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].
Referencias:
- [1]. Francis SH, et al., cGMP-dependent protein kinases and cGMP phosphodiesterases in nitric oxide and cGMP action. Pharmacol Rev. 2010 Sep;62(3):525-63. [Content Brief]
- [2]. Hofmann F, et al., cGMP-dependent protein kinases (cGK). Methods Mol Biol. 2013;1020:17-50. [Content Brief]
- [3]. Karami-Tehrani F, et al., Expression of cGMP-dependent protein kinase, PKGIα, PKGIβ, and PKGII in malignant and benign breast tumors. Tumour Biol. 2012 Dec;33(6):1927-32. [Content Brief]
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Productos relacionados con PKG (40)
Productos relacionados con (40)
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Antibodies (1)
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Protein kinase inhibitor H-7
0 ImagesProtein kinase inhibitor H-7 is a selective inhibitor of PKC and cyclic nucleotide-dependent protein kinases, with a Ki value of 6.0 μM for rabbit protein kinase C, a Ki value of 3.0 μM for rabbit cAMP-dependent protein kinase, and a Ki value of 5.8 μM for porcine cGMP-dependent protein kinase. Protein kinase inhibitor H-7 has no effect on Ca2+-calmodulin-dependent enzymes. Protein kinase inhibitor H-7 regulates the Actin cytoskeleton, inhibits contractility, disrupts stress fibers, induces protrusive activity, stabilizes intercellular junctions, and triggers rapid and reversible cytoskeletal reorganization. Protein kinase inhibitor H-7 serves as a research tool for elucidating the functions of protein kinase C-mediated signaling systems.
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PKG inhibitor peptide
0 ImagesPKG inhibitor peptide is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a Ki of 86 μM.
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SMA4
0 ImagesReferencia número: HY-155106Pureza: 99.18%SMA4 is a selective PKG1α activator with basal EC50 value of 29 μM. SMA4 facilitates phosphorylation of the known PKG1 substrate, vasodilator-stimulated phosphoprotein (VASP), and inhibits human pulmonary arterial smooth muscle cells (hPASMC) proliferation. SMA4 can be used for cardiovascular disease research.
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Rp-8-Br-PET-cGMPS sodium
0 ImagesSynonyms: Rp-8-Bromo-PET-cGMPSRp-8-Br-PET-cGMPS sodium (Rp-8-Bromo-PET-cGMPS) is an analog of cyclic GMP (cGMP). It is a cell permeable, competitive, and reversible inhibitor of cGMP-dependent protein kinases (cGKs) that blocks activation of cGKI and cGKII by cGMP (Kis=35 and 30 nM). It less potently inhibits protein kinase A (Ki=11 μM) and cGMP-induced activation of cyclic nucleotide-gated channels (IC50=25 μM). In the absence of cGMP stimulation, Rp-8-bromo-PET-cGMPS can act as a partial agonist of cGKI (Ki=1 μM). Rp-8-bromo-PET-cGMPS is resistant to hydrolysis by phosphodiesterase 11.
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H-8 dihydrochloride
0 ImagesH-8 dihydrochloride is a selective Cyclic nucleotide-dependent protein kinase inhibitor. H-8 dihydrochloride potently inhibits cGMP- and cAMP-dependent protein phosphorylation. H-8 dihydrochloride enhances the vasodilatory effect induced by 8-bromo-cAMP (HY-12306A). H-8 dihydrochloride fails to attenuate the vasodilatory effects induced by 8-bromo-cGMP (HY-101379A), atrial natriuretic peptide II, or Sodium nitroprusside (HY-B0564) in rat aorta.
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PI4Kβ/PKG-IN-2
0 ImagesPI4Kβ/PKG-IN-2 (Compound 20) is an orally active dual inhibitor of Plasmodium phosphatidylinositol 4-kinase beta (PI4Kβ) and cGMP-dependent protein kinase (PKG). PI4Kβ/PKG-IN-2 has potent inhibitory effects on Plasmodium. PI4Kβ/PKG-IN-2 is promising for research of malaria.
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Rp-8-Br-cGMPS sodium
0 ImagesSynonyms: Rp-8-bromo-Cyclic GMPS sodium
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Rp-8-pCPT-cGMPS sodium
0 ImagesRp-8-pCPT-cGMPS sodium is the sodium salt form of Rp-8-pCPT-cGMPS. Rp-8-pCPT-cGMPS is an inhibitor for cGMP-dependent protein kinase (cGK). Rp-8-pCPT-cGMPS sodium is an agonist for cyclic nucleotide-gated (CNG) channels in a voltage-dependent manner.
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Vasonatrin Peptide (VNP) TFA
0 ImagesReferencia número: HY-P1556APureza: 98.79%Vasonatrin Peptide (VNP) TFA is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide TFA possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide TFA protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway.
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8-pCPT-cGMP-AM
0 ImagesReferencia número: HY-134345No. CAS: 272445-72-4Synonyms: 8-(4-Chlorophenylthio)-cGMP-AM8-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.
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PKG inhibitor peptide TFA
0 ImagesReferencia número: HY-P1292APKG inhibitor peptide TFA is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a Ki of 86 μM.
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Vasonatrin Peptide (VNP)
0 ImagesReferencia número: HY-P1556No. CAS: 141676-35-9Vasonatrin Peptide (VNP) is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway.
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PKG1α activator 3
0 ImagesReferencia número: HY-151203No. CAS: 2773367-58-9PKG1α activator 3 is a PKG1α activator (EC50 basal/partial=13/0.52 μM). PKG1α activator 3 shows anti-proliferative effects to smooth muscle cell, and can be used in cardiovascular disease research.
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DT-3
0 ImagesReferencia número: HY-P0142No. CAS: 329306-46-9DT-3 is a membrane-permeable protein kinase G Iα (PKG Iα) inhibitory peptide and shows pharmacological blockade of the cGMP-PKG signalling.
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AP-C3
0 ImagesReferencia número: HY-153539No. CAS: 682795-78-4AP-C3 is a potent inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 6.3. AP-C3 only weakly inhibits cGKII-dependent anion secretion.
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AP-C6
0 ImagesReferencia número: HY-153542No. CAS: 2234276-60-7AP-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.
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