2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Phosphodiesterase (PDE)

Phosphodiesterase (PDE)

Phosphodiesterase (PDE)

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Phosphodiesterase (PDE) is any enzyme that breaks a phosphodiester bond. Usually, people speaking of phosphodiesterase are referring to cyclic nucleotide phosphodiesterases, which have great clinical significance and are described below. However, there are many other families of phosphodiesterases, including phospholipases C and D, autotaxin, sphingomyelin phosphodiesterase, DNases, RNases, and restriction endonucleases, as well as numerous less-well-characterized small-molecule phosphodiesterases. The cyclic nucleotide phosphodiesterases comprise a group of enzymes that degrade the phosphodiester bond in the second messenger molecules cAMP and cGMP. They regulate the localization, duration, and amplitude of cyclic nucleotide signaling within subcellular domains. PDEs are therefore important regulators ofsignal transduction mediated by these second messenger molecules.

Phosphodiesterase (PDE) Isoform Specific Products:

Phosphodiesterase (PDE) Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-14841
    Gisadenafil
    		Inhibitor
    Gisadenafil (UK-369003) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP).
    Gisadenafil
  • HY-132821B
    (R)-Irsenontrine
    		Inhibitor 99.00%
    (R)-Irsenontrine ((R)-E2027), the R-enantiomer of Irsenontrine (HY-132821), is a potent phosphodiesterase 9 (PDE9) inhibitor with an IC50 value of 0.041 μM. (R)-Irsenontrine can be used for the research of neurological diseases.
    (R)-Irsenontrine
  • HY-153766
    PDE5-IN-9
    		Inhibitor ≥98.0%
    PDE5-IN-9 (Compound 59) is a PDE5 inhibitor (IC50: 11.2 μM). PDE5-IN-9 shows interaction with Gln 817, Tyr 612, and Ala 767 amino acid residues. PDE5-IN-9 can be used for research of cardiovascular disease.
    PDE5-IN-9
  • HY-153733
    PDE5-IN-8
    		Inhibitor
    PDE5-IN-8 (compund 2) is a PDEs inhibitor.
    PDE5-IN-8
  • HY-169300
    KR-40795
    		Inhibitor
    KR-40795 is a potent inhibitor of ATX (autotaxin), with the IC50 of 0.13 μM. KR-40795 plays an important role for liver diseases.
    KR-40795
  • HY-172870
    PDE4B-IN-4
    		Inhibitor
    PDE4B-IN-4 (Compound 11E) is a PDE4B (IC50: 2.82 nM) and TNF-α (IC50: 7.20 nM) inhibitor. PDE4B-IN-4 inhibits neutrophilia in a mouse lipopolysaccharide (LPS)-induced sepsis model and exhibits anti-inflammatory activity.
    PDE4B-IN-4
  • HY-B0442CR
    Vardenafil dihydrochloride (Standard)
    		Inhibitor
    Vardenafil (dihydrochloride) (Standard) is the analytical standard of Vardenafil (dihydrochloride). This product is intended for research and analytical applications. Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes-.
    Vardenafil dihydrochloride (Standard)
  • HY-153334
    Enpp-1-IN-15
    		Inhibitor
    Enpp-1-IN-15 (Compound 88a) is an Ectonucleotide Pyrophosphatase/Phosphodiesterase 1 (Enpp-1) Inhibitor, with a Ki value of 0.00586 nM.
    Enpp-1-IN-15
  • HY-15455S2
    Roflumilast-d3
    		Inhibitor
    Roflumilast-d3 is deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
    Roflumilast-d<sub>3</sub>
  • HY-B0523AR
    Anagrelide hydrochloride (Standard)
    		Inhibitor
    Anagrelide (hydrochloride) (Standard) is the analytical standard of Anagrelide (hydrochloride). This product is intended for research and analytical applications. Anagrelide hydrochloride (BL4162A) is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide hydrochloride, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide hydrochloride inhibits bone marrow megakaryocytopoiesis. Anagrelide hydrochloride decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide hydrochloride is a platelet-lowering agent and plays in the antithrombopoietic action.
