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-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-105520
    ORG-20241
    		Inhibitor
    ORG-20241 is a PDE3/PDE4 dual inhibitor. ORG-20241 has a significant bronchodilator effect and completely prevents allergen induced airway hyperresponsiveness. ORG-20241 can significantly inhibit eosinophil infiltration at high concentrations. ORG-20241 can be used for research on asthma.
    ORG-20241
  • 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-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-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-178987
    BJH-86
    		Inhibitor
    BJH-86 is a soluble mitochondrial complex 1 inhibitor (oxygen consumption rate inhibition IC50 = 5 μM). BJH-86 exhibits weak inhibitory activity against phosphodiesterase 10A (PDE10A) (IC50 >10 μM). BJH-86 can reduce cellular oxygen consumption and inhibit cancer cell proliferation. BJH-86 can be used for the research of cancer, such as lung cancer.
    BJH-86
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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