| Bioactivity | CPI1 is a potent and highly specific multidrug resistance protein 1 (MRP1) inhibitor. CPI1 inhibits MRP1 (Ki: 100 nM) with nanomolar potency but shows minimal inhibition of P-glycoprotein (Pgp). CPI1 and LTC4 compete to bind to the same site of MRP1, inhibiting ATP hydrolysis and substrate transport. CPI1 can be used to study drug delivery and chemotherapy resistance in cancer[1]. |
| Target | Ki: 100 nM (MRP1) |
| Sequence | Cyclo(Ac-{d-Tyr}-Phe-Trp-Gly-Asn-Leu-His-Trp-Tyr-Tyr-Glu-Gln-Phe-Asp-Ser-Thr-Cys) |
| Shortening | Cyclo(Ac-{d-Tyr}-FWGNLHWYYEQFDSTC) |
| Formula | C111H131N23O30S |
| Molar Mass | 2299.43 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Pietz HL, et al. A macrocyclic peptide inhibitor traps MRP1 in a catalytically incompetent conformation. Proc Natl Acad Sci U S A. 2023 Mar 14;120(11):e2220012120. |