UNC0638 - G9a HMTase Inhibitor. CAS# 1255580-76-7 yltransferase PubMed PMID: 22713795

PubMed PMID: 22713795

G-749 retained its inhibitory potency in various drug-resistance milieus such as patient plasma

InChi: InChI=1S/C27H32N8O2/c1-5-13-34-25(36)21-18-28-26(29-19-9-11-20(12-10-19)33-16-14-32(4)15-17-33)31-24(21)35(34)23-8-6-7-22(30-23)27(2

The drug also inhibits the accumulation of all detectable ubiquitin at sites of DNA double-strand breaks (DSBs)

selective androgen receptor modulator MDV3100 inhibits the activity of prostate cancer cell ARs

UNC0638 - G9a HMTase Inhibitor. CAS# 1255580-76-7 yltransferase PubMed PMID: 22713795UNC0638, CAS No. 1255580 76 7, is a potent, selective and cell permeable G9a and GLP inhibitor, with a toxicity function ratio of >100, compared to <6 for BIX01294. UNC0638 inhibits G9a HMTase with an IC50 ~15 nM and GLP, a closely related H3K9 HMTase, with an IC50~19 nM, but is more than 10, 000 fold selective over other epigenetic targets. G9a (EHMT2) and GLP (EHMT1) catalyze the mono and dimethylation of lysine 9 of histone 3 (H3K9) and other non