nMS-873是一种有效的,选择性的VCP/p97抑制剂,在1mM ATP条件下,IC50值为20nM。注:本品仅可用于科研实验,严禁用于临床医疗及其他用途!CAS号:1418013-75-8纯度:99.93%分子式:C27H28N4O3S2分子量:520.67结构式:储存条件:-20℃,有效期2年,溶入溶剂后-20℃请尽量在一个月内使用。相关搜索:VCP/p97抑制剂(NMS...
NMS-873 is a potent, selective allosteric VCP/p97 inhibitor with an IC50 value of 30 nM. IC50 & Target IC50: 30 nM[1]细胞效力(Cellular Effect) Cell Line TypeValueDescriptionReferences BTI-TN-5B1-4 IC50 0.024 μM Inhibition of human recombinant His-GST tagged VCP expressed in baculovirus...
A covalent p97/VCP ATPase inhibitor can overcome resistance to CB-5083 and NMS-873 in colorectal cancer cellsP97Covalent inhibitorATPase activityOrganic synthesisDockingAnti-proliferative activityProteomicsSmall-molecule inhibitors of p97 are useful tools to study p97 function. Human p97 is an ...
Second, inhibition of VCP ATPase activity with the allosteric inhibitor NMS873 has markedly distinct effects on the interaction of different adaptors with VCP. Each of these findings has significant implications, which are discussed in more detail in the following paragraphs. A Cautionary Note for ...
This was phenocopied by the specific VCP inhibitor NMS-873 (Magnaghi et al., 2013) (Figure S7C). Interestingly, the most notable differences between the rescuing activity of VCP(S784D) (more active) and VCP(S784A) (less active) relative to VCP(WT) were detected in the chromatin ...
A covalent p97/VCP ATPase inhibitor can overcome resistance to CB-5083 and NMS-873 in colorectal cancer cells 来自 掌桥科研 喜欢 0 阅读量: 30 作者: Zhang, GangLi, ShanWang, FengJones, Amanda C.Goldberg, Alexander F. G.Lin, BenjaminVirgil, ScottStoltz, Brian M.Deshaies, Raymond J.Chou,...
NMS-873 has been pre- viously shown to be an allosteric inhibitor of VCP and binds at the interface between the D1 and D2 domains.30 Molecular docking of this compound into hexameric VCP with the same search parameters outlined for CB-5083 yielded binding modes at the interface (−9.9 ...
a proteasome inhibitor9. NMS-873 and DBeQ inhibit p97’s ATPase activity and therefore broadly suppress all its functions in the cell10,11. NMS-873 and DBeQ also induce cell death in multiple cancers in vitro and in vivo7,10,11. Because the inhibition of p97 induces a greater anti-pro...
In this study, we tested the safety and efficacy of a novel and potent VCP inhibitor, CB-5083 using VCP patient-derived myoblast cells and an animal model of VCP disease. Methods First, we analyzed the effect of CB-5083 in patient-derived myoblasts on the typical disease autophagy and TDP...
as well as primary MM cells. We chose these two VCP-targeting compounds based on their extensive characterization and mechanistic difference. The quinazoline DBeQ is an ATP competitive VCP inhibitor, whereas NMS-873 is a non-ATP-competitive allosteric inhibitor of VCP.1,27,42Both inhibitors rapidl...