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).

10 Items

  • Sp-8-pCPT-cGMPS
    Cat. No.
    A37205

    Sp-8-pCPT-cGMPS

    Sp-8-pCPT-cGMPS is a potent activator of protein kinase G (PKG) and protein kinase A (PKA) with significant cell membrane permeability and phosphodiesterase stability. This cyclic guanosine monophosphate analog effectively engages PKG types I α, I β, and II, making it invaluable for research in signal transduction pathways. It is utilized to investigate the role of cGMP in neural plasticity, synaptic transmission, and other physiological processes influenced by these kinases.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • 8-Bromo-cGMP sodium
    Cat. No.
    A65976

    8-Bromo-cGMP sodium

    8-Bromo-cGMP sodium is a membrane-permeable analogue of cyclic guanosine monophosphate (cGMP) that acts as a potent activator of protein kinase G (PKG). This compound has been shown to significantly inhibit Ca2+ macroscopic currents and to impair high potassium-induced insulin release. Additionally, 8-Bromo-cGMP sodium exhibits antinociceptive properties and elicits vasodilatory responses, making it valuable for studies investigating cardiovascular and metabolic functions.

    5 mg
    $55.00
    10 mg
    $90.00
    All 5 sizes
  • Rp-8-Br-cGMPS
    Cat. No.
    A66402

    Rp-8-Br-cGMPS

    Synonyms: Rp-8-bromo-Cyclic GMPS

    Rp-8-Br-cGMPS (Rp-8-bromo-Cyclic GMP sodium salt) is an effective activator of Ca2+-ATPase, promoting the reduction of cytosolic Ca2+ levels by enhancing the efflux of Ca2+ from cells. Additionally, it acts as an agonist of the rod cyclic nucleotide-gated (CNG) channel and functions as an inhibitor of protein kinase G (PKG). This compound is valuable for studies involving calcium signaling, cellular response mechanisms, and cardiovascular research.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • 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
  • PKG1α activator 3
    Cat. No.
    A84796

    PKG1α activator 3

    PKG1α activator 3 is a selective activator of Protein Kinase G Iα (PKG1α), exhibiting EC50 values of 13 μM for basal activation and 0.52 μM for partial activation. This compound demonstrates significant anti-proliferative effects on smooth muscle cells, making it a valuable tool for investigating mechanisms underlying cardiovascular diseases. Its ability to modulate PKG1α activity positions it as a potential candidate for research focused on vascular function and related pathologies.

    Out of stock

    All 3 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-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
  • 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

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