2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. HIF/HIF Prolyl-Hydroxylase

HIF/HIF Prolyl-Hydroxylase

Hypoxia-inducible factors; HIFs; HIF-PH

HIF/HIF Prolyl-Hydroxylase

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HIFs (Hypoxia-inducible factors) are transcription factors that respond to changes in available oxygen in the cellular environment, to be specific, to decreases in oxygen, or hypoxia. The HIF signaling cascade mediates the effects of hypoxia, the state of low oxygen concentration, on the cell. Hypoxia often keeps cells from differentiating. However, hypoxia promotes the formation of blood vessels, and is important for the formation of a vascular system in embryos, and cancer tumors. The hypoxia in wounds also promotes the migration of keratinocytes and the restoration of the epithelium. In general, HIFs are vital to development. In mammals, deletion of the HIF-1 genes results in perinatal death. HIF-1 has been shown to be vital to chondrocyte survival, allowing the cells to adapt to low-oxygen conditions within the growth plates of bones. HIF plays a central role in the regulation of human metabolism. Recently, several drugs that act as selective HIF prolyl-hydroxylase inhibitors have been developed.

HIF/HIF Prolyl-Hydroxylase Isoform Specific Products:

HIF/HIF Prolyl-Hydroxylase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-172201
    NF-κB-IN-19
    		Inhibitor
    NF-κB-IN-19 (Compound 8) is an NF-κB inhibitor. NF-κB-IN-19 effectively induces DNA damage, promotes the generation of ROS, and induces autophagy and apoptosis through the NF-κB signaling pathway in tumor cells. In addition, NF-κB-IN-19 can inhibit the levels of VEGF and HIF-1α, and exert antiproliferative activity in tumor cells through the PI3K/AKT and STAT-3 pathways. NF-κB-IN-19 can effectively overcome cisplatin resistance and has anti-tumor activity.
    NF-κB-IN-19
  • HY-W016409R
    Ethyl 3,4-dihydroxybenzoate (Standard)
    		Inhibitor
    Ethyl 3,4-dihydroxybenzoate (Standard) (Protocatechuic acid ethyl ester (Standard)) is the analytical standard of Ethyl 3,4-dihydroxybenzoate (HY-W016409). This product is intended for research and analytical applications. Ethyl 3,4-dihydroxybenzoate (Protocatechuic acid ethyl ester) is an orally effective, blood-brain barrier-permeable, competitive prolyl hydroxylase (PHD) inhibitor that inhibits the hydroxylation modification of hypoxia-inducible factor (HIF) by PHD. Ethyl 3,4-dihydroxybenzoate stabilizes HIF-1α by inhibiting PHD, activates downstream pathways to induce autophagy and apoptosis of tumor cells, and regulates inflammatory responses, inhibits the NF-κB pathway, improves vascular permeability, and promotes osteoblast differentiation. Ethyl 3,4-dihydroxybenzoate has anti-tumor, anti-hypoxic injury, and bone metabolism regulation effects. It can also be used in the research of cardiovascular protection (such as reducing myocardial ischemic damage), bone tissue engineering (promoting osteogenesis/inhibiting osteoclast differentiation), and prevention and treatment of high-altitude cerebral edema.
    Ethyl 3,4-dihydroxybenzoate (Standard)
  • HY-124722
    OHM1
    		Inhibitor
    OHM1 is an analog of HIF1α CTAD that inhibits its binding with p300/CBP. OHM1 targets CH1 domain with an affinity of 0.53 μM.
    OHM1
  • HY-N12041
    Axl-IN-16
    		Inhibitor
    Axl-IN-16 is a dual inhibitor of Axl/HIF. Axl-IN-16 induces fruiting body formation of Flammulina velutipes. Axl-IN-16 inhibits hypoxia-inducible factor activity and receptor tyrosine kinase expression.
    Axl-IN-16
  • HY-163599
    HIF-2α-IN-12
    		Inhibitor
    HIF-2α-IN-12 (9) is a HIF-2α inhibitor, with an IC50 of 0.9 μM.
    HIF-2α-IN-12
  • HY-170917
    PHD2-IN-4
    		Inhibitor
    PHD2-IN-4 (compound 1) is a PHD2 inhibitor. PHD2-IN-4 inhibits PHD2 with an IC50 of 4 nM. PHD2-IN-4 is potential for chronic kidney disease research.
    PHD2-IN-4
  • HY-N13009
    MO-2097
    		Inhibitor
