RGS (Regulators of G protein signaling) are protein structural domains that activate GTPases for heterotrimeric G-protein alpha-subunits.GTPase-accelerating RGS proteins have multiple functions, including promoting GTP hydrolysis by heterotrimeric G protein alpha subunits, which inactivates the G protein and quickly cuts off G protein-coupled receptor signaling pathways. Heterotrimeric G proteins exchange GDP for GTP when GPCRs activate them. They are then freed from the receptor and split into an active, free GTP-bound alpha subunit and a beta-gamma dimer, which both trigger downstream effectors.The alpha subunit's hydrolysis of GTP ends the response, allowing it to bind both the receptor and the beta-gamma dimer. RGS proteins stabilize the G protein transition state, thereby significantly reducing the lifetime of GTP-bound alpha subunits. A component of every RGS protein called the RGS-box, or RGS domain, is necessary for its function. RGS1 and RGS4, two tiny RGS proteins, are essentially just RGS domains, but others have extra domains that add extra functionality.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V2394 | CCG 50014 | 883050-24-6 | CCG 50014 is a novel, potent and selective inhibitor of RGS4 with IC50 of 30 nM. |
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V4959 | CCG-63802 | 620112-78-9 | CCG-63802 is a novel, selective and reversible inhibitor of RGS4 (regulator of G-protein signaling) with IC50 value of 1.9 μM. |
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V4958 | CCG-63808 | 620113-73-7 | CCG-63808 is a novel, potent and reversible inhibitor of regulator of G-protein signaling (RGS) proteins with IC50 value of 1.4 μM for RGS4. |
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