General 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 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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Vedadi, M., et al. 2011. Nat. Chem. Biol.7, 566.r>Liu, F., et al. 2011. J. Med. Chem.54, 6139.
Packaging
Packaged under inert gas
2 mg in Glass bottle
Warning
Toxicity: Regulatory Review (Z)
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