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Description

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 µ,M) and SETD7, SETD8, PRMT3 and SUV39H2 (IC50 >10 µ,M). Shown to lower H3K9Me2 levels in MDA-MB231 cells (IC50 = 81 nM, EC50 = 11.2 µ,M for cell toxicity) and 6-fold more potent than the HMTase Inhibitor, BIX-01294, (Cat. No. 382190). Also, affects the activities of adrenergic alpha1A, adrenergic alpha1B and muscarinic M2 by 90%, 69% and 64% and a panel of 26-receptors and ion-channels by <= 30% at 1 µ,M.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 µ,M) and SETD7, SETD8, PRMT3 and SUV39H2 (IC50 >10 µ,M). Shown to lower H3K9Me2 levels in MDA-MB231 cells (IC50 = 81 nM, EC50 = 11.2 µ,M for cell toxicity) and 6-fold more potent than the HMTase Inhibitor, BIX-01294, (Cat. No. 382190). Also, affects the activities of adrenergic alpha1A, adrenergic alpha1B and muscarinic M2 by 90%, 69% and 64% and a panel of 26-receptors and ion-channels by <= 30% at 1 µ,M.