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CAS No.: 442632-72-6

CK-636 Catalog No. CSN15773

Synonyms: CK-0944636

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.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Arp2/3 complex (bovine)

IC50:32μM Arp2/3 complex (fission yeast)

IC50:24μM Arp2/3 Complex

IC50:4μM
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.
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.5165 mL
- 17.5824 mL
- 35.1647 mL
- 5 mM
- 0.7033 mL
- 3.5165 mL
- 7.0329 mL
- 10 mM
- 0.3516 mL
- 1.7582 mL
- 3.5165 mL

技术信息

CAS号

442632-72-6

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H16N2OS

运输

蓝冰

分子量

284.38

别名

CK-0944636

溶解度

DMSO	57.0 mg/mL (200.4 mM)
Water	Insoluble
Ethanol	50.0 mg/mL (175.8 mM)

动物实验配方

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靶点	Description	IC50
Arp2/3 complex (bovine)		IC50:32μM
Arp2/3 complex (fission yeast)		IC50:24μM
Arp2/3 Complex		IC50:4μM

CK-636 Catalog No. CSN15773

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