A VCP inhibitor (IC50 = 24 nM) that demonstrates potent selectivity for VCP/p97 compared to a panel of other AAA ATPases

NMS-873 – 25 mg

Brand:
Cayman
CAS:
1418013-75-8
Storage:
-20
UN-No:
Non-Hazardous - /

The p97 AAA (ATPase associated with diverse cellular activities) is a ubiquitin-selective chaperone known to play a critical role in the degradation of misfolded membrane and secretory proteins and has been linked to various cellular processes that require unfolding and disassembly of protein complexes.{24975} Valosin-containing protein (VCP), also known as VCP/p97, is an AAA ATPase family member that serves as an integral component of the ubiquitin fusion degradation pathway and is overexpressed in many tumor types. NMS-873 is a VCP inhibitor (IC50 = 24 nM) that demonstrates potent selectivity for VCP/p97 compared to a panel of other AAA ATPases, Hsp90, and 53 additional analyzed kinases (IC50s >10 μM).{28819} It has been shown to inhibit the proliferation of HCT116 cancer cells with an IC50 value of 380 nM.{28819}  

 

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Description

A VCP inhibitor (IC50 = 24 nM) that demonstrates potent selectivity for VCP/p97 compared to a panel of other AAA ATPases, Hsp90, and 53 additional analyzed kinases (IC50s >10 μM). It has been shown to inhibit the proliferation of HCT116 cancer cells with an IC50 value of 380 nM

Formal name: 3-​[3-​(cyclopentylthio)​-​5-​[[[2-​methyl-​4′-​(methylsulfonyl)​[1,​1′-​biphenyl]​-​4-​yl]​oxy]​methyl]​-​4H-​1,​2,​4-​triazol-​4-​yl]​-pyridine

Synonyms:  VCP Inhibitor III

Molecular weight: 520.7

CAS: 1418013-75-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|ATPases||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Cancer||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System

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