A cell-permeable quinazolinamine compound that acts as a potent and reversible inhibitor of G9a and GLP HMTases (histone methyltransferases) (IC50=<15 and 19nM for G9a and GLP, respectively) and displays ~15-fold greater selectivity over DNMT1 and minimally blocks the activities of JMJD2E (IC50=4.66uM) and SETD7, SETD8, PRMT3 and SUV39H2 (IC50>10uM). Shown to lower H3K9Me2 levels in MDA-MB231 cells (IC50=81nM; EC50=11.2uM for cell toxicity) and 6-fold more potent than the HMTase Inhibitor, BIX-01294. Also, affects the activities of adrenergic a1A, adrenergic a and muscarinicM2 by 90%, 69% and 64% and a panel of 26-receptors and ion-channels by <30% at 1uM.
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
