1. GPCR/G Protein
    Neuronal Signaling
    Apoptosis
    Anti-infection
  2. Sigma Receptor
    Apoptosis
    SARS-CoV
  3. PB28

PB28 

Cat. No.: HY-108511A
Handling Instructions

PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity.

For research use only. We do not sell to patients.

PB28 Chemical Structure

PB28 Chemical Structure

CAS No. : 172906-90-0

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Description

PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity[1][2][3][4][5].

IC50 & Target

Ki: 0.68 nM (σ2 receptor); 0.38 nM (σ1 receptor)[4]

In Vitro

PB28 (15-25 nM; 24-48 hours; MCF7 and MCF7 ADR cells) treatment shows an accumulation in the G0-G1 phase for MCF7 and MCF7 ADR cells that are time and concentration independent[1].
PB28 has a higher σ2 receptor affinity expressed as Ki (0.28 nM and 0.17 nM in MCF7 and MCF7 ADR cells, respectively) than σ1 receptor affinity (13.0 nMand 10.0 nM, respectively)[1].
PB28 inhibits cell growth of MCF7 and MCF7 ADR cells with IC50s of 25 nM and 15 nM, respectively after 2-day treatment[1].
PB28 induces apoptosis through a caspase-independent pathway[1].
PB28 also reduces P-gp expression in a concentration- and time-dependent manner (approximately 60% in MCF7 and 90% in MCF7 ADR)[1].
PB28 displays antiproliferative and cytotoxic effects in both C6 rat glioma and SK-N-SH human neuroblastoma cell lines[1].

Cell Cycle Analysis[1]

Cell Line: MCF7 and MCF7 ADR cells
Concentration: 25 nM and 15 nM
Incubation Time: 24 hours, 48 hours
Result: Showed an accumulation in the G0-G1 phase for MCF7 and MCF7 ADR cells that were time and concentration independent.
In Vivo

PB28 (10.7 mg/mL; intraperitoneal injection; daily; for two weeks; C57BL/6 female mice) treatment inhibits tumor growth in Panc02 tumor burden mice. PB28 also conferres a survival advantage for mice[2].

Animal Model: C57BL/6 female mice (10 weeks old) injected with Panc02 cells[2]
Dosage: 10.7 mg/mL
Administration: Intraperitoneal injection; daily; for two weeks
Result: Inhibited tumor growth in Panc02 tumor burden mice.
Molecular Weight

370.57

Formula

C₂₄H₃₈N₂O

CAS No.

172906-90-0

SMILES

COC1=CC=CC2=C1CCCC2CCCN3CCN(C4CCCCC4)CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PB28PB 28PB-28Sigma ReceptorApoptosisSARS-CoVSARS coronavirusCOVID-19SARS-CoV-2interactorcytotoxicp-glycoproteincyclohexylpiperazineantitumorantiproliferativecaspase-independentInhibitorinhibitorinhibit

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