IOX 2
IOX 2 性质
沸点 | 642.8±55.0 °C(Predicted) |
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密度 | 1.470±0.06 g/cm3(Predicted) |
储存条件 | 2-8°C |
溶解度 | DMSO:可溶5mg/mL,澄清(加热) |
酸度系数(pKa) | 3.61±0.10(Predicted) |
形态 | 粉末 |
颜色 | 白色至米色 |
InChIKey | CAOSCCRYLYQBES-UHFFFAOYSA-N |
IOX 2 用途与合成方法
Target | Value |
PHD2
(Cell-free assay) | 21 nM |
IOX2有效抑制PHD2 (IC50为21 nM),比抑制JMJD2A, JMJD2C, JMJD2E, JMJD3, 或2OG加氧酶FIH(IC50<100 μM)选择性高100多倍。IOX2有效作用于细胞,50 μM时,作用于RCC4细胞,抑制HIF-1α羟化。 缺氧诱导因子(HIF)通过在HIF-1α亚单位,由脯氨酰残基在氧依赖性降解结构域的羟化调节。1,2 HIF 脯氨酰羟基化是由脯氨酰羟化酶结构域酶(PHD1, 2, 和 3), Fe(II) 和 2-酮戊二酸 (2OG) 加氧酶家族成员催化。他们需要分子氧作为辅助底物,从而充当HIF系统的缺氧敏感元件。缺氧抑制PHD活性,增加HIF转录复合物的丰度和活性。
To investigate the utility of IOX2 as in vivo functional probes, IOX2 is tested to upregulate HIF signaling in a whole organism, that is, transgenic zebrafish ( Danio rerio ). Because the expression of the PHD3 encoding gene is regulated by HIF in humans and zebrafish, PHD3 levels are a readout of HIF activity. A zebrafish hypoxia reporter line is generated expressing GFP with the phd3 promoter elements. Transgenic wild-type embryos at 3 days postfertilization treated with compounds (10 μM) for 2 days displayed clear increase in phd3:EGFP expression in the liver, relative to controls. Significant increases in GFP levels are observed with IOX2.
IOX 2 价格(试剂级)
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024-11-08 | HY-15468 | IOX 2 | 931398-72-0 | 5mg | 707 |
2024-11-08 | HY-15468 | IOX 2 | 931398-72-0 | 10mM * 1mLin DMSO | 778 |