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- Features Inhibitor of G9a and GLP HMTases
- Cell permeable
- Selectively impairs generation of Histone H3K9me2
BIX-01294, a diazepin-quinazolinamine derivative, is a selective,cell-permeable G9a-like protein and G9a histone lysine methyltransferase (HMTase) inhibitor (IC50 values are 0.7 and 1.7 uM respectively) that displays little or no activity at other HMTases. BIX-01294 has been used in combination with the calcium channel activator BayK8644 to facilitate the generation of induced pluripotent stem cells from somatic cells in vitro. BIX-01294 and valproic acid, a histone deacetylase (HDAC) inhibitor, may replace the requirement for ectopic OCT4 (POU5F1) and cMyc respectively in pluripotent stem cell induction (iPS) recipes.