PDE

Phosphodiesterase (PDE) inhibitors prevent the hydrolysis of cyclic nucleotides, second messengers of many receptors. The PDE superfamily comprises 11 families, PDE1 to PDE11, which differ in substrate preference, regulation and tissue distribution. Some families hydrolyze cyclic adenosine monophosphate (cAMP), others cyclic guanosine monophosphate (cGMP), and several act on both. By controlling the amplitude and location of these signals, PDEs shape inflammation, smooth muscle tone and cardiac function. PDE4 inhibitors in this category include roflumilast and apremilast, which are studied in inflammatory cell signaling. Sildenafil inhibits the cGMP-specific PDE5, and cilostazol is a PDE3 inhibitor. Ibudilast inhibits several families, including PDE3, PDE4, PDE10 and PDE11.

5 Items

  • FPFT-2216
    Cat. No.
    A24013

    FPFT-2216

    FPFT-2216 is a “molecular glue” degrader that facilitates the proteasomal degradation of multiple target proteins, including phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1) and Aiolos (IKZF3), as well as casein kinase 1α (CK1α). By promoting selective ubiquitination through E3 ligase recruitment, FPFT-2216 modulates key regulatory pathways and holds promise for research in oncology and inflammatory diseases.

    5 mg
    $216.00
    10 mg
    $372.00
    All 4 sizes
  • PROTAC PDE4 degrader-1
    Cat. No.
    A26034

    PROTAC PDE4 degrader-1

    PROTAC PDE4 degrader-1 is a selective and orally active degrader targeting phosphodiesterase 4 (PDE4). It exhibits a DC50 of 41.98 μM and effectively inhibits the secretion of pro-inflammatory cytokines such as TNF-α and IL-6. This compound demonstrates significant potential in alleviating pulmonary inflammation in LPS-induced acute lung injury models, making it a valuable tool for studying inflammatory diseases and therapeutic interventions.

    Out of stock

    All 3 sizes
  • TMX-4113
    Cat. No.
    A36880

    TMX-4113

    TMX-4113 is a degrader targeting phosphodiesterase 6D (PDE6D) and casein kinase 1α (CK1α). This compound exhibits significant biological activity in the degradation of these proteins, making it a valuable tool for investigating their roles in cancer research. TMX-4113 can facilitate studies aimed at elucidating the molecular mechanisms underlying tumor progression and treatment responses.

    5 mg
    $330.00
    10 mg
    $570.00
    All 5 sizes
  • PDEδ autophagic degrader 1
    Cat. No.
    A39614

    PDEδ autophagic degrader 1

    PDEδ autophagic degrader 1 is a targeted autophagic degrader of PDEδ, functioning through an autophagosome-tethering mechanism. This compound effectively reduces the levels of PDEδ protein via lysosome-mediated autophagy, while leaving PDEδ mRNA expression unchanged. Its ability to suppress growth in KRAS mutant pancreatic cancer cells highlights its potential applications in cancer research and therapeutic development.

    Out of stock

    All 3 sizes
  • TMX-4100
    Cat. No.
    A41779

    TMX-4100

    TMX-4100 is a selective degrader of phosphodiesterase 6D (PDE6D), exhibiting high degradation efficacy with DC50 values below 200 nM in MOLT4, Jurkat, and MM.1S cell lines. This compound demonstrates potential for targeting PDE6D in research related to multiple myeloma, providing a valuable tool for investigating therapeutic strategies in this area.

    1 mg
    $80.00
    5 mg
    $205.00
    All 7 sizes

5 Items

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