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CAS No.: 587841-73-4

ZCL278 Catalog No. CSN16326

Synonyms: ZCL278

ZCL278 is a modulator of Cdc42 through directly binding to Cdc42 with Kd of 11.4 μM.

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生物活性

实验方案

技术信息

生物活性

描述Cdc42 is a member of the Rho GTPase family that plays crucial roles in cytoskeletal organization, vesicular trafficking and cell cycle control. ZCL278 is a potent and specific inhibitor of Cdc42 that disrupts the interaction between Cdc42 and intersectin, and competes with GTP to influence Cdc42 GTPase activity. The results from surface plasmon resonance experiment showed that the K_d value for Cdc42-ZCL278 affinity was 11.4 μM. In serum-starved Swiss 3T3 fibroblasts, the incubation of 50 μM ZCL278 for 1 hour followed by the stimulation of 1 U/mL Cdc42 activator for 2 min led to significant inhibition of microspike formation compared with cells only treated with the activator. The same treatment of ZCL278 plus the activator also resulted in 80% decrease in GTP-Cdc42 content compared with cells treated solely with the activator. Moreover, ZCL278-treated cells showed reduced immunoreactivity of GM130, a peripheral cytoplasmic protein that is tightly bound to Golgi membrane to maintain cis-Golgi structures. In human metastatic prostate cancer PC-3 cells that were treated with the 50 μM ZCL278 for 5, 10, and 15 min, the phosphorylation of Rac/Cdc42 was increased in a time-dependent manner, but the tyrosine phosphorylation of Wiskott-Aldrich syndrome protein remained unchanged. The neuronal branching in primary neonatal cortical neurons was also inhibited by 50 μM ZCL278 after 5 and 10 min incubation. The inhibitory effect of ZCL278 on Junin virus replication was observed in vivo. Mice were intraperitoneally injected with 100 μg/g ZCL278 every 24 hours for 3 days and 10⁶ PFU of Junin virus were inoculated intraperitoneally 1 hour after the second ZCL278 injection. One day after the last ZCL278 administration, RNA analysis showed that ZCL278 reduced Junin virus RNA in the spleen samples more than 33-fold compared to non-ZCL278-treated group.
作用机制ZCL278 is a small molecule that binds to Cdc42 residues to target the interaction between Cdc42 and intersectin and inhibits Cdc42-mediated cellular processes.
动物研究
剂量
Mice: 0.8 mg/g^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 0.8 mg/g^[3] (i.p.)
给药途径	i.p.

[1] Chou YY, Cuevas C, et al. Identification and Characterization of a Novel Broad-Spectrum Virus Entry Inhibitor. J Virol. 2016 Apr 14;90(9):4494-510.
[2] Friesland A, Zhao Y, et al. Small molecule targeting Cdc42-intersectin interaction disrupts Golgi organization and suppresses cell motility. Proc Natl Acad Sci U S A. 2013 Jan 22;110(4):1261-6.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7097 mL
- 8.5486 mL
- 17.0971 mL
- 5 mM
- 0.3419 mL
- 1.7097 mL
- 3.4194 mL
- 10 mM
- 0.1710 mL
- 0.8549 mL
- 1.7097 mL

技术信息

CAS号

587841-73-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H19BrClN5O4S2

运输

蓝冰

分子量

584.89

别名

ZCL278

溶解度

DMSO	105.0 mg/mL (179.5 mM)
Water	40.0 mg/mL (68.4 mM) warming

动物实验配方

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