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
Biological ActivityNMS 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.
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Complete Your Research
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.
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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