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Description: Potent and selective BCRP inhibitor
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
Purity: ≥99% (HPLC)
Biological Activity for Ko 143
Ko 143 is a 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.
Compound Libraries for Ko 143
Ko 143 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Ko 143
| M. Wt | 469.57 |
| Formula | C26H35N3O5 |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 461054-93-3 |
| PubChem ID | 10322450 |
| InChI Key | NXNRAECHCJZNRF-JBACZVJFSA-N |
| Smiles | O=C(N[C@H]4CCC(OC(C)(C)C)=O)[C@]3([H])CC1=C([C@H](CC(C)C)N3C4=O)NC2=C1C=CC(OC)=C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Ko 143
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 23.48 | 50 | |
| ethanol | 46.96 | 100 |
Preparing Stock Solutions for Ko 143
The following data is based on the product molecular weight 469.57. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.13 mL | 10.65 mL | 21.3 mL |
| 5 mM | 0.43 mL | 2.13 mL | 4.26 mL |
| 10 mM | 0.21 mL | 1.06 mL | 2.13 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
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Product Datasheets for Ko 143
References for Ko 143
References are publications that support the biological activity of the product.
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
Allen et al (2003) Mouse breast cancer resistance protein (Bcrp1/Abcg2) mediates etop. resistance and transport, but etop. oral availability is limited primarily by P-glycoprotein. Cancer Res. 63 1339 PMID: 12649196
Loevezijn et al (2001) Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines. Bioorg.Med.Chem.Letts. 11 29 PMID: 11140726
Weidner et al (2015) The inhibitor Ko143 is not specific for ABCG2. J.Pharmacol.Exp.Ther. 354 384 PMID: 26148857
If you know of a relevant reference for Ko 143, please let us know.
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Keywords: Ko 143, Ko 143 supplier, Potent, selective, BCRP, inhibitors, inhibits, MDR, Breast, Cancer, Resistance, Protein, Multidrug, Transporters, Ko143, ATP-binding, cassette, 3241, Tocris Bioscience
13 Citations for Ko 143
Citations are publications that use Tocris products. Selected citations for Ko 143 include:
Kumar et al (2016) Bioluminescent imaging of ABCG2 efflux activity at the blood-placenta barrier. Sci Rep 6 20418 PMID: 26853103
Ding et al (2016) A role for ABCG2 beyond drug transport: Regulation of autophagy. Autophagy 12 737 PMID: 26983466
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
Coz et al (2016) IGF-1 contributes to the expansion of melanoma-initiating cells through an epithelial-mesenchymal transition process. Oncotarget 7 82511 PMID: 27764776
Westover et al (2015) FL118, a novel camptothecin derivative, is insensitive to ABCG2 expression and shows improved efficacy in comparison with irino. in colon and lung cancer models with ABCG2-induced resistance. Brain Res 14 92 PMID: 25928015
Hoque et al (2015) Raltegravir permeability across blood-tissue barriers and the potential role of drug efflux transporters. Biochem Pharmacol 59 2572 PMID: 25691630
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
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
Morfouace et al (2015) ABCG2 Transporter Expression Impacts Group 3 Medulloblastoma Response to Chemotherapy. Cancer Res 75 3879 PMID: 26199091
Moreno-Sanz et al (2013) Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors. J Med Chem 56 5917 PMID: 23822179
Zander et al (2012) EZN-2208 (PEG-SN38) overcomes ABCG2-mediated topo. resistance in BRCA1-deficient mouse mammary tumors. PLoS One 7 e45248 PMID: 23028879
Lainey et al (2012) Erlotinib antagonizes ABC transporters in acute myeloid leukemia. Cell Cycle 11 4079 PMID: 23095522
Do you know of a great paper that uses Ko 143 from Tocris? Please let us know.
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