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BIX 01294
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BIX 01294图片
CAS NO:935693-62-2
规格:98%
分子量:490.65
包装与价格:
包装价格(元)
5mg电议
25mg电议

产品介绍
G9a and GLP inhibitor
CAS:935693-62-2
分子式:C28H38N6O2
分子量:490.65
纯度:98%
存储:Store at -20°C

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.