b
    1 Publications Verification

    Apoptosis Cancer
    MN58b is a selective choline kinase α (CHKα) inhibitor, and results in inhibition of phosphocholine synthesis. MN58b reduces cell growth through the induction of apoptosis, and also has antitumoral activity .
    MN58b
  • HY-134904
    RMC-6272
    3 Publications Verification

    RM-006

    mTOR Cancer
    RMC-6272 (RM-006) is a bi-steric mTORC1-selective inhibitor. RMC-6272 exhibits potent and selective (> 10-fold) inhibition of mTORC1 over mTORC2. RMC-6272 shows improved inhibition of mTORC1 in comparison to Rapamycin, and induces more cell death in TSC2 null tumors .
    RMC-6272
  • HY-103182

    Adenosine Receptor Others
    PSB-1115 is a selective A2B Adenosine Receptor antagonist. PSB-1115 inhibits the 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced contraction inhibition of acetylcholine (ACh) .
    PSB-1115
  • HY-100585

    Splitomycin

    HDAC Cancer
    Splitomicin (Splitomycin) is a selective Sir2p inhibitor. Splitomicin inhibits NAD +-dependent HDAC activity of Sir2 protein. Splitomicin induces dose-dependent inhibition of HDAC in the yeast extract with an IC50 of 60 μM .
    Splitomicin
  • HY-15687A
    SAR407899
    3 Publications Verification

    ROCK Metabolic Disease
    SAR407899 is a selective, potent and ATP-competitive ROCK inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively. SAR407899 shows stable inhibition of migrasome formation.
    SAR407899
  • HY-N1377

    Lysionotin

    Carboxylesterase (CES) DNA/RNA Synthesis Apoptosis Bacterial Infection Metabolic Disease Inflammation/Immunology Endocrinology Cancer
    Nevadensin (Lysionotin), a natural flavonoid, is a selective human carboxylesterase 1 (hCE1) inhibitor with an IC50 of 2.64 μM. Nevadensin is more selective for hCE1 than hCE2 (IC50 of 132.8 μM). Nevadensin can induce apoptosis and DNA damage in cancer cells. Nevadensin has a variety of pharmacological effects such as anti-inflammatory, anti-tumour, anti-hypertensive, anti-tubercular, antitussive, antioxidant and anti-microbial activities .
    Nevadensin
  • HY-12960

    FLT3-​IN-​1

    FLT3 c-Kit Apoptosis Cancer
    SKLB4771 is a potent and selective Flt3 inhibitor with an IC50 value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue .
    SKLB4771
  • HY-14719
    RO4987655
    5+ Cited Publications

    CH4987655

    MEK Cancer
    RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM for inhibition of MEK1/MEK2.
    RO4987655
  • HY-104013
    Aminopurvalanol A
    1 Publications Verification

    CDK Apoptosis Cancer
    Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization .
    Aminopurvalanol A
  • HY-147655

    RIO Kinase Cancer
    CQ211 is a potent and selective RIOK2 inhibitor with a Kd of 6.1 nM. CQ211 exhibits potent proliferation inhibition activity against multiple cancer cell lines .
    CQ211
  • HY-148949

    Kallikrein Others
    Kallikrein 5-IN-2 (compound 21) is a selective Kallikrein KLK5 inhibitor (pIC50=7.1). KLK5 inhibition may normalise epidermal shedding and reduce the associated inflammation and itching .
    Kallikrein 5-IN-2
  • HY-16965
    TH287
    3 Publications Verification

    DNA/RNA Synthesis Cancer
    TH287 is a potent and selective inhibitor of MTH1, with an IC50 of 0.8 nM. TH287 is highly selective towards MTH1, with no relevant inhibition of MTH2, NUDT5, NUDT12, NUDT14, NUDT16, dCTPase, dUTPase and ITPA at 100 μM. TH287 could act as a chemotherapeutic agent for cancer research .
    TH287
  • HY-112082
    BAY885
    1 Publications Verification

    ERK Cancer
    BAY885, a chemical probe, is a highly potent and selective ERK5 inhibitor with an IC50 of 35 nM. BAY885 shows weak inhibition on others kinases .
    BAY885
  • HY-12089

