Date published: 2025-10-16

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cGKI Activators

cGKI, which stands for cyclic guanosine monophosphate (cGMP)-dependent protein kinase type I, is an enzyme of pivotal significance in the realm of cell signaling. The primary role of cGKI is to mediate the effects of cGMP, a second messenger molecule that is involved in numerous cellular processes. Second messengers are intracellular molecules that relay external signals from cell membrane receptors to target molecules inside the cell. cGMP is generated in response to external stimuli, and once produced, it can activate cGKI. Activators of cGKI are compounds that facilitate or enhance the action of cGKI, enabling it to optimally mediate the effects of cGMP. Diving deeper into the molecular mechanisms, the activation of cGKI by cGMP leads to its phosphorylation of target proteins, bringing about various physiological effects. Given that cGMP signaling plays roles in a plethora of processes ranging from vasodilation and platelet aggregation to synaptic plasticity and smooth muscle relaxation, cGKI activators, by extension, have the potential to influence a wide array of biological functions. The specificity and function of cGKI activators can vary; some might directly bind and enhance cGKI activity, while others may act indirectly, possibly by increasing cGMP availability or by modulating pathways that influence cGKI activation. Understanding the intricacies of these activators, their molecular interactions, and the subsequent cellular consequences is crucial for grasping the wider picture of cell signaling and communication.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

8-Bromo-cGMP

51116-01-9sc-200316
sc-200316A
10 mg
50 mg
$102.00
$347.00
7
(1)

8-Bromo-cGMP is a potent cGMP analog that selectively activates cGMP-dependent protein kinase I (cGKI). Its unique bromine substitution enhances binding affinity, facilitating specific interactions with cGKI's regulatory domain. This compound influences downstream signaling pathways by modulating phosphorylation states, leading to distinct cellular responses. The presence of the bromine atom also alters the compound's stability and reactivity, impacting its kinetics in biochemical assays.

8-pCPT-cGMP, TEA

sc-221150
25 µmol
$660.00
(0)

8-pCPT-cGMP, TEA is a selective cGMP analog that effectively activates cGMP-dependent protein kinase I (cGKI). The presence of the p-chlorophenyl group enhances its lipophilicity, promoting membrane permeability and facilitating rapid cellular uptake. This compound exhibits unique binding dynamics, stabilizing the cGKI conformation and influencing its enzymatic activity. Its distinct structural features also modulate reaction kinetics, allowing for precise control over signaling cascades.

8-Bromoguanosine 3′, 5′ -cyclic monophosphoric acid

31356-94-2sc-291685
sc-291685A
5 mg
10 mg
$116.00
$206.00
(0)

8-Bromoguanosine 3', 5'-cyclic monophosphoric acid is a potent cGKI activator characterized by its brominated guanosine structure, which enhances its interaction with target proteins. The bromine atom introduces unique steric effects, influencing molecular conformation and binding affinity. This compound exhibits distinct allosteric modulation of cGKI, altering its phosphorylation dynamics and enabling fine-tuning of downstream signaling pathways. Its stability in aqueous environments further supports prolonged activity in cellular contexts.

Vardenafil

224785-90-4sc-362054
sc-362054A
sc-362054B
100 mg
1 g
50 g
$516.00
$720.00
$16326.00
7
(1)

Another PDE5 inhibitor similar in action to sildenafil. It's sold under various trade names like Levitra.

Tadalafil

171596-29-5sc-208412
50 mg
$176.00
13
(2)

Yet another PDE5 inhibitor, which goes by the trade name Cialis. It has a longer half-life compared to sildenafil and vardenafil.

Riociguat

625115-55-1sc-476845
5 mg
$300.00
(0)

A soluble guanylyl cyclase (sGC) stimulator studied in the research of pulmonary arterial hypertension (PAH) and chronic thromboembolic pulmonary hypertension (CTEPH). It increases cGMP levels by stimulating sGC.