An inhibitor of Arp2/3 complex action
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].
参考文献:
[1]. Nolen BJ, Tomasevic N, Russell A, et al. Characterization of two classes of small molecule inhibitors of Arp2/3 complex. Nature, 2009, 460(7258): 1031-1034.
[2]. Zhou K, Muroyama A, Underwood J, et al. Actin-related protein2/3 complex regulates tight junctions and terminal differentiation to promote epidermal barrier formation. Proc Natl Acad Sci, 2013, 110(40): E3820-E3829.
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