    CP-529414

    CETP Endocrinology
    Torcetrapib (CP-529414) is a selective, potent cholesteryl ester transfer protein (CETP) inhibitor. A typical inhibition curve for whole human plasma, having a CETP concentration of 37 nM .
    Torcetrapib
  • HY-108530

    RAR/RXR Cancer
    MM11253 is a potent and selective RARγ antagonist with an IC50 of 44 nM. MM11253 has lower inhibition of RARα, RARβ and RXRα. MM11253 blocks the growth inhibitory effects of RARγ-selective agonists .
    MM11253
  • HY-119649

    IKI220

    Environmental Pollutants Parasite Infection
    Flonicamid (IKI220) is a novel systemic insecticide with selective activity against hemipterous pests. The main insecticidal mechanism of flonicamid is starvation based on the inhibition of stylet penetration to plant tissues .
    Flonicamid
  • HY-145072

    CDK Cancer
    BSJ-01-175 is a potent and selective CDK12/13 covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells .
    BSJ-01-175
  • HY-123785
    ORM-10962
    3 Publications Verification

    Na+/Ca2+ Exchanger Metabolic Disease
    ORM-10962 is a potent, highly selective sodium-calcium exchanger (NCX) inhibitor, with IC50 values of 67 and 55 nM for the reverse and forward mode inhibition, respectively. ORM-10962 shows antiarrhythmic effect .
    ORM-10962
  • HY-117960

    LEO-32731

    Phosphodiesterase (PDE) Inflammation/Immunology
    Orismilast (LEO-32731) is an orally active and selective PDE4 inhibitor used for the research of inflammatory diseases. Orismilast demonstrates potent inhibition of PDE4B and PDE4D subtype splice variants .
    Orismilast
  • HY-116506

    RAR/RXR Reactive Oxygen Species (ROS) Apoptosis Autophagy Cancer
    Bigelovin, a sesquiterpene lactone isolated from Inula hupehensis, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation .
    Bigelovin
  • HY-10949

    E1/E2/E3 Enzyme Cancer
    SMER3, a Rapamycin enhancer, is a selective Skp1-Cullin-F-box (SCF) Met30 ubiquitin ligase inhibitor. SMER3 enhances Rapamycin's growth inhibitory effect by inhibition of SCF Met30 .
    SMER3
  • HY-15546

    CCR Inflammation/Immunology
    BMS-817399 is a potent, selective, and orally bioavailable CCR1 antagonist. BMS-817399 exhibits CCR1 binding affinity and chemotaxis inhibition potencies of 1 and 6 nM (IC50), respectively. BMS-817399 can be used for the research of rheumatoid arthritis .
    BMS-817399
  • HY-12528

    Dipeptidyl Peptidase Metabolic Disease
    DBPR108 is a potent, selective, and orally bioavailable dipeptide-derived inhibitor of DPP4 with IC50 of 15 nM; no inhibition on DDP8 and DPP9.
    DBPR108
  • HY-108488

    Src Cancer
    KB SRC 4 is a potent, and highly selective c-Src inhibitor, with a Ki of 44 nM and a Kd of 86 nM, and shows no inhibition on c-Abl up to 125 μM; KB SRC 4 has antitumor activity.
    KB SRC 4
  • HY-14197
    Clorgyline
    5+ Cited Publications

    M&B 9302

    Monoamine Oxidase Neurological Disease
    Clorgyline (M&B 9302) is an orally active, blood-brain barrier permeable and selective monoamine oxidase A (MAO-A) inhibitor. Clorgyline's selective inhibition of MAO-A leads to reduced metabolism of neurotransmitters such as serotonin (5-hydroxytryptamine), which accumulates in the brain. Clorgyline can be used in the study of depression and neurodegenerative diseases .
    Clorgyline
  • HY-132310

    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 .
    MAGL-IN-4
  • HY-156406
    PITCOIN4
    1 Publications Verification

    PI3K Inflammation/Immunology
    PITCOIN4 is a highly selective Class II Alpha PI3K-C2α inhibitor. PITCOIN4 shows nanomolar inhibition of PI3K-C2α and >100-fold selectivity in a general kinase panel .
    PITCOIN4
  • HY-139664A

    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 .
    (R)-GSK-3685032
  • HY-130199

