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4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione

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编辑结构

4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione

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CAS No. 310460-39-0

分子式 C18H13ClN2O2

分子量 324.76

英文名称 4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione

中文同义词 4-(3-(2-氯苯基)亚烯丙基)-1-苯基吡唑烷-3,5-二酮;化合物CPYPP

基本信息

产品名称

4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione

中文同义词

4-(3-(2-氯苯基)亚烯丙基)-1-苯基吡唑烷-3,5-二酮,化合物CPYPP

英文名称

4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione

英文同义词

4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione;CPYPP;3,5-Pyrazolidinedione, 4-[3-(2-chlorophenyl)-2-propen-1-ylidene]-1-phenyl-;4-(3-(2-Chlorophenyl)allylidene)-1-phenylpyrazolidine-3,5-dione

CAS No.

310460-39-0

分子式

C18H13ClN2O2

分子量

324.76

EINECS号

MDL NO.

MFCD00980987

MOL

310460-39-0.mol

性质

密度

1.405±0.06 g/cm3(Predicted)

溶解度

DMSO: 50 mM

储存条件

2-8°C

酸度系数(pKa)

8.26±0.20(Predicted)

用途

靶点

IC50: 22.8 µM (GEF activity of DOCK2 DHR-2 for Rac1)

体内研究

When 2.5 mg/kg of CPYPP is administrated intravenously, the plasma concentration of CPYPP is only 2.4 µM at 30 min. However, by intraperitoneally injecting 250 mg/kg of CPYPP into mice, the plasma concentration of CPYPP reached to 11.3 µM at 30 min and 10.9 µM at 1 hr, respectively. The adoptively transferred spleen cells from mice that has been made by a ‘‘knock-in’’ strategy to express endogenous DOCK2 as a fusion protein with green fluorescent protein (GFP). Intraperitoneal injection of CPYPP (5 mg per mouse) 1 hr before adoptive transfer reduces the percentage of the migrated T cells to <25% of the control level.

体外研究

CPYPP binds to DOCK2 DHR-2 domain in a reversible manner and inhibited its catalytic activity in vitro. When lymphocytes are treated with CPYPP, both chemokine receptor- and antigen receptor-mediated Rac activation are blocked, resulting in marked reduction of chemotactic response and T cell activation. Although overexpression of DOCK2 induces Rac activation in HEK293T cells, this activation is markedly suppressed by treating the cells with CPYPP at 100 µM for 1 hr before assay.

生物活性

CPYPP 是一种 DOCK2-Rac1 相互作用的抑制剂。CPYPP 结合 DOCK2DHR-2 结构域，并以剂量依赖性方式抑制 DOCK2DHR-2 对 Rac1 的鸟嘌呤核苷酸交换因子活性，IC50 为 22.8 µM。CPYPP 还抑制 DOCK180 和 DOCK5，对 DOCK9 的抑制活性较少。

编辑结构

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