hif/hif prolyl-hydroxylase

Prolyl-4-hydroxylase Inhibitor 11, a novel proline 4-hydroxylase inhibitor, shows protective effects against oxidative stress and Cu(II) toxicity in Chlorella vulgaris.

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 alpha (556-574) is a hypoxia-inducible factor-1 19-mer fragment. HIF-1 functions as master regulator of response to oxygen homeostasis. Hypoxia-induced gene expression is initiated when HIF-1subunit is stabilized in response to a lack of oxygen. Thi

HIF-PHD-IN-3 is a potent hiPSC-CM cardioprotective scaffold with potential inhibitory effects on HIF-PHD, regulates heme oxygenase-1, and can be used to study anaemia.

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

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

Prolyl Hydroxylase inhibitor 1 is an orally active inhibitor of hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) (IC50 of 62.23 nM).

HIF-PHD-IN-1 is a pharmacological compound that acts as an orally active inhibitor of the hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), displaying an IC50 of 54 nM for hHIF-PHD2. Its potential as a therapeutic agent for renal anemia is highly promising.

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-1α inhibitor-1 is a HIF-1 alpha inhibitor.

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 inhibitor-1 is an aryl carboxamide compound and a potent hypoxia-inducible factor 1 (HIF-1) inhibitor with an IC50 of 0.32 μM for the cancer metastasi[1]. [1]. Liu M, et al. Discovery of Novel Aryl Carboxamide Derivatives as Hypoxia-Inducible Factor 1α Signaling Inhibitors with Potent Activities of Anticancer Metastasis. J Med Chem. 2019 Oct 24;62(20):9299-9314.

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.

HIF-1α-IN-5 is an inhibitor of HIF-1α with an IC 50 value of 24 nM in HEK293T cells that also inhibits the activity of MAO-A. HIF-1α-IN-5 downregulates the mRNA expressions of VEGF and PDK1 under hypoxia. HIF-1α-IN-5 has the potential to be used in the cancer research[1].

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-3, also known as Compound (S)-3f, is a hypoxia-selective inhibitor of HIF-1α. It exhibits potent antiestrogenic activity [1].

HIF-1 inhibitor-5 (Compound 16e) is a potent inhibitor of HIF-1, exhibiting an IC50 value of 2.38 μM and demonstrating significant anti-angiogenic potential [1].

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-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-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-IN-33 is an inhibitor of HIF pathway.

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

HIF-PHD-IN-2 (compound 25) is a highly effective PHD inhibitor, displaying IC50 values below 100 nM for PHD1, PHD2, and PHD3 [1].

This is a hypoxia-inducible factor-1 (HIF-1 a) 19-mer fragment. HIF-1 functions as master regulator of response to oxygen homeostasis. Hypoxia-induced gene expression is initiated when HIF-1 subunit is stabilized in response to a lack of oxygen. This part

HIF-1α-IN-4 is an inhibitor of HIF-1α with IC50 of 24 nM in HEK293T cells which has potential antitumor effects. HIF-1α-IN-4 downregulates VEGF and PDK1 mRNA expressions under hypoxia [1].

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.

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.

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

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.

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.

1,4-DPCA is an inhibitor of prolyl-hydroxylase with an IC50 of 2.4 µM for collagen hydroxylation in human foreskin fibroblasts and 60 μM for factor inhibiting HIF (FIH).

M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist that enhances the affinity of HIF-2alpha and ARNT for transcriptional activation.M1002 alters the Tyr2 conformation of the HIF-281alpha PAS-B structural domain and acts synergistically with inhibitors of the prolyl hydroxylase structural domain (PHD).

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

1. Deoxyshikonin (Arnebin 7) may be a new drug candidate for wound healing and treatment of lymphatic diseases. 2. Deoxyshikonin enhances the ability of human dermal lymphatic microvascular endothelial cells (HMVEC-dLy) to undergo time-dependent in vitro cord formation. 3. Deoxyshikonin and dodecyl gallate show significantly synergic antimicrobial activity with penicillin in vivo and in vitro, and can effectively reduce nasopharyngeal and lung colonization caused by different penicillin-resistant pneumococcal serotypes.

IDF-11774 is a HIF-1 inhibitor.It reduces hif-1α HRE luciferase activity (IC50 = 3.65 μM).

BAY 87-2243 is a potent and selective inhibitor of hypoxia-inducible factor-1 (HIF-1).

Chlorogenic acid, as a major phenolic compound in honeysuckle, possesses potential antioxidant, antibacterial, anti-inflammatory, and anticancer activities. It can be utilized in research related to the treatment of advanced cancer and impaired glucose tolerance.

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

LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor.

KC7F2 is a potent HIF-1 pathway inhibitor with potential anti-cancer activity.

Molidustat (BAY 85-3934)(BAY-85-3934), an inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase (PH), stimulates erythropoietin (EPO) production and the formation of red blood cells.

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

Chloramphenicol (Chloromycetin), a broad-spectrum antibiotic, blocks bacterial protein synthesis.

1. Oroxylin A (Baicalein 6-methyl ether) has various anti-tumor effects including apoptosis, cell cycle arrest, drug-resistant reversion. 2. Oroxylin A possesses abilities of inhibiting the ATRA-induced IL-6 production via modulation of LAP/LIP/CHOP in leukemia cell lines, which could providing a therapeutic strategy for RAS. 3. Oroxylin A inhibits UCP2s triggers the MPTP opening, and promotes the apoptosis in CaCo-2 cells; uncoupling protein 2 plays a key role in mitochondrial apoptotic pathway. 4. Oroxylin A inhibits N1ICD translocating to the nucleus and binding to epithelial-mesenchymal transition-related transcription factor Snail, thus suppressing the invasion and migration of MCF-7 cells. 5. Oroxylin A improves the sensitivity of K562/ADM cells by increasing apoptosis in leukemic cells and decreasing the expression of CXCR4 and PI3K/Akt/NF-κB pathway, and probably served as a most promising agent for CML treatment.