SUV420H1/H2 lysine methyltransferase inhibitor / A-196 (1982372-88-2) is a potent and selective (over 29 other methyltransferases) inhibitor of the protein lysine methyltransferases SUV420H1(IC50 = 25 nM) and SUV420H2 (IC50 = 144 nM). It substantially inhibited non-homologous end-joining (NHEJ)-directed DNA repair but not homology-directed repair(HDR) in cells treated with ionizing radiation. A-196 is active in cells and displayed no toxicity in several cell lines.
Biochemicals & reagents
1982372-88-2
1) Bromberg et al. (2017), The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity; Nat. Chem. Biol. 13 317
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TARGET: Protein methyltransferase -- PATHWAY: DNA repair; Chromatin; Posttranslational modification -- RESEARCH AREA: Epigenetics