NMS-873

产品说明书

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Chemical Structure| 1418013-75-8 同义名 : VCP Inhibitor III
CAS号 : 1418013-75-8
货号 : A197765
分子式 : C27H28N4O3S2
纯度 : 99%+
分子量 : 520.666
MDL号 : MFCD28009371
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(34.57 mM)，配合低频超声，并水浴加热至45℃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
靶点

  • p97

    p97, IC50:30 nM
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
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.92mL

0.38mL

0.19mL

9.60mL

1.92mL

0.96mL

19.21mL

3.84mL

1.92mL
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.