PB 28 dihydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
PB 28 dihydrochloride, a cyclohexylpiperazine derivative, is sigma (σ) receptor ligand, acting as a σ2 receptor agonist with a Ki value of 0.68 nM, as well as a σ1 receptor antagonist with a Ki of 0.38 nM. The σ receptor, composed of σ1 and σ2 subtypes, is present with high density in central nervous system and peripheral organs, and overexpressed in many tumor cell lines. Selective σ2 receptor agonists have been proposed as anticancer drugs, while selective σ1 receptor ligands have been proposed to develop new classes of central nervous system agents for neuroprotection, anxiety, depression, psychosis, as well as learning and memory improvement.
References:
1. Berardi F, Abate C, Ferorelli S, et al. Exploring the importance of piperazine N-atoms for sigma(2) receptor affinity and activity in a series of analogs of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28). Journal of Medicinal Chemistry, 2009, 52(23): 7817-7828.
2. Azzariti A, Colabufo NA, Berardi F, et al. Cyclohexylpiperazine derivative PB28, a sigma2 agonist and sigma1 antagonist receptor, inhibits cell growth, modulates P-glycoprotein, and synergizes with anthracyclines in breast cancer. Molecular Cancer Therapeutics, 2006, 5(7): 1807-1816.
3. Pati ML, Hornick JR, Niso M, et al. Sigma-2 receptor agonist derivatives of 1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) induce cell death via mitochondrial superoxide production and caspase activation in pancreatic cancer. BMC Cancer, 2017, 17(1): 51.
| Physical Appearance | White solid |
| Storage | Store at 4°C |
| M.Wt | 443.5 |
| Cas No. | 172907-03-8 |
| Formula | C24H38N2O·2HCl |
| Solubility | <8.87mg/ml in H2O |
| Chemical Name | 1-cyclohexyl-4-(3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl)piperazine dihydrochloride |
| SDF | Download SDF |
| Canonical SMILES | COC1=CC=CC2=C1CCCC2CCCN3CCN(C4CCCCC4)CC3.Cl.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Cell experiment:[2] | |
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Cell lines |
Human breast cancer cell lines, MCF7 and MCF7 ADR (resistant to Adriamycin or doxorubicin) |
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Reaction Conditions |
25 and 15 nM PB 28 dihydrochloride for 2 d incubation |
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Applications |
PB 28 dihydrochloride inhibited growth of MCF-7 and multidrug-resistant MCF7 ADR cells, with IC50 values being 25 and 15 nM, respectively. PB 28 dihydrochloride also decreased basal P-glycoprotein levels in the same cells. |
| Animal experiment:[2] | |
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Animal models |
C57BL/6 mice bearing Panc02 tumors |
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Dosage form |
10.7 mg/mL Once daily by intraperitoneal injection for 2 weeks |
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Applications |
PB 28 dihydrochloride treatment inhibited tumor growth in Panc02 tumor burden mice. Even though treatment was discontinued (on day 15), PB 28 dihydrochloride also conferred a survival advantage for mice in this experiment. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Berardi F, Abate C, Ferorelli S, et al. Exploring the importance of piperazine N-atoms for sigma(2) receptor affinity and activity in a series of analogs of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28). Journal of Medicinal Chemistry, 2009, 52(23): 7817-7828. 2. Azzariti A, Colabufo NA, Berardi F, et al. Cyclohexylpiperazine derivative PB28, a sigma2 agonist and sigma1 antagonist receptor, inhibits cell growth, modulates P-glycoprotein, and synergizes with anthracyclines in breast cancer. Molecular Cancer Therapeutics, 2006, 5(7): 1807-1816. 3. Pati ML, Hornick JR, Niso M, et al. Sigma-2 receptor agonist derivatives of 1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) induce cell death via mitochondrial superoxide production and caspase activation in pancreatic cancer. BMC Cancer, 2017, 17(1): 51. |
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