CPYPP 是一种 DOCK2-Rac1 相互作用的抑制剂。CPYPP 结合 DOCK2^DHR-2 结构域，并以剂量依赖性方式抑制 DOCK2^DHR-2 对 Rac1 的鸟嘌呤核苷酸交换因子活性，IC₅₀ 为 22.8 µM。CPYPP 还抑制 DOCK180 和 DOCK5，对 DOCK9 的抑制活性较少。

CPYPP is a DOCK2-Rac1 interaction inhibitor. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2 for Rac1 in a dose-dependent manner with an IC 50 of 22.8 μM. CPYPP also inhibits DOCK180 and DOCK5 and less inhibits DOCK9.

Solid

IC50: 22.8 μM (GEF activity of DOCK2 for Rac1)

CPYPP binds to DOCK2 DHR-2 domain in a reversible manner and inhibited its catalytic activity in vitro. When lymphocytes are treated with CPYPP, both chemokine receptor- and antigen receptor-mediated Rac activation are blocked, resulting in marked reduction of chemotactic response and T cell activation.
Although overexpression of DOCK2 induces Rac activation in HEK293T cells, this activation is markedly suppressed by treating the cells with CPYPP at 100 μM for 1 hr before assay. has not independently confirmed the accuracy of these methods. They are for reference only.

When 2.5 mg/kg of CPYPP is administrated intravenously, the plasma concentration of CPYPP is only 2.4 μM at 30 min. However, by intraperitoneally injecting 250 mg/kg of CPYPP into mice, the plasma concentration of CPYPP reached to 11.3 μM at 30 min and 10.9 μM at 1 hr, respectively.
The adoptively transferred spleen cells from mice that has been made by a ‘‘knock-in’’ strategy to express endogenous DOCK2 as a fusion protein with green fluorescent protein (GFP). Intraperitoneal injection of CPYPP (5 mg per mouse) 1 hr before adoptive transfer reduces the percentage of the migrated T cells to <25% of the control level. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 25 mg/mL (76.98 mM; Need ultrasonic)配制储备液