CDC42 Inhibitor III, ZCL278, CDC42 GTPase Inhibitor III, 4-(3-(2-(4-Bromo-2-chloro-phenoxy)-acetyl)-thioureido)-N-(4,6-dimethyl-pyrimidin-2-yl)-benzenesulfonamide, 2-(4-Bromo-2-chlorophenoxy)-N-((4-((4,6-dimethyl-2-pyrimidinyl)sulfamoyl)phenyl)carbamothioyl)acetamide
A cell-permeable, non-cytotoxic, aqueous soluble (181 µM in PBS, pH 7.4, containing 0.33% DMSO) pyrimidinylthiourea compound that targets Cdc42 GEF ITSN/intersectin and adjacent GTP/GDP binding site (Kd = 6.4 and 11.4 µM by fluorescence titration and SPR, respectively) and effectively inhibits EGF-stimulated Cdc42 activity (by 100% with 1 h pretreatment of 50 µM ZCL278) and Cdc42-dependent microspike/filopodia formation in serum-starved Swiss 3T3 fibroblast cultures without affecting RhoA-dependent cellular processes or Rac1-dependent lamellipodia formation. Short-term ZCL278 exposure in 5 d-cultured primary neonatal cortical neurons from 1 d postnatal mice is shown to dramatically abolish neurite branching (Ave branches per neurite = 21, 7.8, and 6.4, respectively, with 0, 5, and 10 min exposure to 50 µM ZCL278).
Biochem/physiol Actions
Cell permeable: yes
Primary Target CDC42
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze 9-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Friesland, A., et al. 2013. Proc. Natl. Acad. Sci. USA110, 1261.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 2
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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