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-B0639C
    Amifostine sodium
    		Activator
    Amifostine sodium (WR2721 sodium) is a phosphorus sulfate with radioprotective activity. Amifostine sodium can cause splenic vasodilation and may block autonomic ganglia. Amifostine sodium is clinically used to prevent cisplatin-induced ototoxicity.
    Amifostine sodium
  • 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-P10221A
    Cyclo(CKLIIF) TFA
    		Inhibitor
    Cyclo CKLIIF 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 2.6 and 2.2 μM, respectively.
    Cyclo(CKLIIF) TFA
  • HY-B0239S2
    Threo-Chloramphenicol-d6
    Threo-Chloramphenicol-d6 is the deuterium labeled Chloramphenicol[1]. Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research[2][3][4].
    Threo-Chloramphenicol-d<sub>6</sub>
  • 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-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-B1625R
    Deferoxamine (Standard)
    		Activator
    Deferoxamine (Standard) is the analytical standard of Deferoxamine. This product is intended for research and analytical applications. Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19.
    Deferoxamine (Standard)
  • HY-N6030
    (Rac)-Dencichine
    (Rac)-Dencichine ((Rac)-Dencichin) is the racemate of Dencichin. Dencichin is a non-protein amino acid originally extracted from Panax notoginseng, and can inhibit HIF-prolyl hydroxylase-2 (PHD-2) activity.
    (Rac)-Dencichine
  • 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-P5915
    FAM-DEALA-Hyp-YIPMDDDFQLRSF-NH2
    		Agonist
    FAM-DEALA-Hyp-YIPMDDDFQLRSF-NH2, a 5-FAM labeled HIF-1α peptide, is a substrate of VHL. FAM-DEALA-Hyp-YIPMDDDFQLRSF-NH2 binds to VHL protein with a KD of 3 nM. Ex/Em (λ) = 485/520 nm.
    FAM-DEALA-Hyp-YIPMDDDFQLRSF-NH2
  • HY-147426
    Zifcasiran
    		Inhibitor
    Zifcasiran is a hypoxia-inducible factor (HIF) synthesis reducer. Zifcasiran shows antitumor activities and can be used in advanced renal cell carcinoma research.
    Zifcasiran
  • HY-N6905
    Acetylarenobufagin
    		Modulator
    Acetylarenobufagin is a steroidal hypoxia inducible factor-1 (HIF-I) modulator.
    Acetylarenobufagin
  • HY-B0464S
    Hydralazine-d4 hydrochloride
    		Activator
    Hydralazine-d4 hydrochloride is the deuterium labeled Hydralazine hydrochloride. Hydralazine hydrochloride is a direct-acting vasodilator that is used as an antihypertensive agent.
    Hydralazine-d<sub>4</sub> hydrochloride
  • HY-146540
    GEM-5
    		Inhibitor
    GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth.
    GEM-5
  • HY-163603
    HIF-2α-IN-16
    		Inhibitor
    HIF-2α-IN-16 (48) is a HIF-2α inhibitor, with an IC50 of 0.091 μM.
    HIF-2α-IN-16
  • HY-144176
    HIF-2α-IN-5
    		Inhibitor
    HIF-2α-IN-5 is a potent HIF-2α inhibitor with an IC50 of < 50 nM.
    HIF-2α-IN-5
  • HY-N0733S5
    Glucosamine-13C6,15N hydrochloride
    Glucosamine-13C6,15N (hydrochloride) is the 13C and 15N labeled Glucosamine hydrochloride. Glucosamine hydrochloride (D-Glucosamine hydrochloride) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids,
    Glucosamine-<sup>13</sup>C<sub>6</sub>,<sup>15</sup>N hydrochloride
  • HY-156527
    PHD-IN-2
    		Inhibitor
    PHD-IN-2 (Compound 91) is a PHD antagonist (IC50: < 5 nM). PHD-IN-2 induces erythropoietin synthesis in HEP3B cells (EC50: <2.5 μM). PHD-IN-2 can be used for research of cardiovascular disorders, metabolic disorders, hematological disorders, pulmonary disorders, kidney disorders, liver disorders, wound healing disorders, and cancer.
    PHD-IN-2
Cat. No. Product Name / Synonyms Application Reactivity
HIF/HIF Prolyl-Hydroxylase Isoform Comparison

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