Ko 143

Cat. No. 3241

Ko 143 C26H35N3O5 [461054-93-3]

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Chemical Name: (3S,6S,12aS)-1,2,3,4,6,7,12,12a-Octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxopyrazino[1',2':1,6]pyrido[3,4-b]indole-3-propanoic acid 1,1-dimethylethyl ester

Biological Activity

Potent and selective breast cancer resistance protein multidrug transporter (BCRP) inhibitor (EC90 = 26 nM). Displays > 200-fold selectivity over P-gp and MRP-1 transporters. Increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance. Inhibits ABCB1 and ABCC1 at higher concentrations. Rapidly metabolized in rat plasma.

Technical Data

Soluble to 50 mM in DMSO and to 100 mM in ethanol
>99 %
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Weidner et al (2015) The inhibitor Ko143 is not specific for ABCG2. J.Pharmacol.Exp.Ther. 354 384. PMID: 26148857.

Allen et al (2003) Mouse breast cancer resistance protein (Bcrp1/Abcg2) mediates etoposide resistance and transport, but etoposide oral availability is limited primarily by P-glycoprotein. Cancer Res. 63 1339. PMID: 12649196.

Allen et al (2002) Potent and specific inhibition of breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C. Mol.Cancer Ther. 1 417. PMID: 12477054.

Loevezijn et al (2001) Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines. Bioorg.Med.Chem.Letts. 11 29.

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Citations are publications that use Tocris products. Selected citations for Ko 143 include:

Hoque et al (2015) Raltegravir permeability across blood-tissue barriers and the potential role of drug efflux transporters. Biochem Pharmacol 59 2572. PMID: 25691630.

Westover et al (2015) FL118, a novel camptothecin derivative, is insensitive to ABCG2 expression and shows improved efficacy in comparison with irinotecan in colon and lung cancer models with ABCG2-induced resistance. Brain Res 14 92. PMID: 25928015.

Moreno-Sanz et al (2014) Structural determinants of peripheral O-arylcarbamate FAAH inhibitors render them dual substrates for Abcb1 and Abcg2 and restrict their access to the brain. Pharmacol Res 87 87. PMID: 24993496.

Hill et al (2013) Characterisation of the roles of ABCB1, ABCC1, ABCC2 and ABCG2 in the transport and pharmacokinetics of actinomycin D in vitro and in vivo. J Biol Chem 85 29. PMID: 23063411.

Lainey et al (2012) Erlotinib antagonizes ABC transporters in acute myeloid leukemia. Cell Cycle 11 4079. PMID: 23095522.

Watson et al (2012) The transport of nifurtimox, an anti-trypanosomal drug, in an in vitro model of the human blood-brain barrier: evidence for involvement of breast cancer resistance protein. Antimicrob Agents Chemother 1436 111. PMID: 22200378.

Zander et al (2012) EZN-2208 (PEG-SN38) overcomes ABCG2-mediated topotecan resistance in BRCA1-deficient mouse mammary tumors. PLoS One 7 e45248. PMID: 23028879.

Moreno-Sanz et al (2011) The ABC membrane transporter ABCG2 prevents access of FAAH inhibitor URB937 to the central nervous system. Pharmacol Res 64 359. PMID: 21767647.

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Keywords: Ko 143, supplier, Potent, selective, BCRP, inhibitors, inhibits, MDR, Breast, Cancer, Resistance, Protein, Multidrug, Transporters, Ko143, ATP-binding, cassette, Tocris Bioscience, Multidrug Transporter Inhibitor products

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