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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 DOCK2DHR-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]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.08mL 0.62mL 0.31mL |
15.40mL 3.08mL 1.54mL |
30.79mL 6.16mL 3.08mL |
CAS号 | 310460-39-0 |
分子式 | C18H13ClN2O2 |
分子量 | 324.761 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
溶解方案 |
DMSO: 25 mg/mL(76.98 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |