PKG

PKG inhibitors and activators act on protein kinase G (PKG), a kinase switched on by cyclic nucleotides. A kinase activated by guanosine 3',5'-monophosphate (cGMP) was isolated and partially purified in 1970. Nitric oxide and natriuretic peptides raise cGMP, which binds the regulatory domain of PKG and releases its kinase activity. Mice lacking PKG type I showed defective regulation of vascular and intestinal smooth muscle in a 1998 study. KT 5823 and the cGMP analog Rp-8-Br-PET-cGMPS inhibit PKG, while Sp-8-pCPT-cGMPS activates it. MBP146-78 targets the PKG of apicomplexan parasites such as Toxoplasma. Several compounds, for example A-3 Hydrochloride, also inhibit the related protein kinase A (PKA).

3 Items

  • 8-pCPT-cGMP-AM
    Cat. No.
    A84794

    8-pCPT-cGMP-AM

    Synonyms: 8-(4-Chlorophenylthio)-cGMP-AM

    8-pCPT-cGMP-AM is a potent prodrug that serves as an agonist for protein kinase G (PKG). This compound exhibits high membrane permeability, allowing for efficient intracellular conversion to its active form, 8-pCPT-cGMP, through esterase hydrolysis. 8-pCPT-cGMP-AM is utilized in research focusing on cGMP signaling pathways related to neural plasticity and memory formation, providing valuable insights into cognitive processes.

    1 mg
    $640.00
    25 mg
    $1,410.00
    All 4 sizes
  • 8-Br-PET-cGMP
    Cat. No.
    A84806

    8-Br-PET-cGMP

    8-Br-PET-cGMP is a selective agonist of cGMP-dependent protein kinase type I (cGKI). It facilitates the dimerization of cGKI, enhancing its catalytic activity through binding to the regulatory domain. This compound is valuable for investigating cGMP signaling pathways involved in cellular processes such as growth, vasodilation, and the functionality of smooth muscle cells.

    Out of stock

    All 3 sizes
  • Sp-8-Br-PET-cGMPS
    Cat. No.
    A84812

    Sp-8-Br-PET-cGMPS

    Sp-8-Br-PET-cGMPS is a membrane-permeable agonist of protein kinase G (PKG), effectively activating cGMP-dependent protein kinases I α and I β. This compound is also a selective inhibitor of retinal-type cGMP-gated ion channels and exhibits resistance to mammalian cyclic nucleotide-dependent phosphodiesterases. Its enhanced lipophilicity and permeability compared to Sp-8-pCPT-cGMPS make it a valuable tool for investigating cGMP signaling pathways in neurological research.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes

3 Items

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