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-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-137672A
    2',3'-Cyclic NADP disodium
    2',3'-Cyclic NADP disodium (2',3'-cNADP+; β-Nicotinamide adenine dinucleotide-2',3'-cyclic phosphate) is a substrate for 2',3'-cyclic nucleotide 3'-phosphodiesterase (CNP), an enzyme abundant in myelin. It has been used in a coupled enzyme assay to quantify CNP activity. 2',3'-Cyclic NADP disodium (5 μM) increases calcium overload-induced calcium release and prevents calcium-induced swelling in rat brain mitochondria.
    2',3'-Cyclic NADP disodium
  • 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-168930
    ATX inhibitor 25
    		Inhibitor
    ATX inhibitor 25 (Compound 29) is an orally active Autotaxin inhibitor with an IC50 of 1.08 nM. ATX inhibitor 25 exhibits excellent in vitro metabolic stability, with a t1/2 of more than 170 minutes. In the bleomycin (HY-108345)-induced pulmonary fibrosis mouse model, orally administered ATX inhibitor 25 shows anti-fibrotic effects.
    ATX inhibitor 25
  • HY-163285
    PDE3B-IN-1
    		Inhibitor
    PDE3B-IN-1 is a selective inhibitor for phosphodiesterase PDE3B with an IMAP pIC50 of 6.5 and a PDE3B/A selective index >300.
    PDE3B-IN-1
  • HY-129670
    KMUP-1
    		Inhibitor
    KMUP-1 is a xanthine derivative with vasodilator activity. KMUP-1 is a inhibitor of phosphodiesterase (PDE) and activator of soluble guanylyl cyclase (sGC). KMUP-1 stimulates NO/sGC/cyclic GMP pathway. KMUP-1 has K+ channels opening activity. KMUP-1 ameliorates ischemia-induced cardiomyocyte apoptosis. KMUP-1 can be used for cardiovascular and anti-inflammatory study.
    KMUP-1
  • HY-168558
    PDE4B/D-IN-4
    		Inhibitor
    PDE4B/D-IN-4 (compound 4p) is a potent inhibitor of PDE-4B and PDE-4D, with IC50s of 5.50 nM and 6.81 nM, respectively. PDE4B/D-IN-4 shows an increase in the level of intracellular cAMP.
    PDE4B/D-IN-4
  • HY-151917
    Enpp/Carbonic anhydrase-IN-2
    		Inhibitor 99.76%
    Enpp/Carbonic anhydrase-IN-2 (compound 1i) is a potent Enpp and carbonic anhydrase inhibitor with IC50s of 1.13, 1.07, 0.74, 0.33, 0.68 for NPP1, NPP2, NPP3, CA-IX, CA-XII respectively. Enpp/Carbonic anhydrase-IN-2 shows antiproliferative activity for cancer cells and low cytotoxic against normal cells. Enpp/Carbonic anhydrase-IN-2 induces Apoptosis.
    Enpp/Carbonic anhydrase-IN-2
  • HY-W700639
    Tolafentrine
    		Inhibitor
    Tolafentrine, a dual-selective phosphodiesterase 3/4 (PDE3/4) inhibitor, has been shown to have significant acute and chronic effects in a unilateral diacetamide-induced rat pulmonary hypertension model. Experiments show that long-term administration can significantly alleviate all unilateral bisacetamide-induced hemodynamic and gas exchange abnormalities, reduce right ventricular hypertrophy, and normalize pulmonary vascular remodeling changes.
    Tolafentrine
  • HY-155199
    PDE1-IN-5
    		Inhibitor
    PDE1-IN-5 (Compound 10c) is a selective PDE1C inhibitor (IC50: 15 nM). PDE1-IN-5 has anti- inflammatory activity, and inhibits expression of iNOS, TNF-α, IL-1α, IL-1β, and IL-6 induced by LPS. PDE1-IN-5 has anti-inflammatory bowel disease (IBD) effects in the dextran sodium sulfate (DSS)-Induced colitis mice model. PDE1-IN-5 can be used for research of IBD.
    PDE1-IN-5
  • HY-105647
    Ambuphylline
    Ambuphylline (Bufylline) is a bronchodilator. Ambuphylline is a theophylline derivative possibly acting through phosphodiesterase inhibition. Ambuphylline can be used for the research of asthma and other lung diseases.
    Ambuphylline
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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