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同义名 : | - |
CAS号 : | 310460-39-0 | |
货号 : | A1226465 | |
分子式 : | C18H13ClN2O2 | |
纯度 : | 97% | |
分子量 : | 324.76 | |
MDL号 : | MFCD00980987 | |
存储条件: |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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溶解度 : | - | |
动物实验配方: |
生物活性 | |||
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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]. |
实验方案 | |||
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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 |
参考文献 |
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