VCP/p97 inhibitor-1

VCP/p97 inhibitor-1 is a potent inhibitor of VCP/p97 (also called Cdc48, CDC-. 48, or Ter94) with an IC50 of 54.7 nM. VCP/p97 inhibitor-1 causes the dysregulation of protein homeostasis and disturbs the degradation of misfolded polypeptides by the ubiquitin-proteasome system (UPS)[1][2].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> p97

54.7 nM (VCP/p97)[1]

VCP/p97 inhibitor-1 (compound 17) (3-fold serial dilutions with the highest concentration at 10 μM; 72 hours) has anti-proliferation effect with IC50s of 2.9 and 0.86 μM in A549 and RPMI8226 cells, respectively[1]. Cell Viability Assay[1] Cell Line: A549, RPMI8226 cells Concentration: 3-fold serial dilutions with the highest concentration at 10 μM Incubation Time: 72 hours Result: Showed anti-proliferative rates in A549 and RPMI8226 cells (IC50= 2.9 and 0.86 μM, respectively).

[1]. Zhang Y, et al. Discovery of novel pyrimidine molecules containing boronic acid as VCP/p97 Inhibitors. Bioorg Med Chem. 2021;38:116114.

[2]. van den Boom J, et al. VCP/p97-Mediated Unfolding as a Principle in Protein Homeostasis and Signaling. Mol Cell. 2018;69(2):182-194.