CK-0157869

CK 869 is an inhibitor of actin polymerization via inhibition of the actin-related protein 2/3 (Arp2/3) complex, leading to reduced cell motility rate and rearrangement of F-actin in M-1 cells. It inhibits comet tail formation by L. monocytogenes with an IC₅₀ value of 7 μM. It also impairs cell adhesion and cell spreading in MCF10A human breast epithelial cells.

CK-869 binds to the Arp2/3 complex and inhibits nucleation. The Arp2/3 complex is involved with cell motility and F-actin reorganization in M-1 cells.

CK-869 has been used as an Arp2/3 complex inhibitor:

• to treat cultured mammalian cells and study its in vitro and in vivo effects on microtubule assembly
• to induce membrane blebbing in HT1080 fibrosarcoma cells
• to treat KDM3A-null cells and study the relation between actin dynamics and ciliogenesis

CK-0157869 (CK-869) prevents microtubule (MT) assembly, free of Arp2/3 complex.

[1] DARIA V ILATOVSKAYA. Arp2/3 complex inhibitors adversely affect actin cytoskeleton remodeling in the cultured murine kidney collecting duct M-1 cells.[J]. Cell and Tissue Research, 2013, 354 3: 783-792. DOI: 10.1007/s00441-013-1710-y
[2] B. J. NOLEN. Characterization of two classes of small molecule inhibitors of Arp2/3 complex[J]. Nature, 2009, 460 7258: 1031-1034. DOI: 10.1038/nature08231
[3] YVONNE BECKHAM. Arp2/3 inhibition induces amoeboid-like protrusions in MCF10A epithelial cells by reduced cytoskeletal-membrane coupling and focal adhesion assembly.[J]. PLoS ONE, 2014: e100943. DOI: 10.1371/journal.pone.0100943