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CAS No.: 2219320-08-6

MSC1094308 Catalog No. CSN24294

MSC1094308 is a reversible, allosteric inhibitor of the type II AAA ATPase human ubiquitin-directed unfoldase (VCP)/p97 and the type I AAA ATPase VPS4B.

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技术信息

生物活性

描述p97 encodes ubiquitin-directed unfoldase Valosin-containing protein, a member of the AAA ATPase family of proteins. p97 plays a role in the ubiquitin proteasome system and has potential biomedical application in cancer therapy. MSC 1094308 is a non-competitive inhibitor of p97 with IC50 value of 7.2 μM. MSC 1094308 inhibits VPS4B about ten times more potently than p97 with IC50 value of 0.71 μM. In vitro, MSC 1094308 didn't affect the K_M or cooperativity of p97 and VPS4B, but the V_max was progressively reduced with increasing concentrations of MSC 1094308, indicating a non-competitive inhibitory mechanism for ATPases. Incubation with 20 μM MSC 1094308 effectively inhibited D2 ATPase activity by roughly 80% in the mutant deficient in D1 hydrolysis, however, MSC 1094308 inhibited the residual D1 ATPase activity in the D2 hydrolysis mutant only by 30%, suggesting that MSC1094308 targets predominantly the D2 domain of p97. Treatment with 10 μM MSC 1094308 for 8h induced accumulation of polyubiquitinated proteins in HCT116 cells. Treatment Hela cells with 10 μM MSC 1094308 inhibited p97 without proteasomes^[1].
作用机制MSC 1094308 binds to an allosteric binding site, that located at D2 domain in the interface area between the D1 and D2 domain of p97, thereby inhibiting the D2 ATPase activity^[1].
参考文献

[1] Chou TF, Brown SJ, Minond D, Nordin BE, Li K, Jones AC, Chase P, Porubsky PR, Stoltz BM, Schoenen FJ, Patricelli MP, Hodder P, Rosen H, Deshaies RJ. Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways. Proc Natl Acad Sci U S A. 2011 Mar 22;108(12):4834-9.

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
- 2.1619 mL
- 10.8097 mL
- 21.6193 mL
- 5 mM
- 0.4324 mL
- 2.1619 mL
- 4.3239 mL
- 10 mM
- 0.2162 mL
- 1.0810 mL
- 2.1619 mL

技术信息

CAS号

2219320-08-6

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

C29H29F3N2

运输

蓝冰

分子量

462.55

别名

溶解度

DMSO	170.0 mg/mL (367.5 mM)
Water	insoluble

动物实验配方

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