2. Signaling Pathways
  3. Stem Cell/Wnt
  4. PKG

PKG

cGMP-dependent protein kinase

PKG is a cyclic guanosine monophosphate (cGMP) -dependent serine/threonine kinase, which is activated by cGMP, phosphorylates the substrates, and regulates intracellular signal transduction. PKG inhibits β-catenin and cyclin D1 and regulates cell growth and apoptosis. PKG phosphorylates myosin light chains in smooth muscle cells, causing smooth muscle relaxation, thereby regulating vasodilation and blood pressure. PKG phosphorylates calcium channels for calcium homeostasis regulation. PKG regulates gene expression by phosphorylating transcription factors, thereby affecting cell differentiation and proliferation. PKG also regulates circadian rhythm, anxiety and fear memory. PKG has 2 subtypes, PKG I and PKG II. PKG I is mainly expressed in smooth muscle, platelets and specific neuronal areas, participates in vascular smooth muscle relaxation and cardiac function regulation. PKG II is mainly expressed in intestinal secretory epithelial cells, juxtaglomerular cells, adrenal cortex, chondrocytes and suprachiasmatic nucleus, which is mainly involved in the regulation of kidney and adrenal function, as well as bone growth and development. PKG dysfunction could lead to cancer, neurological or cardiovascular diseases[1][2][3].

