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-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-175478
    Enpp-1-IN-27
    		Inhibitor
    Enpp-1-IN-27 is a selective ENPP1 inhibitor with an IC50 of 14.68 nM, exhibiting approximately 410-fold selectivity against ENPP2 and 10-fold selectivity against ENPP3. Enpp-1-IN-27 stabilizes cGAMP levels and activates the STING pathway, promoting cytokine release and enhancing innate immune responses. Enpp-1-IN-27 induces ISRE activation and amplified cGAMP-mediated immune responses and shows the desired antitumor efficacy in the 4T1 and CT26 syngeneic mouse models. Enpp-1-IN-27 can used for the studies of breast cancer and colon cancer.
    Enpp-1-IN-27
  • 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-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
  • HY-124371
    Amentoflavone hexaacetate
    Amentoflavone hexaacetate is a 3,5-cyclic nucleotide phosphodiesterase inhibitor with antiplatelet aggregation activity. Amentoflavone hexaacetate can inhibit the aggregation of eluted human platelets induced by ADP or collagen. Amentoflavone hexaacetate can also inhibit the cAMP phosphodiesterase activity in human platelets. Amentoflavone hexaacetate can significantly increase the cAMP level of platelets in the presence of prostaglandin E1. Amentoflavone hexaacetate has anti-angiogenic and anti-metastatic effects.
    Amentoflavone hexaacetate
  • HY-158237
    PDE10A-IN-3
    		Inhibitor
    PDE10A-IN-3 (Compound 8a) is an inhibitor of phosphodiesterase 10A (PDE10A). PDE10A-IN-3 can be used in schizophrenia research.
    PDE10A-IN-3
  • HY-111164
    CBS-3595
    		Inhibitor
    CBS-3595 is a dual inhibitor of p38 MAP kinase and phosphodiesterase 4 with anti-inflammatory and anti-allodynic activities. CBS-3595 reduces the production of the proinflammatory cytokine IL-6 and increases the levels of the anti-inflammatory cytokine IL-10 in rats. CBS-3595 reduces paw oedema formation in the Complete Freund’s adjuvant (CFA) (HY-153808)-induced arthritis rat model. CBS-3595 is promising for research of autoimmune diseases.
    CBS-3595
  • HY-N1465R
    Aristolochic acid D (Standard)
    		Inhibitor
    Aristolochic acid D (Standard) (Aristolochic acid-IVa (Standard)) is the analytical standard of Aristolochic acid D (HY-N1465). This product is intended for research and analytical applications. Aristolochic acid D (Aristolochic acid-IVa) is an orally active PDE2 (IC50: 4.673 μM) and CDK2 (IC50: 25 μM) inhibitor that can be isolated from Aristolochia indica L. Aristolochic acid D exhibits anti-inflammatory activity and is non-carcinogenic and non-nephrotoxic. Aristolochic acid D can be used in the research of inflammation and tumor-related diseases.
    Aristolochic acid D (Standard)
  • HY-150060
    PDE4-IN-11
    		Inhibitor
    PDE4-IN-11 is an inhibitor of phosphodiesterase isoenzyme 4 (PDE4). PDE4-IN-11 displays highly effective bronchodilatory and anti-inflammatory properties, can be used for obstructive or inflammatory airway diseases research.
    PDE4-IN-11
  • HY-122622
    PF-04471141 hydrochloride
    		Inhibitor
    PF-04471141 (hydrochloride) is a compound that regulates intracellular cAMP and cGMP concentrations. It is a PDE1 inhibitor and has different effects on different PDE enzymes in regulating intracellular signaling molecule concentrations and cell proliferation in vascular smooth muscle cells.
    PF-04471141 hydrochloride
  • HY-161663
    Phosphodiesterase-IN-2
    		Inhibitor
    Phosphodiesterase-IN-2 (Compound C7) is a selective, orally active inhibitor for phosphodiesterase 10A (PDE10A), with an IC50 of 11.9 nM. Phosphodiesterase-IN-2 improves the stability of liver microsomes, and lowers BBB permeability. Phosphodiesterase-IN-2 exhibits good pharmacokinetic characters, and attenuates isoprenaline (HY-108353)-induced cardiac hypertrophic in mouse models.
    Phosphodiesterase-IN-2
  • HY-167891
    GPD-1116
    		Inhibitor
    GPD-1116 is an orally active Phosphodiesterase (PDE) 4 and PDE1 inhibitor. GPD-1116 can reduce smoke-induced apoptosis of lung cells. GPD-1116 is effective in several disease models in animals, including emphysema, acute lung injury, chronic obstructive pulmonary disease (COPD), asthma and pulmonary hypertension.
    GPD-1116
  • HY-146122
    ATX inhibitor 19
    		Inhibitor
    ATX inhibitor 19 (compound 22) is a potent ATX (autotaxin) inhibitor, with an IC50 of 156 nM.
    ATX inhibitor 19
  • HY-120710
    DNS-8254
    		Inhibitor
    DNS-8254 is an oral active and brain-penetrating PDE2a inhibitor with the IC50 of 8 nM. DNS-8254 shows memory enhancing effects in a rat model.
    DNS-8254
  • HY-P2878A
    Phosphodiesterase l, Rattlesnake venom
    Phosphodiesterase l, Rattlesnake venom (PDE, Rattlesnake venom) is a non-selective phosphodiester bond hydrolase targeting phosphodiester bonds in oligonucleotides, catalyzing their hydrolysis into mononucleotides. Phosphodiesterase l, Rattlesnake venom cleaves phosphodiester linkages in DNA fragments digested by DNase I. Phosphodiesterase l, Rattlesnake venom is promising for research of nucleic acid structure and metabolism.
    Phosphodiesterase l, Rattlesnake venom
  • HY-A0140
    Drotaverine
    Drotaverine is a selective phosphodiesterase 4 inhibitor with angina relief activity. Drotaverine is used to suppress angina, including pain in the gastrointestinal tract and biliary tract. Drotaverine may also cause compound-induced priapism, a side effect of sustained penile erection.
    Drotaverine
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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