化合物 T10594
- CAS号:42494-73-5
- 英文名:BPV(PHEN)
- 中文名:化合物 T10594
- CBNumber:CB8434973
- 分子式:C12H8KN2O5V
- 分子量:350.24
- MOL File:42494-73-5.mol
- 储存条件 :-20°C
- 溶解度 :H2O: soluble20mg/mL, clear
- 形态 :Yellow solid
- 颜色 :faint yellow to dark yellow
化合物 T10594性质、用途与生产工艺
- 生物活性 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。
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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.
- 公司名称：KANTO
- 联系电话：--
- 电子邮件：reag-info@gms.kanto.co.jp
- 国家：日本
- 产品数：6756
- 优势度：74
