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。
| 生物活性 | bpV(phen), a insulin-mimetic agent, is a potentprotein tyrosinephosphatase(PTP)andPTENinhibitor withIC50s of 38 nM, 343 nM and 920 nM forPTEN,PTP-βandPTP-1B, respectively. bpV(phen) inhibits proliferation of the protozoanparasiteLeishmaniain vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates aTh1-typepathway (IL-12, IFNγ). bpV(phen) can also induce cellapoptosis, and has anti-angiogenic and anti-tumor activity[1][2][3][4][5]. |
| IC50& Target | IC50: 38 nM (PTEN), 343 nM (PTP-β) and 920 nM (PTP-1B)[3]
ParasiteLeishmania[2]
Apoptosis[1] |
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].
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].
| 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. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
