RGS Protein GAP Assays
- Universal RGS Protein Detection: The only HTS-ready assay method for RGS GAP activity
- A Complete Screening and Profiling Solution: Recombinant Proteins RGS proteins, kinetically enhanced Gα proteins, and Transcreener GDP Assay detection reagents.
Members of the "regulator of G-protein signaling" (RGS)-protein superfumily act as "GTPase-accelerating proteins" (GAP) for heterotrimeric G-protein alpha subunits, thereby attenuating GPCR signaling. Their selectivity for specific GPCRs and downstream signaling components and their tissue- specific expression makes them attractive as potential therapeutic targets, with the potential for modulating the effects of existing GPCR agonists.
RGScreen: The only HTS assay for RGS Protein GAP Activity
The most direct way to detect RGS function is by measuring the increased GTPase activity of the associated Gα protein. However, the GTPase activity of isolated Gα proteins is limited by GDP dissociation, so RGS GAP activity cannot be measured using simple biochemical assays. The RGScreen platform overcomes this kinetic constraint by using proprietary Gα protein variants with altered GTP hydrolysis and GDP dissociation rates that enable detection of RGS GAP activity using the Transcreener® GDP Assay.
In the RGScreen assay, RGS proteins stimulate the GTPase activity of kinetically enhanced Gα proteins, which is detected as an increase in GDP formation using the Transcreener GDP Assay. All of the required protein and detection reagents are available from BellBrook.
Recombinant RGS Proteins and Kinetically Enhanced Gα Proteins
(Quantities of each protein vary; sufficient protein for 1,000 assays in 384-well format.)
|Cat #||Product PDFs||Price|
|8010||RGS2 (71-209)||$250||Buy Now|
|8005||RGS4 (29-198)||$250||Buy Now|
|8006||RGS10 (16-151)||$250||Buy Now|
|8011||RGS12 (101-261)||$250||Buy Now|
|8007||RGS14 (56-207)||$250||Buy Now|
|8012||RGS16 (53-190)||$250||Buy Now|
|8008||RGS17 (72-206)||$250||Buy Now|
|8009||RGS18 (75-223)||$250||Buy Now|
|8013||RGS19 (79-205)||$250||Buy Now|
|Kinetically Enhanced Gα Proteins|
|9033||Gα0 (R179M,A327S)||$250||Buy Now|
|9034||Gαi1 (R178M,A326S)||$250||Buy Now|
|9035||Gαi2 (R179M,A327S)||$250||Buy Now|
|9036||Gαi3 (R178M,A326S)||$250||Buy Now|
|3009-1K||Transcreener GDP FP Assay||1,000 assays (384-well format)||$614.00||Buy Now|
|30014-1K||Transcreener GDP FI Assay||1,000 assays (384-well format)||$614.00||Buy Now|