hif-2α

HIF-2α agonist 2 is an HIF-2α agonist with an EC50 value of 1.68 μM for HIF-2α. HIF-2α agonist 2 can promote the stability of the ARNT A/B ring in the 3z structure of HIF-2a-ARNT complex without cytotoxicity to 786-o-Reha-Luc cells. HIF-2α agonist 2 can be used in the study of oxygen metabolism and is closely related to the occurrence of cancer.

HIF-2α-IN-2 is a hypoxia-inducible factor (HIF-2α) inhibitor with an IC50 of 16 nM in scintillation proximity assay (SPA).

HIF-2a translation inhibitor is a potent HIF-2α translation inhibitor with IC50=5 μM that inhibits constitutive and hypoxia-induced HIF-2α protein expression. Among them, HIF-2α-IN-4 associates the 5'UTR iron response element with oxygen sensing.

HIF-2α-IN-3 is a HIF-2α alteration inhibitor with anti-tumor properties and may be used in the study of cardiovascular disease.

HIF-2α-IN-1 is a potent inhibitor of HIF-2α, with IC50 values below 500 nM.

Belzutifan (MK-6482) is a potential treatment for clear cell renal cell carcinoma (ccRCC). Belzutifan is an orally active and selective HIF-2α inhibitor (IC50: 9 nM). Belzutifan , as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile.

AKB-6899 is an inhibitor of prolyl hydroxylase domain 3 (PHD3) and increases the soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages. AKB-6899 leads to stabilization of HIF-2α which induces sVEGFR-1 production from tumor-associated macrophages and decreases tumor growth.

M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist that enhances the affinity of HIF-2alpha and ARNT for transcriptional activation. It alters the Tyr2 conformation of the HIF-2alpha PAS-B structural domain and acts synergistically with inhibitors of the prolyl hydroxylase structural domain (PHD).

PT-2385 is a selective inhibitor of HIF-2α with a dissociation constant (Kd) of less than 50 nM (Kd<50 nM).

Allopurinol (Zyloric) is a Xanthine Oxidase Inhibitor. The mechanism of action of allopurinol is as a Xanthine Oxidase Inhibitor.

2-Methoxyestradiol (2-ME2) is an orally bioavailable estradiol metabolite with potential antineoplastic activity. 2-Methoxyestradiol inhibits angiogenesis by reducing endothelial cell proliferation and inducing endothelial cell apoptosis. This agent also inhibits tumor cell growth by binding to tubulin, resulting in antimitotic activity, and by inducing caspase activation, resulting in cell cycle arrest in the G2 phase, DNA fragmentation, and apoptosis.

(Rac)-PT2399 is a potent and specific inhibitor of hypoxia-inducible factor 2a (HIF-2α)(IC50 of 0.01 μM).

PT2399 shows effective antitumor activity in vivo. PT2399 is an effective and selective HIF-2α antagonist, which directly binds to the HIF-2α PAS B domain (IC50: 6 nM).

THS-044 (N-[2-Nitro-4-(Trifluoromethyl)phenyl]morpholin-4-Amine) binding stabilizes the HIF2α PAS-B folded state with a kd of 2 μM and regulates HIF2 activity in endogenous and clinical settings.

TC-S 7009 is a potent and selective HIF-2α inhibitor (Kd: 81 nM) with significantly higher affinity for HIF-2α than HIF-1α (Kd >> 5μM). TC-S 7009 disrupts HIF-2α heterodimerization, reduces HIF-2α target gene expression, and diminishes DNA binding activity.

HIF-2α agonist 3 (Compound 14d) is an orally active HIF-2α agonist with an EC50 value of 1.78 μM and is applicable in research on renal anemia.

HIF-2α-IN-6 (117) is a HIF-2α inhibitor [1].

HIF-2α-IN-5 is a potent HIF-2α inhibitor with an IC50 of less than 50 nM [1].

Allopurinol Sodium is a xanthine oxidase inhibitor with an IC50 of 7.82±0.12 μM.

HIF-2α-IN-7 is a hypoxia inducible factor 2α (HIF-2α) inhibitor. HIF-2α-IN-7 can inhibit HIF-2α with an EC 50 value of 6 nM. HIF-2α-IN-7 can be used for the research of various types of diseases including cancer , liver disease, inflammatory disease, pulmonary diseases and iron load disorders .

M1001 is a HIF-2α agonist.

HIF-2α-IN-9 (compound 35r) is an HIF-2α inhibitor that effectively suppresses VEGF-A with an IC50 of 305 nM, modulates growth-promoting genes within tumor cells, and reactivates macrophage-mediated tumor immunity [1].

HIF-2α-IN-13 (18) acts as a HIF-2α inhibitor and exhibits an IC 50 value of 2.7 μM.

HIF-2α-IN-14 (18) acts as a HIF-2α inhibitor, exhibiting an IC 50 value of 0.27 μM.