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Beschreibung

A cell-permeable, non-cytotoxic, aqueous soluble (181 µ,M 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 µ,M) 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 µ,M).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 µ,M 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 µ,M by fluorescence titration and SPR, respectively) and effectively inhibits EGF-stimulated Cdc42 activity (by 100% with 1 h pretreatment of 50 µ,M 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 µ,M ZCL278).