bpV(phen) trihydrate，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) trihydrate 在体外抑制原生动物寄生虫利什曼原虫的增殖。bpV(phen) trihydrate 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) trihydrate 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) trihydrate, 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) trihydrate inhibits proliferation of the protozoanparasiteLeishmaniain vitro. bpV(phen) trihydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates aTh1-typepathway (IL-12, IFNγ). bpV(phen) trihydrate 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 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 18.18 mg/mL(44.97 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.4735 mL | 12.3674 mL | 24.7347 mL | | 5 mM | 0.4947 mL | 2.4735 mL | 4.9469 mL | | 10 mM | 0.2473 mL | 1.2367 mL | 2.4735 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 25 mg/mL (61.84 mM); Clear solution; Need ultrasonic and warming
*以上所有助溶剂都可在本网站选购。 |
