CAS:1154097-71-8tert-Butyl 6-(5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinate

IOX4 is a selective HIF-PHD2 inhibitor with IC50 value of 1.6nM.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

技术信息

CAS号

1154097-71-8

储存条件

分子式

C15H16N6O3

运输

蓝冰

分子量

328.33

别名

溶解度

DMSO	97.5 mg/mL (297.0 mM)
Water	insoluble

动物实验配方

生物活性

描述The α/β heterodimeric hypoxia-inducible factor (HIF) complex is responsible for the activation of a large set of genes in response to hypoxia. IOX4 is a potent inhibitor of the HIF prolyl-hydroxylase 2 (PHD2) with an IC50 value of 1.6 nM. The IC50 values of IOX4 for other human 2-oxoglutarate-dependent dioxygenases, such as JMJD3, FBXL11, FIH, and FTO are 1.4, 20, 23.9, and 49μM, respectively. IOX4 inhibited the prolyl-hydroxylation of HIF1α at both NODD (HyPro402) and CODD (HyPro564) without affecting the level of PHD2 in HIFα-stabilized RCC4 cells. In von Hippel-Lindau-competent HeLa cells, IOX4 induced HIF1α at a concentration of ≥ 1μM. The EC50 values of IOX4 for HIF1α induction in MCF-7, Hep3B, and U2OS cell lines are 11.7, 11.1, and 5.6μM, respectively. Treatment of mice with 35mg/kg IOX4 for 1 h induced HIF1α and HIF2α in the liver and brain compared to the vehicle control group^[2].
作用机制IOX4 is a potent PHD2 inhibitor. It inhibits PHD2 via binding to the 2-oxoglutarate binding site^[2].