中文名称: BIX 01294 促销
英文名称: BIX 01294
CAS No: 1392399-03-9
分子式: C28H38N6O2.3HCl
分子量: 600.02
B10032 BIX 01294 ≥98% (HPLC) (psaitong)
包装规格:
5mg 25mg 100mg in glass bottle
溶解性:
溶于水(>20 mg/mL)和DMSO(98 mg/mL)
产品描述:

基本信息

产品编号:B10032 

产品名称:BIX 01294

CAS:

1392399-03-9

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C28H38N6O2.3HCl

溶于液体

-80℃

六个月

分子量:

600.02

-20℃

一个月

化学名: 

 

 

Solubility (25°C)

 

体外

DMSO

100mg/mL (166.66mM)

Ethanol

100mg/mL (166.66mM)

Water

100mg/mL (166.66mM)

体内(现配现用)

 

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

1.6666mL

8.3331mL

16.6661mL

5mM

0.3333mL

1.6666mL

3.3332mL

10mM

0.1667mL

0.8333mL

1.6666mL

50mM

0.0333mL

0.1667mL

0.3333mL

 

生物活性

产品描述

一种选择性的组蛋白甲基转移酶(HMTASE)抑制剂。

靶点/IC50

G9a
(Cell-free assay)

2.7μM

 

体外研究

BIX-01294 (2μM;48h) selectively inhibits recurrent tumor cell growth.BIX-01294 (1μM) leads to a marked increase in phosphorylation of S345 of MLKL.BIX-01294 (1μM) significantly upregulates the canonical p53 targets Cdkn1a (p21) and Gadd45a in recurrent tumor cell lines.BIX-01294 (1μM;6 days) causes the reduction in H3K9me2 levels in primary and recurrent tumor cells.BIX-01294 leads to necroptotic cell death in recurrent tumor cells.Necrostatin-1 (30μM) partially reverses cell death induced by BIX-01294 (750nM;24h).BIX-01294 (4.1μM;for 2 days) causes around a 20% reduction,concomitant with a comparable increase in the unmodified H3K9 fragment in H3K9me2 in mouse ES cells.BIX-01294 causes pronounced reduction in H3K9me2 and a small decrease for H3K9me3 and H3K9me1 in wild-type ES cells.BIX-01294 has no inhibition of the other histone methyltransferases even at concentrations of 45μM.BIX-01294 does not affect SUV39H1 (H320R) and PRMT1 within the tested concentration range (up to 10μM).BIX-01294 inhibits G9a in an uncompetitive manner with S-adenosyl-methionine (SAM).BIX-01294 (1µg/mL) causes reduction in the BrdU incorporation of fetal PASMCs.BIX-01294 treatment decreases the PASMCs migration induced by PDGF.
Cell Viability Assay

Cell Line:

Primary or recurrent tumor cells

Concentration:

2μM

Incubation Time:

48 hours

Result:

Selectively inhibited recurrent tumor cell growth.

体内研究

BIX-01294 (10mg/kg; IP;three times a week for 2 weeks) significantly reduces tumor growth and tumor burden in recurrent tumor cells.Primary tumor growth is not inhibited.

Animal Model:

Female MMTV-rtTA;TetO-Her2/neu (MTB;TAN) and TetO-Her2/neu (TAN) mice with recurrent or primary tumor cells.

Dosage:

10mg/kg

Administration:

IP;three times a week for 2 weeks

Result:

Significantly reduced tumor growth and tumor burden in recurrent tumor cells.Primary tumor growth was not inhibited. Slowed the growth of orthotopic recurrent tumors in athymic nude recipients.

 

推荐实验方法(仅供参考)

激酶实验:

HMTase实验

在涂有Neutravidin的白色不透明384孔板中进行解离增强镧系荧光免疫分析(DELFIA)。实验化合物在含4% DMSO的12μg/ml 50mM Tris-HCl pH 8.5中稀释,每孔分配10μl。空白和对照孔只有化合物缓冲液。10μg/ml GST-G9a和40μM SAM在50mM Tris HCl pH 8.5/10mM DTT 中稀释,然后加入20μL。空白孔只有Tris/DTT缓冲液。加入溶于50mM Tris pH 8.5,体积为10μl的800nM H3(1-20)-cysbiotin 底物,开始反应,在室温下温育60分钟。使用100μl 洗涤缓冲液洗涤实验板3次。然后实验板的每孔中加入含5ng α-2X-二甲基-H3-K9 和 5ng 山羊抗兔Eu螯合物的50μl 荧光免疫(FI) 缓冲液,在室温下再温育1小时。使用100μl洗涤缓冲液 洗涤实验板3次,每孔加入50μl增强液。45分钟后在Viewlux微孔板成像仪成像15秒,测量时间分辨荧光。

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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