BIX01294 hydrochloride CAS: 1392399-03-9
MF: C28H38N6O2•3HCl
MW: 600.00
A selective histone methyl transferase (HMTase) inhibitor..

BIX01294 hydrochloride (CAS 1392399-03-9)

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BIX01294 hydrochloride is rated 5.0 out of 5 by 1.
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Alternate Names: 2-(Hexahydro-4-Methyl-1H-1,4-Diazepin-1-yl)-6,7-Dimethoxy-[1-(Phenylmethyl)-4-Piperidynyl]-4-Quinazolinamine Trihydrochloride
Application: BIX01294 hydrochloride is a selective histone methyl transferase (HMTase) inhibitor.
CAS Number: 1392399-03-9
Purity: ≥98%
Molecular Weight: 600.00
Molecular Formula: C28H38N6O23HCl
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).
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BIX01294 hydrochloride inhibits G9a. 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 is a selective inhibitor of G9a HMTase (IC50 = 1.7 μM). It less effectively inhibits the HMTase G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other known HMTases. BIX01294 hydrochloride 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 is an inhibitor of HDAC.


参考文献

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 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 181 485-493 (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. Molecular 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).

Physical State :
Solid
Solubility :
Soluble in water (20 mg/ml).
Storage :
Store at -20° C
IC50 :
G9a HMTase: IC50 = 1.7 µM; HMTase G9a-like protein: IC50 = 38 µM; Histone-lysine N-methyltransferase, H3 lysine-9 specific 5: IC50 = 27 nM (human); Histone-lysine N-methyltransferase, H3 lysine-9 specific 3: IC50 = 110 nM (human)
仅供科研使用。不可用于诊断或治疗。
WGK Germany :
3
PubChem CID :
SMILES :
CN1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)CC5=CC=CC=C5)OC)OC.Cl.Cl.Cl

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