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-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-174339
    Neuroprotective agent 12
    Neuroprotective agent 12 is an orally active and BBB-penetrable neuroprotective agent. Neuroprotective agent 12 has potent neuroprotective effects with robust anti-oxidation and anti-inflammation. Neuroprotective agent 12 significantly inhibits glutamate- and acrolein-induced cell death, reduces PDE4B expression but increases the HO-1, p-CREB and BDNF levels. Neuroprotective agent 12 exhibits potent neuroprotection in traumatic brain injury (TBI) mice model, promising for TBI and other central nervous system diseases.
    Neuroprotective agent 12
  • 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-177298
    PDE5-IN-15
    		Inhibitor
    PDE5-IN-15 (compound 21) is a xanthine derivative and PDE5 inhibitor, with IC50 values of 0.002, 0.180, 2.85 and 2.22 μM against hPDE5, bPDE6, bPDE1 and hPDE3, respectively. PDE5-IN-15 has good oral bioavailability in dogs. PDE5-IN-15 can be used in research on male erectile dysfunction.
    PDE5-IN-15
  • 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>
  • HY-162911
    Enpp-1-IN-22
    		Inhibitor
    Enpp-1-IN-22 is an orally bioavailable prodrug of the potent ENPP1 inhibitor paraformaldehyde with antitumor activity.
    Enpp-1-IN-22
  • HY-W759997
    Reproterol-d3
    Reproterol-d3 is the deuterium labeled Reproterol (HY-135490). Reproterol is a dual acting β2-adrenoceptor agonist and PDE inhibitor. The theophylline constituent of Reproterol inhibits phosphodiesterase activity induced by adenylyl cyclase. Reproterol has the potential for asthma research.
    Reproterol-d<sub>3</sub>
  • HY-175602
    TM-04-064-02
    		Degrader
    TM-04-064-02 is a molecular glue degrader. TM-04-064-02 induces proteins (such as IKZF1/3, PPIL4, ETF1 and PDE6D) to bind to CRBN, promoting their ubiquitination and degradation.
    TM-04-064-02
  • HY-108620
    CDP-840
    		Inhibitor
    CDP-840 (GR259653X) is a potent, selective and orally active phosphodiesterase IV (PDE IV) inhibitor. CDP-840 inhibits antigen-induced early and late phase bronchoconstriction in conscious squirrel monkeys.
    CDP-840
  • HY-106245
    HT-0712
    		Inhibitor
    HT-0712 is a Phosphodiesterase Type 4 (PDE4) inhibitor. HT-0712 enhances rehabilitation-dependent motor recovery and cortical reorganization after focal cortical ischemia.
    HT-0712
  • HY-135089
    Autotaxin-IN-5
    		Inhibitor
    Autotaxin-IN-5 (compound 63), extracted from patent WO2018212534A1, is an Autotaxin inhibitor. Autotaxin-IN-5 has the potential to treat idiopathic pulmonary fibrosis.
    Autotaxin-IN-5
  • HY-126754
    Archangelicin
    		Inhibitor
    Archangelicin is an inhibitor for cAMP-phosphodiesterase (cAMP-PDE) with IC50 >400 μM. Archangelicin inhibits nuclear factor of activated T cell (NFAT) with IC50 of 9 μM. Archangelicin exhibits antitumor and anti-inflammatory.
    Archangelicin
  • HY-B0549S
    Flavoxate-d5
    Flavoxate-d5 is deuterium labeled Flavoxate.
    Flavoxate-d<sub>5</sub>
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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