BIX-01294
Histone Methyl transferase inhibitor+D257 / BIX-01294 is a selective inhibitor of G9a histone methyltransferase (G9aHMTase; IC50 = 1.7 µM) as well as GLP HMTase (IC50 = 38 µM) leading to a decrease in H3K9me2(histone H3 lysine 9 methylation) in vitro.1 BIX-01294 facilitates the reactivation of pluripotency genes and induces passive demethylation, thus promoting reprogramming. BIX-01294, in combination with BAY K8644 (a calcium channel agonist), was found to improve reprogramming efficiencies of Oct4-Klf4-(OK)-infected neural progenitor cells.3
Biochemicals & reagents
935693-62-2
1) Kubicek et al. (2007) Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase Mol. Cell. 25 473 / 2) Huangfu et al. (2008) Induction of pluripotent stem cells by defined factors is greatly improved by small-molecule compounds Nat. Biotechnol. 26 795 / 3) Shi Y et al., (2008) A combined chemical and genetic approach for the generation of induced pluripotent stem cells. Cell Stem Cell. 2 525
RT
TARGET: Protein methyltransferase -- PATHWAY: Chromatin; Posttranslational modification -- RESEARCH AREA: Epigenetics; Neuroscience; Stem cells