tcsc2551 CK-636

CK-636 is a cell permeable inhibitor of Arp2/3 complex, that could inhibit actin polymerization, with IC₅₀ values of 4 μM, 24 μM and 32 μM for human, fission yeast and bovine, respectively.

IC50 & Target: IC50: 4/24/32 uM (Human/fission yeast/bovine Arp2/3)^[1].

In Vitro: CK-636 binds between Arp2 and Arp3, where it appears to block movement of Arp2 and Arp3 into their active conformation. CK-636 inserts into the hydrophobic core of Arp3 and alters its conformation. CK-636 prevents actin polymerization and the formation of actin filament comet tails by Listeria in infected SKOV3 cells (IC₅₀=22 µM)^[1]. Additionally, CK-636-treated T cells exhibits elongated morphology with sharp pseudopodia at the leading edges, while the breadth of the CK-636-treated T cells is about 30% less than that of DMSO-treated T cells^[2].