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

Phosphodiesterase (PDE)

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-W011293
    DTA
    Inhibitor 99.98%
    DTA (2,4-Disulfamyl-5-trifluoromethylaniline) is a cyclic AMP phosphodiesterase inhibitor that binds to erythrocyte carbonic anhydrase.
    DTA
  • HY-143683S
    Theophylline-13C2,d6
    Theophylline-13C2,d6 (1,3-Dimethylxanthine-13C2,d6) is the deuterium labeled and 13C-labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    Theophylline-<sup>13</sup>C<sub>2</sub>,d<sub>6</sub>
  • HY-170431
    SAL-0010042
    Inhibitor
    SAL-0010042 is the inhibitor for Plasmodium phosphodiesterase β (PDEβ), that inhibits the hydrolysis of cAMP and cGMP (IC50=48.9 nM) in gametocytes, activates PKG, and inhibits the growth and development of Plasmodium (IC50 for 3D7 and Dd2 is 142 nM and 218 nM). SAL-0010042 inhibits hPDE5 and hPDE6 with IC50 of 632 nM and 73 nM.
    SAL-0010042
  • HY-108047
    MK-0873
    Inhibitor
    MK-0873 is a selective phosphodiesterase-4 (PDE4) inhibitor. MK-0873 increases intracellular levels of cyclic adenosine phosphate (cAMP) by inhibiting the activity of the PDE4 enzyme and subsequently activates protein kinase A (PKA). Activated PKA inhibits the activity of inflammatory cells and leads to direct relaxation of airway smooth muscle. MK-0873 can be used in studies of chronic obstructive pulmonary disease (COPD).
    MK-0873
  • 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-171544
    AGS-16C3F
    AGS-16C3F is an antibody-drug conjugate (ADC) targeting ENPP3. AGS-16C3F is composed of ENPP3-targeting Anti-ENPP3/CD203c Antibody (HY-P990315) linked to Monomethyl auristatin F (HY-15579) via a linker. AGS-16C3F has anti-tumor activity and can be used in the study of metastatic renal cell carcinoma (mRCC).
    AGS-16C3F
  • 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-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-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-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-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
Cat. No. Product Name / Synonyms Application Reactivity

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