Wiskostatin

Wiskostatin is a potent and selective inhibitor of neuronal Wiskott-Aldrich syndrome protein (N-WASP)-mediated actin polymerization by stabilization of the closed, autoinhibited conformation, thereby preventing Arp2/3 complex activation. Wiskostatin is also a dynamin inhibitor with an IC₅₀ value of 20.7 μM and a potent inhibitor of clathrin-mediated endocytosis with an IC₅₀ value of 6.9 μM. Wiskostatin causes a rapid, profound, and irreversible decrease in cellular ATP levels. Wiskostatin also induces disassembly of podosomes in a murine monocyte cell line^{[1][2][3][4][5]}. In Vitro:Wiskostatin (10-50 μM, 2 h) inhibits Arp2/3-dependent apical biosynthetic traffic and decreases the accumulation of sialylated HA in Madin-Darby canine kidney cells^[1].
Wiskostatin (5 μM, 5-15 min) inhibits activation of the WASp biosensor, revealing a reduction in the number of cells displaying podosomes as a function of time in RAW/LR5 cells^[4].
Wiskostatin (5 μM, 5 min) inhibits phagocytosis of EIgG by bone marrow-derived macrophage (BMM) and RAW/LR5 cells and decreases phagocytosis in BMM from WASP-deficient mice^[5].