bpV(phen) (potassium hydrate)

生物活性靶点体外研究体内研究 bpV(phen) (potassium hydrate) 试剂级价格

CAS号:171202-16-7
英文名:bpV(phen) (potassium hydrate)
中文名:bpV(phen) (potassium hydrate)
CBNumber:CB13152565
分子式:C12H10KN2O6V
分子量:368.26
MOL File:171202-16-7.mol

bpV(phen) (potassium hydrate)化学性质

储存条件 :Store at -20°C
溶解度 :DMSO: 1 mg/ml; PBS (pH 7.2): 10 mg/ml
形态 :A crystalline solid
颜色 :Yellow to orange

bpV(phen) (potassium hydrate)性质、用途与生产工艺

生物活性 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。
靶点

IC50: 38 nM (PTEN), 343 nM (PTP-β) and 920 nM (PTP-1B)
Parasite Leishmania
Apoptosis

体外研究

bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment causes a further decrease of cell viability in H/R-injured H9c2 cells.
bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment increases the apoptosis of H/R-injured H9c2 cells.
bpV(phen) (5 μM; 24.5 hours; H9c2 cells) treatment significantly promotes the accumulation of cytoplasmic Cytochrome C in H/R-injured H9c2 cells.
After stimulation of bpV(phen), PTEN-induced putative kinase protein 1 (PINK1)/Parkin-mediated mitophagy is inhibited.
bpV(phen) is an insulin-mimetic agent following insulin-receptor tyrosine kinase hyperphosphorylation and activation.

Cell Viability Assay

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

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

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

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.

Animal Model:	Male BALB/c nude (nu/nu) athymic mice (6-7 weeks old) injected with PC-3 cells
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; daily; for 38 days
Result:	Caused a significant reduction in average tumor volume.