| Description | CPYPP is an inhibitor of DOCK2-Rac1 interaction. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2DHR-2 for Rac1 in a dose-dependent manner(IC50 : 22.8 μM). CPYPP also inhibits DOCK180, DOCK5 and less DOCK9 |
| In vitro | CPYPP 作为小分子抑制剂，针对 DOCK2 施加作用。CPYPP 以可逆方式结合到 DOCK2 的 DHR-2 域，并在体外抑制其催化活性。当淋巴细胞被 CPYPP 处理时，无论是趋化因子受体还是抗原受体介导的 Rac 激活都被阻断，从而显著降低了趋化反应和 T 细胞激活。这些结果为 DOCK2 靶向免疫抑制剂的开发提供了合理的依据和化学框架[1]。 |
| Target activity | GEF activity of DOCK2DHR-2 for Rac1:22.8 µM |
| molecular weight | 324.76 |
| Molecular formula | C18H13ClN2O2 |
| CAS | 310460-39-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 23 mg/mL (70.82 mM), Sonication is recommended. |
| References | 1. Nishikimi A, et al. Blockade of inflammatory responses by a small-molecule inhibitor of the Rac activator DOCK2. Chem Biol. 2012 Apr 20;19(4):488-97. 2. Ferrandez Y , Zhang W , Peurois F , et al. Allosteric inhibition of the guanine nucleotide exchange factor DOCK5 by a small molecule[J]. entific Reports, 2017, 7(1):14409. |