Application

MS-873 has been used as an allosteric inhibitor of ATPase valosin-containing protein (VCP)/p97.

Biochem/physiol Actions

NMS-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.

Packaging

5, 25 mg in glass bottle