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-N0560R
    Oroxylin A (Standard)
    		Inhibitor
    Oroxylin A (Standard) is the analytical standard of Oroxylin A. This product is intended for research and analytical applications. Oroxylin A is an active flavonoid compound with strong anti-cancer effects. Oroxylin A inhibits the IL-6/STAT3 pathway and NF-κB signaling, inhibits cell proliferation and induces apoptosis. Oroxylin A inhibits colitis-related carcinogenesis.
    Oroxylin A (Standard)
  • HY-169100
    Antiproliferative agent-57
    		Inhibitor
    Antiproliferative agent-57 (compound M2) is a tumor angiogenesis inhibitor. Antiproliferative agent-57 inhibits the secretion of VEGF in SiHa cells under hypoxic conditions (IC50=0.68 μM) without inducing cytotoxicity. Antiproliferative agent-57 can modulate the PI3K/AKT/mTOR and MAPK signaling pathways in tumor cells to inhibit the expression of HIF-1α and VEGF in tumor tissues.
    Antiproliferative agent-57
  • HY-N0596R
    Panaxadiol (Standard)
    		Inhibitor
    Panaxadiol (Standard) is the analytical standard of Panaxadiol. This product is intended for research and analytical applications. Panaxadiol (20(R)-Panaxadiol) is an orally active HIF-1α/STAT3 inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities.
    Panaxadiol (Standard)
  • HY-161586
    Chloramphenicol/BSA
    		Inhibitor
    Chloramphenicol/BSA is the antigen-adjuvant conjugate formed by the coupling of Chloramphenicol (HY-B0239) with Bovine Serum Albumin (BSA). By conjugating the antigen with a protein adjuvant, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or disrupt major epitopes, and it can enhance cross-presentation and the generation of antigen-specific T cells.
    Chloramphenicol/BSA
  • HY-180490
    eIF3e-IN-1
    		Inhibitor
    eIF3e-IN-1 (Compound 209) is an elF3e inhibitor with an EC50 of 18.3 μM. eIF3e-IN-1 significantly reduces the accumulation of HIF1α protein induced by hypoxia and inhibits the acute translation hypoxia response. eIF3e-IN-1 significantly inhibits the expression of ATF4 protein. eIF3e-IN-1 can be used in cancer research, such as in breast cancer studies.
    eIF3e-IN-1
  • HY-181097
    EGFR-IN-192
    		Inhibitor
    EGFR-IN-192 is an anticancer agent. EGFR-IN-192 inhibits EGFR (IC50: 0.12 μM), downregulates the HIF-VEGF and PI3K/AKT/mTOR pathways, upregulates the tumor suppressor gene PTEN, and induces cell cycle arrest and apoptosis in tumor cells. EGFR-IN-192 exhibits antitumor activity and can be used in tumor research.
    EGFR-IN-192
  • HY-181270
    RH01504
    		Inhibitor
    RH01504 is a HIF2α inhibitor with a Kd value of 5.42 nM against human HIF2α. RH01504 inhibits the growth of renal cancer cells. RH01504 can be used in research related to renal cell carcinoma.
    RH01504
  • HY-18259
    103D5R
    		Inhibitor
    103D5R (Compound 15) is an inhibitor for the activation of hypoxia-inducible factor-1 (HIF-1) with an IC50 of 35 µM, through reduction of the HIF-1α protein synthesis. 103D5R inhibits the proliferation of LN229 with IC50 of 26 µM.
    103D5R
  • HY-170027
    LW1564
    		Inhibitor
    LW1564 is an inhibitor for HIF-1α with an IC50 of 1.2 µM in HepG2. LW1564 inhibits mitochondrial respiration, reduces ATP production, stimulates HIF-1α degradation, and inhibits proliferation of various cancer cells with GI50 of 0.4-4.6 μM. LW1564 activates AMPK signaling pathway and inhibits lipid synthesis. LW1564 exhibits antitumor in HepG2 xenograft mouse model.
