1. Neuronal Signaling Apoptosis Anti-infection
  2. Sigma Receptor Apoptosis SARS-CoV
  3. PB28

PB28 是一种环己基哌嗪衍生物,是一种 Ki 值为 0.68 nM 的高亲和力和选择性 sigma 2 (σ2) 受体激动剂。PB28 也是一种 σ1 受体拮抗剂,Ki 为 0.38 nM,对其他受体的亲和力较小。PB28 抑制豚鼠膀胱和回肠中的电诱发抽搐,其 EC50 值分别为 2.62 μM 和 3.96 μM。PB28 可以调节 SARS-CoV-2-人之间的蛋白质与蛋白质的相互作用。PB28 可诱导非 caspase 依赖性的细胞凋亡 (apoptosis),并具有抗肿瘤活性。

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PB28 Chemical Structure

PB28 Chemical Structure

CAS No. : 172906-90-0

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  • 生物活性

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  • 参考文献

生物活性

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]

体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
体内研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
分子量

370.57

Formula

C24H38N2O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PB28
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HY-108511A
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