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. BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a HMTase (IC = 1.7 μM). It less effectively inhibits the HMTase G9a-like protein (GLP; IC = 38 μM) and has no effect on other known HMTases. 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.
BIX01294 (hydrochloride hydrate) is a histone-lysine methyltransferase (HMTase) inhibitor, which selective inhibits the G9aHMTase with IC50 of 1.7 μM, reduces histone-3 lysine (9) methylation (H3K9me), induces autophagy and apoptosis in human glioma cells.
体外研究
BIX01294 (hydrochloride hydrate) (1-10 μM) induces autophagy and apoptosis in LN18 glioma cells, reducing cell viability. BIX01294 (hydrochloride hydrate) (1-10 μM) upregulates the levels of autophagy-related genes LC3B and WIPI1 while downregulating differentiation-related genes GFAP and TUBB3, promoting autophagy-dependent differentiation in glioma stem-like cells (GSCs) .
Cell Viability Assay
Cell Line:
LN18
Concentration:
1–10 μM
Incubation Time:
24-72 hours
Result:
Reduced cell viability of LN18 in a dose-dependent manner.
Western Blot Analysis
Cell Line:
LN18
Concentration:
1–10 μM
Incubation Time:
24-72 hours
Result:
Increased levels of cleaved caspase3/7 and cleaved PARP. Decreased levels of H3K9me2, H3K27me3 and accumulation of LC3-II.
分子式
C28H38N6O2.3HCl[XH2O]
CAS号
1808255-64-2
运输条件
Room temperature in continental US; may vary elsewhere.