CPYPP 是DOCK2-Rac1相互作用的抑制剂。它能够结合DOCK2DHR-2结构域，并以剂量依赖性方式抑制 DOCK2DHR-2 (IC50:22.8 μM) 对 Rac1 的鸟嘌呤核苷酸交换因子活性。它还抑制DOCK180和DOCK5，对 DOCK9 的抑制作用较小。

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

CPYPP as a small-molecule inhibitor of DOCK2.?CPYPP bound to DOCK2 DHR-2 domain in a reversible manner and inhibited its catalytic activity in vitro.?When lymphocytes were treated with CPYPP, both chemokine receptor- and antigen receptor-mediated Rac activation were blocked, resulting in marked reduction of chemotactic response and T cell activation.?These results provide a rational of and a chemical scaffold for development of the DOCK2-targeting immunosuppressant[1].

310460-39-0

C18H13ClN2O2

324.76

CPYPP

DMSO:23 mg/mL (70.82 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years