| Bioactivity | 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. CK636 blocks cell migration. | ||||||||||||
| Target | IC50: 4/24/32 µM (Human/fission yeast/bovine Arp2/3). | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | CK-636 | ||||||||||||
| CAS | 442632-72-6 | ||||||||||||
| Formula | C16H16N2OS | ||||||||||||
| Molar Mass | 284.38 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Nolen BJ, et al. Characterization of two classes of small molecule inhibitors of Arp2/3 complex. Nature. 2009 Aug 20;460(7258):1031-4. [2]. Kwon KW, et al. Migration of T cells on surfaces containing complex nanotopography. PLoS One. 2013 Sep 12;8(9):e73960. [3]. Liang Ma, et al. Discovery of the migrasome, an organelle mediating release of cytoplasmic contents during cell migration. Cell Res. 2015 Jan;25(1):24-38. |