Pifithrin-α, p-Nitro, Cyclic

• 常用名: Pifithrin-α, p-Nitro, Cyclic
• 英文名: Pifithrin-α, p-Nitro, Cyclic
• CAS号: 60477-38-5
• 分子量: 299.348
• 密度: 1.5±0.1 g/cm3
• 沸点: N/A
• 分子式: C₁₅H₁₃N₃O₂S
• 熔点: N/A
• 闪点: N/A

Pifithrin-α, p-Nitro, Cyclic用途

Pifithrin-α, p-Nitro, Cyclic (PFN-α),是细胞通透性的 p53 抑制剂。Pifithrin-α, p-Nitro, Cyclic 对暴露于 Etoposide 的皮层神经元的保护作用比 Pifithrin-α 强一个数量级 (ED50=30 nM)。Pifithrin-α, p-Nitro, Cyclic 也作为 p53 转录后活性抑制剂。Pifithrin-α, p-Nitro, Cyclic 不阻止 p53 上的 S15 残基磷酸化。

Pifithrin-α, p-Nitro, Cyclic名称

• 中文名: 环丙硫蛋白-α-对硝基
• 英文名: 2-(4-Nitrophenyl)-5,6,7,8-tetrahydroimidazo[2,1-b][1,3]benzothiazole

Pifithrin-α, p-Nitro, Cyclic生物活性

• 描述: Pifithrin-α, p-Nitro, Cyclic (PFN-α),是细胞通透性的 p53 抑制剂。Pifithrin-α, p-Nitro, Cyclic 对暴露于 Etoposide 的皮层神经元的保护作用比 Pifithrin-α 强一个数量级 (ED50=30 nM)。Pifithrin-α, p-Nitro, Cyclic 也作为 p53 转录后活性抑制剂。Pifithrin-α, p-Nitro, Cyclic 不阻止 p53 上的 S15 残基磷酸化。
• 相关类别:
  信号通路 >> 细胞凋亡 >> MDM-2/p53
  研究领域 >> 神经疾病
• 体外研究: 哌非特林-α,对硝基,环(PFN-α)能有效阻断足叶乙甙浓度低于PFT-α1个数量级的皮质神经元p53诱导的细胞死亡和p21/WAF1的表达。
• 体内研究: 在6μM浓度下,眼内注射哌非特林-α可略微提高视网膜神经节细胞(RGC)的存活率,但在0.06μM浓度下不明显。即使在6μM浓度下,哌非特林-α、对硝基、环(PFN-α)在体内也无效[1]。对硝基哌非特林-α,环状,半衰期(t1/2)为6小时(在生物条件下培养时)[1]。
• 参考文献:

  [1]. Pietrancosta N, et al. Imino-tetrahydro-benzothiazole derivatives as p53 inhibitors: discovery of a highly potent in vivo inhibitor and its action mechanism. J Med Chem. 2006 Jun 15;49(12):3645-52.

  [2]. Dinca EB, et al. p53 Small-molecule inhibitor enhances temozolomide cytotoxic activity against intracranial glioblastoma xenografts. Cancer Res. 2008 Dec 15;68(24):10034-9.

Pifithrin-α, p-Nitro, Cyclic物理化学性质

• 密度: 1.5±0.1 g/cm3
• 分子式: C₁₅H₁₃N₃O₂S
• 分子量: 299.348
• 精确质量: 299.072845
• LogP: 5.63
• InChIKey: XMFNSEDROOHGBY-UHFFFAOYSA-N
• SMILES: O=[N+]([O-])c1ccc(-c2cn3c4c(sc3n2)CCCC4)cc1
• 折射率: 1.780
• 储存条件: -20°C，密闭，干燥

Pifithrin-α, p-Nitro, Cyclic靶点实验

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实验名称：Protection against axotomy-induced RGC apoptosis in Wistar rat intravitreally injecte... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL863155

实验名称：Protection against axotomy-induced RGC apoptosis in Wistar rat intravitreally injecte... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL863161

实验名称：Toxicity against mouse E15.5 cortical neurones at 10 uM 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL863162

实验名称：Inhibition of p53-mediated increase in p21/WAF1 level at 30 nM 来源：ChEMBL 靶标：Cellular tumor antigen p53 External Id：CHEMBL863154

实验名称：Cell-based high throughput primary assay to identify activators of GPR151 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=G-protein coupled receptor 151; AltName: Full=G-protein coupled receptor PGR7; AltName: Full=GPCR-2037; AltName: Full=Galanin receptor 4; AltName: Full=Galanin-receptor-like protein; Short=GalRL External Id：GPR151_PHUNTER_AG_LUMI_1536_1X%ACT

实验名称：AlphaScreen-based biochemical high throughput primary assay to identify activators of... 来源：The Scripps Research Institute Molecular Screening Center 靶标：N/A External Id：FBW7_ACT_ALPHA_1536_1X%ACT PRUN

实验名称：AlphaScreen-based biochemical high throughput primary assay to identify inhibitors of... 来源：The Scripps Research Institute Molecular Screening Center External Id：MITF_INH_Alpha_1536_1X%INH PRUN

实验名称：Inhibition of etoposide-induced death of mouse E15.5 cortical neurones 来源：ChEMBL 靶标：Cortical neurone External Id：CHEMBL861311

实验名称：Average percent survival of C57Bl/6 mice thymocytes from Dexamethasone (5 uM) induced... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL883957

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Pifithrin-α, p-Nitro, Cyclic英文别名

• 2-(4-Nitrophenyl)-5,6,7,8-tetrahydroimidazo[2,1-b][1,3]benzothiazole
• MFCD05670249