GPR113 Activators
Chemical activators of GPR113 can initiate a cascade of intracellular events leading to the protein's activation. Forskolin is known to directly stimulate adenylate cyclase, which causes an increase in cyclic AMP (cAMP) within the cell. This rise in cAMP activates protein kinase A (PKA), which then can phosphorylate GPR113, leading to its activation. Similarly, Isoproterenol, through its action as a beta-adrenergic agonist, also raises intracellular cAMP levels via G protein-coupled receptor signaling. This process also involves the activation of PKA, which then acts on GPR113. Phorbol 12-myristate 13-acetate (PMA) takes a different route; it activates protein kinase C (PKC), another kinase that can phosphorylate GPR113. Activation of PKC does not rely on the cAMP pathway but can still result in the phosphorylation and subsequent activation of GPR113.
Other activators work by modulating the G protein signaling pathway, which is essential for GPR113 activity. GTPγS, a non-hydrolyzable analog of GTP, binds to G proteins and maintains them in an active state, which can enhance GPR113 signaling. Sodium Fluoride and Cholera Toxin both act to increase the levels of active G proteins; Sodium Fluoride by inhibiting GTPase and Cholera Toxin by ADP-ribosylation of the Gs alpha subunit, which leads to a continuous increase in cAMP. Pertussis Toxin, on the other hand, inhibits the Gi alpha subunits, which typically serve to decrease cAMP levels, thereby indirectly promoting an increase in cAMP that activates PKA and acts on GPR113. BAY 60-6583 acts through adenosine A2B receptors to raise cAMP levels, which, like the other cAMP-elevating agents, leads to PKA activation and subsequent phosphorylation of GPR113. Lastly, calcium ionophores like ionomycin and A23187 increase intracellular calcium levels, leading to the activation of calcium-dependent kinases that can also target and phosphorylate GPR113.
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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 | |
Isoproterenol, a beta-adrenergic agonist, elevates intracellular cAMP levels through G protein-coupled receptor signaling, which could lead to the activation of PKA. PKA, in turn, can phosphorylate GPR113, leading to its functional activation. | ||||||
Guanosine 5′-O-(3-thiotriphosphate) tetralithium salt | 94825-44-2 | sc-202639 | 10 mg | $465.00 | ||
GTPγS is a non-hydrolyzable analog of GTP. It can bind to G proteins and stabilize their active form, potentially enhancing GPR113 signaling by facilitating its interaction with G proteins. | ||||||
Sodium Fluoride | 7681-49-4 | sc-24988A sc-24988 sc-24988B | 5 g 100 g 500 g | $40.00 $46.00 $100.00 | 26 | |
Sodium Fluoride is an activator of G proteins through inhibition of GTPase, which can potentiate the GPR113 signaling pathway by maintaining G proteins in their active state, facilitating the interaction with GPR113. | ||||||
Pertussis Toxin (islet-activating protein) | 70323-44-3 | sc-200837 | 50 µg | $451.00 | 3 | |
Pertussis Toxin can inhibit Gi alpha subunits, which normally act to decrease cAMP levels. Inhibition of Gi can thus lead to increased cAMP, activating PKA, and potentially leading to the phosphorylation and activation of GPR113. | ||||||
Ionomycin | 56092-82-1 | sc-3592 sc-3592A | 1 mg 5 mg | $78.00 $270.00 | 80 | |
Ionomycin is a calcium ionophore that increases intracellular Ca2+ concentration. Elevated Ca2+ can activate calmodulin-dependent kinase, which may phosphorylate GPR113, leading to its activation. | ||||||
A23187 | 52665-69-7 | sc-3591 sc-3591B sc-3591A sc-3591C | 1 mg 5 mg 10 mg 25 mg | $55.00 $131.00 $203.00 $317.00 | 23 | |
A23187, like ionomycin, is a calcium ionophore. It raises intracellular calcium levels, potentially leading to the activation of calcium-dependent kinases that can phosphorylate and activate GPR113. | ||||||
IBMX | 28822-58-4 | sc-201188 sc-201188B sc-201188A | 200 mg 500 mg 1 g | $260.00 $350.00 $500.00 | 34 | |
3-Isobutyl-1-methylxanthine (IBMX) is a non-specific inhibitor of phosphodiesterases, which increases cAMP levels by preventing its degradation. The resultant elevated cAMP can lead to activation of PKA, which may then activate GPR113. | ||||||
PMA | 16561-29-8 | sc-3576 sc-3576A sc-3576B sc-3576C sc-3576D | 1 mg 5 mg 10 mg 25 mg 100 mg | $41.00 $132.00 $214.00 $500.00 $948.00 | 119 | |
PMA activates protein kinase C (PKC), which can phosphorylate target proteins. PKC-mediated phosphorylation can activate GPR113 by modifying its conformation or affecting its interaction with other cellular components. | ||||||
BAY 60-6583 | 910487-58-0 | sc-503262 | 10 mg | $210.00 | ||
BAY 60-6583 selectively activates adenosine A2B receptors, which are G protein-coupled receptors that can increase intracellular cAMP levels, potentially leading to PKA activation and subsequent phosphorylation and activation of GPR113. | ||||||