产品说明
一般描述
A cell-permeable, quinazoline analog that potently and selectively inhibits PKMT G9a (IC50 = 6 nM and 9 nM in two biochemical assays for CLOT and ECSD, respectively, and Ki = 63 pM, which is approximately 250-fold more potent than a closely-related analog, BIX01294 (Cat. No. 382190)). It inhibits GLP with reduced potency (15 nM) and is found to be inactive (IC50 >40 µM) toward other protein lysine and arginine methyltransferases, such as SET7/9 (aH3K4 PKMT), SET8/PreSET7 (aH4K20 PKMT), and PRMT3, as well as JMJD2E (>1000-fold selectivity) in ECSD enzymatic assays. It also inhibits H3K9me2 accumulation (IC50 = 11,000 nM) in MDA-MB-231 cells, in comparison to BIX01294 (IC50 = 500 nM).
Please note that the molecular weight for this compound is batch-specific due to variable water content.
A cell-permeable quinazoline analog that potently and selectively inhibits PKMT G9a with IC50s equal to 6 µM and 9 µM in two biochemical assays (CLOT and ECSD respectively), and a Morrison Ki of 63 pM, which is about 250-fold more potent compared with a close analog BIX01294 (Cat. No. 382190). Also inhibited GLP with reduced potency (15 µM in an ECSD enzymatic assay). It was found to be inactive (IC50>40 µM) toward other protein lysine and arginine methyltransferases, such as SET7/9 (aH3K4 PKMT), SET8/PreSET7 (aH4K20 PKMT), and PRMT3 in the ECSD assays as well as JMJD2E with >1000-fold selectivity.
包装
5 mg in Glass bottle
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Liu, F., et al. 2010. J. Med. Chem.53, 5844.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C27H45N7O3 |
分子量 | 515.69 |
产品性质
测定 | >98% (HPLC) |
质量水平 | 100 |
形式 | solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
颜色 | light tan |
溶解性 | DMSO: 100 mg/mL |
运输 | wet ice |
储存温度 | −20℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich