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-179647
    ZG-2686
    		Agonist
    ZG-2686 is a potent and selective HIF-2α agonist with an EC50 of 0.25 µM. ZG-2686 exhibits selectivity over PHD2. ZG-2686 binds to a specific internal cavity of HIF-2α, forming hydrogen bonds via structural water molecules, which stabilizes the HIF-2α/β heterodimer and enhances transcriptional activity. ZG-2686 synergizes with Vadadustat (HY-101277) to upregulate HIF-2α-dependent EPO gene expression both in vitro and in vivo. ZG-2686 can be used for the research of renal anemia.
    ZG-2686
  • HY-179424
    PROTAC HIF-1α degrader-2
    		Degrader
    PROTAC HIF-1α degrader-2 is a highly efficient and selective PROTAC degrader targeting HIF-1α. PROTAC HIF-1α degrader-2 promotes HIF-1α degradation via the ubiquitin-proteasome pathway by facilitating the formation of a HIF-1α/VHL ternary complex. PROTAC HIF-1α degrader-2 inhibits HeLa cell proliferation, migration, and colony formation, and induces apoptosis. PROTAC HIF-1α degrader-2 reduces p-MEK and p-AKT expression in the MAPK and PI3K/AKT pathways. PROTAC HIF-1α degrader-2 can be used for the study of cervical cancer.
    PROTAC HIF-1α degrader-2
  • HY-183996
    PHD-1 ligand-1
    PHD-1 ligand-1 (Compound 1) is a PHD-1 ligand. PHD-1 ligand-1 serves as a target protein ligand for the synthesis of PHD-1 PROTAC degraders, such as SH-26 (HY-183995). PHD-1 ligand-1 is applicable to studies on ischemia/reperfusion injury.
    PHD-1 ligand-1
  • HY-141625A
    TRC160334 sodium
    		Inhibitor
    TRC160334 sodium is a hypoxia-inducible factor (HIF) hydroxylase inhibitor. TRC160334 sodium can be used for the research of ischemia/reperfusion injury.
    TRC160334 sodium
  • HY-163600
    HIF-2α-IN-13
    		Inhibitor
    HIF-2α-IN-13 (18) is a HIF-2α inhibitor, with an IC50 of 2.7 μM.
    HIF-2α-IN-13
  • HY-179434
    HIF-1α-IN-10
    		Inhibitor
    HIF-1α-IN-10 is a ligands for target protein for PROTAC (HIF-1α). HIF-1α-IN-10 can be used to synthesize PROTAC HIF-1α degrader-2 (HY-179424).
    HIF-1α-IN-10
  • HY-179341
    CHNQD-03301
    		Inhibitor
    CHNQD-03301 is an orally active hypoxia-inducible factor-1α (HIF-1α) inhibitor (IC50 = 10.97 nM). CHNQD-03301 promotes the proteasomal degradation of HIF-1α protein, leading to its significant suppression. CHNQD-03301 can reverse HIF accumulation-induced angiogenesis and mitigate the HIF-induced erythrocytosis phenotype in zebrafish models. CHNQD-03301 can be used for the study of colon cancer.
    CHNQD-03301
  • 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-124079
    HIF-1/2α-IN-3
    HIF-1/2α-IN-3 (compund 33) is a HIF-1/2α inhibitor.
    HIF-1/2α-IN-3
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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