Ko 143

• CAT Number: I003608
• CAS Number: 461054-93-3
• Molecular Formula: C26H35N3O5
• Molecular Weight: 469.6
• 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

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.

Reference

1: Abdel Gaber SA, Müller P, Zimmermann W, Hüttenberger D, Wittig R, Abdel Kader
MH, Stepp H. ABCG2-mediated suppression of chlorin e6 accumulation and
photodynamic therapy efficiency in glioblastoma cell lines can be reversed by
KO143. J Photochem Photobiol B. 2017 Oct 28;178:182-191. doi:
10.1016/j.jphotobiol.2017.10.035. [Epub ahead of print] PubMed PMID: 29156346.

2: Liu K, Zhu J, Huang Y, Li C, Lu J, Sachar M, Li S, Ma X. Metabolism of KO143,
an ABCG2 inhibitor. Drug Metab Pharmacokinet. 2017 Aug;32(4):193-200. doi:
10.1016/j.dmpk.2017.02.003. Epub 2017 Mar 6. PubMed PMID: 28619281.

3: Weidner LD, Zoghbi SS, Lu S, Shukla S, Ambudkar SV, Pike VW, Mulder J,
Gottesman MM, Innis RB, Hall MD. The Inhibitor Ko143 Is Not Specific for ABCG2. J
Pharmacol Exp Ther. 2015 Sep;354(3):384-93. doi: 10.1124/jpet.115.225482. Epub
2015 Jul 6. PubMed PMID: 26148857; PubMed Central PMCID: PMC4538874.

4: Zander SA, Beijnen JH, van Tellingen O. Sensitive method for plasma and tumor
Ko143 quantification using reversed-phase high-performance liquid chromatography
and fluorescence detection. J Chromatogr B Analyt Technol Biomed Life Sci. 2013
Jan 15;913-914:129-36. doi: 10.1016/j.jchromb.2012.11.003. Epub 2012 Dec 6.
PubMed PMID: 23291288.