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CK-869

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Chemical Structure| 388592-44-7 同义名 : CK-0157869
CAS号 : 388592-44-7
货号 : A1001760
分子式 : C17H16BrNO3S
纯度 : 99%+
分子量 : 394.283
MDL号 : MFCD01844129
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: 25 mg/mL(63.41 mM)，配合低频超声助溶，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 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.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.54mL

0.51mL

0.25mL

12.68mL

2.54mL

1.27mL

25.36mL

5.07mL

2.54mL
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.