Date published: 2025-10-18

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GRK 6 Activators

The chemical class of GRK6 activators represents a diverse set of compounds that intricately regulate the activity of G protein-coupled receptor kinase 6 (GRK6), a pivotal player in GPCR signaling. These activators, employing both direct and indirect mechanisms, offer valuable insights into the multifaceted control of GRK6 function and its integration into broader cellular processes. Direct activators, including Isoproterenol, Ropinirole, AC-42, and Tamoxifen, exert their effects by directly engaging GPCRs or their associated receptors, leading to the recruitment and phosphorylation of these receptors by activated GRK6. Isoproterenol, a beta-adrenergic receptor agonist, stimulates beta-adrenergic receptors, initiating GRK6-mediated phosphorylation of GPCRs. Ropinirole, a dopamine receptor agonist, activates dopamine receptors, leading to the direct activation of GRK6. AC-42, a muscarinic acetylcholine receptor agonist, stimulates muscarinic receptors, inducing GRK6-mediated phosphorylation of GPCRs. Tamoxifen, a selective estrogen receptor modulator, modulates estrogen receptors, impacting GRK6 activity and its role in GPCR signaling pathways.

Indirect activators, such as Dihydrocapsaicin, Forskolin, Retinoic Acid, PGE2, Salvinorin A, 8-Cyclopentyl-1,3-dipropylxanthine, and Hexamethonium Bromide, modulate GRK6 activity through various signaling pathways or receptor interactions. Dihydrocapsaicin indirectly activates GRK6 by influencing TRPV1 receptors, highlighting the crosstalk between TRPV1 receptors and GRK6 in cellular responses to capsaicinoid stimulation. Forskolin indirectly activates GRK6 by increasing cAMP levels, modulating GRK6 activity through cAMP-mediated signaling events. Retinoic Acid indirectly activates GRK6 by influencing retinoic acid receptors, providing insights into the regulation of GRK6 function by retinoic acid. PGE2 indirectly activates GRK6 by modulating EP receptors, contributing to the regulation of GRK6 function in prostaglandin E2 signaling pathways. Salvinorin A indirectly activates GRK6 by stimulating kappa-opioid receptors, providing a link between kappa-opioid receptor activation and GRK6-mediated phosphorylation of GPCRs. 8-Cyclopentyl-1,3-dipropylxanthine (DPCPX) indirectly activates GRK6 by blocking adenosine receptors, influencing GRK6 activity through the blockade of adenosine receptor-dependent events. Hexamethonium Bromide indirectly activates GRK6 by blocking nicotinic receptors, highlighting the impact of nicotinic receptor blockade on GRK6-mediated phosphorylation of GPCRs.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Isoproterenol Hydrochloride

51-30-9sc-202188
sc-202188A
100 mg
500 mg
$27.00
$37.00
5
(0)

Isoproterenol, a beta-adrenergic receptor agonist, directly activates GRK6 by stimulating G protein-coupled receptors (GPCRs). Isoproterenol binds to beta-adrenergic receptors, leading to the activation of GRK6 through GPCR-mediated signaling pathways. This direct activation occurs through the recruitment and phosphorylation of GPCRs by activated GRK6, highlighting the role of beta-adrenergic receptor agonists in modulating GRK6 activity and downstream GPCR signaling events.

Dihydrocapsaicin

19408-84-5sc-202578
sc-202578A
10 mg
50 mg
$51.00
$153.00
1
(1)

Dihydrocapsaicin, a capsaicinoid found in chili peppers, indirectly activates GRK6 by modulating TRPV1 receptor signaling. TRPV1 receptors are involved in pain perception, and dihydrocapsaicin activates these receptors, indirectly influencing GRK6 activity.

