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).

Items 26-31 of 31

  • Sp-8-pCPT-PET-cGMPS
    Cat. No.
    A84808

    Sp-8-pCPT-PET-cGMPS

    Sp-8-pCPT-PET-cGMPS is a selective activator of PKG-I (protein kinase G I). This compound has demonstrated pivotal biological activity by facilitating NO/NOS/sGC/PKG-I signaling pathways, making it an invaluable tool for research in cardiac differentiation. Its ability to modulate these pathways contributes to a deeper understanding of cardiovascular biology and potential therapeutic interventions.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • 8-Br-cGMP-AM
    Cat. No.
    A84809

    8-Br-cGMP-AM

    8-Br-cGMP-AM is a potent activator of cGMP-dependent protein kinase (PKG). This compound induces various biological effects, including vasodilation and inhibition of platelet aggregation. Its ability to modulate cardiovascular responses makes it a valuable tool in the study of cardiovascular diseases and related physiological processes.

    Out of stock

    All 3 sizes
  • Sp-cGMPS
    Cat. No.
    A84810

    Sp-cGMPS

    Sp-cGMPS is an activator of cGMP-dependent protein kinases (PKGs), which play a crucial role in signal transduction pathways. This compound enhances PKG activity, making it valuable for studying various physiological processes and pathologies. Its application is particularly relevant in cardiovascular disease research, where modulation of PKG activity can influence vascular function and cardiomyocyte signaling.

    Out of stock

    All 3 sizes
  • Rp-8-pCPT-cGMPS
    Cat. No.
    A84811

    Rp-8-pCPT-cGMPS

    Rp-8-pCPT-cGMPS is a competitive inhibitor of cGMP-dependent protein kinase (PKG) with a Ki value of 0.5 μM. Its high lipid solubility facilitates cellular penetration, enabling effective inhibition of PKG activity within cells. This reagent is valuable for investigating the role and function of PKG in cellular processes, particularly in platelets.

    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
  • AP-C5
    Cat. No.
    A89133

    AP-C5

    AP-C5 is a selective inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII), demonstrating a pIC50 of 7.2. This compound is useful for investigating the mechanisms underlying diarrheal diseases. Additionally, AP-C5 features an alkyne group that enables its application in click chemistry, allowing for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules.

    5 mg
    $25.00
    10 mg
    $45.00
    All 6 sizes

Items 26-31 of 31

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