    MO-2097 is a RAF-1/HIF-1α inhibitor. MO-2097 induces RAF-1 destabilization, leading to a reduction in EMT-associated transcription factors and mesenchymal markers. MO-2097 inhibits HIF-1a protein expression mediated by hnRNPA2B1 under hypoxic and mimetic hypoxia. MO-2097 induces mitochondrial ROS, which leads to apoptosis in cells. MO-2097 effectively suppresses colorectal cancer metastasis by inhibiting the RAF/MEK/ERK signaling pathway. MO-2097 attenuates tumor growth in a xenograft HCT116 cell mouse model. MO-2097 can be used for the study of colorectal cancer.
    MO-2097
  • HY-164259
    AJM 290
    		Inhibitor
    AJM 290 is a Trx-1 inhibitor. AJM 290 is an inhibitor of the HIF-1α COOH-terminal transactivation domain, and blocks HIF-1 binding to DNA.
    AJM 290
  • HY-149260
    HIF-1 inhibitor-5
    		Inhibitor
    HIF-1 inhibitor-5 (Compound 16e) is a potent HIF-1 inhibitor with an IC50 of 2.38 μM. HIF-1 inhibitor-5 possesses anti-angiogenic potential.
    HIF-1 inhibitor-5
  • HY-15893G
    DMOG (GMP)
    		Inhibitor
    DMOG (GMP) is the GMP level of DMOG (HY-15893). GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. DMOG (GMP) is a HIF-1α stabilizer. DMOG (GMP) promotes the osteogenic, angiogenic, and chondrogenic differentiation of stem cells by stabilizing the expression of HIF-1α. DMOG (GMP) can enhance the osteogenic and angiogenic differentiation potential of stem cells, thereby improving bone regeneration in bone defects. DMOG (GMP) can be used in the research of bone defect repair, vascularized bone regeneration, and the treatment of bone-related diseases (such as osteoporosis and femoral head necrosis) .
    DMOG (GMP)
  • HY-162601
    D-01
    		Inhibitor
    D-01 is a dual-targeting inhibitor of HIF-1α and EZH2 (IC50: 4.86 μM and 0.99 μM respectively). D-01 inhibits the expression of H3K27me3 protein. D-01 inhibits the migration, clone and the invasion of A549 cells, and also inhibits tube formation of HUVECs. D-01 can be used for research of lung cancer.
    D-01
  • HY-180164
    DS79540454
    		Inhibitor
    DS79540454 is a HIF-PHD2 inhibitor with an IC50 0.26 μM. DS79540454 can be used in the research of renal anemia.
    DS79540454
  • HY-139993
    HIF-PHD-IN-2
    		Inhibitor
    HIF-PHD-IN-2 (compound 25) is a potent PHD inhibitor with IC50s of <100 nM for PHD1, PHD2 and PHD3, respectively.
    HIF-PHD-IN-2
  • HY-163597
    HIF-2α-IN-10
    		Inhibitor
    HIF-2α-IN-10 (17) is a HIF-2α inhibitor, with an IC50 of 0.05 μM.
    HIF-2α-IN-10
  • HY-P10223
    Cyclo(CRVIIF)
    		Inhibitor
    Cyclo CRVIIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains KD of 65 and 123 μM, respectively.
    Cyclo(CRVIIF)
  • HY-149635
    HIF-1α-IN-6
    		Inhibitor
    HIF-1α-IN-6 (compound 3s) is a HIF-1α inhibitor with IC50 values of 0.6 and 53.3 nM observed in MiaPaCa-2 and MDA-MB-231 cells. HIF-1α-IN-6 can inhibit HIF-1α expression by decreasing the level of HIF-1α mRNA.
    HIF-1α-IN-6
  • HY-170914
    JPHM-2-167
    		Inhibitor
    JPHM-2-167 (Compound 11) is a selective PHD (prolyl hydroxylase domain enzyme) inhibitor. JPHM-2-167 inhibits PHD2, PHD3 with IC50s of 0.253 μM and 3.95 μM, respectively. JPHM-2-167 can be used for chronic kidney disease .
    JPHM-2-167
  • HY-124875
    Arylsulfonamide 64B
    		Inhibitor
    Arylsulfonamide 64B (HIF inhibitor 64B) is an inhibitor of the hypoxia-induced factor (HIF). Arylsulfonamide 64B inhibits hypoxia/HIF-induced expression of c-Met and CXCR4 and reduces primary tumor growth and metastasis of uveal melanoma mouse model.
    Arylsulfonamide 64B
  • HY-W747868
    Molidustat sodium
    		Inhibitor
    Molidustat sodium is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat sodium can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat sodium can be utilized in the research of renal anemia.
    Molidustat sodium
  • HY-153510
    PHD-1-IN-2
    		Inhibitor
    PHD-1-IN-2 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain 1 (PHD-1) with an IC50 of 0.07 μM. PHD-1-IN-2 acts as a substrate of MDR1 in MDR1-MDCK cell monolayer assays. PHD-1-IN-2 can be used in the research of ischemia, inflammatory responses and neurodegenerative diseases, such as inflammatory bowel disease and ischemia-reperfusion injury.
    PHD-1-IN-2
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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