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-124775
    (S)-C33
    		Inhibitor 99.46%
    (S)-C33 is a potent and selective PDE9 (phosphodiesterase-9) inhibitor, with an IC50 of 11 nM. (S)-C33 can be used for central nervous system diseases and diabetes research.
    (S)-C33
  • HY-160991A
    Menabitan dihydrochloride
    		Inhibitor
    Menabitan dihydrochloride (SP-204 dihydrochloride) is the dihydrochloride form of Menabitan (HY-160991). Menabitan dihydrochloride is an inhibitor for phosphodiesterase 9 (PDE 9), which acts as a non-opioid analgesic agent. Menabitan dihydrochloride lowers the intraocular pressure in rabbit model.
    Menabitan dihydrochloride
  • HY-172365
    P7–2302
    		Inhibitor
    P7-2302 inhibits PDE7 and PDE4B with IC50 of 0.18 nM and 77.3 nM. P7-2302 inhibits the efflux of P-gp and BCRP (breast cancer resistance protein), exhibits low uptake in rats brain. P7-2302 can be used as a PET tracer when labeled with 18F.
    P7–2302
  • HY-152838
    Gemlapodect
    		Inhibitor
    Gemlapodect (RO554965) is an inhibitor of phosphodiesterase 10A (PDE10A). Gemlapodect can be used for researching schizophrenia.
    Gemlapodect
  • HY-153802A
    Antitumor agent-100 hydrochloride
    Antitumor agent-100 (compound A6) hydrochloride is an orally potent apoptosis inducer and molecular gel targeting PDE3A-SLFN12 (IC50: 0.3 μM) with antitumor activity. Antitumor agent-100 hydrochloride binds to the PDE3A enzyme pocket to recruit and stabilize SLFN12, thereby preventing protein translation and leading to apoptosis.
    Antitumor agent-100 hydrochloride
  • HY-147998
    Enpp-1-IN-13
    		Inhibitor
    Enpp-1-IN-13 (Compound 1a) is an ectonucleotide pyrophosphatase/phosphodiesterase (ENPP) inhibitor with IC50 values of 1.29 μM and 20.2 μM against ENPP1 and ENPP3, respectively. Enpp-1-IN-13 shows anticancer activity.
    Enpp-1-IN-13
  • 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-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-130368
    W-7
    		Inhibitor
    W-7 is a selective calmodulin antagonist. W-7 inhibits the Ca2+-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC50 values of 28 μM and 51 μM, respectively. W-7 induces apoptosis and has antitumor and vascular relaxing activity. W-7 is a blocker of Kv4.3 and can be used for research of arrhythmias.
    W-7
  • 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-15025AS
    Sildenafil citrate-d8
    Sildenafil (citrate)-d8 is the deuterium labeled Sildenafil citrate. Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.
    Sildenafil citrate-d<sub>8</sub>
  • HY-N2658
    5,7-Diacetoxy-8-methoxyflavone
    		Inhibitor
    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-N8209
    (+)-Medioresinol Di-O-β-D-glucopyranoside
    		Inhibitor
    (+)-Medioresinol Di-O-β-D-glucopyranoside is a lignan glucoside with strong inhibitory activity of 3', 5'-cyclic monophosphate (cyclic AMP) phosphodiesterase.
    (+)-Medioresinol Di-O-β-D-glucopyranoside
  • HY-131101
    Nor-Acetildenafil
    Nor-Acetildenafil is an Acetildenafil derivative. Acetildenafil is a synthetic agent which acts as a phosphodiesterase inhibitor.
    Nor-Acetildenafil
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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