The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono-
or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development.
1,2,3 BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a HMTase (IC
50 = 1.7 μM).
4 It less effectively inhibits the HMTase G9a-
like protein (GLP; IC
50 = 38 μM) and has no effect on other known HMTases.
4 BIX01294 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.
5
