357649-93-5

中文名称 CPTH2

英文名称 Histone Acetyltransferase Inhibitor IV, CPTH2

CAS 357649-93-5

分子式 C14H14ClN3S

分子量 291.8

MOL 文件 357649-93-5.mol

更新日期 2023/11/13 22:19:01

357649-93-5 结构式

基本信息物理化学性质安全数据图谱信息常见问题列表

基本信息

中文别名

4-(4-CHLOROPHENYL)-N-(CYCLOPENTYLIDENEAMINO)-1,3-THIAZOL-2-AMINE

英文别名

CPTH2
Histone Acetyltransferase Inhibitor IV, CPTH2
Cyclopentylidene-[4-(4-chlorophenyl)thiazol-2-yl)hydrazone
Cyclopentanone, 2-[4-(4-chlorophenyl)-2-thiazolyl]hydrazone

物理化学性质

熔点190-191 °C

沸点460.3±37.0 °C(Predicted)

密度1.38±0.1 g/cm3(Predicted)

储存条件2-8°C

溶解度溶于二甲基亚砜

酸度系数(pKa)14.57±0.20(Predicted)

形态粉末

颜色白色至米色

水溶解性Water: < 0.1 mg/mL (insoluble)

敏感性感光

稳定性可在-20°下的DMSO中的溶液储存长达1个月。

安全数据

WGK Germanynwg

图谱信息

CPTH2(357649-93-5)核磁图(¹HNMR)

常见问题列表

生物活性

CPTH2 是一种有效的 histone acetyltransferase (HAT) 的抑制剂，可调节Gcn5p网络。CPTH2 通过抑制 KAT3B 诱导凋亡并降低ccRCC细胞系的侵袭性。

靶点

Target	Value
HAT ()
Gcn5p ()
KAT3B ()

体外研究

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

Cell Viability Assay

Cell Line:	K1 and ccRCC-786-O cell lines
Concentration:	100 μM
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:	100 μM
Incubation Time:	48 hours
Result:	Produced a drastic increase in apoptotic/dead cell population after 48 h.

Western Blot Analysis

Cell Line:	ccRCC-786-O cells
Concentration:	100 μM
Incubation Time:	12, 24, 48 hours
Result:	Showed a reduced acetylation of both global AcH3 histone and H3AcK18.