PB28 is a cyclohexylpiperazine derivative and a high affinity and selectivesigma 2 (σ2) receptoragonist with aK_iof 0.68 nM. PB28 is also aσ1antagonist with aK_iof 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum withEC₅₀values of 2.62 μM and 3.96 μM, respectively. PB28 can modulateSARS-CoV-2-humanprotein-protein interaction. PB28 induces caspase-independentapoptosisand has antitumor activity^{[1][2][3][4][5]}.

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

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 K_i(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].

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].

370.57

C₂₄H₃₈N₂O

172906-90-0

Room temperature in continental US; may vary elsewhere.

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