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-N11965
    4'-Methoxyisoagarotetrol
    		Inhibitor
    4'-Methoxyisoagarotetrol is chromone derivative and shows moderate PDE 3A inhibitory activity (IC50=54 μM).
    4'-Methoxyisoagarotetrol
  • HY-149782
    Phosphodiesterase-IN-1
    		Inhibitor
    Phosphodiesterase-IN-1 (Compound 7) is a phosphodiesterase (PDE) inhibitor with anti-Plasmodium activity. Phosphodiesterase-IN-1 has antiproliferative activity against P. falciparum (strain 3D7) with an IC50 value of 0.64 μM.
    Phosphodiesterase-IN-1
  • HY-B0442S
    Vardenafil-d5
    		Inhibitor
    Vardenafil-d5 is deuterium labeled Vardenafil. Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction.
    Vardenafil-d<sub>5</sub>
  • HY-132821A
    Irsenontrine maleate
    		Inhibitor
    Irsenontrine (E2027) maleate is an orally active and selective phosphodiesterase 9 (PDE9) inhibitor. Irsenontrine maleate can be used for the research of neurological diseases.
    Irsenontrine maleate
  • HY-A0027AS
    Fenspiride-d5
    		Inhibitor
    Fenspiride-d5 is the deuterium labeled Fenspiride. Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.
    Fenspiride-d<sub>5</sub>
  • HY-160864
    Torbafylline
    		Inhibitor
    Torbafylline is a PDE inhibitor. Torbafylline mitigates protein breakdown in rat skeletal muscle following burns by activating the PDE4/cAMP/EPAC/PI3K/Akt signaling pathway. Torbafylline suppresses the increased ubiquitin-proteasome-dependent protein degradation observed in the skeletal muscles of rats susceptible to cancer and sepsis.
    Torbafylline
  • 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-180803
    LH17
    		Inhibitor
    LH17, a Kaempferol (HY-14590) derivative, is a potent and selective PDE4 inhibitor (PDE4D2 IC50 = 73 nM, PDE4B2 IC50 = 190 nM). LH17 exhibits remarkable selectivity (>136-fold) against other PDE isoforms (PDE1B/2A/3A/5A/8A/9A/10A) (IC50 > 10000 nM), with the exception of PDE7A1 (IC50 = 300 nM). LH17 distinctly interacts with PDE4 M-pocket. LH17 demonstrates remarkable anti-fibrotic efficacy in both in vitro and in vivo models. LH17 can be used for idiopathic pulmonary fibrosis (IPF) research.
    LH17
  • HY-N10156
    1,3,5-Trihydroxy-4-prenylxanthone
    		Inhibitor
    1,3,5-Trihydroxy-4-prenylxanthone is a Na+/H+ exchange system inhibitor with a minimum inhibitory concentration of 10 μg/mL. 1,3,5-Trihydroxy-4-prenylxanthone is a phosphodiesterase type 5 (PDE5) inhibitor with an IC50 value of 3.0 μM. 1,3,5-Trihydroxy-4-prenylxanthone inhibits Lipopolysaccharide (LPS) (HY-D1056)-induced NO production in RAW264.7 macrophages, and has anti-inflammatory activities.
    1,3,5-Trihydroxy-4-prenylxanthone
  • HY-117390
    FR-181074
    		Inhibitor
    FR-181074 is a selective and orally active PDE V inhibitor. FR-181074 can specifically block PDE V to inhibit the degradation of cyclic guanosine monophosphate (cGMP) in order to relax smooth muscle. FR-181074 can be used for the researches of cardiovascular disease and endocrinology, such as hypertension and erectile dysfunction.
    FR-181074
  • HY-181549
    PDE4-IN-32
    		Inhibitor
    PDE4-IN-32 (Compound B05) is a selective, blood-brain barrier permeable PDE4B and PDE4D inhibitor with IC50 values of 13.7 nM and 23.8 nM, respectively. PDE4-IN-32 promotes the recovery of motor and cognitive function in MCAO/R mouse models. PDE4-IN-32 reduces cerebral edema. PDE4-IN-32 can be used for the research of ischemic stroke.
    PDE4-IN-32
  • HY-114052
    NVP-ABE171
    		Inhibitor
    NVP-ABE171 is an efficient, long-lasting and orally active PDE4 inhibitor with IC50 values for PDE4D, PDE4B, PDE4A and PDE4C of 1.5, 34, 602 and 1230 nM respectively. NVP-ABE171 enhances the cAMP accumulation induced by isoproterenol, inhibits the oxidative burst of eosinophils and the release of inflammatory cytokines from T cells and monocytes. NVP-ABE171 exhibits potent anti-inflammatory activity in animal models of asthma and pulmonary inflammation. NVP-ABE171 can be used for research on asthma and chronic obstructive pulmonary disease.
    NVP-ABE171
  • HY-175832
    PDE4B-IN-5
    		Inhibitor
    PDE4B-IN-5 (compound 84) is a PDE4B inhibitor, with an IC50 value <10 nM. PDE4B-IN-5 has anti-inflammatory activity.
    PDE4B-IN-5
  • HY-181684
    PDE5/CA-IN-1
    		Inhibitor
    PDE5/CA-IN-1 is a dual PDE5 and carbonic anhydrase (CA) inhibitor, with IC50 values of 0.41, 38.4, and 9.1 nM against PDE5, hCA II, and hCA VA, respectively. PDE5/CA-IN-1 inhibits multiple hCA subtypes associated with Alzheimer's disease. As a cytoprotective agent and oxidative stress alleviator, PDE5/CA-IN-1 reduces oxidative stress, and prevents recognition memory and working memory impairments. PDE5/CA-IN-1 is available for the research of Alzheimer's disease.
    PDE5/CA-IN-1
  • HY-182327
    PDE1-IN-12
    		Inhibitor
    PDE1-IN-12 (P78, the first compound in 12) is a PDE1 inhibitor. PDE1-IN-12 inhibits PDEl-mediated suppression of the dopamine D1 receptor intracellular pathway and can be used for narcolepsy.
    PDE1-IN-12
  • HY-126229
    PAT-078
    		Inhibitor
    PAT-078 is a type II autotaxin (ATX) inhibitor. PAT-078 mainly occupies the hydrophobic pocket of ATX, blocks the bottleneck region between the hydrophobic channel and the catalytic site, and does not interact with the zinc ion at the catalytic site.
    PAT-078
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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