RGS11 Activators
RGS11 activators encompass a range of chemical compounds that indirectly amplify the functional activity of RGS11 via distinct signaling cascades. Forskolin, through its elevation of intracellular cAMP levels, indirectly augments the functional role of RGS11 by activating protein kinase A (PKA), which can phosphorylate and enhance the GTPase-activating protein (GAP) function of RGS11, allowing more efficient termination of GPCR signaling. Similarly, the nonspecific phosphodiesterase inhibitor IBMX, and the selective inhibitor Rolipram, elevate cAMP, indirectly promoting RGS11's ability to deactivate G proteins, thereby quickening the resolution of GPCR signaling. Other phosphodiesterase inhibitors like Zaprinast, Sildenafil, Vardenafil, and Tadalafil, while primarily increasing cGMP levels, may indirectly bolster RGS11's activity through cGMP-cAMP signalingcrosstalk. Y-27632, a ROCK inhibitor, and L-NAME, a nitric oxide synthase inhibitor, modify cytoskeletal dynamics and the cGMP-cAMP balance, respectively, which could potentially stabilize the cellular environment or enhance the cAMP signal to indirectly promote RGS11's GAP activity.
The activity of RGS11 is further influenced by compounds that modulate G protein signaling in more targeted ways. Gallein, an inhibitor of Gβγ signaling, can potentiate the GAP activity of RGS11 by reducing Gβγ-mediated signaling, allowing RGS11 to exert greater control over G protein deactivation. Cholera toxin and Pertussis toxin, by permanently modifying Gs and Gi protein functions, respectively, create an environment that may indirectly heighten the activity of RGS11 by shifting the balance towards Gs-coupled GPCR pathways where RGS11 is naturally more active. Collectively, these RGS11 activators, through their targeted effects on cellular signaling pathways and the cAMP-cGMP balance, collectively facilitate the enhanced function of RGS11 in the termination of GPCR signaling without the need for upregulating its expression or direct activation of the protein itself.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
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 | |
Forskolin raises intracellular cAMP levels, leading to the activation of PKA. PKA phosphorylation can enhance the GTPase-activating protein (GAP) activity of RGS11, thus increasing its ability to terminate G protein-coupled receptor (GPCR) signaling more efficiently. | ||||||
IBMX | 28822-58-4 | sc-201188 sc-201188B sc-201188A | 200 mg 500 mg 1 g | $260.00 $350.00 $500.00 | 34 | |
IBMX is a nonspecific inhibitor of phosphodiesterases, which increases intracellular cAMP by preventing its breakdown. Elevated cAMP levels can enhance RGS11 activity via the same mechanism as Forskolin, indirectly leading to more rapid deactivation of G proteins. | ||||||
Rolipram | 61413-54-5 | sc-3563 sc-3563A | 5 mg 50 mg | $77.00 $216.00 | 18 | |
Rolipram is a selective phosphodiesterase-4 inhibitor, which increases cAMP in specific tissues. The rise in cAMP can activate PKA, which then can enhance the activity of RGS11 by increasing its GAP activity towards GPCRs. | ||||||
Zaprinast (M&B 22948) | 37762-06-4 | sc-201206 sc-201206A | 25 mg 100 mg | $105.00 $250.00 | 8 | |
Zaprinast is another phosphodiesterase inhibitor, with a particular affinity for PDE5, which leads to increased cGMP levels. While cGMP-specific effects are less direct, increased cGMP can have a crosstalk with cAMP pathways, potentially enhancing RGS11 activity. | ||||||
Y-27632, free base | 146986-50-7 | sc-3536 sc-3536A | 5 mg 50 mg | $186.00 $707.00 | 88 | |
Y-27632 is a ROCK inhibitor that can decrease the phosphorylation of myosin light chain (MLC), altering cytoskeletal dynamics. This might indirectly enhance RGS11 GAP activity by stabilizing the cellular context in which GPCRs and RGS11 operate. | ||||||
L-NG-Nitroarginine Methyl Ester (L-NAME) | 51298-62-5 | sc-200333 sc-200333A sc-200333B | 1 g 5 g 25 g | $48.00 $107.00 $328.00 | 45 | |
L-NAME is an inhibitor of nitric oxide synthase which can lead to reduced cGMP levels. This could indirectly increase cAMP by altering the balance between cGMP and cAMP, potentially enhancing RGS11 activity. | ||||||
Gallein | 2103-64-2 | sc-202631 | 50 mg | $85.00 | 20 | |
Gallein is an inhibitor of Gβγ signaling. By inhibiting Gβγ, Gallein may potentiate RGS11's GAP activity indirectly since RGS11 can also act to turn off Gβγ-mediated signaling pathways. | ||||||
Pertussis Toxin (islet-activating protein) | 70323-44-3 | sc-200837 | 50 µg | $451.00 | 3 | |
Pertussis toxin permanently inactivates Gi alpha subunits, which could potentially lead to a relative increase in Gs-mediated signaling. This may indirectly enhance RGS11 activity by shifting the balance towards Gs-coupled GPCR pathways where RGS11 is more active. | ||||||
Vardenafil | 224785-90-4 | sc-362054 sc-362054A sc-362054B | 100 mg 1 g 50 g | $526.00 $735.00 $16653.00 | 7 | |
Similar to Sildenafil, Vardenafil is also a PDE5 inhibitor. By increasing cGMP, it may influence cAMP pathways and indirectly enhance RGS11's GAP activity on GPCR signaling. | ||||||
Tadalafil | 171596-29-5 | sc-208412 | 50 mg | $180.00 | 13 | |
Tadalafil, another PDE5 inhibitor, increases cGMP levels. It may also engage in crosstalk with cAMP pathways, potentially enhancing the GAP activity of RGS11. | ||||||