GSK-A is a novel and potent inhibitor of the Histone Lysine Methyltransferase EZH2 (Enhancer of zeste homolog 2) with anticancer activity. EZH2 is a histone-lysine N-methyltransferase enzyme (EC 2.1.1.43) encoded by EZH2 gene, that participates in histone methylation and, ultimately, transcriptional repression. EZH2 catalyzes the addition of methyl groups to histone H3 at lysine 27, by using the cofactor S-adenosyl-L-methionine. Methylation activity of EZH2 facilitates heterochromatin formation thereby silences gene function. Remodeling of chromosomal heterochromatin by EZH2 is also required during cell mitosis.
纯度:≥98%
CAS:923894-97-7