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-W700638A
    Benafentrine maleate
    		Inhibitor
    Benafentrine maleate is a platelet activating factor receptor (PAFR) antagonist and a PDE 4 inhibitor.
    Benafentrine maleate
  • HY-N13132
    Hellicoside
    		Inhibitor
    Hellicoside is a natural product that can be obtained from plantain. Hellicoside has inhibitory activity against cAMP phosphodiesterase and 5-lipoxygenase.
    Hellicoside
  • HY-N10149
    Nauclefine
    		Modulator
    Nauclefine is an indole alkaloid isolated from Nauclea officinalis. Nauclefine acts as a PDE3A modulator to induce cancer cell apoptosis through a PDE3A-SLFN12-dependent death pathway.
    Nauclefine
  • HY-P991677
    Efmirenpase alfa
    Efmirenpase alfa is an Fc-ENPP1 fusion protein (human IgG1 Fc domain linked to a modified human ENPP1). Efmirenpase alfa has prolonged half-life and enhanced receptor affinity compared with native human ENPP1. Efmirenpase alfa can be used as an enzyme replacement therapy for ENPP1 deficiency such as arterial calcification and hypophosphatemic rickets research.
    Efmirenpase alfa
  • HY-175047
    Enpp-1-IN-26
    		Inhibitor
    Enpp-1-IN-26 (Compound 4e) is an ENPP1 inhibitor with an IC50 of 0.188 μM. Enpp-1-IN-26 enhances IFN-β expression in vivo by preventing ENPP1 from hydrolyzing cGAMP. Enpp-1-IN-26 can be used in the research of metastatic breast cancer.
    Enpp-1-IN-26
  • HY-B1726
    Phenacaine
    		Inhibitor
    Phenacaine (Holocaine) is a local agent that can suppress or relieve pain. Phenacaine inhibits the specific calmodulin-dependent stimulation of erythrocyte Ca2+-ATPase and cyclic nucleotide phosphodiesterases from brain and heart.
    Phenacaine
  • HY-148625
    PDE9-IN-2
    		Inhibitor
    PDE9-IN-2 (compound 6) is a PDE9 inhibitor that improves heart failure.
    PDE9-IN-2
  • HY-90009AS1
    Tadalafil-13C2,d3-1
    Tadalafil-13C2,d3-1 (IC-351-13C2,d3-1) is the deuterium and 13C-labeled Tadalafil (HY-90009A). Tadalafil (IC-351) is a PDE5 inhibitor with an IC50 value of 1.8 nM.
    Tadalafil-13</sup>C<sub>2</sub>,d<sub>3</sub>-1
  • HY-125738
    Obscurolide A1
    		Inhibitor
    Obscurolide A1 is a Phosphodiesterase (PDE) inhibitor (IC50=8 mM) that can be obtained from Streptomyces viridochromogenes culture. Obscurolide A1 has the potential to study neurological and inflammatory diseases.
    Obscurolide A1
  • HY-145064
    Enpp-1-IN-6
    		Inhibitor
    Enpp-1-IN-6 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-6 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51).
    Enpp-1-IN-6
  • HY-P4108C
    Cys-TAT-HA2
    Cys-TAT-HA2 is a conjugate of Cys and TAT-HA2 (HY-P4108). Cys-TAT-HA2 is a transduction complex that can be introduced protein (such as Cardiac troponin C) into the cytoplasm of living cells. Cys-TAT-HA2 can be used for live tracking of exogenous proteins research.
    Cys-TAT-HA2
  • HY-18252S1
    Avanafil-13C5,15N,d2
    		Inhibitor
    Avanafil-13C5,15N,d2 is 15N and deuterated labeled Avanafil (HY-18252). Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis.
    Avanafil-<sup>13</sup>C<sub>5</sub>,<sup>15</sup>N,d<sub>2</sub>
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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