PB28 dihydrochloride | Potent sigma2 agonist
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $45.00 | ||
| 25 mg | $160.00 |
PB28 (172907-03-8) is a very potent high affinity (Ki = 5.3 nM1, 0.34 nM2) σ2 agonist. Selective for σ2 over σ1 (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 σ-independent manner.4 PB28 was recently found to have potent (IC50 = 280 nM) anti-SARS-CoV2 activity.5
References:
- Berardi et al. (1996), New s and 5-HT1A Receptor Ligands: w-(Tetralin-1-yl)-n-alkylamine Derivatives; J. Med. Chem. 39 176
- Berardi et al. (2004), 4-(Tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl Derivatives of 1-Cyclohexylpiperazine as s Receptor Ligands with Agonist s2 Activity; J. Med. Chem. 47 2308
- Azzariti et al. (2006), Cyclohexylpiperazine derivative PB28, a s2 agonist and s1 antagonist receptor, inhibits cell growth, modulates P-glycoprotein, and synergizes with anthracyclins in breast cancer; Cancer Ther. 5 1807
- Liu et al. (2017), Potential independent action of sigma receptor ligands through inhibition of the Kv2.1 channel; Oncotarget 8 59345
- Gordon et al. (2020), A SARS-CoV-2 protein interaction map reveals targets for drug repurposing; Nature 583 459
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
PB28 (172907-03-8) is a very potent high affinity (Ki = 5.3 nM1, 0.34 nM2) σ2 agonist. Selective for σ2 over σ1 (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 σ-independent manner.4 PB28 was recently found to have potent (IC50 = 280 nM) anti-SARS-CoV2 activity.5
References:
- Berardi et al. (1996), New s and 5-HT1A Receptor Ligands: w-(Tetralin-1-yl)-n-alkylamine Derivatives; J. Med. Chem. 39 176
- Berardi et al. (2004), 4-(Tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl Derivatives of 1-Cyclohexylpiperazine as s Receptor Ligands with Agonist s2 Activity; J. Med. Chem. 47 2308
- Azzariti et al. (2006), Cyclohexylpiperazine derivative PB28, a s2 agonist and s1 antagonist receptor, inhibits cell growth, modulates P-glycoprotein, and synergizes with anthracyclins in breast cancer; Cancer Ther. 5 1807
- Liu et al. (2017), Potential independent action of sigma receptor ligands through inhibition of the Kv2.1 channel; Oncotarget 8 59345
- Gordon et al. (2020), A SARS-CoV-2 protein interaction map reveals targets for drug repurposing; Nature 583 459
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