NMS 873

NMS 873 Basic information
Product Name:NMS 873
Synonyms:NMS 873;NMS873;NMS-873;NMS873/NMS-873;3-[3-(CYCLOPENTYLSULFANYL)-5-({[2-METHYL-4'-(METHYLSULFONYL)-4-BI PHENYLYL]OXY}METHYL)-4H-1,2,4-TRIAZOL-4-YL]PYRIDINE;CS-952;Pyridine, 3-[3-(cyclopentylthio)-5-[[[2-methyl-4'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]oxy]methyl]-4H-1,2,4-triazol-4-yl]-;3-[3-(Cyclopentylthio)-5-[[[2-methyl-4'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]oxy]methyl]-4H-1,2,4-triazol-4-yl]pyridine NMS-873
CAS:1418013-75-8
MF:C27H28N4O3S2
MW:520.67
EINECS:200-256-5
Product Categories:Inhibitors;api
Mol File:1418013-75-8.mol
NMS 873 Structure
NMS 873 Chemical Properties
Melting point >220°C (dec.)
Boiling point 769.3±70.0 °C(Predicted)
density 1.33±0.1 g/cm3(Predicted)
storage temp. 2-8°C
solubility DMSO: soluble25mg/mL, clear
pka2.48±0.12(Predicted)
form powder
color white to beige
Safety Information
Hazard Codes Xn
Risk Statements 22
WGK Germany 3
MSDS Information
NMS 873 Usage And Synthesis
DescriptionThe 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. 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). It has been shown to inhibit the proliferation of HCT116 cancer cells with an IC50 value of 380 nM.
UsesNMS-873 is a potent and specific VCP inhibitor, which has shown to activate the unfolded protein response, interfere with autophagy and induce cancer cell death.
Biochem/physiol ActionsNMS-873 is a selective allosteric non–ATP-competitive inhibitor of the AAA ATPase family member valosine containing protein (VCP), also known as p97 (VCP/p97), an integral component of the ubiquitin fusion degradation (UFD) pathway. VCP/p97 plays a role in degradation of misfolded proteins, Golgi membrane reassembly, membrane transport, myofibril assembly, autophagosome maturation, and cell division, and is overexpressed in many tumor types. NMS-873 is the most potent and specific VCP inhibitor described to date. NMS-873 has an IC50 of 30 nM for VCP/p97 compared to IC50 >10 μM against all of the AAA ATPases, HSP90 or the 53 kinases analyzed. NMS-873 inhibited proliferation of HCT116 cancer cell line cells with an IC50 value of 400 nM.
targetp97
storageStore at +4°C
references[1] magnaghi p, d'alessio r, valsasina b, avanzi n, rizzi s, asa d, gasparri f, cozzi l, cucchi u, orrenius c, polucci p, ballinari d, perrera c, leone a, cervi g, casale e, xiao y, wong c, anderson dj, galvani a, donati d, o'brien t, jackson pk, isacchi a. covalent and allosteric inhibitors of the atpase vcp/p97 induce cancer cell death. nat chem biol. 2013 sep;9(9):548-56. doi: 10.1038/nchembio.1313. epub 2013 jul 28.
NMS 873 Preparation Products And Raw materials
Ruxolitinib DBeQ CHIR-99021 MG-132 MK-2206 2HCl Bortezomib

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