    Anagrelide hydrochloride (Standard)
  • HY-106137
    Tofimilast
    		Inhibitor
    Tofimilast is an inhibitor of Phosphodiesterase 4 (PDE4) with an IC50 of 0.14 μM. Tofimilast exerts its anti-inflammatory effects by inhibiting the activity of PDE4, thereby increasing intracellular levels of cAMP.
    Tofimilast
  • HY-146123
    ATX inhibitor 20
    		Inhibitor
    ATX inhibitor 20 (compound 24) is a potent ATX (autotaxin) inhibitor, with an IC50 of 2.3 nM.
    ATX inhibitor 20
  • HY-169071S
    ATX-1905
    		Inhibitor
    ATX-1905 is a positron emission tomography (PET) tracer that demonstrates good autotaxin (ATX) binding specificity and achieves semiquantification of lung ATX expression levels, which are elevated in fibrotic lungs. ATX-1905 exhibits elevated uptake in Bleomycin (HY-108345)-induced pulmonary fibrosis (BPF) lungs. ATX-1905 is promising for research of idiopathic pulmonary fibrosis (IPF).
    ATX-1905
  • HY-19003A
    Isomazole hydrochloride
    		Inhibitor
    Isomazole (323MHb) hydrochloride is a cardiotonic agent. Isomazole hydrochloridei increases the calcium sensitivity in atrial fibers and has a direct effect on contractile proteins.
    Isomazole hydrochloride
  • HY-129210
    KMUP-4
    		Inhibitor
    KMUP-4, as a xanthine derivative with cGMP-enhancing activity, induces aortic relaxation through endothelium-dependent and independent mechanisms. KMUP-4 increases cytoplasmic cyclic guanosine monophosphate (cGMP) and cyclic adenosine monophosphate (cAMP) levels by inhibiting phosphodiesterases (PDEs) and activating K+ channels. KMUP-4 can be used in the study of cardiovascular diseases.
    KMUP-4
  • HY-121421
    Diniprofylline
    		Inhibitor
    Diniprofylline, a bronchodilator, is a phosphodiesterase inhibitor. Diniprofylline possesses the potential to interact with human ACE2 and prevent its recognition by SARS-CoV-2.
    Diniprofylline
  • HY-143420
    ATX inhibitor 15
    		Inhibitor
    ATX inhibitor 15 (compound 30), a indole-based carbamate derivative, is a potent autotaxin (ATX) inhibitor with an IC50 of 2.17 nM. ATX inhibitor 15 inhibits in vivo ATX and the gene expression of pro-fibrotic factors. ATX inhibitor 15 has lung protection effects in Bleomycin challenged mice lung fibrosis model.
    ATX inhibitor 15
  • HY-147991
    PDE5/HDAC-IN-1
    		Inhibitor
    PDE5/HDAC-IN-1 (Compound 26) is a potent phosphodiesterase 5 (PDE5) and HDAC inhibitor with IC50 values of 46.3 nM and 14.5 nM, respectively. PDE5/HDAC-IN-1 induces cell apoptosis and shows anticancer activities.
    PDE5/HDAC-IN-1
  • HY-N3180
    Norbraylin
    		Inhibitor
    Norbraylin, a natural prenylated coumarin, is a PDE4D2 inhibitor with an IC50 value of 7.15 μM.
    Norbraylin
  • HY-162797
    PDE4-IN-18
    		Inhibitor
    PDE4-IN-18 (compound 1l) is a PDE4 inhibitor (IC50=1.55 μM) with anti-inflammatory activity. PDE4-IN-18 exerts anti-inflammatory effects by reducing excessive immune cell infiltration and intestinal membrane formation, as well as reducing the mRNA expression of pro-inflammatory cytokines (such as TNF-α and IL-6) in synovial tissue. PDE4-IN-18 can be used in the study of rheumatoid arthritis and psoriasis.
    PDE4-IN-18
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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