hif-1α/2α inhibitor

Allopurinol (Zyloric) 是一种黄嘌呤氧化酶(XO)抑制剂，IC50=7.82±0.12 μM。

2-Methoxyestradiol (2-ME2) 是一种口服生物可利用的雌二醇代谢物，具有抗肿瘤活性。它通过减少内皮细胞增殖和诱导内皮细胞凋亡来抑制血管生成，也可破坏微管的稳定。它可诱导半胱天冬酶活化，导致细胞周期停滞在 G2 期、DNA 断裂和细胞凋亡。

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......

Chetomin (BRN0077366) 是球毛壳菌的活性成分，是一种无毒的非小细胞肺癌干细胞靶向分子。它是一种热休克蛋白90 缺氧诱导因子1α 途径的抑制剂。

HIF-1 2α-IN-1, an orally active compound, functions as an inhibitor of HIF-2α. Its inhibitory effect on HIF-2α activity is significant, with an IC 50 value of 0.92 μM. Furthermore, HIF-1 2α-IN-1 has the ability to decrease HIF-1α levels. This compound is particularly valuable for research on clear cell renal cell carcinoma (ccRCC) [1].

TAT-cyclo-CLLFVY acetate(1446322-66-2 Free base) 是一种选择性 HIF-1 二聚化抑制剂。 TAT-cyclo-CLLFVY acetate 阻断重组 HIF-1α 与 HIF-1β 的蛋白质-蛋白质相互作用，但不阻断 HIF-2α 与 HIF-1β (IC50 = 1.3 μM)。 TAT-cyclo-CLLFVY acetate 在体外抑制缺氧诱导的 HIF-1 活性，并降低骨肉瘤和乳腺癌细胞中 VEGF 和 CAIX 的表达。 TAT-cyclo-CLLFVY acetate 减少缺氧 HUVEC 的管状化。

Allopurinol Sodium 是黄嘌呤氧化酶抑制剂，其IC50= 0.2~50 μM。它能够抗利什曼原虫，也可用于研究痛风以及高尿酸血症。

Selective HIF-1 dimerization inhibitor. Blocks protein-protein interaction of recombinant HIF-1α, but not HIF-2α, with HIF-1β (IC50 = 1.3 μM). Inhibits hypoxia-induced HIF-1 activity, and decreases VEGF and CAIX expression in osteosarcoma and breast cance

TC-S 7009是一种有效的和具有选择性的HIF-2α抑制剂(Kd: 81 nM)。TC-S 7009对HIF-2α的亲和力大于HIF-1α (Kd >> 5 μM)。 TC-S 7009破坏HIF-2α异源二聚化，降低HIF-2α靶基因表达，降低dna 结合活性。

FM19G11 是一种低氧诱导因子 (HIF) α-亚基抑制剂（在低氧诱导的荧光素酶试验中 IC50 为 80 nM）。