DMU2139 |
| カタログ番号GC19416 |
DMU2139 は強力で特異的な CYP1B1 阻害剤で、CYP1B1 と CYP1A1 の IC50 はそれぞれ 9 nM と 795 nM です。
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Cas No.: 1821143-80-9
Sample solution is provided at 25 µL, 10mM.
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DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
DMU2139 (6j) shows 88 and 133-fold selectivity for CYP1B1 over CYP1A1 and CYP1A2. In the presence of DMU2139, the EC50 is reversed back to 8.3 μM from 61 μM (seen in CYP1B1-expressing cells without any inhibitor). The EC50 value, in the presence of DMU2139, resembles the EC50 of cisplatin, 8.7μM, in cells transfected with the empty plasmid which has no CYP1B1 gene and therefore cannot express CYP1B1 protein[1].
[1]. Horley NJ, et al. Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines. Eur J Med Chem. 2017 Mar 31;129:159-174.
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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