CDC42 INHIBITOR III ZCL278 1PC X 25MG

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).

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