    LW1564
  • HY-176724
    ZnPc-O3-JQ1
    		Inhibitor
    ZnPc-O3-JQ1 is a light-triggered BRD4 degrader. Under illumination, ZnPc-O3-JQ1 generates reactive oxygen species (ROS) that degrades BRD4. The degradation of BRD4 results in downregulation of HIF-1α, thereby counteracting the photodynamic therapy (PDT) resistance induced by tumor hypoxia. ZnPc-O3-JQ1 exhibits both Type I and Type II PDT mechanisms. The structure of ZnPc-O3-JQ1 consists of three parts: BRD4 ligand (HY-78695); Linker (HY-W040165); Photosensitizer (HY-176725).
    ZnPc-O3-JQ1
  • HY-183638
    T7117
    		Inhibitor
    T7117 is a TRIM25-HIF-1α inhibitor. T7117 disrupts the interaction between TRIM25-HIF-1α. T7117 can be used for the research of glioblastoma.
    T7117
  • HY-P10222
    Cyclo(CRLLIF)
    		Inhibitor
    Cyclo CRLLIF 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 14.5 and 10.2 μM, respectively.
    Cyclo(CRLLIF)
  • HY-130133
    DHW-221
    		Inhibitor
    DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research.
    DHW-221
  • HY-173488
    NF-κB/HIF-1α-IN-1
    		Inhibitor
    NF-κB/HIF-1α-IN-1 (compound 9c) is a potent blocker of the NF-κB activation pathway and demonstrates selective anti-fibrotic activity. NF-κB/HIF-1α-IN-1 shows no significant cytotoxicity in NCI tumor cell lines. In rat models. NF-κB/HIF-1α-IN-1 has been shown to effectively ameliorate liver fibrosis by inhibiting the expression levels of NF-κB and HIF-1α, while simultaneously inducing the activation of Nrf2.
    NF-κB/HIF-1α-IN-1
  • HY-17412S
    Minocycline-d6 hydrochloride
    		Inhibitor
    Minocycline-d6 hydrochloride is deuterated labeled Minocycline hydrochloride (HY-17412). Minocycline hydrochloride is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline hydrochloride is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline hydrochloride shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline hydrochloride reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline hydrochloride inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect.
    Minocycline-d<sub>6</sub> hydrochloride
  • HY-147813
    HIF-1α-IN-3
    		Inhibitor
    HIF-1α-IN-3 (Compound (S)-3f) is a hypoxia-selective HIF-1α inhibitor. HIF-1α-IN-3 shows strong antiestrogenic potency.
    HIF-1α-IN-3
  • HY-124133
    JNJ-42905343
    		Inhibitor
    JNJ-42905343 is an orally active and highly selective prolyl hydroxylase (PHD1/2/3) inhibitor with pKI values of 8.07, 7.48 and 7.27 for PHD1, PHD2 and PHD3, respectively. JNJ-42905343 is promising for research of functional iron deficiency (FID) and anemia of chronic disease (ACD).
    JNJ-42905343
  • HY-163601
    HIF-2α-IN-14
    		Inhibitor
    HIF-2α-IN-14 (18) is a HIF-2α inhibitor, with an IC50 of 0.27 μM.
    HIF-2α-IN-14
  • HY-N0234R
    Bavachinin (Standard)
    		Inhibitor
    Bavachinin (Standard) is the analytical standard of Bavachinin. This product is intended for research and analytical applications. Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC50 value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity..
    Bavachinin (Standard)
  • HY-172257
    HIF-PHD-IN-4
    		Inhibitor
    HIF-PHD-IN-4 (Compound 13) is an orally active PHD2 inhibitor with an IC50 of 100 nM. HIF-PHD-IN-4 can effectively enhance the mobilization of hematopoietic stem cells induced by G-CSF in mice at a dose of 2 mg/kg. HIF-PHD-IN-4 is suitable for research in the field of tumor therapy .
    HIF-PHD-IN-4
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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