IOX4
货号：
18181-50mg 基本售价：
6608.0 元 规格：
50 mg
产品信息
概述| 货号 | 18181-50mg |
| 描述 | Hypoxia-inducible factors (HIFs) are regulated by the hydroxylation of prolyl residues in oxygen-dependent degradation domains, which leads to 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 co-substrate, thus acting as the hypoxia-sensing component of the HIF system. IOX4 is a potent inhibitor of PHD2 (IC50 = 1.6 nM).3 It displays >1,000-fold selectivity for PHD2 over other 2OG-dependent dioxygenases, including JMJD isoforms, FBXL11, JARID1C, BBOX1, FIH, and FTO. IOX4 is active in vivo, inhibiting prolyl hydroxylation and increasing HIF-1α levels in cells (IC50 values range from 5.6 to 11.7 µM) and inducing HIF-1α and HIF-2α expression in mice.3 The induction of HIF expression in mice occurs in the brain as well as in the liver, kidney, and heart, indicating that IOX4 penetrates the blood-brain barrier.3 |
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.Chan, M.C.,Atasoylu, O.,Hodson, E., et al. Potent and selective triazole-based inhibitors of the hypoxia-inducible factor prolyl-hydroxylases with activity in the murine brain. PLoS One 10(7), 1-17 (2015).
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| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 328.3 |
| 分子式 | C15H16N6O3 |
| CAS号 | 1154097-71-8 |
| 稳定性 | ≥ 2 years |
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