Cat. No. 6180
Chemical Name: 3-[3-(Cyclopentylthio)-5-[[[2-methy
Biological ActivityPotent valosine containing protein (VCP; p97) allosteric inhibitor (IC50 = 30 nM). Selective over all other AAA ATPases, HSP90 and kinases tested (IC50 >10 nM). 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 VCP-sensitization to trypsin digestion.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Anderson et al (2015) Targeting the AAA ATPase p97 as an approach to treat cancer through disruption of protein homeostasis. Cancer Cell 28 653. PMID: 26555175.
Magnaghi et al (2013) Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death. Nat.Chem.Biol. 9 548. PMID: 23892893.
Polucci et al (2013) Alkylsulfanyl-1,2,4-triazoles, a new class of allosteric valosine containing protein inhibitors. Synthesis and structure-activity relationships. J.Med.Chem. 56 437. PMID: 23245311.
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Keywords: NMS 873, supplier, NMS873, Potent, selective, valosine, containing, protein, VCP, p97, allosteric, inhibitors, inhibits, unfolded, protein, response, UPR, autophagosome, maturation, antiproliferative, anticancer, Tocris Bioscience, Other ATPase Inhibitor products
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July 8 - 12, 2017