CK869 is an inhibitor of actin polymerization, it functions by inhibiting the actin-related protein 2/3 (Arp2/3) complex and reduced cell motility rate and rearrangement of F-actin in M-1 cells.
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Actin-related protein 2/3 (Arp2/3) complex is a seven-subunit assembly that nucleates branched actin filaments[2]. CK869 is an ARP2/3 complex inhibitor with an IC50 of 7 μM[2]. Treatment of cultured mammalian cells with 50 μM CK869 dramatically decreased microtubule (MT) networks and, instead, accumulated tubulin at the cell periphery, as did nocodazole that inhibits MT assembly. An in vitro MT-sedimentation assay revealed that CK869 significantly suppressed MT polymerization[3].
作用机制
CK869 binds to a serendipitous pocket on Arp3 and allosterically destabilizes the short pitch Arp3-Arp2 interface.
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