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-121041
    GEBR-7b
    GEBR-7b is a selective PDE4D inhibitor with an IC50 of 0.67 μM. GEBR-7b increases hippocampal cAMP and does not influence Aβ levels in rodents. GEBR-7b also improves spatial and can be used for the study of cognitive deficits.
    GEBR-7b
  • HY-121421
    Diniprofylline
    		Inhibitor
    Diniprofylline, a bronchodilator, is a phosphodiesterase inhibitor. Diniprofylline possesses the potential to interact with human ACE2 and prevent its recognition by SARS-CoV-2.
    Diniprofylline
  • HY-143420
    ATX inhibitor 15
    		Inhibitor
    ATX inhibitor 15 (compound 30), a indole-based carbamate derivative, is a potent autotaxin (ATX) inhibitor with an IC50 of 2.17 nM. ATX inhibitor 15 inhibits in vivo ATX and the gene expression of pro-fibrotic factors. ATX inhibitor 15 has lung protection effects in Bleomycin challenged mice lung fibrosis model.
    ATX inhibitor 15
  • HY-147991
    PDE5/HDAC-IN-1
    		Inhibitor
    PDE5/HDAC-IN-1 (Compound 26) is a potent phosphodiesterase 5 (PDE5) and HDAC inhibitor with IC50 values of 46.3 nM and 14.5 nM, respectively. PDE5/HDAC-IN-1 induces cell apoptosis and shows anticancer activities.
    PDE5/HDAC-IN-1
  • HY-175779
    TDP1-IN-4
    		Inhibitor
    TDP1-IN-4 (Compound 33) is a Tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitor with an IC50 of 0.90  μM. TDP1-IN-4 has a strong synergistic effect with Camptothecin (HY-16560) in SK-Mel-2 cells, but not in cancer cells (A549, HCT-116 and MCF-7 cells) and non-cancerous Ges-1 cells. TDP1-IN-4 can be used for cancer chemotherapy and radiotherapy research.
    TDP1-IN-4
  • HY-N3180
    Norbraylin
    		Inhibitor
    Norbraylin, a natural prenylated coumarin, is a PDE4D2 inhibitor with an IC50 value of 7.15 μM.
    Norbraylin
  • HY-W705784A
    T-1032
    		Inhibitor
    T-1032 is a selective phosphodiesterase 5 (PDE5) inhibitor with an IC50 value of 1.0 nM. T-1032 shows relaxant effect on isolated rabbit corpus cavernosum. T-1032 can be used for the research of erectile dysfunction.
    T-1032
  • HY-162797
    PDE4-IN-18
    		Inhibitor
    PDE4-IN-18 (compound 1l) is a PDE4 inhibitor (IC50=1.55 μM) with anti-inflammatory activity. PDE4-IN-18 exerts anti-inflammatory effects by reducing excessive immune cell infiltration and intestinal membrane formation, as well as reducing the mRNA expression of pro-inflammatory cytokines (such as TNF-α and IL-6) in synovial tissue. PDE4-IN-18 can be used in the study of rheumatoid arthritis and psoriasis.
    PDE4-IN-18
  • HY-108974S
    Drotaverine-d10 hydrochloride
    		Inhibitor
    Drotaverine-d10 (hydrochloride) is the deuterium labeled Drotaverine hydrochloride. Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine hydrochloride exhibits in vivo antispasmodic efficacy without anticholinergic effects.
    Drotaverine-d<sub>10</sub> hydrochloride
  • HY-144743
    ATX inhibitor 12
    		Inhibitor
    ATX inhibitor 12 (compound 20) is an orally active and potent ATX (autotaxin) inhibitor, with an IC50 of 1.72 nM. ATX inhibitor 12 effectively alleviates lung structural damage with fewer fibrotic lesions at an oral dose of 60 mg/kg in C57Bl/6J mice. ATX inhibitor 12 can be uesd for idiopathic pulmonary fibrosis (IPF) research.
    ATX inhibitor 12
  • HY-155819
    M3/PDE4 modulator-1
    		Inhibitor
    M3/PDE4 modulator-1 (compound 10f) is a bifunctional molecule that is an M3 mAChR antagonist and a PDE4 inhibitor. M3/PDE4 modulator-1 (10-1000 nM/kg; iv) reduces cysteine eosinophil influx in the OVA rat model.
    M3/PDE4 modulator-1
  • HY-172135
    PDE4-IN-26
    		Inhibitor
    PDE4-IN-26 (Compound A5) is an orally active and highly selective PDE4 inhibitor. PDE4-IN-26 has anti-inflammatory activity and can inhibit the phosphorylation of p38 MAPK. In mouse models of acute lung injury and chronic obstructive pulmonary disease, PDE4-IN-26 can improve pulmonary inflammation, injury and fibrosis, promote sputum secretion and relieve cough in mice. PDE4-IN-26 can be used for the research of lung injury-related diseases.
    PDE4-IN-26
  • HY-N8092
    Kushenol B
    		Inhibitor
    Kushenol B is an isoprenoid flavonoid isolated from S. flavescens, has antimicrobial, anti-inflammatory and antioxidant activities. Kushenol B has inhibitory activity against cAMP phosphodiesterase (PDE), with an IC50 of 31 µM.
    Kushenol B
  • HY-B0523B
    Anagrelide hydrochloride monohydrate
    		Inhibitor
    Anagrelide hydrochloride monohydrate is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide hydrochloride monohydrate, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide hydrochloride monohydrate inhibits bone marrow megakaryocytopoiesis. Anagrelide hydrochloride monohydrate decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide hydrochloride monohydrate is a platelet-lowering agent and plays in the antithrombopoietic action.
    Anagrelide hydrochloride monohydrate
  • HY-103024
    ICI-63197
    		Inhibitor 99.14%
    ICI-63197 is a phosphodiesterase 3 (PDE3) and PDE4 inhibitor with Ki values of 9 µM and 10 µM, respectively. ICI-63197 is selectivity against PDE1 and PDE2. ICI-63197 has antidepressant effects.
    ICI-63197
  • HY-114990
    EMD 57439
    		Inhibitor
    EMD 57439 is a selective PDE-III inhibitor. EMD 57439 does not significantly increase c-AMP concentration and has little effect on Ca(50).
    EMD 57439
  • HY-11072
    MK-0359
    		Inhibitor
    MK-0359 (L-454,560) is a selective and orally active PDE4 inhibitor, and can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    MK-0359
  • HY-157997
    MHC02181
    		Inhibitor
    MHC02181 is a potent inhibitor of Autotaxin (ATX), with IC50 of 9.41 μM.
    MHC02181
  • HY-118408
    D-4418
    D-4418 serves as a PDE4 inhibitor and is under development as a new anti-inflammatory treatment, primarily targeting asthma and chronic obstructive pulmonary disease.
    D-4418
  • HY-141831
    STF-1084
    		Inhibitor
    STF-1084 is a specific, cell-impermeable, competitive inhibitor of ENPP1 (Ki = 33 nM). STF-1084 increases extracellular cGAMP concentrations by preventing its degradation by ENPP1, thereby enhancing immune infiltration. STF-1084 acts synergistically with ionizing radiation (IR) and cGAMP to delay tumor progression. STF-1084 can be used to study cancers with low immunogenicity.
    STF-1084
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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