CAS NO: | 935693-62-2 |
规格: | 98% |
分子量: | 490.65 |
包装 | 价格(元) |
5mg | 电议 |
25mg | 电议 |
Background:
BIX-01294 is a small molecule inhibitor of G9a and GLP (a H3K9 PKMT that shares 80% sequence identity with G9a in their respective SET domains) that was discovered via screening of a library of 125,000 synthetic compounds.?BIX-01294 is selective for G9a and GLP over several H3K9 PKMTs including SUV39H1 and ESET, other KMTs such as SET7/9, and the arginine methyltransferase PRTM1.?The X-ray crystal structure of GLP and BIX-01294 confirmed that BIX-01294 bound to the histone peptide binding pocket but failed to interact with the lysine binding channel.?Cells dosed with BIX-01294 at 4.1 μM were characterized by reduced H3K9me2 levels in several cell lines but toxicity to cells at > 4.1 μM was observed.?
Reference
?[1].William P. Janzen, Tim J. Wigle, Jian Jin, Stephen V. Frye. Epigenetics: tools and technologies. Drug Discov Today Technol. 2010 ; 7(1): 59 – 65.