PI-1840

PI-1840 is an inhibitor of chymotrypsin-like (CTL) proteasome activity (IC₅₀ = 27 nM).¹ It is selective for the CTL activity over the trypsin-like (TL) and peptidylglutamyl peptide hydrolyzing (PGPH) activities (IC₅₀s = >100 µM for both), as well as for the 20S constitutive proteasome over the immunoproteasome (IC₅₀s = 18 and 2,170 nM, respectively). PI-1840 decreases the viability of a panel of cancer cell lines (IC₅₀s = 2.2-45.2 µM). It induces cell cycle arrest at the G₂/M phase, apoptosis, and autophagy, as well as inhibits migration and invasion, in U2OS and MG-63 osteosarcoma cells when used at concentrations of 40 and 60 µM, respectively.² PI-1840 (150 mg/kg) decreases tumor volume in an MDA-MB-231 breast cancer mouse xenograft model.¹

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1. Kazi, A., Ozcan, S., Tecleab, A., et al. Discovery of PI-1840, a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity. The Journal of Biological Chemisty 289(17), 11906-11915 (2014).

2. Chen, Y., Chen, H., Xie, H., et al. Non‑covalent proteasome inhibitor PI‑1840 induces apoptosis and autophagy in osteosarcoma cells. Oncol. Rep. 41(5), 2803-2817 (2019).