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].

References:

[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]

PKG Related Products (39)
Antibodies (1)

By Effects:	Inhibitors (18) Agonists (4) Substrate (1) Activators (7)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-P2692B

DT-2 acetate	Inhibitor	98.17%
DT-2 is a potent and selective inhibitor of the cGMP-dependent protein kinase (PKG). DT-2 inhibits PKG catalyzed phosphorylation (K_i: 12.5 nM).

HY-P1292

PKG inhibitor peptide		99.81%
PKG inhibitor peptide is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a K_i of 86 μM.

HY-P0142A

DT-3 acetate	Inhibitor	99.95%
DT-3 acetate is a membrane-permeable protein kinase G Iα (PKG Iα) inhibitory peptide and shows pharmacological blockade of the cGMP-PKG signalling.

HY-155106

SMA4		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.

HY-108548

Rp-8-Br-PET-cGMPS sodium	Inhibitor	99.42%
Rp-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.

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.

HY-180585

LOXL2/sGC modulator-2	Inhibitor
LOXL2/sGC modulator-2 (Compound 9k) is a selective and orally active lysyl oxidase-like 2 (LOXL2) and soluble guanylate cyclase (sGC) dual-target regulator. LOXL2/sGC modulator-2 shows inhibitory activity for LOXL2 with an IC₅₀ of 0.1 μM and can activate sGC. LOXL2/sGC modulator-2 can ameliorate vascular remodeling and reduce pulmonary artery pressure. LOXL2/sGC modulator-2 can downregulate PKG1, PCNA, α-SMA, collagen I and fibronectin levels. LOXL2/sGC modulator-2 can be used for the research of pulmonary arterial hypertension .

HY-112465

H-8 dihydrochloride	Inhibitor	99.19%
H-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.

HY-174134

PI4Kβ/PKG-IN-2	Inhibitor	99.34%
PI4Kβ/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.

HY-112197

PKG drug G1		99.11%
PKG agent G1 targets C42 of PKG Iα. PKG agent G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.

HY-P1561

PKG Substrate		98.97%
PKG Substrate is a selective substrate for cGMP-dependent protein kinase (PKG).

HY-135110

Rp-8-Br-cGMPS sodium	Inhibitor	99.9%
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.

HY-110221

Rp-8-pCPT-cGMPS sodium	Inhibitor	99.9%
Rp-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.

HY-P1556A

Vasonatrin Peptide (VNP) TFA		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.

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.

HY-P1292A

PKG inhibitor peptide TFA
PKG inhibitor peptide TFA is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a K_i of 86 μM.

HY-P1556

Vasonatrin Peptide (VNP)
Vasonatrin 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.

HY-151203

PKG1α activator 3
PKG1α 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.

HY-P0142

DT-3	Inhibitor
DT-3 is a membrane-permeable protein kinase G Iα (PKG Iα) inhibitory peptide and shows pharmacological blockade of the cGMP-PKG signalling.

HY-153539

AP-C3	Inhibitor
AP-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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PKG

PKG Related Products (39)

Antibodies (1)

PKG Related Products (39):