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G9a/GLP covalent inhibitor

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-150510
    MS8511

    		Histone Methyltransferase Neurological Disease Cancer
    MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS) .
    MS8511
  • HY-156285
    ZZM-1220

    		Histone Methyltransferase Apoptosis Cancer
    ZZM-1220 is a histone lysine methyltransferase G9a/GLP covalent inhibitor with IC50s of of 458 nM and 924 nM, respectively. ZZM-1220 inhibits H3K9me2 in cells and significantly induces apoptosis of triple-negative breast cancer (TNBC) cells and blocks the cell cycle in the G2/M phase .
    ZZM-1220
  • HY-155020
    Antitumor agent-101

    		Histone Methyltransferase GLP Receptor Cancer
    Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model .
    Antitumor agent-101

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