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bpV(phen)
bpV(phen),一种胰岛素模拟物,是一种有效的蛋白酪氨酸磷酸酶 (PTP) 和 PTEN 抑制剂,对 PTEN,PTP-β 和 PTP-1B 的 IC50 为 38 nM,343 nM 和 920 nM。bpV(phen) 在体外抑制原生动物寄生虫利什曼原虫的增殖。bpV(phen) 强烈诱导大量趋化因子和促炎性细胞因子的分泌,并激活 Th1 型途径 (IL-12,IFNγ)。bpV(phen) 还可以诱导细胞凋亡 (apoptosis),并具有抗血管生成和抗肿瘤活性。
bpV(phen) Chemical Structure
CAS No. : 42494-73-5
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是否有货 |
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100 mg |
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询价 |
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250 mg |
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500 mg |
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* Please select Quantity before adding items.
bpV(phen) 的其他形式现货产品:
bpV(phen) trihydrate
生物活性 |
bpV(phen), a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity[1][2][3][4][5].
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IC50 & Target |
IC50: 38 nM (PTEN), 343 nM (PTP-β) and 920 nM (PTP-1B)[3] Parasite Leishmania[2] Apoptosis[1]
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体外研究 (In Vitro) |
bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment causes a further decrease of cell viability in H/R-injured H9c2 cells[1]. bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment increases the apoptosis of H/R-injured H9c2 cells[1]. bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment significantly promotes the accumulation of cytoplasmic Cytochrome C in H/R-injured H9c2 cells[1]. After stimulation of bpV(phen), PTEN-induced putative kinase protein 1 (PINK1)/Parkin-mediated mitophagy is inhibited[1]. bpV(phen) is an insulin-mimetic agent following insulin-receptor tyrosine kinase hyperphosphorylation and activation[4].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line: |
Hypoxia/reoxygenation (H/R)-injured H9c2 cells |
Concentration: |
5 μM |
Incubation Time: |
24.5 hours (hypoxia for 24 h; reoxygenation for 30 minutes) |
Result: |
Caused a further decrease of cell viability. |
Apoptosis Analysis[1]
Cell Line: |
Hypoxia/reoxygenation (H/R)-injured H9c2 cells |
Concentration: |
5 μM |
Incubation Time: |
24.5 hours (hypoxia for 24 h; reoxygenation for 30 minutes) |
Result: |
Increased the apoptosis of H/R-injured H9c2 cells. |
Western Blot Analysis[1]
Cell Line: |
Hypoxia/reoxygenation (H/R)-injured H9c2 cells |
Concentration: |
5 μM |
Incubation Time: |
24.5 hours (hypoxia for 24 h; reoxygenation for 30 minutes) |
Result: |
Showed an increased release of Cytochrome C. |
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体内研究 (In Vivo) |
bpV(phen) (5 mg/kg; intraperitoneal injection; daily; for 38 days; male BALB/c nude (nu/nu) athymic mice) treatment causes a significant reduction in average tumor volume[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: |
Male BALB/c nude (nu/nu) athymic mice (6-7 weeks old) injected with PC-3 cells[2] |
Dosage: |
5 mg/kg |
Administration: |
Intraperitoneal injection; daily; for 38 days |
Result: |
Caused a significant reduction in average tumor volume. |
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运输条件 |
Room temperature in continental US; may vary elsewhere.
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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参考文献 |
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[1]. Tang W, et al. PTEN-mediated mitophagy and APE1 overexpression protects against cardiac hypoxia/reoxygenation injury. In Vitro Cell Dev Biol Anim. 2019 Oct;55(9):741-748.
[2]. Caron D, et al. Protein tyrosine phosphatase inhibition induces anti-tumor activity: evidence of Cdk2/p27 kip1 and Cdk2/SHP-1 complex formation in human ovarian cancer cells. Cancer Lett. 2008 Apr 18;262(2):265-75.
[3]. Schmid AC, et al. Bisperoxovanadium compounds are potent PTEN inhibitors. FEBS Lett. 2004 May 21;566(1-3):35-8.
[4]. Band CJ, et al. Early signaling events triggered by peroxovanadium [bpV(phen)] are insulin receptor kinase (IRK)-dependent: specificity of inhibition of IRK-associated protein tyrosine phosphatase(s) by bpV(phen). Mol Endocrinol. 1997 Dec;11(13):1899-910.
[5]. Chen Q, et al. Potassium Bisperoxo(1,10-phenanthroline)oxovanadate (bpV(phen)) Induces Apoptosis and Pyroptosis and Disrupts the P62-HDAC6 Protein Interaction to Suppress the Acetylated Microtubule-dependent Degradation of Autophagosomes. J Biol Chem. 2015 Oct 23;290(43):26051-8.
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