1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)

Phosphodiesterase (PDE)

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-108436
    Deltazinone 1
    Inhibitor
    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-104028B
    (S)-BAY 73-6691
    Control 99.51%
    (S)-BAY 73-6691 is the isomer of BAY 73-6691 (HY-104028), and can be used as an experimental control. BAY 73-6691 ((R)-BAY 73-6691) is a potent, brain penetrant, and selective PDE9A inhibitor.
    (S)-BAY 73-6691
  • 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-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
  • HY-103267A
    S32826
    Inhibitor
    S32826 is a potent autotaxin inhibitor, with an IC50 of 8.8 nM. S32826 shows similar inhibitory effects at various autotaxin isoforms (α, β and γ). S32826 inhibits LPA release from adipocytes.
    S32826
  • HY-110137A
    Furamidine
    Inhibitor
    Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent.
    Furamidine
  • HY-142644
    ATX inhibitor 7
    Inhibitor
    ATX inhibitor 7 is a autotaxin inhibitor and shows good oral exposure.
    ATX inhibitor 7
  • HY-W011293R
    DTA (Standard)
    Inhibitor
    DTA (Standard) is the analytical standard of DTA. This product is intended for research and analytical applications. DTA (2,4-Disulfamyl-5-trifluoromethylaniline) is a cyclic AMP phosphodiesterase inhibitor that binds to erythrocyte carbonic anhydrase.
    DTA (Standard)
  • HY-106325
    AA 2379
    Inhibitor
    AA 2379 is an orally active antirheumatic agent. AA 2379 has antiinflammatory, antipyretic activities and reduces pain sensation.
    AA 2379
  • HY-131710
    PDE5-IN-3
    Inhibitor
    PDE5-IN-3 (compound 11j) is a potent PDE5 inhibitor with an IC50 of 1.57 nM. PDE5-IN-3 shows moderate EGFR inhibition with IC50 of 5.827 µM. PDE5-IN-3 significantly inhibits the Wnt/β-catenin pathway (IC50=1286.96 ng/mL). PDE5-IN-3 induces the intrinsic apoptotic mitochondrial pathway in HepG2 cells. PDE5-IN-3 has strong antitumor activity.
    PDE5-IN-3
  • HY-106045A
    Imazodan hydrochloride
    Inhibitor
    Imazodan hydrochloride is the hydrochloride form of Imazodan (HY-106045). Imazodan hydrochloride is a selective inhibitor for phosphodiesterase III (PDE III), which increases myocardial contractility by blocking the cAMP degradation, and improves the contractile function of heart. Imazodan hydrochloride serves also as a peripheral vasodilator.
    Imazodan hydrochloride
  • HY-N3464
    Isopedicin
    Inhibitor
    Isopedicin potently and concentration-dependently inhibits superoxide anion (O2 U?) production in formyl-L-methionyl-L-leucyl-L-phenylalanine (FMLP)-activated cells. Isopedicin increases cAMP formation and PKA activity in FMLP-activated cells by inhibiting phosphodiesterase (PDE) activity.
    Isopedicin
  • HY-168147
    Enpp-1-IN-24
    Inhibitor
    Enpp-1-IN-24 (compund 7) is an ENPP1 inhibitor that, in combination with anti-PD-1 antibodies, achieves 77.7% tumor growth inhibition and improves survival in mouse models.
    Enpp-1-IN-24
  • HY-117605S
    N-Desmethyl Sildenafil-d8
    N-Desmethyl Sildenafil-d8 is the deuterium labeled N-Desmethyl Sildenafil (HY-117605). N-Desmethyl Sildenafil is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor.
    N-Desmethyl Sildenafil-d<sub>8</sub>
  • HY-170435
    PDE5-IN-13
    Inhibitor
    PDE5-IN-13 (Compound 14b) inhibits phosphodiesterase 5 (PDE5A) with an IC50 of 3 nM. PDE5-IN-13 is a potential candidate for PAH (pulmonary arterial hypertension) research. PDE5-IN-13 has high selectivity for targets over PDE1, PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11. PDE5-IN-13 is orally active.
    PDE5-IN-13
  • HY-157457
    Z21090
    Inhibitor
    Z21090 (ZL40) is a potent inhibitor of PDE4 with the IC50 value of 37.4 nM and oral bioavailability. Z21090 plays an important role in alcohol-related diseases research.
    Z21090
  • HY-123446
    JNJ-42259152
    JNJ-42259152 is a phosphodiesterase 10A (PDE10A) positron emission tomography (PET) tracer that is specific for PDE10A activity. JNJ-42259152 can be dynamically scanned in healthy volunteers to assess its kinetic properties in the brain. The half-life of JNJ-42259152 in the blood is an average of 90 minutes. JNJ-42259152 has demonstrated reliable binding potential (BPND) in different target areas (such as the lentiform nucleus, caudate nucleus, ventral striatum, etc.), providing an important tool for studying neuropsychiatric diseases.
    JNJ-42259152
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