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Description: BIX01294 triHCl (the tri-hydrochloride salt of BIX01294) is a novel and potent inhibitor of G9a histone methyltransferase with IC50 of 2.7 uM in a cell-free assay. BIX-01294 was discovered by screening a library of 125, 000 synthetic and preselected compounds against G9a. BIX-01294 is selective for G9a and GLP (G9a-like protein) over several H3K9 PKMTs including SUV39H1 and ESET, other KMTs such as SET7/9, and the arginine methyltransferase PRTM1. The X-ray crystal structure of GLP and BIX-01294 confirmed that BIX-01294 bound to the histone peptide binding pocket but failed to interact with the lysine binding channel.
References: Mol Cell. 2007 Feb 9; 25(3):473-81; J Biol Chem. 2010 May 28; 285(22):16538-45.
Related CAS: 935693-62-2 (free base); 1392399-03-9 (triHCl salt)
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