| Hazard Information | Back Directory | [Description]
MS453 is a potent and selective SETD8 inhibitor. MS453 specifically modifies a cysteine residue near the inhibitor binding site, has an IC50 value of 804 nM, reacts with SETD8 with nearquantitative yield, and is selective for SETD8 against 28 other methyltransferases. SETD8 (also known as SET8, R-SET7, or KMT5A) is the only methyltransferase known to catalyze monomethylation of histone H4 lysine 20 (H4K20). SETD8 inhibitors could be valuable anticancer agents. |
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