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-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-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-134345
    8-pCPT-cGMP-AM
    		Agonist
    8-pCPT-cGMP-AM (8-(4-Chlorophenylthio)-cGMP-AM) is a highly membrane permeable prodrug of the PKG agonist 8-pCPT-cGMP, which increases the membrane permeability of cGMP and is converted to its active form by esterase hydrolysis within the cell, thereby activating PKG. 8-pCPT-cGMP-AM can be used to explore the role of cGMP signaling in neural plasticity and memory formation.
    8-pCPT-cGMP-AM
  • 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