Potent, high affinity (Ki = 0.34 nM) σ2 agonist. Its antiproliferative (EC50 ~ 0.4 µM) and cytotoxic (EC50 ~ 12 µM) effects on glioma and neuroblastoma cell lines indicate it is also a σ1 antagonist. PB28 also inhibited cell growth in MCF7 breast cancer lines, and was strongly synergistic with...
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Potent, high affinity (Ki = 0.34 nM) σ2 agonist. Its antiproliferative (EC50 ~ 0.4 µM) and cytotoxic (EC50 ~ 12 µM) effects on glioma and neuroblastoma cell lines indicate it is also a σ1 antagonist. PB28 also inhibited cell growth in MCF7 breast cancer lines, and was strongly synergistic with doxorubicin. PB28 potently inhibited Kv2.1 channels in a σ-independent manner. Recently, PB28 showed potent (IC50 = 280 nM; 20-fold more than hydroxychloroquine) anti-SARS-CoV2 activity, without cardiac side effects
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