IOX4

• 常用名: IOX4
• 英文名: IOX4
• CAS号: 1154097-71-8
• 分子量: 328.326
• 密度: 1.4±0.1 g/cm3
• 沸点: 502.2±60.0 °C at 760 mmHg
• 分子式: C₁₅H₁₆N₆O₃
• 熔点: N/A
• 闪点: 257.5±32.9 °C

IOX4用途

IOX4 是一种选择性 PHD2 抑制剂,IC50 值为 1.6 nM,在细胞和野生型小鼠中诱导 HIFα 表达,可通透血脑屏障。IOX4 与 PHD2 活性位点的 2-氧代戊二酸 (2OG) 竞争并置换。

IOX4名称

• 英文名: 2-Methyl-2-propanyl 6-[5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl]nicotinate

IOX4生物活性

• 描述: IOX4 是一种选择性 PHD2 抑制剂,IC50 值为 1.6 nM,在细胞和野生型小鼠中诱导 HIFα 表达,可通透血脑屏障。IOX4 与 PHD2 活性位点的 2-氧代戊二酸 (2OG) 竞争并置换。
• 相关类别:
  研究领域 >> 炎症/免疫
  信号通路 >> 代谢酶/蛋白酶 >> HIF/HIF脯氨酰-羟化酶
  研究领域 >> 神经疾病
• 靶点实验:

  IC50: 1.6 nM (PHD2)[1]

• 体外研究: IOX4(1-100μM; 5小时)确定MCF-7,Hep3B和U2OS中HIF1α诱导的EC50分别为114μM,86μM和49.5μM[1]。
• 参考文献:

  [1]. Chan MC, et al. Potent and Selective Triazole-Based Inhibitors of the Hypoxia-Inducible Factor Prolyl-Hydroxylases with Activity in the Murine Brain. PLoS One. 2015 Jul 6;10(7):e0132004.

IOX4物理化学性质

• 密度: 1.4±0.1 g/cm3
• 沸点: 502.2±60.0 °C at 760 mmHg
• 分子式: C₁₅H₁₆N₆O₃
• 分子量: 328.326
• 闪点: 257.5±32.9 °C
• 精确质量: 328.128387
• LogP: 0.73
• InChIKey: HWQQDVNGHZIALS-UHFFFAOYSA-N
• SMILES: CC(C)(C)OC(=O)c1ccc(-n2[nH]cc(-n3ccnn3)c2=O)nc1
• 蒸汽压: 0.0±1.3 mmHg at 25°C
• 折射率: 1.673
• 储存条件: -20°C，密闭，干燥

IOX4靶点实验

查看更多实验

实验名称：Inhibition of human TET3 catalytic domain (E824 to I1795 residues) expressed in mamma... 来源：ChEMBL 靶标：Methylcytosine dioxygenase TET3 External Id：CHEMBL5337144

实验名称：Inhibition of N-terminal His-tagged recombinant human TET2 catalytic domain LCIdel mu... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5337141

实验名称：Inhibition of His10-FLAG tagged human TET2 catalytic domain (Q969 to I2002 residues) ... 来源：ChEMBL 靶标：Methylcytosine dioxygenase TET2 External Id：CHEMBL5337139

实验名称：Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VER... 来源：ChEMBL 靶标：Severe acute respiratory syndrome coronavirus 2 External Id：CHEMBL4513082

实验名称：Inhibition of N-terminal 3xFlag-tagged human TET1 catalytic domain (E1418 to V2136 re... 来源：ChEMBL 靶标：Methylcytosine dioxygenase TET1 External Id：CHEMBL5337138

实验名称：Inhibition of recombinant human OGFOD1 using 2OG as substrate and Fe2 as co-factor as... 来源：ChEMBL 靶标：Prolyl 3-hydroxylase OGFOD1 External Id：CHEMBL4340711

实验名称：Inhibition of recombinant human FIH using 2OG as substrate and Fe2 as co-factor asses... 来源：ChEMBL 靶标：Hypoxia-inducible factor 1-alpha inhibitor External Id：CHEMBL4340710

实验名称：Inhibition of recombinant human PHD2 using 2OG as substrate and Fe2 as co-factor asse... 来源：ChEMBL 靶标：Egl nine homolog 1 External Id：CHEMBL4340709

实验名称：Inhibition of N-terminal His6-tagged recombinant Paramecium bursaria chlorella virus ... 来源：ChEMBL 靶标：Prolyl 4-hydroxylase External Id：CHEMBL4340708

实验名称：SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response f... 来源：ChEMBL 靶标：Replicase polyprotein 1ab External Id：CHEMBL4495582

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IOX4英文别名

• 2-Methyl-2-propanyl 6-[5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl]nicotinate
• 3-Pyridinecarboxylic acid, 6-[2,5-dihydro-5-oxo-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-1-yl]-, 1,1-dimethylethyl ester