| Identification | Back Directory | [Name]
BIX01294 (hydrochloride hydrate) | [CAS]
1808255-64-2 | [Synonyms]
BIX01294 (hydrochloride hydrate)
BIX01294 (hydrochloride hydrate),BIX-01294 (hydrochloride hydrate) | [Molecular Formula]
C28H41ClN6O3 | [MOL File]
1808255-64-2.mol | [Molecular Weight]
545.13 |
| Hazard Information | Back Directory | [Description]
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 (IC50 = 1.7 μM).4 It less effectively inhibits the HMTase G9a-like protein (GLP; IC50 = 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 | [Uses]
BIX-01294 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[1][2]. | [IC 50]
G9a: 1.7 μM (IC50); GLP: 38 μM (IC50) | [References]
1. Tachibana, M., Sugimoto, K., Nozaki, M., et al. G9a histone methyltransferase plays a dominant role in euchromatic histone H3 lysine 9 methylation and is essential for early embryogenesis Genes Dev. 16(14),1779-1791(2002).
2. Wagschal, A., Sutherland, H.G., Woodfine, K., et al. G9a histone methyltransferase contributes to imprinting in the mouse placenta Mol. Cell Biol. 28(3),1104-1113(2008).
3. Thomas, L.R., Miyashita, H., Cobb, R.M., et al. Functional analysis of histone methyltransferase G9a in B and T lymphocytes J. Immunol. 181(1),485-493(2008).
4. Kubicek, S., O'Sullivan, R.J., August, E.M., et al. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase Mol. Cell 25,473-481(2007).
5. Shi, Y., Desponts, C., Do, J.T., et al. Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds Cell Stem Cell 3(5),568-574(2008). |
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