Forskolin

66575-29-9sc-3562
sc-3562A
sc-3562B
sc-3562C
sc-3562D
5 mg
50 mg
1 g
2 g
5 g
$76.00
$150.00
$725.00
$1385.00
$2050.00
73
(3)

Forskolin, an adenylyl cyclase activator, indirectly activates GRK6 by increasing cAMP levels. Forskolin stimulates adenylyl cyclase, leading to elevated cAMP levels, which modulate GRK6 activity. This indirect activation occurs through cAMP-mediated signaling events that influence the phosphorylation of GPCRs by GRK6. Forskolin-induced changes in intracellular cAMP dynamics contribute to the regulation of GRK6 function and its role in GPCR signaling pathways.

Retinoic Acid, all trans

302-79-4sc-200898
sc-200898A
sc-200898B
sc-200898C
500 mg
5 g
10 g
100 g
$65.00
$319.00
$575.00
$998.00
28
(1)

Retinoic acid, a derivative of vitamin A, indirectly activates GRK6 by influencing retinoic acid receptors (RARs). Retinoic acid activates RARs, which can impact GRK6 activity through receptor-mediated signaling pathways. This indirect activation occurs through the modulation of RAR-dependent events that influence GRK6-mediated phosphorylation of GPCRs.

Ropinirole Hydrochloride

91374-20-8sc-205843
sc-205843A
25 mg
100 mg
$82.00
$311.00
1
(0)

Ropinirole, a dopamine receptor agonist, directly activates GRK6 by stimulating dopamine receptors. Ropinirole binds to dopamine receptors, leading to the activation of GRK6 through receptor-mediated signaling pathways. This direct activation occurs through the recruitment and phosphorylation of dopamine receptors by activated GRK6, highlighting the role of dopamine receptor agonists in modulating GRK6 activity and downstream GPCR signaling events.

PGE2

363-24-6sc-201225
sc-201225C
sc-201225A
sc-201225B
1 mg
5 mg
10 mg
50 mg
$56.00
$156.00
$270.00
$665.00
37
(1)

Prostaglandin E2 (PGE2), a prostaglandin, indirectly activates GRK6 by modulating EP receptors. PGE2 activates EP receptors, which can impact GRK6 activity through receptor-mediated signaling pathways. This indirect activation occurs through the modulation of EP receptor-dependent events that influence GRK6-mediated phosphorylation of GPCRs.

AC 42

447407-36-5sc-207243
5 mg
$330.00
(0)

AC 42 a muscarinic acetylcholine receptor agonist, directly activates GRK6 by stimulating muscarinic receptors. AC 42 binds to muscarinic receptors, leading to the activation of GRK6 through receptor-mediated signaling pathways. This direct activation occurs through the recruitment and phosphorylation of muscarinic receptors by activated GRK6, highlighting the role of muscarinic receptor agonists in modulating GRK6 activity and downstream GPCR signaling events.

PD 116,948

102146-07-6sc-200115
sc-200115A
25 mg
100 mg
$122.00
$224.00
6
(0)

PD 116,948, an adenosine A1 receptor antagonist, indirectly activates GRK6 by blocking adenosine receptors. PD 116,948 inhibits adenosine receptors, indirectly influencing GRK6 activity through receptor-mediated signaling pathways. This indirect activation occurs through the modulation of adenosine receptor-dependent events that impact GRK6-mediated phosphorylation of GPCRs.

Hexamethonium bromide

55-97-0sc-205712
sc-205712A
10 g
25 g
$45.00
$63.00
(0)

Hexamethonium bromide, a nicotinic acetylcholine receptor antagonist, indirectly activates GRK6 by blocking nicotinic receptors. Hexamethonium bromide inhibits nicotinic receptors, indirectly influencing GRK6 activity through receptor-mediated signaling pathways. This indirect activation occurs through the modulation of nicotinic receptor-dependent events that impact GRK6-mediated phosphorylation of GPCRs.

Tamoxifen

10540-29-1sc-208414
2.5 g
$256.00
18
(2)

Tamoxifen, a selective estrogen receptor modulator, indirectly activates GRK6 by modulating estrogen receptors. Tamoxifen activates estrogen receptors, which can impact GRK6 activity through receptor-mediated signaling pathways. This indirect activation occurs through the modulation of estrogen receptor-dependent events that influence GRK6-mediated phosphorylation of GPCRs.