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-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-174379
    KRAS IN-44
    		Degrader
    KRAS IN-44 (Compound S2C2M2) is a PDE6D degrader. KRAS IN-44 inhibits PDE6D-dependent KRAS trafficking and KRAS downstream signaling pathways. KRAS IN-44 down-regulates EGF-induced the phosphorylation of PI3K, AKT, and mTOR. KRAS IN-44 increases Apoptosis. KRAS IN-44 has antitumor activity against hepatoblastoma.
    KRAS IN-44
  • HY-131101
    Nor-Acetildenafil
    Nor-Acetildenafil is an Acetildenafil derivative. Acetildenafil is a synthetic agent which acts as a phosphodiesterase inhibitor.
    Nor-Acetildenafil
  • 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
  • HY-153093A
    (1R,2R)-Elpipodect
    		Inhibitor
    (1R,2R)-Elpipodect ((1R,2R)-MK-8189) is the (1R,2R) enantiomer of Elpipodect (HY-153093). Elpipodect (MK-8189) is an orally active and selective PDE10A inhibitor with a Ki of 29 pM. Elpipodect can be used in research of schizophrenia.
    (1R,2R)-Elpipodect
  • HY-181646
    PDE4-IN-34
    		Inhibitor
    PDE4-IN-34 is a phosphodiesterase 4 (PDE4) inhibitor, with IC50 values of 19 pM and 14 pM against PDE4B1 and PDE4D2, respectively. PDE4-IN-34 shows weak inhibitory activity against PDE8A1, with an IC50 value of 4.092 μM, and exhibits significant selectivity over other subtypes (IC50 > 10 μM). PDE4-IN-34 improves pulmonary function, reduces inflammatory responses and alleviates lung tissue damage in a rat model induced by cigarette smoke combined with LPS (HY-D1056). PDE4-IN-34 can be used for research related to chronic obstructive pulmonary disease.
    PDE4-IN-34
  • HY-179042
    TGF-β/Smad-IN-3
    		Inhibitor
    TGF-β/Smad-IN-3 (Compound 4w) is an effective TGF-β/Smad inhibitor. TGF-β/Smad-IN-3 exerts anti-pulmonary fibrosis activity by simultaneously inhibiting the TGF-β/Smad and MAPK signaling pathways. TGF-β/Smad-IN-3 significantly inhibits collagen deposition induced by TGF-β1, with its IC50 value being 3.21 μM. TGF-β/Smad-IN-3 has an IC₅₀ of 46.77 nM for the autocrine motility factor (ATX). TGF-β/Smad-IN-3 significantly reduces the expression levels of α-SMA, COL1A1 and FN in TGF-β1-induced CCC-HPF-1 cells, and effectively inhibited TGF-β1-induced cell migration. TGF-β/Smad-IN-3 can be used for the study of pulmonary fibrosis.
    TGF-β/Smad-IN-3
  • HY-156434
    PDE11A4-IN-1
    		Inhibitor
    PDE11A4-IN-1 (compound 23b) is a potent and selective PDE11A4 inhibitor with an IC50 of 12 nM. PDE11A4-IN-1 show high selectivity for PDE11A4 over PDE1, PDE2, PDE7, PDE8, and PDE9.
    PDE11A4-IN-1
  • HY-172527
    CD73-IN-20
    		Inhibitor
    CD73-IN-20 (Compound 5c) is an e5′NT (CD73) inhibitor (IC50: 0.37 μM). CD73-IN-20 also inhibits other ectonucleotidases, with IC50s of 1.12 μM (h-ENPP1), 1.37 μM (h-ENPP3), 1.66 μM (r-e5′NT), 1.48 μM (h-TNAP), respectively. CD73-IN-20 can be used for cancer research.
    CD73-IN-20
  • HY-176524S
    PDE3/4-IN-3
    		Inhibitor
    PDE3/4-IN-3 (Compound 7) is an orally active dual PDE3/4 inhibitor with IC50 s of 0.17 and ≤50 nM for PDE3A and PDE4B2, respectively. PDE3/4-IN-3 significantly inhibits methacholine-induced bronchoconstriction in guinea pigs. PDE3/4-IN-3 can be used for chronic obstructive pulmonary disease (COPD) and asthma research.
    PDE3/4-IN-3
  • HY-119291
    RA642
    		Inhibitor
    RA642 is a compound with vasodilatory and hypertensive effects, with the activity of increasing arterial blood pressure, enhancing cerebral blood flow, reducing cerebrovascular resistance and peripheral resistance, and having a papaverine-like relaxant effect on smooth muscle in anesthetized animals.
    RA642
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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