CK-666

CK-666 is an inhibitor of the actin-related protein 2/3 (Arp2/3) complex (IC₅₀s = 4, 17, and 5 μM for the human, bovine, and S. pombe complexes, respectively, in an actin polymerization assay).¹ It binds at the Arp2/3 interface, stabilizing the inactive conformation of the complex.² CK-666 (40 μM) inhibits actin comet tail formation around intracellular L. monocytogenes in infected SKOV3 cells.¹ It induces actin remodeling, inhibits lamellipodia formation, and reduces the motility rate in M-1 epithelial cells when used at a concentration of 200 μM.³ CK-666 (100 μM) impairs long-term fear memory formation in rats when microinjected into the lateral amygdala.⁴

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1. Nolen, B.J., Tomasevic, N., Russell, A., et al. Characterization of two classes of small molecule inhibitors of Arp2/3 complex. Nature 460(7258), 1031-1034 (2009).

2. Hetrick, B., Han, M.S., Helgeson, L.A., et al. Small molecules CK-666 and CK-869 inhibit actin-related protein 2/3 complex by blocking an activating conformational change. Chem. Biol. 20(5), 701-712 (2013).

3. Ilatovskaya, D.V., Chubinskiy-Nadexhdin, V., Pavlov, T.S., et al. Arp2/3 complex inhibitors adversely affect actin cytoskeleton remodeling in the cultured murine kidney collecting duct M-1 cells. Cell Tissue Res. 354(3), 783-792 (2013).

4. Basu, S., Kustanovich, I., and Lamprecht, R. Arp2/3 and VASP are essential for fear memory formation in lateral amygdala. eNeuro 3(6), pii:ENEURO.0302-0316.2016 (2016).

Brazzo, J.A., Biber, J.C., Nimmer, E., et al. Mechanosensitive expression of lamellipodin promotes intracellular stiffness, cyclin expression, and cell proliferation. J. Cell Sci. (2021).