HIF-1/2α-IN-2

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-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。

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].

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。

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。