bpV(phen)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

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 PTENPTP-βPTP-1BIC50 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)

bpV(phen) Chemical Structure

CAS No. : 42494-73-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* 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].

IC50 & Target

IC50: 38 nM (PTEN), 343 nM (PTP-β) and 920 nM (PTP-1B)[3]
Parasite Leishmania[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].

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.

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.

分子量

350.24

Formula

C12H8KN2O5V

CAS 号

42494-73-5

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.

参考文献
  • [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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务