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KS 176
- Soluble in DMSO
- MF: C22H19N3O5
- MW: 405.4
Description
KS 176 is an inhibitor of the ABC transporter BCRP/ABCG2. It blocks BCRP-mediated efflux and can increase intracellular accumulation of transporter substrates. KS 176 is ca 50-fold more potent than Novobiocin (IC50 value 65 µM), and nearly equipotent compared to KO 143 (Axon 1409), and does not show inhibition of P-gp and MRP1.
BCRP/ABCG2 contributes to multidrug resistance, xenobiotic efflux, tissue-barrier transport and pharmacokinetic disposition. KS 176 is useful for studying transporter-mediated drug resistance and ABCG2 substrate handling.
Key Features
- BCRP/ABCG2 transporter inhibitor
- Reported IC50: 1.39 µM
- More potent than novobiocin in reported comparative assays
- Blocks breast cancer resistance protein-mediated efflux
Applications
- ABC transporter pharmacology
- Multidrug resistance research
- Drug efflux and accumulation assays
- Pharmacokinetic transporter interaction studies
More Information
| Parent CAS No. | 1253452-78-6 |
|---|---|
| Chemical Name | N-[4-(2-hydroxyethyl)phenyl]-2-[(4-nitrobenzoyl)amino]benzamide |
| SMILES | C1(C(=O)NC2C=CC(CCO)=CC=2)C=CC=CC=1NC(C1C=CC([N+]([O-])=O)=CC=1)=O |
| MFCD | MFCD22666402 |
| InChi | InChI=1S/C22H19N3O5/c26-14-13-15-5-9-17(10-6-15)23-22(28)19-3-1-2-4-20(19)24-21(27)16-7-11-18(12-8-16)25(29)30/h1-12,26H,13-14H2,(H,23,28)(H,24,27) |
| InChiKey | LTWQQWSXYYXVGA-UHFFFAOYSA-N |
| CID | 49779726 |
| Short Description | BCRP inhibitor |
References
- F. Marighetti et al. Synthesis and quantitative structure-activity relationships of selective BCRP inhibitors. ChemMedChem. 2013 Jan;8(1):125-35.
- A. Pick et al. Specific inhibitors of the breast cancer resistance protein (BCRP). ChemMedChem. 2010 Sep 3;5(9):1498-505.
- K. Steggemann. Design und Synthese neuartiger Inhibitoren für den ABC-Transporter Breast Cancer Resistance Protein. Thesis, RFWU Bonn, 2011.
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