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CK-636 is an Arp2/3 complex inhibitor with IC50 of 4 μM, 24 μM and 32 μM for inhibition of actin polymerization induced by human, fission yeast and bovine Arp2/3 complex, respectively [1].

The Arp2/3 complex is expected to be involved in morphogenesis and cell adhesion and is essential for epidermal function. It regulates tight junctions and terminal differentiation to promote epidermal barrier formation [2].

CK-636 binds between Arp2 and Arp3 where it appears to block movement of Arp2 and Arp3 into their active conformation and inhibits Arp2/3 complex's ability to nucleate actin filaments. Using a Listeria motility assay to determine whether CK-636 can inhibit actin polymerization mediated by Arp2/3 complex in live cells. In a concentration dependence way, CK-636 reduced the formation of actin filament comet tails by Listeria with IC50 value of 22 μM in infected SKOV3 cells [1].

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