RGS18 Activators
RGS18 Activators are a collection of chemical compounds that indirectly yet significantly enhance the functional activity of RGS18 by targeting various signaling pathways and cellular processes. Forskolin, by increasing intracellular cAMP levels, indirectly promotes RGS18's GTPase-accelerating function on GPCRs, which is crucial for modulating downstream signals, typically through PKA-mediated phosphorylation. Similarly, PMA activates PKC, which then phosphorylates a myriad of proteins, potentially including RGS18, and this modification can change RGS18's interaction with GPCR-Gα subunits, enhancing the quick termination of GPCR signaling. IBMX and Sildenafil both act to elevate levels of cyclic nucleotides, leading to the enhanced activity of PKA and PKG, respectively. This consequential phosphorylation elevates the functionality of RGS18 in its role as a GAP for Gα subunits, thus fine-tuning GPCR-mediated responses. Zaprinast follows a similar route as Sildenafil, raising cGMP levels and activating PKG, which may further RGS18's interaction with Gα subunits, amplifying its GAP activity.
Y-27632, by hampering ROCK activity, potentially decreases the inhibitory phosphorylation on RGS18, maintaining its active state and facilitating the attenuation of GPCR signaling. Conversely, L-NAME acts to diminish the regulatory effects of NO on guanylyl cyclase, which could indirectly maintain or increase RGS18 activity by reducing cGMP-dependent signaling. Rolipram and Milrinone, by selectively inhibiting PDE4 and PDE3 respectively, raise cAMP levels and activate PKA, which is likely to phosphorylate and thus enhance RGS18's regulatory actions in GPCR signaling. LY294002's inhibition of PI3K may prevent the phosphorylation of targets that indirectly influence RGS18, potentially bolstering its GAP activity. Vinpocetine, a PDE1 inhibitor, increases cAMP and cGMP in neuronal cells, and through PKA and PKG activation, it could augment RGS18 activity in modulating neurotransmitter GPCR signaling. Lastly, A23187 increases intracellular calcium levels, potentially activating CaMK, which may phosphorylate RGS18, enhancing its role in GPCR signaling pathways, making it a crucial regulator of GPCR-mediated cellular responses.
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| 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 is known to activate adenylyl cyclase, which increases intracellular cAMP levels. Elevated cAMP activates PKA, which can phosphorylate RGS18, enhancing its GTPase-accelerating function on G-protein coupled receptors (GPCRs), thereby modulating downstream signaling events. | ||||||
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 is a PKC activator that phosphorylates a wide range of cellular proteins. PKC-mediated phosphorylation of proteins can alter the binding affinity of RGS18 to GPCR-Gα subunits, thereby enhancing its regulatory function and accelerating the termination of GPCR signaling. | ||||||
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 non-selective inhibitor of phosphodiesterases, which prevents the breakdown of cAMP and cGMP, leading to their accumulation. Elevated levels of these cyclic nucleotides enhance PKA and PKG activity, respectively, which can phosphorylate RGS18, thereby increasing its activity in terminating GPCR signaling. | ||||||
Zaprinast (M&B 22948) | 37762-06-4 | sc-201206 sc-201206A | 25 mg 100 mg | $105.00 $250.00 | 8 | |
Zaprinast is another PDE5 inhibitor, similarly to Sildenafil, which increases cGMP levels within the cell. The increased cGMP activates PKG which could enhance RGS18 activity by promoting its interaction with Gα subunits, thus increasing its GAP activity and modulating GPCR signaling. | ||||||
Y-27632, free base | 146986-50-7 | sc-3536 sc-3536A | 5 mg 50 mg | $186.00 $707.00 | 88 | |
Y-27632 is an inhibitor of ROCK (Rho-associated protein kinase), which through its action can lead to a reduction in the inhibitory phosphorylation of RGS18. This allows RGS18 to maintain its active state, more effectively accelerating GTP hydrolysis on Gα subunits and attenuating GPCR-mediated signaling. | ||||||
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 inhibits nitric oxide synthase, reducing NO levels, which might otherwise lead to the activation of guanylyl cyclase and increased levels of cGMP, which activates PKG. Inhibiting this pathway with L-NAME could potentially enhance the activity of RGS18 by removing competing cGMP-dependent regulatory effects on GPCR signaling. | ||||||
Rolipram | 61413-54-5 | sc-3563 sc-3563A | 5 mg 50 mg | $77.00 $216.00 | 18 | |
Rolipram is a selective inhibitor of PDE4, leading to an increase in intracellular cAMP levels. This elevation in cAMP activates PKA, which could phosphorylate RGS18, thereby increasing its regulatory function on GPCR signaling. | ||||||
Milrinone | 78415-72-2 | sc-201193 sc-201193A | 10 mg 50 mg | $165.00 $697.00 | 7 | |
Milrinone is a selective PDE3 inhibitor, which increases intracellular cAMP levels in cardiac tissue. Through the activation of PKA, it could potentially enhance the activity of RGS18 in cardiac myocytes, thereby modulating the GPCR signaling involved in cardiac function. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $123.00 $400.00 | 148 | |
LY294002 is a PI3K inhibitor. By inhibiting PI3K, it may prevent the phosphorylation of downstream targets that can indirectly affect the function of RGS18, potentially enhancing its GTPase-accelerating activity in GPCR signaling pathways. | ||||||
Vinpocetine | 42971-09-5 | sc-201204 sc-201204A sc-201204B | 20 mg 100 mg 15 g | $55.00 $214.00 $2400.00 | 4 | |
Vinpocetine is a PDE1 inhibitor, which increases cAMP and cGMP levels in the brain. Through the activation of PKA and PKG, it may enhance RGS18 activity in neuronal cells, potentially modulating neurotransmitter GPCR signaling. | ||||||