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Protein Lysine Methyltransferase Inhibitor, UNC0321-Calbiochem

品牌
Sigma-Aldrich
货号
476496
包装型号
规格纯度
参考价格
2741.8 *本价格含增值税费
促销
服务
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数量
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产品名称:
Protein Lysine Methyltransferase Inhibitor, UNC0321-Calbiochem
7-(2-(2-(Dimethylamino)ethoxy)ethoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
产品介绍:

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/tradenameCalbiochem®
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
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

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