In vitro study | BIX01294 is a selective G9a histone methyltransferase inhibitor that does not affect SUV39H1(H320R) and PRMT1 over the range of concentrations tested. BIX-01294 specifically inhibits G9a (H3K9me2) and, to a lesser extent, the closely related GLP enzymes (mainly H3K9me3), acting on G9a and GLP, the IC50 values were 1.7 μm and 38 μm, respectively. BIX-01294 inhibited G9a in a non-competitive manner with SAM. BIX-01294 (4.1 μm) reduced H3K9me2 levels by acting on wild-type ES cells, mouse embryonic fibroblasts, and HeLa cells, but not G9a deficient stem cells. BIX-01294 is an inhibitor of the transient modulation of the valuable chromosome H3K9me2. BIX-01294 H3K9me2 was reduced on some G9a targeted genes, including Bim1 and serac1. BIX01294 reexpresses HIV-1 Virus from latently infected cells such as ACH-2 and om101. BIX01294 is a selective G9a histone methyltransferase inhibitor that does not affect SUV39H1(H320R) and PRMT1 in the experimental concentration range. BIX-01294 specifically inhibits G9a (H3K9me2) and, to a lesser extent, the closely related GLP enzymes (mainly H3K9me3), acting on G9a and GLP, the IC50 values were 1.7 μm and 38 μm, respectively. BIX-01294 inhibited G9a in a non-competitive manner with SAM. BIX-01294 (4.1 μm) reduced H3K9me2 levels by acting on wild-type ES cells, mouse embryonic fibroblasts, and HeLa cells, but not G9a deficient stem cells. BIX-01294 is an inhibitor of the transient modulation of the valuable chromosome H3K9me2. BIX-01294 H3K9me2 was reduced on some G9a targeted genes, including Bim1 and serac1. BIX01294 reexpresses HIV-1 Virus from latently infected cells such as ACH-2 and om101. |