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-17464S1
    Cilostazol-d4
    		Inhibitor
    Cilostazol-d4 is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM.
    Cilostazol-d<sub>4</sub>
  • HY-120997
    E6 Berbamine
    		Inhibitor
    E6 Berbamine (Berbamine p-nitrobenzoate) is a potent calmodulin (CaM) antagonist. E6 Berbamine inhibits the activities of calmodulin-dependent myosin light chain kinase (MLCK) and phosphodiesterase (PDE). E6 Berbamine exhibits anti-leukemic activity. E6 Berbamine can be used in research related to cardiovascular abnormalities and chronic myeloid leukemia.
    E6 Berbamine
  • HY-128234
    PDE11-IN-1
    		Inhibitor 98.23%
    PDE11-IN-1 is a PDE11 inhibitor and can be used for adrenal insufficiency research.
    PDE11-IN-1
  • HY-172919
    PDEδ/NAMPT IN-1
    		Inhibitor
    PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) (KD=0.410 nM) and nicotinamide phosphoribosyl transferase (NAMPT) (IC50=2.21 nM). PDEδ/NAMPT IN-1 blocks KRAS-related signal transduction and interferes with the synthesis of nicotinamide adenine dinucleotide (NAD+), inducing apoptosis in KRAS mutant pancreatic cancer cells. PDEδ/NAMPT IN-1 is promising for research of KRAS mutant pancreatic cancer.
    PDEδ/NAMPT IN-1
  • HY-115913
    PDE4-IN-6
    		Inhibitor
    PDE4-IN-6 is a potent, safe and moderately selective PDE4 inhibitor with IC50s of 0.125 and 0.43 µM for PDE4B and PDE4D, respectively. PDE4-IN-6 can downregulate the expression level of TNF-α and IL-6. PDE4-IN-6 has potent immunomodulatory activity thereby its potential against rheumatoid arthritis. Anti-inflammatory and anti-arthritic effects.
    PDE4-IN-6
  • HY-19035
    DN-9693 dihydrochloride
    		Inhibitor
    DN-9693 dihydrochloride is a phosphodiesterase inhibitor with a platelet membrane effect. DN-9693 dihydrochloride can increase platelet cyclic AMP and inhibit ristocetin-induced platelet agglutination and adhesion.
    DN-9693 dihydrochloride
  • HY-N2658
    5,7-Diacetoxy-8-methoxyflavone
    		Inhibitor 98.04%
    5,7-Diacetoxy-8-methoxyflavone is a natural product that could come from scutellaria genus plants. 5,7-Diacetoxy-8-methoxyflavone has inhibitory activity for cAMP phosphodiesterase.
    5,7-Diacetoxy-8-methoxyflavone
  • HY-146889
    ATX inhibitor 16
    		Inhibitor
    ATX inhibitor 16 is a potent ATX inhibitor with an IC50 of 0.0021 μM. ATX inhibitor 16 shows excellent anti-proliferative activities in breast cancer cells.
    ATX inhibitor 16
  • HY-101826A
    ER21355 hydrochloride
    		Inhibitor
    ER21355 hydrochloride is the hydrochloride form of ER21355 (HY-101826). ER21355 hydrochloride is an inhibitor for phosphodiesterase (PDE), which is potent for ameliorating benign prostatic hyperplasia (BPH) and prostatism through increasing levels of cAMP and cGMP, and resulting a relaxation of the smooth muscle cell.
    ER21355 hydrochloride
  • HY-161381
    PDE4-IN-15
    		Inhibitor
    PDE4-IN-15 (compound 7b-1) is an inhibitor of PDE4 (IC50 = 0.17 μM) and has anti-TNF-α activity (EC50 = 0.19 μM). PDE4-IN-15 has a good skin permeability.
    PDE4-IN-15
  • HY-181020
    Deltafluorine
    		Inhibitor
    Deltafluorine is a phosphodiesterase delta (PDEδ) inhibitor with an IC50 of 27 nM, a KD of 148 nM. Deltafluorine covalently modifies the specific glutamate residue p.E88 in the ligand binding site of PDEδ, interfering with its chaperone function. Deltafluorine inhibits signaling through the MAPK and Akt-mTOR pathway, reduces ERK1/2 expression. Deltafluorine reduces tumor volume in an autochthonous mouse model of Kras-driven lung adenocarcinoma. Deltafluorine can be used for the research of lung adenocarcinoma.
    Deltafluorine
  • HY-165436
    Toborinone
    		Inhibitor
    Toborinone is an inotropic agent. Toborinone increases cAMP and intracellular calcium levels through inhibiting PDE. Toborinone inhibits thrombin-induced platelet aggregation with an IC50 of 9.7 μM.
    Toborinone
  • HY-106474
    Meribendan
    		Inhibitor
    Meribendan is a phosphodiesterase (PDE)-III inhibitor.
    Meribendan
  • HY-123522
    PAT-048
    		Inhibitor
    PAT-048 is a potent, selective and orally active autotaxin inhibitor, inhibits IL-6 mRNA expression, but shows no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in lung fibrosis model. PAT-048 shows an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouse plasma. PAT-048 reduces dermal fibrosis in vivo.
    PAT-048
  • HY-145062
    Enpp-1-IN-4
    		Inhibitor
    Enpp-1-IN-4 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). Enpp-1-IN-4 has the potential for the research of cancer diseases (extracted from patent WO2019177971A1, compound 1).
    Enpp-1-IN-4
  • HY-157458
    PDEδ autophagic degrader 1
    		Inhibitor
    PDEδ autophagic degrader 1 (compound 12c), an autophagosome-tethering compound (ATTEC). is a potent PDEδ autophagic degrader. PDEδ autophagic degrader 1 reduces the PDEδ protein level through lysosome-mediated autophagy without affecting the PDEδ mRNA expression. PDEδ autophagic degrader 1 suppresses the growth in KRAS mutant pancreatic cancer cells.
    PDEδ autophagic degrader 1
  • HY-117848
    PDE8B-IN-1 hydrochloride
    		Inhibitor
    PDE8B-IN-1 hydrochloride (compound 42) is a potent, selective PDE8B inhibitor with a IC50 value of 1.5 nM. PDE8B-IN-1 hydrochloride can be used in the study of diabetes.
    PDE8B-IN-1 hydrochloride
  • HY-119611
    Thioquinapiperifil
    		Inhibitor
    Thioquinapiperifil (KF31327 free base), a potent, selective and non-competitive phosphodiesterase-5 (PDE-5, IC50 of 0.074 nM) inhibitor, is used for sexual enhancement study.
    Thioquinapiperifil
  • HY-130054
    Theophylline L-lysine
    		Inhibitor
    Theophylline L-lysine (Lysine theophyllinate) is a soluble derivative of Theophylline (HY-B0809). Theophylline L-lysine is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline L-lysine inhibits PDE3 activity to relax airway smooth muscle. Theophylline L-lysine has anti-inflammatory activity by increasing IL-10 and inhibiting NF-κB into the nucleus. Theophylline L-lysine induces apoptosis. Theophylline L-lysine can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    Theophylline L-lysine
  • HY-108436
    Deltazinone 1
    		Inhibitor 98.79%
    Deltazinone 1, a pyrazolopyridazinone, is a highly selective PDEδ inhibitor with a KD of 8 nM. Deltazinone 1 inhibits the PDEδ-Ras interaction. Deltazinone 1 shows a dose-dependent inhibitory response on proliferation in oncogenic KRas-dependent cell lines.
    Deltazinone 1
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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