187-1, N-WASP inhibitor (TFA)

187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein[1][2].

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[1]Peterson, et al. A chemical inhibitor of N-WASP reveals a new mechanism for targeting protein interactions. Proc Natl Acad Sci U S A. 2001 Sep 11;98(19):10624-9.|[2]S Suetsugu, et al. Identification of another actin-related protein (Arp) 2/3 complex binding site in neural Wiskott-Aldrich syndrome protein (N-WASP) that complements actin polymerization induced by the Arp2/3 complex activating (VCA) domain of N-WASP. J Biol Chem. 2001 Aug 31;276(35):33175-80.