HMTase Inhibitor IV, UNC0638-Calbiochem

产品说明

一般描述

A cell-permeable quinazolinamine compound that acts as a potent and reversible inhibitor of G9a and GLP HMTases (histone methyltransferases) (IC₅₀ = ≤ 15 and 19 nM for G9a and GLP, respectively) and displays ~15-fold greater selectivity over DNMT1 and minimally blocks the activities of JMJD2E (IC₅₀ = 4.66 µM) and SETD7, SETD8, PRMT3 and SUV39H2 (IC₅₀ >10 µM). Shown to lower H3K9Me2 levels in MDA-MB231 cells (IC₅₀ = 81 nM; EC₅₀ = 11.2 µM for cell toxicity) and 6-fold more potent than the HMTase Inhibitor, BIX-01294, (Cat. No. 382190). Also, affects the activities of adrenergic α_1A, adrenergic α_1B and muscarinic _M2 by 90%, 69% and 64% and a panel of 26-receptors and ion-channels by ≤ 30% at 1 µM.




This probe is supplied in conjunction with the Structural Genomics Consortium (SGC). For further characterization details, please visit the UNC0638 probe summary on the SGC website.
A cell-permeable quinazolinamine compound that acts as a potent and reversible inhibitor of G9a and GLP HMTases (histone methyltransferases) (IC₅₀ = ≤ 15 and 19 nM for G9a and GLP, respectively) and displays ~15-fold greater selectivity over DNMT1 and minimally blocks the activities of JMJD2E (IC₅₀ = 4.66 µM) and SETD7, SETD8, PRMT3 and SUV39H2 (IC₅₀ >10 µM). Shown to lower H3K9Me2 levels in MDA-MB231 cells (IC₅₀ = 81 nM; EC₅₀ = 11.2 µM for cell toxicity) and 6-fold more potent than the HMTase Inhibitor, BIX-01294, (Cat. No. 382190). Also, affects the activities of adrenergic α_1A, adrenergic α_1B and muscarinic _M2 by 90%, 69% and 64% and a panel of 26-receptors and ion-channels by ≤ 30% at 1 µM.

包装

2 mg in Glass bottle
Packaged under inert gas

警告

Toxicity: Regulatory Review (Z)

其他说明

Vedadi, M., et al. 2011. Nat. Chem. Biol.7, 566.

Liu, F., et al. 2011. J. Med. Chem.54, 6139.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

产品性质

安全信息