hif

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

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-1α-IN-6 (compound 3s) is a potent inhibitor of HIF-1α with IC50 values of 0.6 nM and 53.3 nM in MiaPaCa-2 and MDA-MB-231 cells, respectively, and it suppresses HIF-1α expression by reducing HIF-1α mRNA levels [1].

HIF-1 alpha (556-574) TFA is a 19-residue fragment of hypoxia-inducible factor-1 (HIF-1), the master regulator of oxygen homeostasis [1].

Deferoxamine(Desferrioxamine B) is an iron chelator (binds Fe(III) and many other metal cations) that inhibits neuronopathy, may be used to modify the reduction of iron accumulation and deposition in tissues, and may improve neurological dysfunction by inhibiting ferroptosis and neuroinflammation following traumatic brain injury.Desferrioxamin-B has antioxidant, antiproliferative, Deferoxamine has antioxidant, antiproliferative, and antitumor activities, and can induce HIF-1α production, apoptosis and autophagy in cancer cells.Desferrioxamin-B can be used in the treatment of acute iron toxicity and COVID-19 related diseases.

PX-478 is a HIF-1α inhibitor with selectivity, oral activity, and blood-brain barrier permeability. PX-478 has antitumor activity and also protects pancreatic β-cell function in diabetes mellitus and is used in type 2 diabetes mellitus research.

Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) is the major active ingredient of Garcinia cambogia and a derivative of citric acid, which effectively inhibits stone formation and HIF, and has antioxidation, anti-inflammation, and anti-tumor effects. It also competitively inhibits ATP citrate lyase, offering weight loss benefits.

DMOG (Dimethyloxalylglycine), an antagonist of the α-ketoglutarate cofactor, is an inhibitor for HIF prolyl hydroxylase.

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

HIF-IN-1 is a potent inhibitor of hypoxia-inducible factor (HIF-1), which is associated with tumor and cancer cell proliferation and inhibits HIF-1α protein aggregation.

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

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.

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-1 inhibitor-4 (HIF-1 inhibitor-4) is a HIF-1 inhibitor with IC50 of 560 nM. HIF-1 inhibitor-4 reduces the HIF-1α protein level without affecting its mRNA level.

Deferoxamine Mesylate (DFOM) is an iron chelator and ferroptosis inhibitor. Deferoxamine Mesylate binds free iron into a stable complex and reduces iron accumulation. Deferoxamine Mesylate up-regulates HIF-1α levels and induces apoptosis.

Citric acid trilithium salt tetrahydrate (Lithium citrate tribasic tetrahydrate) , the active component of Lithium, is a medicine used in the therapy of psychiatric disease. It has shown the effects of signaling pathways and metabolic in the brain based on the particular disease and clinical condition model. According to the reports, Citric acid trilithium salt tetrahydrate was used as a mood stabilizer when treating bipolar mood disorders (BD) and lower the risk of self-harm in BD patient. In addition,Citric acid trilithium salt tetrahydrate has been the choice drug in the therapy of acute manic episodes.Citric acid trilithium salt tetrahydrate also could dissolve uric acid crystals in urine achieved from patients with gout. Besides,Citric acid trilithium salt tetrahydrate have some dose-dependent side-effects. The the main side-effects of Lithium Citrate is the tendency to inhibit the prostatic acid phosphatase enzyme (PAP), which result in the accumulation of PAP.

Glucosamine (Chitosamine) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids. Supplemental glucosamine may help to rebuild cartilage and treat arthritis.

Minocycline hydrochloride (Minocycline HCl) is a tetracycline antibiotic with excellent absorption and tissue penetration that is used for several bacterial infections as well as treatment of acne. Minocycline hydrochloride can cause both an acute hepatitis-like syndrome occurring within 1 to 3 months of starting therapy or a more insidious chronic hepatitis with autoimmune features typically after long-term treatment.

Fenbendazole (Fenbendazol) is an antinematodal benzimidazole used in veterinary medicine.

Albendazole (SKF-62979) is used as a drug indicated for the treatment of a variety of worm infestations.

Chloramphenicol (Chloromycetin) is a broad-spectrum antibiotic that inhibits the biosynthesis of bacterial proteins. Chloramphenicol acts primarily on the 50S subunit of the bacterial 70S ribosome and is active against peptidyltransferases, inhibiting the formation of peptide bonds.

IOX2 (IOX 2) is a selective inhibitor of the Hypoxia Inducible Factor (HIF) Prolyl-Hydroxylases (PHD); active in cells with the IC50 value of 21 nM for PHD2 ELGN-1 and no inhibition at FIH (20uM).