hif-2α-in-1

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

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

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-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。

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].

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-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-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-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。

Emetine hydrochloride (NSC 33669)，一种从ipecac根部提取的生物碱，用于临床上作为催吐及抗原生动物药物。它能够降低HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α)、PDK1、RhoA、Rho-kinases (ROCK1 and ROCK2)和BRD4，抑制细胞自噬，并展现抗疟疾、抗病毒、抗细菌及抗变形虫效果。

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

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。