Biochem/physiol Actions

Primary TargetCDC42

Reversible: yes

Cell permeable: yes

General description

A cell-permeable, non-cytotoxic, aqueous soluble (181 µM in PBS, pH 7.4) pyrimidinylthiourea that targets Cdc42 GEF ITSN/intersectin and adjacent GTP/GDP binding site and effectively inhibits EGF-stimulated Cdc42 activity (1 h pretreatment; 50 µM) and Cdc42-dependent microspike/filopodia formation in serum-starved Swiss 3T3 fibroblast cultures without affecting RhoA- or Rac1-dependent functions. Short-term ZCL278 exposure in primary murine neonatal cortical neurons is shown to dramatically abolish neurite branching (50 µM).Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

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 (K_d = 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).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Friesland, A., et al. 2013. Proc. Natl. Acad. Sci. USA110, 1261.

Packaging

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze 9-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)