ZCL 278 CAS NO.587841-73-4

zcl278 is a cdc42 small molecule modulator that directly binds to cdc42 (kd=11.4 um) and inhibits cdc42-intersectin interaction.
ic50 value: 11.4 um (kd, spr experiment) [1]
target: cdc42
in vitro: as zcl278 has a weak absorption peak at 310 nm, to avoid any experimental error that might result from potential fluorescence quenching by zcl278, the fluorescence emission of cdc42 was monitored at 350 nm, at which zcl278 has a negligible absorption. thus, a kd value of 6.4 μm was obtained. to further demonstrate the direct interaction between zcl278 and cdc42, a surface plasmon resonance (spr) experiment was performed by covalently immobilizing purified cdc42 onto cm5 chips and varying zcl278 concentration. the spr response was observed to increase along with elevated zcl278 concentrations, and eventually gave a kd of 11.4 μm [1]. the experimental pka values of zcl278 were determined to be 3.48 ± 0.04, 6.61 ± 0.02, and 7.45 ± 0.01, the pka value of 3.48 is associated to pyrimidine nitrogen that should stay in a neutral form at ph 7.4 [1]. zcl278-induced disruption of perinuclear distribution of active cdc42 reflected its effects on golgi organization, we examined gm130, a peripheral cytoplasmic protein that is tightly bound to golgi membranes and helps to maintain cis-golgi structures.