5.00503

CDC42 Inhibitor III, ZCL278

• Synonyme(s) : 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
• Formule empirique (notation de Hill): C₂₁H₁₉BrClN₅O₄S₂
• Numéro CAS: 587841-73-4
• Poids moléculaire : 584.89
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥94% (HPLC)
• Niveau de qualité: 100
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: light beige
• Solubilité: DMSO: 50 mg/mL
• Température de stockage: 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)
• Clé InChI: XKZDWYDHEBCGCG-UHFFFAOYSA-N

Description

Description générale

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).

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
CDC42

Reversible: yes

Conditionnement

Packaged under inert gas

Avertissement

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.

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 2
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable