IOX2
货号：
11573-50mg 基本售价：
6608.0 元 规格：
50 mg
产品信息
概述| 货号 | 11573-50mg |
| 描述 | Hypoxia-inducible factor (HIF) is regulated by the hydroxylation of prolyl residues in oxygen-dependent degradation domains in the HIF-1α subunit, which mark it for degradation by the proteasome.1,2 HIF prolyl hydroxylation is catalyzed by prolyl hydroxylase domain enzymes (PHD1, 2, and 3), members of the Fe(II) and 2-oxoglutarate (2OG) oxygenase family. They require dioxygen as a cosubstrate, thus acting as the hypoxia-sensing component of the HIF system. The activity of PHD is suppressed by hypoxia, increasing both the abundance and activity of the HIF transcriptional complex.1,2 IOX2 potently inhibits PHD2 (IC50 = 21 nM) with over 100-fold selectivity compared to inhibition of JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH (IC50s > 100 μM).3 IOX2 is active in cells, inhibiting HIF-1α hydroxylation in RCC4 cells at 50 μM.3 See the Structural Genomics Consortium (SGC) website for more information. |
性能| 供应商 | Cayman |
| 应用文献 |
1.Tian, Y.M.,Yeoh, K.K.,Lee, M.K., et al. Differential sensitivity of hypoxia inducible factor hydroxylation sites to hypoxia and hydroxylase inhibitors. The Journal of Biological Chemisty 286(15), 13041-13051 (2011).
2.Murray, J.K.,Balan, C.,Allgeier, A.M., et al. Dipeptidyl-quinolone derivatives inhibit hypoxia inducible factor-1α prolyl hydroxylases-1, -2, and -3 with altered selectivity. J.Comb.Chem. 12, 676-686 (2010).
3.. IOX2: A selective inhibitor of the hypoxia inducible factor (HIF) prolyl-hydroxylases. .
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 352.3 |
| 分子式 | C19H16N2O5 |
| CAS号 | 931398-72-0 |
| 稳定性 | ≥ 2 years |
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