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Beschreibung

A cell-permeable thiazolo-benzimidazolone compound that inhibits Trio N-terminal RhoGEF domain- (TrioN) mediated RhoG activation (IC50 = 76 microM) and effectively reduces cellular Rac activation (by 80% with 50 microM ITX3) caused by TrioN, but not GEF337 (RhoA GEF), Tiam1 (Rac GEF), or Vav2 (Rac1/RhoA/Cdc42 GEF), overexpression in HEK293T cells. Culture treatment of ITX at 100 microM is shown to reduce NGF-induced neurite outgrowth of rat PC12 pheochromocytoma cells by 50% and block the formation of multinucleated myotubes by 78% in C2C12 mouse myoblasts cultures induced for differentiation, while the differentiation-associated Myogenin and Troponin T expressions in Trio knock-down C2C12 cells are not affected by ITX at the same concentration.