hif 2α in 2

HIF-2α-IN-2 是低氧诱导因子抑制剂，IC50=16 nM。

HIF-2α agonist 2 是一种 HIF-2α 激动剂，对HIF-2α的EC50 值为 1.68 μM。HIF-2α agonist 2可以促进HIF-2a-ARNT 复合物3z 结构中ARNT A B 环的稳定性， 对 786-O-HRE-Luc 细胞无细胞毒性。HIF-2α agonist 2可用于氧代谢研究，与癌症的发生密切相关。

HIF-1 2α-IN-2 is a potent inhibitor of HIF-1 2α, which effectively reduces the levels of HIF-1 2α. This compound elicits an iron starvation response by specifically targeting ISCA2, a key protein involved in Iron Sulfur Cluster Assembly 2. [1]

HIF-2α-IN-3 是一种 HIF-2α 变构抑制剂，具有抗肿瘤特性，可用于研究心血管疾病。

HIF-2α-IN-1是一种有效的 HIF-2α 抑制剂, IC50值小于500 nM。

HIF-2a translation inhibitor 是一种有效的HIF-2α翻译抑制剂，IC50=5 μM，能够抑制组成型和缺氧诱导的 HIF-2α 蛋白表达。其中 HIF-2α-IN-4 将 5'UTR 铁响应元件与氧传感联系起来。

HIF-1α-IN-2 是一种新型高效的 HIF-1α 抑制剂，具有抗癌抗肿瘤活性，以剂量依赖的方式抑制 HIF-1α 和 VEGF 的表达，抑制细胞迁移。

HIF-2α-IN-6 (117) 是HIF-2α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].

HIF-PHD-IN-2 (compound 25) is a highly effective PHD inhibitor, displaying IC50 values below 100 nM for PHD1, PHD2, and PHD3 [1].

HIF-2α-IN-5 是一种有效的 HIF-2α的抑制剂，IC50小于 50 nM。

HIF-2α-IN-7 是一种缺氧诱导因子 2α(HIF-2α)抑制剂。HIF-2α-IN-7 抑制 HIF-2α，EC50值为 6 nM。HIF-2α-IN-7 可用于多种疾病的研究，包括癌症、肝病、炎性疾病、肺病和铁负荷紊乱。

HIF-1α-IN-2 hydrochloride 是一款有效的 HIF-1α 抑制剂，对抗癌活性显著，其在MDA-MB-231细胞和MiaPaCa-2细胞中的IC50值分别为28 nM和15 nM。该化合物主要通过抑制转录和阻碍蛋白质合成来下调HIF-1α的表达。

HIF-2α-IN-9（compound 35r）为HIF-2α抑制剂，能够抑制VEGF-A（IC50=305 nM），影响肿瘤细胞生长基因表达并促进巨噬细胞介导的肿瘤免疫反应。

HIF-2α-IN-13 (18) 作为一种HIF-2α的抑制剂，展示出IC50为2.7 μM的效力。

HIF-2α-IN-14 (18) 作为HIF-2α的抑制剂，展示了0.27 μM的IC50值。

HIF-2α-IN-15 (35) 作为一种HIF-2α的抑制剂，具有0.41 μM的IC50值。

HIF-2α-IN-10 (17) 作为一种HIF-2α的抑制剂，显示出优异的活性，具体表现在其IC50值为0.05 μM。

HIF-2α-IN-11 (1) 作为HIF-2α的抑制剂，显示出IC50为59.2 nM。

HIF-2α-IN-12 (9) 作为HIF-2α的抑制剂，展现出0.9 μM的IC50值。

HIF-2α-IN-16 (48) 作为HIF-2α的高效抑制剂，其IC50为0.091 μM。

PT2399 是高选择性的HIF-2α拮抗剂，能直接结合 HIF-2α PAS B 结构域，IC50=6 nM，具有显著的体内抗肿瘤特性。

CMC2.24 (TRB-N0224) is an orally active tricarbonylmethane agent that demonstrates effectiveness in inhibiting Ras activation and the downstream effector ERK1 2 pathway, thus effectively combating pancreatic tumor formation in mice. Additionally, CMC2.24 exerts potent inhibitory effects on zinc-dependent MMPs, with IC50s ranging from 2.0-69 μM. Furthermore, CMC2.24 aids in alleviating the progression of osteoarthritis by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis through the NF-κB HIF-2α axis[1][2][3].

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......