|2-(3-溴苯基)-3-(2,4-二甲氧基苯基)噻唑烷-4-酮|CsnPharm

CAS No.: 388592-44-7

CK-869 Catalog No. CSN23713

Synonyms: CK 0157869;2-(3-Bromophenyl)-3-(2,4-dimethoxyphenyl)-4-thiazolidinone

CK869 is an inhibitor of actin polymerization, it functions by inhibiting the actin-related protein 2/3 (Arp2/3) complex and reduced cell motility rate and rearrangement of F-actin in M-1 cells.

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实验方案

技术信息

生物活性

描述Actin-related protein 2/3 (Arp2/3) complex is a seven-subunit assembly that nucleates branched actin filaments^[2]. CK869 is an ARP2/3 complex inhibitor with an IC₅₀ of 7 μM^[2]. Treatment of cultured mammalian cells with 50 μM CK869 dramatically decreased microtubule (MT) networks and, instead, accumulated tubulin at the cell periphery, as did nocodazole that inhibits MT assembly. An in vitro MT-sedimentation assay revealed that CK869 significantly suppressed MT polymerization^[3].
作用机制CK869 binds to a serendipitous pocket on Arp3 and allosterically destabilizes the short pitch Arp3-Arp2 interface.
参考文献

[2] Hetrick B, Han MS, Helgeson LA, Nolen BJ. Small molecules CK-666 and CK-869 inhibit actin-related protein 2/3 complex by blocking an activating conformational change. Chem Biol. 2013 May 23;20(5):701-12. doi: 10.1016/j.chembiol.2013.03.019. Epub 2013 Apr 25. PMID: 23623350; PMCID: PMC3684959.
[3] Yamagishi Y, Oya K, Matsuura A, Abe H. Use of CK-548 and CK-869 as Arp2/3 complex inhibitors directly suppresses microtubule assembly both in vitro and in vivo. Biochem Biophys Res Commun. 2018 Feb 12;496(3):834-839. doi: 10.1016/j.bbrc.2018.01.143. Epub 2018 Feb 1. PMID: 29395083.

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
- 2.5363 mL
- 12.6813 mL
- 25.3627 mL
- 5 mM
- 0.5073 mL
- 2.5363 mL
- 5.0725 mL
- 10 mM
- 0.2536 mL
- 1.2681 mL
- 2.5363 mL

技术信息

CAS号

388592-44-7

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

C17H16BrNO3S

运输

蓝冰

分子量

394.28

别名

CK 0157869;2-(3-Bromophenyl)-3-(2,4-dimethoxyphenyl)-4-thiazolidinone

溶解度

DMSO	73.0 mg/mL (185.1 mM) warming
Water	Insoluble

动物实验配方

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CK-869 Catalog No. CSN23713

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