CK-636 是一种细胞渗透性 Arp2/3 复合物抑制剂，可抑制肌动蛋白聚合，对人、裂殖酵母和牛的 IC50 值分别为 4 μM、24 μM 和 32 μM。
| Cas No. | 442632-72-6 |
| 别名 | CK-0944636 |
| 化学名 | N-[2-(2-methyl-1H-indol-3-yl)ethyl]thiophene-2-carboxamide |
| Canonical SMILES | CC1=C(C2=CC=CC=C2N1)CCNC(=O)C3=CC=CS3 |
| 分子式 | C16H16N2OS |
| 分子量 | 284.38 |
| 溶解度 | ≥ 10.8mg/mL in DMSO |
| 储存条件 | Store at -20° C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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 [1].
The Arp2/3 complex is expected to be involved in morphogenesis and cell adhesion and is essential for epidermal function. It regulates tight junctions and terminal differentiation to promote epidermal barrier formation [2].
CK-636 binds between Arp2 and Arp3 where it appears to block movement of Arp2 and Arp3 into their active conformation and inhibits Arp2/3 complex's ability to nucleate actin filaments. Using a Listeria motility assay to determine whether CK-636 can inhibit actin polymerization mediated by Arp2/3 complex in live cells. In a concentration dependence way, CK-636 reduced the formation of actin filament comet tails by Listeria with IC50 value of 22 μM in infected SKOV3 cells [1].
References:
[1]. Nolen BJ, Tomasevic N, Russell A, et al. Characterization of two classes of small molecule inhibitors of Arp2/3 complex. Nature, 2009, 460(7258): 1031-1034.
[2]. Zhou K, Muroyama A, Underwood J, et al. Actin-related protein2/3 complex regulates tight junctions and terminal differentiation to promote epidermal barrier formation. Proc Natl Acad Sci, 2013, 110(40): E3820-E3829. |
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