ZCL 278 是一种选择性 Cdc42 GTPase 抑制剂,与Cdc42结合,Kd为 11.4 μM。
产品描述
ZCL278 is a selective Cdc42 GTPase inhibitor.
体内活性
ZCL278 reduces the JUNV RNA load in the spleen more than 33-fold, with JUNV RNA being undetectable in 5 out of 8 mice. These results are similar to those seen in Gabapentin-treated mice, indicating that ZCL278 is able to abrogate JUNV replication[2].
激酶实验
Lyophilized Cdc42 protein is reconstituted to 5 mg/mL in a buffer consisting of 50 mM Tris, 0.5 mM MgCl2, 50 mM NaCl, 3% (wt/vol) sucrose, and 0.6% dextran. The stock solution is then diluted to 1 μM in 5 mM phosphate buffer, pH 7.4. Into a quartz cuvettete containing Cdc42 solution, aliquots of ZCL278 are added and incubated for 5 min before each fluorescent measurement. The excitation wavelength is 275 nm, and the fluorescence of tryptophan at 350 nm is measured after each addition. The titration curve is fitted using the equimolar specific binding model in GraphPad, and the Kd is calculated[1].
细胞实验
ZCL278 is prepared in DMSO and stored, and then diluted with appropriate medium before use[1]. To determine cell viability, PC-3 cells are incubated for 24 h with or without the Cdc42 activator, ZCL278, or NSC23766. By using the trypan blue dye exclusion method, the numbers of live and dead cells are obtained with a Countess Automated Cell Counter. P values are assigned in each experiment, and any null hypothesis with probability level<95% is rejected[1].
Cas No.
587841-73-4
分子式
C21H19BrClN5O4S2
分子量
584.89
别名
ZCL 278
储存和溶解度
DMSO:58.5 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years