|N-(1-苄基哌啶-4-基)-6,7-二甲氧基-2-(4-甲基-1,4-二氮杂卓-1-基)喹唑啉-4-胺|CsnPharm

CAS No.: 935693-62-2

N-(1-Benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine Catalog No. CSN15763

Synonyms: BIX-01294

BIX-01294 is a G9a histone methyltransferase inhibitor with IC50 of 1.9 μM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 EHMT2

IC50:1.9μM
描述BIX-01294 is a G9a histone methyltransferase inhibitor with IC50 value of 1.9μM and reduces H3K9me2 levels at several G9a target genes. It was used as a replacement of Oct3/4 - one of the four original genetic factors used for reprogramming of mammalian somatic cells into induced pluripotent stem (iPS) cells-in generating iPS cells from mouse fetal neural precursor cells, consistent with the observation that repressive H3K9 methylation by G9a is associated with Oct3/4 inactivation during differentiation^[4]. BIX-01294 does not compete with the cofactor S-adenosyl-methionine, and selectively impairs the G9a HMTase and the generation of H3K9me2 in vitro^[5]. BIX-01294 inhibited P. falciparum 3D7 parasites in culture with IC50 values of ∼100 nM and irreversibly arrested parasite growth at all stages of the intraerythrocytic life cycle^[3].
作用机制BIX-01294 occupies the binding site of histone peptide.^[4]
动物研究
剂量
Mice: 5 mg/kg, 10 mg/kg^[4] (i.p.), 0.5 mg/kg - 1 mg/kg^[5] (i.p.); 40 mg/kg - 100 mg/kg^[2] (p.o.)

给药途径
i.p., p.o.
参考文献

动物研究
剂量	Mice: 5 mg/kg, 10 mg/kg^[4] (i.p.), 0.5 mg/kg - 1 mg/kg^[5] (i.p.); 40 mg/kg - 100 mg/kg^[2] (p.o.)
给药途径	i.p., p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0382 mL
- 10.1908 mL
- 20.3815 mL
- 5 mM
- 0.4076 mL
- 2.0382 mL
- 4.0763 mL
- 10 mM
- 0.2038 mL
- 1.0191 mL
- 2.0382 mL

技术信息

CAS号

935693-62-2

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H38N6O2

运输

蓝冰

分子量

490.64

别名

BIX-01294

溶解度

DMSO	110.0 mg/mL (224.2 mM)
Water	Insoluble

动物实验配方

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N-(1-Benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine Catalog No. CSN15763

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