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 (IC50: 16 nM in scintillation proximity assay).

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-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 .

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-6 (117) is a HIF-2α inhibitor [1].

HIF-2α-IN-5 is a potent HIF-2α inhibitor with an IC 50 of < 50 nM [1].

HIF-2α-IN-9 (compound 35r) serves as an HIF-2α inhibitor, effectively suppressing VEGF-A with an IC50 of 305 nM, and modulating growth-promoting genes within tumor cells while reactivating macrophage-mediated tumor immunity [1].

HIF-2α-IN-1 is a potent HIF-2α inhibitor with IC50 values less than 500 nM.

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-1α-IN-2 is a novel and highly potent HIF-1α inhibitor with anticancer and antitumor activity that inhibits the expression of HIF-1α and VEGF in a dose-dependent manner and inhibits cell migration.

HIF-1α-IN-2 hydrochloride is a potent HIF-1α inhibitor exhibiting anticancer activity, demonstrated by IC50 values of 28 nM in MDA-MB-231 cells and 15 nM in MiaPaCa-2 cells. It effectively suppresses HIF-1α expression by inhibiting both transcription and protein translation [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].

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.

PT-2385 is a selective HIF-2α inhibitor (Kd<50 nM).

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

This novel compound is an orally bioavailable antagonist of P2X3/P2X2/3 receptors, exhibiting potent activity with a pIC50 of 8 in both human and rat, and a pIC50 of 7.3 specifically for the human P2X2/3 receptor. It demonstrates high brain penetration, evidenced by a brain to plasma ratio of 6, and effectively blocks agonist-evoked intracellular Ca2+ flux and inward currents within the nanomolar range (10 nM to 1 µM) in cell lines that express human P2X3 and P2X2/3 receptors recombinantly. The compound also shows favorable pharmacokinetic properties, with a half-life (t1/2) of 1.63 hours and a time to reach maximum concentration (Tmax) of 30 minutes.

Chetomin (BRN0077366) is an inhibitor of HIF-1 by weaken transcription of HIF-1, disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar concentrations.

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

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......

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].

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

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

T1001 is an antagonist of hypoxia-inducible factor-2α subunit (HIF-2α) which displaces residue M252 from inside the HIF-2α PAS-B pocket toward the ARNT subunit to weaken heterodimerization.

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.

M1001 is a HIF-2α agonist.

FM19G11 is an inhibitor of hypoxia inducible factor (HIF) α-subunit (IC50 = 80 nM in hypoxia induced luciferase assay).

TC-S 7009 is a potent and selective HIF-2α inhibitor (Kd: 81 nM). The affinity of TC-S 7009 to HIF-2α was higher than that of HIF-1α (Kd >> 5μM). TC-S 7009 disrupts HIF-2α heterodimerization, reduces HIF-2α target gene expression, and reduces dna binding activity.

Roxadustat-13C-15N is 13C and 15N labeled Roxadustat.

Roxadustat (FG-4592) is an orally bioavailable, hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI), with potential anti-anemic activity.

Roxadustat-13C2-15N is 13C and 15N labeled Roxadustat.