PKG

MBP146-78 is a potent and selective inhibitor of cGMP dependent protein kinases.

A-3 Hydrochloride is an inhibitor of PKA (cAMP-dependent protein kinase, Ki=4.3μM) and cGMP-dependent protein kinase, Ki=3.8μM, PKC (protein kinase C, Ki=47μM), casein kinase I and II, and MLCK (myosin light chain kinase) ( Ki=7.4μM).

KT 5823 is a potent, selective inhibitor of cGMP-dependent protein kinase (PKG) (in vitro IC50 = 234 nM).

Rp-8-Br-PET-cGMPS is metabolically stable, competitive inhibitor of cGKI (Ki = 30 nM) and cGKII (cGMP-dependent protein kinase G) and blocks cGMP-gated retinal type ion channels (IC50 = 25 μM).

cGMP Dependent Kinase Inhibitor Peptid is a specific cGKI (cyclic GMP-dependent protein kinase) inhibitor. Data indicates that it does not block cyclic GMP-dependent protein kinase phosphorylation of intact histones and has been used to study Plasmodium falciparum.

PKG drug G1 targets C42 of PKG Iα. PKG drug G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.

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.

Protein kinase G inhibitor-1 is a selective inhibitor targeting protein kinase G (PKG) with an IC50 of 0.9 μM. This compound is utilized primarily in research related to mycobacterial infections, providing insights into the mechanisms of pathogenesis and potential therapeutic approaches. Its efficacy in inhibiting PKG activity makes it a valuable tool for exploring mycobacterial biology and developing novel treatments.

PI4Kβ/PKG-IN-2 is a potent dual inhibitor targeting Plasmodium phosphatidylinositol 4-kinase beta (PI4Kβ) and cGMP-dependent protein kinase (PKG). This compound demonstrates significant inhibitory activity against Plasmodium, making it a valuable tool for investigating malaria pathogenesis and potential therapeutic strategies. Its oral bioavailability further supports its use in preclinical studies aimed at understanding malaria biology.

Protein kinase G inhibitor-2 is a selective inhibitor of mycobacterial protein kinase G, exhibiting an IC50 value of 3 μM. This compound is utilized in the investigation of mycobacterial infections and their associated signaling pathways. Its efficacy as a PKG inhibitor supports research into therapeutic strategies targeting mycobacterial diseases.

Dibutyryl-cGMP sodium is a cell-permeable analogue of cyclic guanosine monophosphate (cGMP) that primarily activates cGMP-dependent protein kinase (PKG). This compound has been shown to inhibit the release of [3H]-arachidonic acid from γ-thrombin-stimulated human platelets, demonstrating its role in modulating platelet activity. Additionally, Dibutyryl-cGMP sodium induces peripheral antinociception through the activation of ATP-sensitive potassium channels, making it a valuable tool for research in pain modulation and cardiovascular physiology.

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.

Rp-8-pCPT-cGMPS sodium is a selective inhibitor of cGMP-dependent protein kinase (cGK), functioning primarily through the modulation of cGMP signaling pathways. This compound also acts as an agonist for cyclic nucleotide-gated (CNG) channels in a voltage-dependent manner, making it valuable for studying the intricate roles of cyclic nucleotides in cellular processes. Its applications extend to research in cardiovascular physiology, neurobiology, and signal transduction mechanisms.

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.

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.

DT-3 is a selective inhibitor of protein kinase G Iα (PKG Iα), designed to impede the cGMP-PKG signaling pathway. This membrane-permeable peptide demonstrates significant pharmacological activity, making it valuable for research applications focused on cardiovascular function and signaling related diseases. DT-3 enables the investigation of the roles of PKG Iα in various cellular processes and helps elucidate its contributions to cardiovascular health and disease.

AP-C3 is a selective inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII), exhibiting a pIC50 of 6.3. This compound demonstrates limited inhibition of cGKII-dependent anion secretion, making it a valuable tool for studying cGKII signaling pathways. AP-C3 is applicable in research focused on cardiovascular and gastrointestinal functions mediated by cGKII.

AP-C6 is a selective inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII), demonstrating a pIC50 of 6.5. This compound effectively inhibits human cGKII activity in a concentration-dependent manner in vitro. Additionally, AP-C6 enhances cAMP signaling through phosphodiesterase (PDE) inhibition, making it a valuable tool for research involving cGKII and related signaling pathways.

AP-C7 is a selective inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII), exhibiting a pIC50 value of 5.0. This compound demonstrates weak inhibition of cGKII-dependent anion secretion, making it a valuable tool for exploring the role of cGKII in cellular signaling pathways and its impact on various physiological processes. AP-C7 can be utilized in research focused on cardiovascular biology, gastrointestinal function, and related areas studying cGMP signaling mechanisms.

AP-C1 is a selective inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII), demonstrating a pIC50 of 6.5. This compound primarily attenuates cGKII activity while displaying minimal effects on cGKII-mediated anion secretion. AP-C1 is valuable for research applications focused on investigating the role of cGKII in cellular signaling and related physiological processes.

AP-C4 is a selective inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII), exhibiting a pIC50 value of 5.2. This compound demonstrates the ability to effectively inhibit cGKII without affecting cGKII-dependent anion secretion. AP-C4 is valuable for research examining the role of cGKII in various physiological and pathological processes, enabling further exploration of cGKII's functions in signaling pathways.

1-NH2-cGMP is an analog of cyclic guanosine monophosphate (cGMP), designed to serve as a potent signaling molecule in various biological systems. This compound exhibits activity in modulating nitric oxide signaling pathways and influencing smooth muscle relaxation. 1-NH2-cGMP is applicable in research exploring cardiovascular function, neuronal signaling, and cellular proliferation, making it a valuable tool for studies involving cGMP-dependent signaling mechanisms.

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.

PET-cGMP is a cyclic guanosine monophosphate analog that selectively activates protein kinase G (PKG) I, with an EC50 of 3.8 nM for the PKG Iβ isoform and 193 nM for PKG II. Its potent agonistic properties make it a valuable tool in studying signaling pathways involving PKG I, particularly in cardiovascular and neuronal research. Researchers can utilize PET-cGMP to elucidate the roles of cGMP signaling in various physiological and pathological contexts.

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.

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.

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.

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.

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.