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EPZ-6438 - EZH2 Methyltransferase Inhibitor. CAS# 1403254-99-8 nsferase 131(8):1735-44

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Description

131(8):1735-44

the genes coding for isocitrate dehydrogenases 1 and 2

(2012) PLoS One

Robert A Copeland

EPZ-6438 - EZH2 Methyltransferase Inhibitor. CAS# 1403254-99-8 nsferase 131(8):1735-44EPZ 6438 (E7438), CAS No. 1403254 99 8, is a potent and selective small molecule inhibitor of histone methyltransferase EZH2. It inhibited the activity of human PRC2 containing wild type EZH2 with an inhibition constant (Ki) value of 2. 5 0. 5 nM, and similar potency was observed for EZH2 proteins bearing all known lymphoma change of function mutations. EPZ 6438 inhibits EZH2 in a manner competitive with the substrate S adenosylmethionine (SAM). EPZ

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