product name ZCL278
Description: ZCL278 is a potent and selective Cdc42 GTPase inhibitor with Kd of 11.4 μM. In human metastatic prostate cancer PC-3 cells, ZCL278 showed inhibitory function on Rac/Cdc42 phosphorylation and the function increasing as the more-treated time. In cortical neurons, ZCL278 treatment suppressed neuronal branch number and inhibited growth cone motility. Treated serum-starved Swiss 3T3 fibroblasts Cdc42 activator following administration of ZCL278 at the dose of 50 μM for 1 h exhibited a significant decrease (nearly 80%) in GTP-Cdc42 and disrupted perinuclear distribution of active Cdc42.
References: Proc Natl Acad Sci U S A. 2013 Jan 22;110(4):1261-6.
584.89
Formula
C21H19BrClN5O4S2
CAS No.
587841-73-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (170.9 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: ZCL278 inhibits Cdc42 GTPase activity by the competition with GTP and inhibits Rac/Cdc42 phosphorylation in a time-dependent manner. ZCL278 (50 μM) inhibits Cdc42-mediated microspike formation and disrupts GM130-docked Golgi structures in serum-starved Swiss 3T3 fibroblasts. In addition, ZCL278 also suppresses Cdc42-mediated neuronal branching and growth cone dynamics as well as actin-based motility and migration in a metastatic prostate cancer PC-3 cell line without cytotoxicity. Kinase Assay: Inorganic phosphate produced as a result of GTPase activity was measured by using a p50RhoGAP or Cdc42GAP assay and absorbance-based detection method. Briefly, Cdc42 was preloaded with GTP or ZCL278 and incubated in the reaction buffer for 20 mins at 37 °C. GAP was then added for an additional 20 mins at 37 °C. Following a 10-min incubation in CytoPhos reagent, inorganic phosphate was detected at 650 nm. Cell Assay: In ZCL278-treated neurons, neuronal branching was significantly suppressed over the time course. In addition, ZCL278 markedly inhibited Cdc42-mediated growth cone motility. |
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| In Vivo | |
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| Formulation & Dosage | |
| References | Proc Natl Acad Sci U S A. 2013 Jan 22;110(4):1261-6. |
