Sigma-Aldrich Cdc42 Inhibitor Iii Zcl278

Assay

≥94% (HPLC)

Quality Level

100

Form

solid

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

light beige

Solubility

DMSO: 50 mg/mL

Storage Temp.

2-8°C

Inchi

1S/C21H19BrClN5O4S2/c1-12-9-13(2)25-20(24-12)28-34(30,31)16-6-4-15(5-7-16)26-21(33)27-19(29)11-32-18-8-3-14(22)10-17(18)23/h3-10H,11H2,1-2H3,(H,24,25,28)(H2,26,27,29,33)

Inchi Key

XKZDWYDHEBCGCG-UHFFFAOYSA-N

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: yesPrimary Target
CDC42Reversible: 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. USA 110,1261.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany