PTX80

PTX80 is an antagonist of p62 (IC₅₀ = 31.18 nM for the human receptor).¹ It decreases the soluble fraction of p62 in MM.1S multiple myeloma cells when used at a concentration of 1.5 µM. PTX80 (200 nM) increases the levels of polyubiquitinated proteins in MM.1S cells. It induces apoptosis in MM.1S cells when used at a concentration of 100 nM. PTX80 (50-400 nM) decreases the survival of CD138⁺ cells, but not CD138^- cells, in primary plasma cells derived from patients with multiple myeloma. It reduces the viability of tumor tissue samples isolated from ten patient-derived xenograft (PDX) mouse models of colorectal cancer (IC₅₀s = 113-1,220 nM). In vivo, PTX80 (8 or 12 mg/kg twice per week) reduces tumor volume in an HCT116 colorectal cancer mouse xenograft model.

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1. Kalid, O., Gotliv, I., Levy-Apter, E., et al. PTX80, a novel compound targeting the autophagy receptor p62/SQSTM1 for treatment of cancer. Chem. Biol. Drug Des. 100(5), 623-638 (2022).