GRK 1 Activators
GRK1 Activators encompass a range of chemical compounds that indirectly promote the functional activity of GRK1 through various intracellular signaling pathways. Isoproterenol functions as a beta-adrenergic agonist, activating adrenergic receptors and facilitating GRK1 recruitment and subsequent phosphorylation of these receptors, while Forskolin directly stimulates adenylate cyclase, causing an increase in cAMP and activation of PKA, which can then phosphorylate GRK1, leading to enhanced receptor phosphorylation. Similarly, IBMX acts as a phosphodiesterase inhibitor, preventing cAMP degradation and indirectly fostering PKA activity that could enhance GRK1 function. GTPγS, a GTP analog, sustains GPCRs in their active form, which could augment GRK1's ability to phosphorylate these receptors.
Further contributing to the activation of GRK1 are PDE inhibitors such as Zaprinast and Vardenafil, which elevate cGMP levels and can indirectly promote GRK1 activity through PKG-related pathways. Rolipramraises cAMP, possibly enhancing GRK1 activity by PKA-mediated phosphorylation. Gallein's inhibition of the Gβγ subunit might lift the Gβγ-mediated inhibition of GRK1, thus enhancing GRK1's interactions with GPCRs. The endogenous compound adenosine, upon activating its receptors, could recruit GRK1 to the receptor complexes, potentially facilitating the phosphorylation process that GRK1 mediates. Nicotine, through activation of nicotinic acetylcholine receptors, may amplify GRK1's role in receptor phosphorylation and desensitization. Lastly, Alprostadil, a prostaglandin E1 analog, triggers E-type prostanoid receptors, causing a rise in cAMP that could activate PKA, thereby potentially heightening GRK1's role in GPCR phosphorylation.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Isoproterenol Hydrochloride | 51-30-9 | sc-202188 sc-202188A | 100 mg 500 mg | $28.00 $38.00 | 5 | |
A synthetic catecholamine and non-selective beta-adrenergic agonist that leads to the activation of adrenergic receptors, which can facilitate the recruitment and activation of GRK1 to phosphorylate the activated receptors. | ||||||
Forskolin | 66575-29-9 | sc-3562 sc-3562A sc-3562B sc-3562C sc-3562D | 5 mg 50 mg 1 g 2 g 5 g | $78.00 $153.00 $740.00 $1413.00 $2091.00 | 73 | |
Directly stimulates adenylate cyclase, increasing cAMP levels within the cell. Elevated cAMP activates PKA, which can phosphorylate GRK1, leading to its activation and subsequent phosphorylation of G protein-coupled receptors (GPCRs). | ||||||
IBMX | 28822-58-4 | sc-201188 sc-201188B sc-201188A | 200 mg 500 mg 1 g | $260.00 $350.00 $500.00 | 34 | |
A non-selective inhibitor of phosphodiesterases (PDEs), IBMX prevents the breakdown of cAMP and cGMP, thereby indirectly promoting PKA activity which can enhance GRK1 function by phosphorylating its substrates. | ||||||
Guanosine 5′-O-(3-thiotriphosphate) tetralithium salt | 94825-44-2 | sc-202639 | 10 mg | $465.00 | ||
A non-hydrolyzable analog of GTP that activates G proteins. GRK1 is known to phosphorylate activated G protein-coupled receptors (GPCRs), and GTPγS can enhance this activity by maintaining GPCRs in an active conformation. | ||||||
Zaprinast (M&B 22948) | 37762-06-4 | sc-201206 sc-201206A | 25 mg 100 mg | $105.00 $250.00 | 8 | |
A selective inhibitor of PDE5, increasing cGMP levels, which can indirectly enhance GRK1 activity through cGMP-dependent protein kinase (PKG) pathways that may phosphorylate GRK1 or its associated partners. | ||||||
Vardenafil | 224785-90-4 | sc-362054 sc-362054A sc-362054B | 100 mg 1 g 50 g | $526.00 $735.00 $16653.00 | 7 | |
Another selective inhibitor of PDE5, it increases cGMP levels, potentially enhancing GRK1 activity through PKG-related pathways that may influence GRK1 phosphorylation or its interactions with GPCRs. | ||||||
Rolipram | 61413-54-5 | sc-3563 sc-3563A | 5 mg 50 mg | $77.00 $216.00 | 18 | |
A selective PDE4 inhibitor, which increases cAMP levels, potentially enhancing the activity of PKA. PKA can then phosphorylate GRK1, leading to increased GRK1-mediated phosphorylation of GPCRs. | ||||||
Gallein | 2103-64-2 | sc-202631 | 50 mg | $85.00 | 20 | |
A Gβγ subunit inhibitor which could enhance GRK1 activity by disrupting Gβγ-mediated inhibition of GRK1, therefore increasing GRK1’s interaction with and phosphorylation of GPCRs. | ||||||
Adenosine | 58-61-7 | sc-291838 sc-291838A sc-291838B sc-291838C sc-291838D sc-291838E sc-291838F | 1 g 5 g 100 g 250 g 1 kg 5 kg 10 kg | $34.00 $48.00 $300.00 $572.00 $1040.00 $2601.00 $4682.00 | 1 | |
Through activation of adenosine receptors, which are GPCRs, adenosine can recruit GRK1 to the receptor complex, potentially enhancing the GRK1-mediated phosphorylation process. | ||||||
PGE1 (Prostaglandin E1) | 745-65-3 | sc-201223 sc-201223A | 1 mg 10 mg | $31.00 $145.00 | 16 | |
A prostaglandin E1 analog that activates E-type prostanoid receptors, leading to increased intracellular cAMP. This elevation in cAMP can activate PKA and potentially enhance GRK1’s phosphorylation of GPCRs. | ||||||