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HMTase Inhibitor IV, UNC0638
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 α1A, adrenergic α1B 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.
产品信息
Form Off-white powder
Molar mass 509.7
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥99% by HPLC
Solubility DMSO
Chemical formula C30H47N5O2
商店和运输信息
Storage -20°C
Ship Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Regulatory Review |