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G9A+inhibitor

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12583
    A-366
    Maximum Cited Publications
    6 Publications Verification

    		 Histone Methyltransferase Epigenetic Reader Domain Cancer
    A-366, a chemical probe, is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families .
    A-366
  • HY-13808
    UNC 0631
    5 Publications Verification

    		 Histone Methyltransferase Cancer
    UNC 0631 is a potent histone methyltransferase G9a inhibitor with an IC50 of 4 nM. UNC 0631 potently reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 25 nM .
    UNC 0631
  • HY-10929
    UNC0224
    2 Publications Verification

    		 Histone Methyltransferase Cancer
    UNC0224 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 2.6 nM, an IC50 of 15 nM and a Kd of 23 nM. UNC0224 also potently inhibits b>GLP with assay-dependent IC50 values of 20-58 nM. UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E .
    UNC0224
  • HY-16705
    BRD4770
    5 Publications Verification

    		 Histone Methyltransferase Cancer
    BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC50 of 5 μM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence .
    BRD4770
  • HY-10930
    UNC0321
    2 Publications Verification

    		 Histone Methyltransferase GCGR Apoptosis Cancer
    UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 63 pM and with assay-dependent IC50 values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC50 values of 15-23 nM. UNC0321 has anti-apoptotic activity and has potential application in diabetic vascular complications .
    UNC0321
  • HY-15647
    BRD9539
    1 Publications Verification

    		 Histone Methyltransferase Cancer
    BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1 .
    BRD9539
  • HY-13807
    UNC0646
    1 Publications Verification

    		 Histone Methyltransferase Cancer
    UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC50 of 6 nM. UNC0646 is also a potent GLP inhibitor (IC50 <15 nM) and highly selective for G9a/GLP over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 26 nM .
    UNC0646
  • HY-13808R
    UNC 0631 (Standard)

    		Reference Standards Histone Methyltransferase Cancer
    UNC 0631 (Standard) is the analytical standard of UNC 0631. This product is intended for research and analytical applications. UNC 0631 is a potent histone methyltransferase G9a inhibitor with an IC50 of 4 nM. UNC 0631 potently reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 25 nM .
    UNC 0631 (Standard)
  • HY-178378
    G9a-IN-4

    		Histone Methyltransferase GLP Receptor Reactive Oxygen Species (ROS) Autophagy Apoptosis Cancer
    G9a-IN-4 is a G9a inhibitor with high selectivity (IC50 = 32 nM). G9a-IN-4 shows high selectivity against the other tested lysine/arginine methyltransferases. G9a-IN-4 exhibits high enzymatic activity against G9a and more potent antiproliferative effects against all tested cancer cells. G9a-IN-4 significantly suppresses the H3K9me2 level. G9a-IN-4 triggers autophagy by inducing the production of ROS, thus leading to cell apoptosis and cell cycle arrest at G0/G1 in CT26 colon cells. G9a-IN-4 can be used for the study of colon cancer .
    G9a-IN-4
  • HY-133031
    CSV0C018875

    		Histone Methyltransferase Cancer
    CSV0C018875 is a quinoline-based EHMT2/G9a inhibitor. CSV0C018875 exhibits lesser cytotoxicity than BIX-01294 .
    CSV0C018875
  • HY-172894
    G9a-IN-3

    		Histone Methyltransferase Cardiovascular Disease Cancer
    G9a-IN-3 (compound 16g) is a potent G9a inhibitor with an IC50 of 0.002 μM. G9a-IN-3 can be used in the study of sickle cell disease .
    G9a-IN-3
  • HY-152775A
    RK-0133114

    		Histone Methyltransferase Metabolic Disease
    RK-0133114 is a G9a inhibitor and a R-enantiomer of RK-701 (HY-152775). RK-0133114 inhibits G9a with an IC50 value of 3.7 μM. RK-0133114 can be used for the research of sickle cell disease (SCD) .
    RK-0133114
  • HY-146285
    LSD1-IN-20

    		Histone Demethylase Histone Methyltransferase Cancer
    LSD1-IN-20 (compound 1) is a potent dual non-covalent LSD1/G9a inhibitor, with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.51 and 1.60 μM, respectively .
    LSD1-IN-20
  • HY-133031A
    CSV0C018875 hydrochloride

    		Histone Methyltransferase Others
    CSV0C018875 hydrochloride is a G9a (EHMT2) inhibitor that inhibits G9a activity. CSV0C018875 can effectively inhibit G9a activity in both enzyme and cell-based assays, and its toxicity is much lower than that of the known G9a inhibitor BIX-01294. CSV0C018875 binds tightly to the active site cavity of G9a, thereby improving the binding firmness and prolonging the residence time of the compound, further enhancing the inhibitory effect of G9a. CSV0C018875 has the potential to improve its ADME (absorption, distribution, metabolism and excretion) and pharmacodynamic properties through further optimization .
    CSV0C018875 hydrochloride

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