T1637
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Mitophagy
Beta Amyloid
Others
Ferroptosis
HIF/HIF Prolyl-Hydroxylase
Autophagy
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Deferoxamine Mesylate (DFOM) 是一种铁螯合剂和铁死亡抑制剂。Deferoxamine Mesylate 可将游离铁结合成稳定的复合物,减少铁的积累。Deferoxamine Mesylate 可以上调 HIF-1α 水平,诱导细胞凋亡。 |
T6823
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HIF/HIF Prolyl-Hydroxylase
DNA/RNA Synthesis
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E3330 是一种口服有效的选择性 AP 内切核酸酶 1 (APE1; REF-1) 抑制剂,可抑制NF-κB DNA 结合活性。它阻断 TNF-α 诱导的肝癌细胞系中 IL-8 的激活,可以抑制癌细胞的生长和迁移,具有抗癌活性。 |
T5S1569
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Others
Reactive Oxygen Species
HIF/HIF Prolyl-Hydroxylase
Endogenous Metabolite
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AKBA (3-O-Acetyl-11-keto-beta-boswellic acid) 是一种从乳香中分离的天然成分,是新颖的 Nrf2 的活化剂。 |
T7692
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HIF
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2,4-DPD 是氧感应酶 HIF-α 脯氨酰羟化酶 (HIF-PH) 的竞争性抑制剂。 |
T36953
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HIF
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Naphthofluorescein (Naphthafluorescein)是一种 Mint3 抑制剂,具有潜在的抗肿瘤和抗炎活性,抑制 HIF-1 和 Mint3 之间的相互作用,抑制 Mint3 依赖性 HIF-1 活性,抑制癌细胞和巨噬细胞的糖酵解活动,同时未显示出明显的体外细胞毒性和体内副作用。Naphthofluorescein 也是一种荧光 pH 敏感探针,可用于功能性切伦科夫成像。 |
T69966
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Roxadustat-d5 is intended for use as an internal standard for the quantification of roxadustat by GC- or LC-MS. Roxadustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH; IC50s = 1.4, 1.26, and 1.32 µM for HIF-PH1, HIF-PH2, and HIF-PH3, respectively). It is selective for HIF-PH over other 2-oxoglutarate-dependent dioxygenases, including lysine-specific demethylase 5A (KDM5A), KDM5B, -5C, -5D, and -6B (IC50s = >100 µM for all). Roxadustat (10-200 µM) stabilizes HIF-1α and HIF-2α in Hep3B hepatocellular carcinoma cells. It increases levels of secreted erythropoietin in Hep3B cells in a concentration-dependent manner and increases erythropoiesis in rats when administered at doses of 25 and 50 mg/kg. Roxadustat reverses anemia in a rat model of chronic inflammation induced by peptidoglycan-polysaccharide, as well as a rat model of chronic kidney disease induced by 5/6 nephrectomy. It reduces tumor growth and increases survival in a murine Lewis lung carcin...... |