NMS-873

The 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.¹ 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).² It has been shown to inhibit the proliferation of HCT116 cancer cells with an IC₅₀ value of 380 nM.²

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1. Chou, T.F., and Deshaies, R.J. Development of p97 AAA ATPase inhibitors. Autophagy 7(9), 1091-1092 (2011).

2. Polucci, P., Magnaghi, P., Angiolini, M., et al. Alkylsulfanyl-1,2,4-triazoles, a new class of allosteric valosine containing protein inhibitors. Synthesis and structure-activity relationships. J. Med. Chem. 56(2), 437-450 (2013).