MS8511 is a selective, irreversible inhibitor of G9a and GLP that covalently targets a cysteine residue within the substrate binding site. It demonstrates IC50 values of 100 nM for G9a and 140 nM for GLP, with Kd values of 44 nM and 46 nM, respectively. MS8511 effectively decreases cellular levels of H3K9me2 and enhances antiproliferative activity, making it a valuable tool for researching various cancers, including brain, breast, ovarian, lung, bladder, melanoma, and colorectal cancers, as well as conditions such as Alzheimer’s disease, sickle cell disease, and Prader−Willi syndrome.
MS8511 is a selective, irreversible inhibitor of G9a and GLP that covalently targets a cysteine residue within the substrate binding site. It demonstrates IC50 values of 100 nM for G9a and 140 nM for GLP, with Kd values of 44 nM and 46 nM, respectively. MS8511 effectively decreases cellular levels of H3K9me2 and enhances antiproliferative activity, making it a valuable tool for researching various cancers, including brain, breast, ovarian, lung, bladder, melanoma, and colorectal cancers, as well as conditions such as Alzheimer’s disease, sickle cell disease, and Prader−Willi syndrome.
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