Catalog Number: 3241
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
  • M.Wt:
    469.57
  • Formula:
    C26H35N3O5
  • Solubility:
    Soluble to 50 mM in DMSO and to 100 mM in ethanol
  • Purity:
    >99%
  • Storage:
    Store at -20°C
  • CAS No:
    461054-93-3
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.
Background References
  1. Potent and specific inhibition of breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C.
    Allen et al.
    Mol.Cancer Ther., 2002;1:417
  2. Mouse breast cancer resistance protein (Bcrp1/Abcg2) mediates etoposide resistance and transport, but etoposide oral availability is limited primarily by P-glycoprotein.
    Allen et al.
    Cancer Res., 2003;63:1339
  3. Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines.
    Loevezijn et al.
    Bioorg.Med.Chem.Letts., 2001;11:29
  4. The inhibitor Ko143 is not specific for ABCG2.
    Weidner et al.
    J.Pharmacol.Exp.Ther., 2015;354:384
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Ko 143 include:

8 Citations: Showing 1 - 8
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  1. Raltegravir permeability across blood-tissue barriers and the potential role of drug efflux transporters.
    Authors: Hoque Et al.
    Biochem Pharmacol 2015;59:2572
  2. 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.
    Authors: Westover Et al.
    Brain Res 2015;14:92
  3. Structural determinants of peripheral O-arylcarbamate FAAH inhibitors render them dual substrates for Abcb1 and Abcg2 and restrict their access to the brain.
    Authors: Moreno-Sanz Et al.
    Pharmacol Res 2014;87:87
  4. Characterisation of the roles of ABCB1, ABCC1, ABCC2 and ABCG2 in the transport and pharmacokinetics of actinomycin D in vitro and in vivo.
    Authors: Hill Et al.
    J Biol Chem 2013;85:29
  5. EZN-2208 (PEG-SN38) overcomes ABCG2-mediated topotecan resistance in BRCA1-deficient mouse mammary tumors.
    Authors: Zander Et al.
    PLoS One 2012;7:e45248
  6. 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.
    Authors: Watson Et al.
    Antimicrob Agents Chemother 2012;1436:111
  7. Erlotinib antagonizes ABC transporters in acute myeloid leukemia.
    Authors: Lainey Et al.
    Cell Cycle 2012;11:4079
  8. The ABC membrane transporter ABCG2 prevents access of FAAH inhibitor URB937 to the central nervous system.
    Authors: Moreno-Sanz Et al.
    Pharmacol Res 2011;64:359

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