化合物IOX4 T7880

Product Introduction
Bioactivity


英文名: IOX4

描述: IOX4 是选择性 PHD2抑制剂，IC50=1.6 nM，在细胞和野生型小鼠中诱导 HIFα表达，可透过血脑屏障。它与 PHD2 特性位点的 2-氧代戊二酸竞争并置换。

体内活性: IOX4 as a highly potent and selective inhibitor of human PHD2, As shown by studies with mice, IOX4 is useful for in vivo work;?it will then be useful for investigations on the suitability of the PHDs as targets for cerebral diseases such as stroke.?The combined kinetic and biophysical analyses reveal that IOX4 (and IOX2) compete with 2OG for binding to PHD2;?the triazole rings of the inhibitors bind in the pocket occupied by the CH2CH2COOH side chain of 2OG.?The results thus reveal the potential of non-acid containing PHD inhibitors—an important finding given the potential of HIFα upregulation mediated by PHD inhibition in the treatment of stroke, as acids do not often permeate the blood-brain barrier efficiently[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 83.33 mg/mL (253.80 mM)


关键字: HIF-PH | HIFs | Hypoxia-inducible factors | inhibit | IOX 4 | IOX4 | HIF/HIF Prolyl-Hydroxylase | Inhibitor | IOX-4

相关产品: AKBA | HIF-1α-IN-6 | LW6 | Deoxyshikonin | β,β-Dimethylacrylshikonin | HIF-1α-IN-2 hydrochloride | Fenbendazole | Glucosamine | PHD-1-IN-1 | PT-2385

相关库: Anti-Cancer Compound Library | Glutamine Metabolism Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | Inhibitor Library | Epigenetics Compound Library | Metabolism Compound Library | Anti-Pancreatic Cancer Compound Library | Reprogramming Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途