Active Motif's BIX-01294 is a selective inhibitor of G9a histone methyltransferase (IC50 = 1.7 uM) as well as GLP histone methyltransferase (IC50 = 38 uM) leading to a decrease in histone H3 lysine 9 methylation (H3K9me2) in vitro. It 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. It induced apoptosis and decreased proliferation, mobility and invasion in human neuroblastoma cells.
