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-N3324
    Mangostanol
    		Inhibitor
    Mangostanol ((+)-Mangostanol) is a polyoxygenated xanthone mangostanol, which can be isolated from the shell of Garcinia mangostana, and has inhibitory effect on cAMP phosphodiesterase (PDE).
    Mangostanol
  • HY-124176
    L-6355
    		Inhibitor
    L-6355 is an Amiodarone (HY-14187) related compound, which inhibits Ca2+/calmodulin activated cyclic nucleotide phosphodiesterase with an IC50 value of 0.65 μM. L-6355 is promising for research of antiarrhythmic and antianginal agent.
    L-6355
  • HY-155687
    PDE5-IN-10
    		Inhibitor
    PDE5-IN-10 (compound 4b) is a potent PDE5 inhibitor with an IC50 of 20 nM. PDE5-IN-10 improves in vitro microsomal stability (t1/2 = 44.6 min) as well as excellent efficacy in restoring long-term potentiation. PDE5-IN-10 can be used for Alzheimer’s disease (AD) research.
    PDE5-IN-10
  • HY-B0523S
    Anagrelide-13C2,15N,d2
    		Inhibitor
    Anagrelide-13C2,15N,d2 is 15N and deuterated labeled Anagrelide (HY-B0523). Anagrelide is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide inhibits bone marrow megakaryocytopoiesis. Anagrelide decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide is a platelet-lowering agent and plays in the antithrombopoietic action.
    Anagrelide-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N,d<sub>2</sub>
  • HY-123743
    JNJ-42314415
    		Inhibitor
    JNJ-42314415 is a centrally active phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 35 nM and 64 nM for human recombinant PDE10A and rPDE10A, respectively.
    JNJ-42314415
  • HY-N10156
    1,3,5-Trihydroxy-4-prenylxanthone
    		Inhibitor
    1,3,5-Trihydroxy-4-prenylxanthone is a Na+/H+ exchange system (Na+/H+ Exchanger (NHE)) inhibitor with a minimum inhibitory concentration of 10 μg/mL. 1,3,5-Trihydroxy-4-prenylxanthone is a phosphodiesterase type 5 (PDE5) (Phosphodiesterase (PDE)) inhibitor with an IC50 value of 3.0 μM. 1,3,5-Trihydroxy-4-prenylxanthone inhibits Lipopolysaccharide (LPS) (Lipopolysaccharides (HY-D1056))-induced NO production in RAW264.7 macrophages, and has anti-inflammatory activities.
    1,3,5-Trihydroxy-4-prenylxanthone
  • HY-163604
    PDE4B/D-IN-1
    		Inhibitor
    PDE4B/D-IN-1 (example 8) is a potent inhibitor of PDE4B, with IC50s of 0.07 nM and 0.09 nM for PDE4B2 and PDE4D, respectively.
    PDE4B/D-IN-1
  • HY-161772
    (S)-Gebr32a
    		Inhibitor
    (S)-Gebr32a is a potent PDE4 inhibitor with IC50 values of 19.5, 2.1 µM for PDE4 cat; PDE4D3, respectively.
    (S)-Gebr32a
  • HY-126763
    ATI22-107
    		Inhibitor
    ATI22-107 is a dual-pharmacophore compound designed to simultaneously inhibit cardiac phosphodiesterase (PDE-III) and L-type calcium channels (LTCC), with activity that has specific effects on calcium cycling and contractility in cat ventricular myocytes and trabeculae.
    ATI22-107
  • HY-173483
    ATX inhibitor 26
    		Inhibitor
    ATX inhibitor 26 is an Autotaxin (ATX) inhibitor with an IC50 of 57 nM in human plasma. ATX inhibitor 26 inhibits cell migration and collagen gel contraction. ATX inhibitor 26 has significant anti-fibrotic effects, reducing collagen deposition in a Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis model.
    ATX inhibitor 26
  • HY-121162
    Mesembrine
    		Inhibitor
    Mesembrine ((+)-Mesembrine) a main alkaloid that features an aryloctahydroindole skeleton. Mesembrine is a 5-HT transporter inhibitor with a Ki of 1.4 nM. Mesembrine also inhibits phosphodiesterase 4B (PDE4B) with an IC50 of 7.8 μM.
    Mesembrine
  • HY-90009B
    12-epi-Tadalafil
    		Inhibitor
    12-epi-Tadalafil is a PDE5 inhibitor (IC50: 0.09 μM). 12-epi-Tadalafil can be used for research of cardiovascular diseases.
    12-epi-Tadalafil
  • HY-161506
    PDE1-IN-7
    		Inhibitor
    PDE1-IN-7 (Compound 13h) is a selective inhibitor of bPDE1 (IC50= 10 nM). PDE1-IN-7 exhibits significant anti-fibrotic effects in a BDL-induced liver fibrosis rat model. PDE1-IN-7 can be used for research in liver fibrosis.
    PDE1-IN-7
  • HY-100639R
    Roflumilast N-oxide (Standard)
    		Inhibitor
    Roflumilast N-oxide (Standard) is the analytical standard of Roflumilast N-oxide. This product is intended for research and analytical applications. Roflumilast N-oxide is a PDE type 4 inhibitor.
    Roflumilast N-oxide (Standard)
  • HY-157522
    NCI-14465
    		Inhibitor
    NCI-14465 is an ectonucleotide pyrophosphatase/phosphodiesterase (ENPP1) inhibitor with an IC 50 of 26.4 μM. NCI-14465 can be used in cancer research.
    NCI-14465
  • HY-167906S
    Hexadecyl 2-((4-Nitrophenyl)thio)acetate-13C2
    Hexadecyl 2-((4-Nitrophenyl)thio)acetate-13C2 is the 13C-labeled Lunamarine (HY-167906). Lunamarine is a inhibitor of PDE5 with BBB permeability. Lunamarine can be used in the reseach of Pulmonary Arterial Hypertension (PAH) and Erectile Dysfunction (ED).
    Hexadecyl 2-((4-Nitrophenyl)thio)acetate-<sup>13</sup>C<sub>2</sub>
  • HY-106088
    Tibenelast free acid
    		Inhibitor
    Tibenelast (LY186655) free acid is a potent and orally active is a phosphodiesterase inhibitor. Tibenelast free acid is an anti-asthma agent Tibenelast free acid increases the heart rate response to isoproterenol (HY-108353). Tibenelast free acid shows anti-anaphylactic shock activity. Tibenelast free acid has the potential for the research of asthma and other respiratory diseases.
    Tibenelast free acid
  • HY-132887
    PDE4-IN-3
    		Inhibitor
    PDE4-IN-3 is a novel and orally active PDE4 inhibitor with potent inhibitory affinity (IC50 = 4.2 nM).
    PDE4-IN-3
  • HY-161851
    MDL3
    		Inhibitor
    MDL3 is a novel inhibitor of PDE4B and PDE5A. MDL3 against liver injury and inflammation and inhibits the pathological remodeling of adipose tissue.
    MDL3
  • HY-14252S
    Milrinone-d3
    		Inhibitor
    Milrinone-d3 is deuterium labeled Milrinone. Milrinone is a PDE3 inhibitor, and also an inotrope and vasodilator.
    Milrinone-d<sub>3</sub>
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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