中文名称: CPTH2
英文名称: CPTH2
CAS No: 357649-93-5
分子式: C14H14ClN3S
分子量: 291.8
C10820 CPTH2 ≥95% (psaitong)
包装规格:
100mg 250mg 1g in glass bottle
溶解性:
溶于DMSO(25 mg/mL 超声)
产品描述:

基本信息

产品编号:C10820

产品名称:CPTH2

CAS:

357649-93-5

 

储存条件

粉末

-20℃

四年

分子式:

C14H14ClN3S

溶于液体

-80℃(避光)

六个月

分子量:

291.80

-20℃(避光)

一个月

化学名: 

 

 

Solubility (25°C)

 

体外

DMSO

58mg/mL (198.76mM)

Ethanol

Insoluble

Water

Insoluble

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

3.4270mL

17.1350mL

34.2700mL

5mM

0.6854mL

3.4270mL

6.8540mL

10mM

0.3427mL

1.7135mL

3.4270mL

50mM

0.0685mL

0.3427mL

0.6854mL

 

生物活性

产品描述

一种有效的组蛋白乙酰基转移酶 (HAT) 抑制剂。CPTH2 选择性地抑制 Gcn5 对组蛋白 H3 的乙酰化。

靶点/IC50

HAT 

Gcn5p 

KAT3B

 

体外研究

CPTH2 (100μM;12,24,48 hours) causes a decrease in cell proliferation after as early as 12h with a further significant reduction after 48h stimulation.CPTH2 (100μM;12 or 48 hours) causes a comparable drop of the activity in both cell lines.CPTH2 (100μM; 48 hours) produces a drastic increase in apoptotic/dead cell population after 48h.CPTH2 (100μM;12,24,48 hours) shows a reduced acetylation of both global AcH3 histone and H3AcK18.CPTH2 (100μM;24,48 hours) is capable to counteract invasion and migration of ccRCC-786-O cells in culture.CPTH2 (0.2,0.5,1mM) inhibits the growth of a GCN5 deleted strain and a single catalytic mutant E173H.CPTH2 (0.6,0.8mM;for 24 hours) inhibits histone H3 acetylation in yeast cell cultures.CPTH2 inhibits the Gcn5p dependent functional network.

Cell Proliferation Assay

Cell Line:

Papillary thyroid (K1) and clear cell Renal Cell Carcinoma (ccRCC-786-O) cell lines

Concentration:

100μM

Incubation Time:

12,24,48 hours

Result:

Caused a decrease in cell proliferation after as early as 12h with a further significant reduction after 48h stimulation.

Cell Viability Assay

Cell Line:

K1 and ccRCC-786-O cell lines

Concentration:

100μM

Incubation Time:

24 hours (K1 cell) and 48 hours (ccRCC-786-O cell)

Result:

Caused a comparable drop of the activity in both cell lines.

Apoptosis Analysis

Cell Line:

ccRCC-786-O cells

Concentration:

100μM

Incubation Time:

48 hours

Result:

Produced a drastic increase in apoptotic/dead cell population after 48h.

Western Blot Analysis

Cell Line:

ccRCC-786-O cells

Concentration:

100μM

Incubation Time:

12,24,48 hours

Result:

Showed a reduced acetylation of both global AcH3 histone and H3AcK18.

 

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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