ATPase ABC efflux transporter assays
ATPase assay an is ideal, cost effective first assay to identify interaction between test compounds and ABC transporters. Activation and inhibition modes in combination give the best safety to detect any interaction, and may identify substrate nature of the test compound.
For more details on the scientific background of ATPase assays please click here.
List of transporters for ATPase assay screens:| Transporter | Membrane used | Probe (reference substrate) |
Positive
control activation / inhibition |
| MDR1/P-gp (ABCB1) | SB-MDR1-Sf9-ATPase | Verapamil | Digoxin / Cyclosporine A |
| ratMdr1b | SB-ratMdr1b-Sf9-ATPase | Verapamil | Quinidine / Cyclosporine A |
| MRP1 (ABCC1) | SB-MRP1-Sf9-ATPase | NEM-GS | Indomethacin / Benzbromarone |
| MRP2 (ABCC2) | SB-MRP2-Sf9-ATPase | Probenecid | Sulfasalazine / Benzbromarone |
| MRP3 (ABCC3) | SB-MRP3-Sf9-ATPase | Benzbromarone | E217βG / Cyclosporine A |
| BCRP (ABCG2) |
SB-BRCP-M-ATPase or SB-BCRP-HAM-Sf9-ATPase |
Sulfasalazine, Hoechst 33342, KO134 | Topotecan / KO134 |
| BCRP-R482G (ABCG2-R482G) | SB-BCRP-R482G-Sf9-ATPase | Prazosin, Hoechst 33342, KO134 | Mitoxantrone / KO134 |
| Mouse Bsep | SB-mouseBsep-HAM-Sf9-ATPase | Taurochenodeoxycholate |