ZCL278---Cdc42 GTPase Inhibitor


Catalog No. size PriceQuantity
M60133-2S 2mg solid $119
M60133-10S 10mg solid $482

Description

Product Information
Molecular Weight: 584.89
Formula: C21H19BrClN5O4S2
Purity: ≥98%
CAS#: 587841-73-4
Solubility: DMSO up to 100 mM
Chemical Name: 2-(4-bromo-2-chlorophenoxy)-N-((4-(N-(4,6-dimethylpyrimidin-2-yl)sulfamoyl)phenyl)carbamothioyl)acetamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

ZCL278 is a potent and selective inhibitor of Cdc42 GTPase. It directly binds to the binding site of the Cdc42 guanine nucleotide exchange factor intersectin (ITSN) and inhibits its functions (Kd ~6-11 µM). In Swiss 3T3 fibroblast cultures, ZCL278 abolished microspike formation and disrupted GM130-docked Golgi structures, two of the most prominent Cdc42-mediated subcellular events. ZCL278 reduces the perinuclear accumulation of active Cdc42 in contrast to NSC23766, a selective Rac inhibitor. ZCL278 suppresses Cdc42-mediated neuronal branching and growth cone dynamics as well as actin-based motility and migration in a metastatic prostate cancer cell line (i.e., PC-3) without disrupting cell viability. ZCL278 could be a powerful chemical tool for research of Cdc42 subclass of Rho GTPases in human pathogenesis, such as those of cancer and neurological disorders. 

 

How to Use:

 

  • In vitro:  ZCL278 was used at 50 µM final concentration in various in vitro assays.
  • In vivo: not reported

 

 

Reference: 

  1. Friesland A, et al. Small molecule targeting Cdc42-intersectin interaction disrupts Golgi organization and suppresses cell motility. (2013) Proc Natl Acad Sci USA. 110(4):1261-6. 

Products are for research use only. Not for human use.

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