PB28 dihydrochloride
High affinity sigma 2 ligand / Anti-SARS-COV2 / PB28 is a very potent high affinity (Ki = 5.3 nM1, 0.34 nM2) sigma 2 agonist. Selective for sigma 2 over sigma1 (approx 30-40x).1,2 PB28 inhibited cell growth in MCF7 and MCF7 ADR breast cancer cells and displayed strong synergism with doxorubicin.3 PB28 potently inhibited Kv2.1 currents in a sigma-independent manner.4 PB28 was recently found to have potent (IC50 = 280 nM) anti-SARS-CoV2 activity.5
Biochemicals & reagents
172907-03-8
1) Berardi et al. (1996), New ? and 5-HT1A Receptor Ligands: ?-(Tetralin-1-yl)-n-alkylamine Derivatives; J. Med. Chem. 39 176 2) Berardi et al. (2004), 4-(Tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl Derivatives of 1-Cyclohexylpiperazine as ? Receptor Ligands with Agonist ?2 Activity; J. Med. Chem. 47 2308 3) Azzariti et al. (2006), Cyclohexylpiperazine derivative PB28, a ?2 agonist and ?1 antagonist receptor, inhibits cell growth, modulates P-g;lycoprotein, and synergizes with anthracyclins in breast cancer; Mol. Cancer Ther. 5 1807 4) Liu et al. (2017), Potential independent action of sigma receptor ligands through inhibition of the Kv2.1 channel; Oncotarget 8 59345 5) Gordon et al. (2020), A SARS-CoV-2 protein interaction map reveals targets for drug repurposing; Nature 583 4591) Berardi et al. (1996), New ? and 5-HT1A Receptor Ligands: ?-(Tetralin-1-yl)-n-alkylamine Derivatives; J. Med. Chem. 39 176 2) Berardi et al. (2004), 4-(Tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl Derivatives of 1-Cyclohexylpiperazine as ? Receptor Ligands with Agonist ?2 Activity; J. Med. Chem. 47 2308 3) Azzariti et al. (2006), Cyclohexylpiperazine derivative PB28, a ?2 agonist and ?1 antagonist receptor, inhibits cell growth, modulates P-g;lycoprotein, and synergizes with anthracyclins in breast cancer; Mol. Cancer Ther. 5 1807 4) Liu et al. (2017), Potential independent action of sigma receptor ligands through inhibition of the Kv2.1 channel; Oncotarget 8 59345 5) Gordon et al. (2020), A SARS-CoV-2 protein interaction map reveals targets for drug repurposing; Nature 583 459
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TARGET: ER/Golgi; Ion channel -- PATHWAY: Calcium signaling; Cation channel -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Cancer; Infectious diseaseNeurodegeneration; Diabetes