NMS 873
Chemical Name: 3-[3-(Cyclopentylthio)-5-[[[2-methyl-4'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]oxy]methyl]-4H-1,2,4-triazol-4-yl]pyridine
Purity: ≥98%
Biological Activity
NMS 873 is a potent p97 ATPase (VCP) allosteric inhibitor (IC50 = 30 nM). Selective over all other AAA ATPases, HSP90 and kinases tested (IC50 >10 μM). Activates the unfolded protein response (UPR) and modulates autophagosome maturation. Exhibits antiproliferative activity in cancer cells in vitro (IC50 values are 400 and 700 nM for HCT116 and HeLa cells respectively). Reduces p97-sensitization to trypsin digestion.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death.
Magnaghi P, D'Alessio R, Valsasina B et al.
Nat Chem Biol -
Alkylsulfanyl-1,2,4-triazoles, a new class of allosteric valosine containing protein inhibitors. Synthesis and structure-activity relationships.
Polucci et al.
J.Med.Chem., 2013;56:437 -
Targeting the AAA ATPase p97 as an approach to treat cancer through disruption of protein homeostasis.
Anderson et al.
Cancer Cell, 2015;28:653
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Citations for NMS 873
The citations listed below are publications that use Tocris products. Selected citations for NMS 873 include:
4 Citations: Showing 1 - 4
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Compounds activating VCP D1 ATPase enhance both autophagic and proteasomal neurotoxic protein clearance.
Authors: Keith Et al.
Nat Commun 2022;13:4146
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USP7 and VCPFAF1 define the SUMO/Ubiquitin landscape at the DNA replication fork.
Authors: Oscar Et al.
Cell Rep 2021;37:109819
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Tandem Deubiquitination and Acetylation of SPRTN Promotes DNA-Protein Crosslink Repair and Protects against Aging.
Authors: Yong Et al.
Mol Cell 2020;79:824-835.e5
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Protein translocation and retro-translocation across the endoplasmic reticulum are crucial to inflammatory effector CD4+ T cell function.
Authors: Manu Et al.
Cytokine 2020;129:154944
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