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 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.

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.

Packaged under inert gas

Toxicity: Regulatory Review (Z)

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

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

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