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The intact ARP2/3 complex is first purified from Acanthamoeba castellanii based on its affinity for the actin-binding protein profilin, and is shown to consist of a stable assembly of seven polypeptides. Two of the subunits are actin-related proteins of the ARP2 and ARP3 subfamilies, giving the complex its name.

The ARP2/3 complex possesses little biochemical activity on its own. However, when engaged by nucleation-promoting factor (NPF) proteins, it is activated to initiate the formation of a new (daughter) filament that emerges from an existing (mother) filament in a y-branch configuration with a regular 70° branch angle. This coupling of nucleation and branching by the ARP2/3 complex is referred to as autocatalytic branching or dendritic nucleation, and is central to its functions in vivo.

Polymerization of actin filaments directed by the Arp2/3 complex supports many types of cellular movements.

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CK-636 is a small molecule Arp2/3 complex inhibitor that inhibits actin polymerization stimulated by fission yeast Arp2/3 complex (SpArp2/3 complex, IC50 = 24 uM); inhibits formation of actin filament comet tails by Listeria and podosomes by monocytes.


CK 869


CK 869(CK-0157869) is an inhibitor of human and bovine actin-related protein 2/3 (Arp2/3) complex, inhibits actin polymerization (IC50=11 uM); does not inhibit budding or fission yeast Arp2/3 complexes.


CK 666


CK 666 (CK 0944666) is a small molecule Arp2/3 complex inhibitor with IC50 of 4 uM, inhibits actin polymerization with either BtArp2/3 complex (IC50=17 uM) or SpArp2/3 complex (IC50=5 uM); reduces actin polymerization around intracellular Listeria to background levels (Fig. 2e and g) at lower concentrations than CK-636; alters the morphology and slightly slowed but did not stop the gliding motility of fish keratocytes

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