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-153542
    AP-C6
    		Inhibitor
    AP-C6 is a potent inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 6.5. AP-C6 concentration-dependently inhibits human cGKII activity in vitro. AP-C6 potentiate cAMP signaling by PDE inhibition.
    AP-C6
  • HY-P11034
    BPDEtide
    		Substrate
    BPDEtide is a synthetic peptide. BPDEtide has apparent Km values of 68 and 320 μM for cGK and cAK, respectively. BPDEtide is the most selective peptide substrate for measuring cGK activity.
    BPDEtide
  • HY-161578
    Dithio-CN03
    		Inhibitor
    Dithio-CN03 is a compound with the highest neuroprotective efficacy. Dithio-CN03 fights the progression of retinitis pigmentosa (RP) by inhibiting the cGMP mediated signaling pathway and reducing photoreceptor cell death. Dithio-CN03 can be used in research into RP and other retinal degenerative diseases.
    Dithio-CN03
  • HY-153541
    AP-C7
    		Inhibitor
    AP-C7 is an inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 5.0. AP-C7 only weakly inhibits cGKII-dependent anion secretion.
    AP-C7
  • HY-179550
    Avanafil metabolite M4
    		Activator
    Avanafil metabolite M4 (Compound M-4ii) is a metabolite of Avanafil (HY-18252). Avanafil is a selective Phosphodiesterase-5 (PDE-5) inhibitor with IC50s of 5.2, 630, 5700, 6200, 12000, 27000, 51000 and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cGMP hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis.
    Avanafil metabolite M4
  • HY-153537
    AP-C1
    		Inhibitor
    AP-C1 is a potent inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 6.5. AP-C1 only weakly inhibits cGKII-dependent anion secretion.
    AP-C1
  • HY-P10036
    G-Subtide
    G-Subtide is a G-substrate peptide localized in Purkinje cells of the cerebellum. G-Subtide has little activity distinct from background and is a preferentially phosphorylated peptide substrate of recombinant PfPKG2 protein.
    G-Subtide
  • HY-153540
    AP-C4
    		Inhibitor
    AP-C4 is an inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 5.2. AP-C3 does not inhibit cGKII-dependent anion secretion.
    AP-C4
  • HY-131737
    1-NH2-cGMP
    		Activator
    1-NH2-cGMP is an analog of cGMP.
    1-NH2-cGMP
  • HY-137378A
    8-Br-PET-cGMP
    		Agonist
    8-Br-PET-cGMP is an agonist of cGMP-dependent protein kinase type I (cGKI). 8-Br-PET-cGMP promotes the dimerization of cGKI and activates its catalytic activity by binding to the regulatory domain of cGKI. 8-Br-PET-cGMP can be used to study the role of cGMP signaling pathways in cell growth, vasodilation, and smooth muscle cell function.
    8-Br-PET-cGMP
  • HY-137665
    PET-cGMP
    		Agonist
    PET-cGMP is a cyclic guanosine monophosphate analog and an effective selective agonist of PKG I, the EC50 of PET-cGMP for PKG Iβ is 3.8 nM, while for PKG II, it's 193 nM.
    PET-cGMP
  • HY-137108
    Sp-8-pCPT-cGMPS
    		Activator
    Sp-8-pCPT-cGMPS is a potent cyclic guanosine monophosphate-gated channel agonist and a lipophilic activator of protein kinase G (types I α, I β, and II) and protein kinase A type II with excellent cell membrane permeability and phosphodiesterase stability. Sp-8-pCPT-cGMPS can be used to study the role of cGMP in neural plasticity and synaptic transmission.
    Sp-8-pCPT-cGMPS
  • HY-174130
    PI4Kβ/PKG-IN-1
    		Inhibitor
    PI4Kβ/PKG-IN-1 (Compound 19) is an orally active dual inhibitor targeting Plasmodium phosphatidylinositol 4-kinase beta (PI4Kβ) and cGMP-dependent protein kinase (PKG). PI4Kβ/PKG-IN-1 exhibits potent antiplasmodial activity. PI4Kβ/PKG-IN-1 is promising for research of malaria.
    PI4Kβ/PKG-IN-1
  • HY-137629
    Sp-8-pCPT-PET-cGMPS
    		Activator
    Sp-8-pCPT-PET-cGMPS is an activator for PKG-I. Sp-8-pCPT-PET-cGMPS can be used for research of NO/NOS/sGC/PKG-I signaling pathway in cardiac differentiation.
    Sp-8-pCPT-PET-cGMPS
  • HY-134271
    8-Br-cGMP-AM
    		Activator
    8-Br-cGMP-AM is a derivative of 8-Br-cGMP. As an activator of PKG (cGMP-dependent protein kinase), it can lead to a variety of biological effects such as vasodilation and platelet inhibition. 8-Br-cGMP-AM can be used in the study of cardiovascular diseases.
    8-Br-cGMP-AM
  • HY-134332
    8-pCPT-5'-AMP
    		Activator
    8-pCPT-5'-AMP is an analogue of 5'-AMP and a lipophilic activator of PKA, PKG and Epac (exchange protein activated by cAMP).
    8-pCPT-5'-AMP
  • HY-137622
    Sp-cGMPS
    		Activator
    Sp-cGMPS is an activator of cGMP-dependent protein kinases (PKGs). Sp-cGMPS can be used in cardiovascular disease-related research.
    Sp-cGMPS
  • HY-135110A
    Rp-8-Br-cGMPS
    		Inhibitor
    Rp-8-Br-cGMPS (Rp-8-bromo-Cyclic GMPS) sodium salt is a potent Ca2+-ATPase activator. Rp-8-Br-cGMPS is also an agonist of the rod CNG channel and an inhibitor of PKG. Rp-8-Br-cGMPS sodium salt mediates cytosolic Ca2+ reduction by activating Ca2+-ATPase and subsequently removing Ca2+ from the cell.
    Rp-8-Br-cGMPS
  • HY-137373
    Rp-8-pCPT-cGMPS
    		Inhibitor
    Rp-8-pCPT-cGMPS is a competitive inhibitor of cGMP-dependent protein kinase (PKG) (Ki=0.5 μM). Rp-8-pCPT-cGMPS has high lipid solubility and can more easily penetrate the cell membrane and reach sufficient concentration inside the cell to inhibit cGMP-dependent protein kinase. Rp-8-pCPT-cGMPS can be used to study the activity and function of cGMP-dependent protein kinase in platelets.
    Rp-8-pCPT-cGMPS
  • HY-137633
    Sp-8-Br-PET-cGMPS
    		Agonist
    Sp-8-Br-PET-cGMPS is a membrane-permeable PKG agonist and a membrane-permeable inhibitor of retinal-type cGMP-gated ion channels, as well as an activator of cGMP-dependent protein kinases I α and I β. Sp-8-Br-PET-cGMPS is resistant to mammalian cyclic nucleotide-dependent phosphodiesterases, has no metabolic side effects, and is more lipophilic and permeable than Sp-8-pCPT-cGMPS. Sp-8-Br-PET-cGMPS can be used to study the role of cGMP signaling pathways in the nervous system.
    Sp-8-Br-PET-cGMPS
Cat. No. Product Name / Synonyms Application Reactivity