187-1, N-WASP INHIBITOR

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

Primary Target
Neural Wiskott Aldrich syndrome protein (N-WASP)', 'Target IC50: ~ 2 μM blocking phosphatidylinositol 4,5-bisphosphate (PIP2)-induced actin assembly in Xenopus egg cytoplasmic extract

[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. DOI:10.1073/pnas.201393198
[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 DOI:10.1074/jbc.M102866200