    Parellic acid

    Others Metabolic Disease
    Psoromic acid is a potent and selective RabGGTase (Rab geranylgeranyl transferase) inhibitor with an IC50 value of 1.3 µM. Psoromic acid is an antioxidative agent. Psoromic acid exhibits a competitive type of HMGR inhibition and mixed type of ACE (angiotensin converting enzyme) inhibition .
    Psoromic acid
  • HY-139001

    Glutathione Peroxidase Ferroptosis Others
    JKE-1716 is a potent and selective nitrolic acid-containing GPX4 inhibitor. JKE-1716 is able of inducing ferroptosis selectively through covalent GPX4 inhibition .
    JKE-1716
  • HY-132808

    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 .
    Atuzabrutinib
  • HY-115909

    CDK Cancer
    ZDLD20, a β-carboline, is orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 6.51  μM. ZDLD20 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD20 exhibits potent anticancer activity .
    ZDLD20
  • HY-108579

    Potassium Channel Cardiovascular Disease
    UCL 1684 (dibromide) is a first nanomolar, non-peptidic small conductance calcium-activated potassium (SK) channel blocker. UCL 1684 (dibromide) is effective in preventing the development of atrial fibrillation due to potent atrial-selective inhibition of INa. UCL 1684 (dibromide) causes atrial-selective prolongation of ERP secondary to induction of postrepolarization refractoriness .
    UCL 1684 dibromide
  • HY-N3035
    Tetrahydroepiberberine
    1 Publications Verification

    Fungal Influenza Virus Infection
    Tetrahydroepiberberine is a isoquinoline alkaloid isolated from Corydalis impatiens (Pall). Tetrahydroepiberberine has antifungal and selective inhibition against the PI-3 virus activities .
    Tetrahydroepiberberine
  • HY-116482

    Herbicide Others
    Desmedipham is a selective systemic phenyl-carbamate herbicide. Desmedipham acts by disrupting CO2 fixation and the production of intermediary energy components-ATP and NADPH2 and inhibition of Hill reaction .
    Desmedipham
  • HY-170360

    AMPK JAK Cancer
    UCB9386 is the selective and brain penetrant inhibitor for Nuak1 with a pIC50 of 10.1. UCB9386 inhibits Nuak2 and Kak2 with an inhibition rate of ca. 50% at 10 nM .
    UCB9386
  • HY-101436A

    CK-1752 hydrochloride

    Potassium Channel Cardiovascular Disease
    Sematilide hydrochloride (CK-1752 hydrochloride) is a selective IKr channel blocker. Sematilide causes a concentration-dependent inhibition of the delayed rectifier K + current (IC50=25 μM). Sematilide is a class III antiarrhythmic agent .
    Sematilide hydrochloride
  • HY-121242

    VEL-5026

    Photosystem II Others
    Buthidazole is a selective herbicide for weed control in corn. Buthidazole inhibits photosynthetic electron transport at two distinct sites in the photosynthetic electron transport chain. The major site of inhibition was on the reducing side of photosystem II. Another site of electron transport inhibition is on the oxidizing side of photosystem II. Buthidazole inhibits corn photosynthesis and prevents starch accumulation in bundle sheath chloroplasts and some ultrastructural disruption of mesophyl chloroplasts of corn plants .
    Buthidazole
  • HY-122369

    Carboxypeptidase Metabolic Disease
    Histargin is a selective carboxypeptidase B inhibitor with an IC50 of 17 μg/mL and a Ki of 30 μM. Histargin exerts competitive inhibition with substrate, with inhibitory activity abolished by metal cations. Histargin shows no significant inhibitory activity against carboxypeptidase A, aminopeptidase A, or aminopeptidase B .
    Histargin
  • HY-147986

    Carbonic Anhydrase Cancer
    hCA I-IN-2 (Compound 6d) is a selective human carbonic anhydrase I (hCA I) inhibitor with Ki values of 18.8, 375.1, 1721 and 283.9 nM against hCA I, hCA II, hCAIX and hCAXII, respectively .
    hCA I-IN-2
  • HY-147985

    Carbonic Anhydrase Cancer
    hCA I-IN-1 (Compound 6q) is a human carbonic anhydrase I (hCA I) inhibitor with Ki values of 38.3, 716.4, 940.1 and 192.8 nM against hCA I, hCA II, hCAIX and hCAXII, respectively .
    hCA I-IN-1

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