310460-39-0|4-(3-(2-Chlorophenyl)allylidene)-1-phenylpyrazolidine-3,5-dione|CsnPharm

CAS No.: 310460-39-0

CPYPP Catalog No. CSN27183

CPYPP is a DOCK2 inhibitor which bounds to DOCK2 DHR-2 domain in a reversible manner and inhibited its catalytic activity in vitro. It also inhibits DOCK1 and DOCK5 and exhibits selectivity over DOCK9.

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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

描述DOCK2 is an atypical Rac activator predominantly expressed in hematopoietic cells. CPYPP is a small-molecule inhibitor of DOCK2. It dose-dependently inhibited the nucleotide exchange factor activity of DOCK2^DHR-2 for Rac1 with an IC50 value of 22.8±2.4μM. DOCK2 overexpression-induced activation of Rac in HEK293T cells was significantly suppressed by one-hour pretreatment with CPYPP (100μM). Pretreatment of T cells or B cells with CPYPP at a concentration of 100μM for one hour almost completely inhibited Rac activation in response to CCL21 or CXCL13, respectively. One-hour treatment with CPYPP at 100μM inhibited TCR-mediated Rac activation in T cells. Treatment with 100μM CPYPP severely impaired CpG-A-induced Rac activation in pDCs. Intraperitoneal administration of mice with 5mg of CPYPP one hour before adoptive transfer reduced the percentage of migrated T cells to < 25% as compared to the control group^[1].
作用机制CPYPP is a small-molecule inhibitor of DOCK2 that reversibly binds to the DOCK2 DHR-2 domain and inhibited catalytic activity of DOCK2 in vitro^[1].
参考文献

[1] Nishikimi A, Uruno T, Duan X, Cao Q, Okamura Y, Saitoh T, Saito N, Sakaoka S, Du Y, Suenaga A, Kukimoto-Niino M, Miyano K, Gotoh K, Okabe T, Sanematsu F, Tanaka Y, Sumimoto H, Honma T, Yokoyama S, Nagano T, Kohda D, Kanai M, Fukui Y. Blockade of inflammatory responses by a small-molecule inhibitor of the Rac activator DOCK2. Chem Biol. 2012 Apr 20;19(4):488-97. doi: 10.1016/j.chembiol.2012.03.008

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
- 3.0792 mL
- 15.3959 mL
- 30.7919 mL
- 5 mM
- 0.6158 mL
- 3.0792 mL
- 6.1584 mL
- 10 mM
- 0.3079 mL
- 1.5396 mL
- 3.0792 mL

技术信息

CAS号

310460-39-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H13ClN2O2

运输

蓝冰

分子量

324.76

别名

溶解度

DMSO	25.0 mg/mL (77.0 mM) warming

动物实验配方

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