BIX-01294, a diazepin-quinazolinamine derivative, is a selective inhibitor of G9a histone methyl transferase (G9a HMTase) that impairs G9a HMTase and generation of H3K9me2 in vitro. In its inhibition of the histone lysine methyltransferases, BIX-01294 does not compete with cofactor S-adenosyl-methionine. G9a HMTase regulates gene expression including one of the pluripotency genes Oct4. It is reported that BIX-01294 enhances reprogramming efficiency of neural progenitor cells to the same levels as when four transcription factors (Oct4, Klf4, Sox2 and c-Myc) were introduced to somatic cells for generation of induced pluripotent stem cells. 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.