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-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-116755S2
    Tiropramide-d5 oxalate
    Inhibitor
    Tiropramide-d5 oxalate (CR 605-d5 oxalate) is the deuterium labeled Tiropramide oxalate. Tiropramide (CR 605) is a tyrosine derivative with antispastic properties. Tiropramide hydrochloride inhibits phosphodiesterase activity involved in cAMP catabolism in rabbit colon homogenates. Tiropramide relaxes smooth muscle in rabbit isolated colon. Tiropramide can be used for the research of irritable colon and biliary dyskinesia.
    Tiropramide-d<sub>5</sub> oxalate
  • HY-W705784
    T-1032 free base
    Inhibitor
    T-1032 free base is a selective phosphodiesterase 5 (PDE5) inhibitor with an IC50 value of 1.0 nM. T-1032 free base shows relaxant effect on isolated rabbit corpus cavernosum. T-1032 free base can be used for the research of erectile dysfunction.
    T-1032 free base
  • HY-176874
    Enpp-1-IN-29
    Inhibitor
    Enpp-1-IN-29 (Compound 1) is a highly selective ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) inhibitor (IC50=0.05 nM). Enpp-1-IN-29 is promising for research of ENPP1-overexpressing cancers (e.g., breast cancer, head/neck cancer, metastatic chromosome-unstable tumors) and immune-related diseases (e.g., autoimmune disorders, tumor immune evasion).
    Enpp-1-IN-29
  • 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-180526
    PDE2A-IN-2
    Inhibitor
    PDE2A-IN-2 is a selective and brain-penetrant PDE2A inhibitor (Ki = 5.49 nM and 100 > fold selectivity over other PDE isoforms). The 11C-labeled PDE2A-IN-2 serves as a positron emission tomography (PET) tracer for brain imaging in patients with neurodegenerative diseases. PDE2A-IN-2 educes the radiotracer signal in PDE2A-rich regions in vitro. PDE2A-IN-2 exhibits low binding affinity in vivo. PDE2A-IN-2 can be used for neurodegenerative diseases .
    PDE2A-IN-2
  • 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
    99.3%
    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-179580
    EL244
    Inhibitor 99.55%
    EL244 is a dua Autotaxin (ATX) (IC50 = 50 nM) inhibitor and PPARγ (IC50 = 1.3 μM; Kd = 1.3 μM) agonist. EL244 demonstrates low cytotoxicity in human HepG2 cells (EC50 = 81.2 μM) with minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 significantly reduces pulmonary Lysophosphatidic Acid (LPA) levels, attenuates fibrosis, and restores respiratory function with limited systemic absorption in vivo. EL244 can be used for idiopathic pulmonary fibrosis and interstitial lung disease (ILD) research.
    EL244
  • HY-182772
    Enpp-1-IN-31
    Inhibitor
    Enpp-1-IN-31 is a ENPP1 inhibitor with an IC50 of <20 nM (using cGAMP as the substrate). Enpp-1-IN-31 exhibits potential anticancer activity and inhibits the growth and proliferation of mouse colon cancer cells and breast cancer cells.
    Enpp-1-IN-31
  • 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-174405
    PROTAC PDE4 degrader-1
    Degrader
    PROTAC PDE4 degrader-1 (Compound 9m) is a selective and orally active PDE4 PROTAC degrader with a DC50 of 41.98 μM. PROTAC PDE4 degrader-1 potently inhibits the secretion of pro-inflammatory cytokines such as TNF-α and IL-6. PROTAC PDE4 degrader-1 significantly alleviates pulmonary inflammation in LPS (HY-D1056)-induced acute lung injury (ALI) mice Model. Pink: PDE4 ligand (HY-174410); Blue: CRBN ligase ligand (HY-10984); Black: linker
    PROTAC PDE4 degrader-1
  • HY-136520A
    (R)-Xanthoanthrafil
    Inhibitor
    (R)-Xanthoanthrafil is a phosphodiesterase-5 (PDE5) inhibitor. (R)-Xanthoanthrafil selectively inhibits PDE5, increasing cyclic guanosine monophosphate (cGMP) levels, leading to smooth muscle relaxation and promoting penile erection. (R)-Xanthoanthrafil can be used to study erectile dysfunction.
    (R)-Xanthoanthrafil
  • 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
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