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KO 143
- Soluble in DMSO and EtOH
- MF: C26H35N3O5
- MW: 469.57
Description
KO 143 is a potent and selective ABCG2/breast cancer resistance protein inhibitor that blocks transporter-mediated drug efflux.
ABCG2 limits intracellular exposure to many xenobiotics and anticancer agents and contributes to multidrug resistance, intestinal absorption and blood–tissue barriers. KO 143 is a standard inhibitor for transporter function and substrate-identification studies.
Key Features
- Potent and selective ABCG2/BCRP inhibitor
- Blocks ATP-dependent xenobiotic efflux
- Reverses BCRP-mediated multidrug resistance in model systems
- Reference compound for transporter-selectivity studies
Applications
- ABCG2 transport and ATPase assays
- Drug-efflux and multidrug-resistance research
- Intestinal and blood–brain barrier studies
- Transporter substrate and drug–drug interaction profiling
More Information
| Parent CAS No. | 461054-93-3 |
|---|---|
| Chemical Name | 3-((3S,6S,12aS)-6-Isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydro-pyrazino[1',2':1,6]pyrido[3,4-b]indol-3-yl)-propionic acid tert-butylester |
| MFCD | MFCD11042273 |
| Short Description | BCRP inhibitor |
References
- JD Allen et al. 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. Mol Cancer Ther. 2002 Apr;1(6):417-25.
- A van Loevezijn et al. Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines. Bioorg Med Chem Lett. 2001 Jan 8;11(1):29-32.
- List of publications using KO143 (Axon 1409) purchased from Axon Medchem
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