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CAS No.: 1418013-75-8

NMS-873 Catalog No. CSN15917

Synonyms: VCP Inhibitor III

NMS-873 is a potent, selective allosteric VCP/p97 inhibitor with IC50 value of 20 nM (Wild Type, 1 mM ATP).

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 p97

IC50:20nM
描述P97 is an AAA+ ATPase regulating endoplasmic reticulum–associated degradation. NMS-873 is a potent and selective p97 ATPase allosteric inhibitor with IC50 value of 30 nM, selective over all other AAA ATPases, HSP90 and kinases tested with IC50 >10 μM. NMS-873 exhibited antiproliferation on HCT116 cancer cell line cells with IC50 value of 0.4μM. It induced clear, dose-dependent accumulation of poly-Ub proteins and stabilization of cyclin E and Mcl-1 at concentration at 0.5, 2.5 and 5μM in HCT116 cells at 8h and 24h post treatment^[1]. NMS-873 also showed potent HCMV antiviral effect with potential as a novel host targeting therapeutic for HCMV infection. Pretreatment with NMS-873 at 1μM clearly inhibited the production of infectious virus in human primary fibroblast cells infected at high multiplicity of infection with HCMV^[2]
作用机制NMS-873 is a non–ATP-competitive p97 inhibitor with a new allosteric mechanism.^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HCT116 cells	-	Cytotoxic assay	72 h	Cytotoxicity against human HCT116 cells after 72 hrs by luciferase reporter gene assay, IC50=0.38 μM	71521142
Hi5 cells	-	Function assay	20 mins	Inhibition of human recombinant His-GST tagged VCP expressed in baculovirus infected Hi5 cells assessed as ADP formation incubated for 20 mins proir to substrate addition measured after 90 mins by NADH coupled assay, IC50=0.024 μM	23245311

参考文献

[1] Magnaghi P, D'Alessio R, et al. Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death. Nat Chem Biol. 2013 Sep;9(9):548-56.
[2] Lin YT, Prendergast J, et al. The host ubiquitin-dependent segregase VCP/p97 is required for the onset of human cytomegalovirus replication. PLoS Pathog. 2017 May 11;13(5):e1006329.

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
- 1.9206 mL
- 9.6031 mL
- 19.2062 mL
- 5 mM
- 0.3841 mL
- 1.9206 mL
- 3.8412 mL
- 10 mM
- 0.1921 mL
- 0.9603 mL
- 1.9206 mL

技术信息

CAS号

1418013-75-8

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H28N4O3S2

运输

蓝冰

分子量

520.67

别名

VCP Inhibitor III

溶解度

DMSO	100.0 mg/mL (192.1 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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