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.
The Arp2/3 complex consists of seven evolutionarily conserved subunits (Arp2, Arp3 and ARPC1-5) and plays an essential role in polymerization of actin filaments which supports many types of cellular movements[3]. CK-636 is a inhibitor of Arp2/3 complex which could inhibit actin polymerization stimulated by Arp2/3 complex with IC50 values of 4 μM, 24 μM and 32 μM for human, fission yeast and bovine, respectively[3]. By the THP-1 monocyte cell line, CK-636 inhibited the formation of podosomes which are adhesive structures depending on Arp2/3 complex, WASP (Wiskott–Aldrich syndrome protein) and actin polymerization[3]. When the formation of lamellipodia was inhibited by CK-636, a substantial fraction of T cells on those surfaces containing zigzag patterns with an acute turning angle were trapped at the interfaces formed by the turning points of the zigzag patterns[4].
作用机制
CK-636 binds in a pocket between subdomain 4 of Arp2 and subdomain 1 of Arp3.
搜索
