Molecular structure of Ko 143, CAS Number: 461054-93-3
Ko 143 (CAS 461054-93-3)
See product citations (21)
Alternate Names:
(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
Application:
Ko 143 is a selective BCRP multidrug transporter inhibitor
CAS Number:
461054-93-3
Purity:
≥99%
Molecular Weight:
469.57
Molecular Formula:
C26H35N3O5
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Ko 143 is a potent and selective ABCG2 (breast cancer resistance protein multidrug transporter, BCRP) inhibitor (EC90 = 26 nM). It displays > 200-fold selectivity over P-gp and MRP-1 transporters. Ko 143 also increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance.
Ko 143 (CAS 461054-93-3) References
- Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines. | van Loevezijn, A., et al. 2001. Bioorg Med Chem Lett. 11: 29-32. PMID: 11140726
- Potent and specific inhibition of the breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C. | Allen, JD., et al. 2002. Mol Cancer Ther. 1: 417-25. PMID: 12477054
- Mouse breast cancer resistance protein (Bcrp1/Abcg2) mediates etoposide resistance and transport, but etoposide oral availability is limited primarily by P-glycoprotein. | Allen, JD., et al. 2003. Cancer Res. 63: 1339-44. PMID: 12649196
- Breast cancer resistance protein-mediated efflux of luteolin glucuronides in HeLa cells overexpressing UDP-glucuronosyltransferase 1A9. | Tang, L., et al. 2014. Pharm Res. 31: 847-60. PMID: 24092055
- Jadomycins are cytotoxic to ABCB1-, ABCC1-, and ABCG2-overexpressing MCF7 breast cancer cells. | Issa, ME., et al. 2014. Anticancer Drugs. 25: 255-69. PMID: 24231527
- Bioluminescent imaging of drug efflux at the blood-brain barrier mediated by the transporter ABCG2. | Bakhsheshian, J., et al. 2013. Proc Natl Acad Sci U S A. 110: 20801-6. PMID: 24297888
- Role of ABCG2 in transport of the mammalian lignan enterolactone and its secretion into milk in Abcg2 knockout mice. | Miguel, V., et al. 2014. Drug Metab Dispos. 42: 943-6. PMID: 24568887
- Inhibition of breast cancer resistance protein (ABCG2) in human myeloid dendritic cells induces potent tolerogenic functions during LPS stimulation. | Jin, JO., et al. 2014. PLoS One. 9: e104753. PMID: 25111504
- The EGFR pathway regulates BCRP expression in NSCLC cells: role of erlotinib. | Porcelli, L., et al. 2014. Curr Drug Targets. 15: 1322-30. PMID: 25479544
- The antiepileptic drug lamotrigine is a substrate of mouse and human breast cancer resistance protein (ABCG2). | Römermann, K., et al. 2015. Neuropharmacology. 93: 7-14. PMID: 25645391
- Characterization of multidrug transporter-mediated efflux of avermectins in human and mouse neuroblastoma cell lines. | Dalzell, AM., et al. 2015. Toxicol Lett. 235: 189-98. PMID: 25865432
- The Inhibitor Ko143 Is Not Specific for ABCG2. | Weidner, LD., et al. 2015. J Pharmacol Exp Ther. 354: 384-93. PMID: 26148857
- Enhanced efficacy of photodynamic therapy by inhibiting ABCG2 in colon cancers. | Kim, JH., et al. 2015. BMC Cancer. 15: 504. PMID: 26149077
- Interplay of metabolizing enzymes and transporter of xenobiotics. | Lim, HY., et al. 2016. Xenobiotica. 46: 25-33. PMID: 26226519
- Efflux transport of chrysin and apigenin sulfates in HEK293 cells overexpressing SULT1A3: The role of multidrug resistance-associated protein 4 (MRP4/ABCC4). | Li, W., et al. 2015. Biochem Pharmacol. 98: 203-14. PMID: 26291395
Inhibitor of:
ABC-me, ABCC11, ABCD2, ABCF3, ABCG2, Amino acid-binding ABC transporter, GlnP, and MRP1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Ko 143, 1 mg | sc-204030 | 1 mg | $109.00 | |||
Ko 143, 10 mg | sc-204030A | 10 mg | $261.00 |