For research use only. Not for therapeutic Use.
Ko 143(CAT: I003608) is a potent and selective breast cancer resistance protein multidrug transporter (BCRP) inhibitor (EC90 = 26 nM), Ko 143 displays > 200-fold selectivity over P-gp and MRP-1 transporters. Ko143 appears to be the most potent BCRP inhibitor known thus far. In contrast, the compounds have only low activity against P-glycoprotein, the multidrug resistance-associated protein (MRP1), or other known drug transporters.
| Catalog Number | I003608 |
| CAS Number | 461054-93-3 |
| Synonyms | tert-butyl 3-((3R,6S,12aR)-6-isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydropyrazino[1/’,2/’:1,6]pyrido[3,4-b]indol-3-yl)propanoate |
| Molecular Formula | C26H35N3O5 |
| Purity | ≥95% |
| Target | BCRP |
| Solubility | Soluble to 50 mM in DMSO and to 100 mM in ethanol |
| Storage | Store at -20°C |
| IC50 | 26 nM (EC90) |
| InChIKey | NXNRAECHCJZNRF-JBACZVJFSA-N |
| SMILES | COC(C=C1)=CC2=C1C3=C(N2)[C@H](CC(C)C)N([C@@]4([H])C3)C([C@H](CCC(OC(C)(C)C)=O)NC4=O)=O |
| Reference | 1: Abdel Gaber SA, Müller P, Zimmermann W, Hüttenberger D, Wittig R, Abdel Kader <br> 3: Weidner LD, Zoghbi SS, Lu S, Shukla S, Ambudkar SV, Pike VW, Mulder J, <br> |
