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-135632
    Hydroxychlorodenafil
    		Inhibitor
    Hydroxychlorodenafil (compound 40) is a phosphodiesterase (PDE) inhibitor. Hydroxychlorodenafil can be used in cancer research.
    Hydroxychlorodenafil
  • HY-171780
    ASP9831
    		Inhibitor
    ASP9831 is an orally active PDE4 inhibitor. ASP9831 inhibits LSP-induced TNF-α production and has anti-inflammatory activity. ASP9831 can be used in fatty liver disease research.
    ASP9831
  • HY-170765
    ATX-IN-1
    		Inhibitor
    ATX-IN-1 (compound 35) is an inhibitor of ATX (IC50=0.7 nM) with anti-inflammatory activity. ATX-IN-1 can inhibit TGF-β/Smad pathway and reduce collagen deposition to alleviate Bleomycin (HY-108345)-induced fibrosis in mice. ATX-IN-1 has good oral bioavailability (F=69.5%) and particle stability.
    ATX-IN-1
  • HY-167906
    Lunamarine
    		Inhibitor
    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).
    Lunamarine
  • HY-B0763S2
    Ibudilast-d7-1
    Ibudilast-d7-1 is the deuterium labeled Ibudilast. Ibudilast (KC-404;AV-411;MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia.
    Ibudilast-d<sub>7</sub>-1
  • HY-173509
    ATX inhibitor 27
    		Inhibitor
    ATX inhibitor 27 (Compound 31) is an ATX inhibitor. The IC50 values of ATX inhibitor 27 against human autotaxin (hATX) and lysophosphatidylcholine (LPC) are 13 nM and 23 nM, respectively. ATX inhibitor 27 reduces LPA levels in vivo by inhibiting ATX enzyme. ATX inhibitor 27 can be used in the study of ATX-LPA-related diseases such as inflammation, neurodegenerative diseases and cancer.
    ATX inhibitor 27
  • HY-143255
    Enpp-1-IN-11
    		Inhibitor
    Enpp-1-IN-11 (compound 23) is a potent Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor with an Ki value of 45 nM. Enpp-1-IN-11 exhibits low clearance in human and mouse liver microsomes, good plasma stability in human and mouse plasma. Enpp-1-IN-11 can be used for researching anticancer.
    Enpp-1-IN-11
  • HY-162582
    Z19153
    		Inhibitor
    Z19153 is a PDE4 inhibitor with IC50 values of 110 and 1160 nM for PDE4B1 and PDE4D7, respectively. Z19153 shows good liver protection against hepatic sepsis.
    Z19153
  • 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-163605
    PDE4B/D-IN-2
    		Inhibitor
    PDE4B/D-IN-2 (example 19) is a potent inhibitor of PDE4, with IC50s of 0.023 nM and 0.066 nM for PDE4B2 and PDE4D, respectively.
    PDE4B/D-IN-2
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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