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CK-636

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Chemical Structure| 442632-72-6 同义名 : CK-0944636
CAS号 : 442632-72-6
货号 : A237397
分子式 : C16H16N2OS
纯度 : 99%+
分子量 : 284.376
MDL号 : MFCD03036245
存储条件:

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(175.82 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 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.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.52mL

0.70mL

0.35mL

17.58mL

3.52mL

1.76mL

35.16mL

7.03mL

3.52mL

参考文献

[1]Kwon KW, Park H, Doh J. Migration of T cells on surfaces containing complex nanotopography. PLoS One. 2013 Sep 12;8(9):e73960.

[2]Nolen BJ, Tomasevic N, et al. Characterization of two classes of small molecule inhibitors of Arp2/3 complex. Nature. 2009 Aug 20;460(7258):1031-4.

[3]Nolen BJ, Tomasevic N, Russell A, Pierce DW, Jia Z, McCormick CD, Hartman J, Sakowicz R, Pollard TD. Characterization of two classes of small molecule inhibitors of Arp2/3 complex. Nature. 2009 Aug 20;460(7258):1031-4. doi: 10.1038/nature08231. Epub 2009 Aug 2. PMID: 19648907; PMCID: PMC2780427.

[4]Kwon KW, Park H, Doh J. Migration of T cells on surfaces containing complex nanotopography. PLoS One. 2013 Sep 12;8(9):e73960. doi: 10.1371/journal.pone.0073960. PMID: 24069255; PMCID: PMC3771970.