BIX-01294

[2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine trihydrochloride]; [N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine].

BIX-01294 is a selective pharmacological inhibitor of G9a histone methyltransferase, an enzyme known also as EHMT2 [euchromatic histone-lysine N-methyltransferase 2] and lysine (K) methyltransferase 1C (Allis et al, 2007). BIX-01294 inhibits the activities of this enzyme and the related G9a-like protein lysine methyltransferase (IC50 in low μM range) (Kubicek et al, 2007; Chang Y et al, 2009; Liu F et al, 2009). Liu F et al (2010) have reported the design of further enzyme inhibitors.

The major substrate of this enzyme is the lysine 9 residue of histone H3 ... ... ... ...
 
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Entry last modified: June 2013