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DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.

DMU2105 (Compound 7k) shows 74 and 120-fold selectivity for CYP1B1 over CYP1A1 and CYP1A2. In the presence of DMU2105 however, the EC50 goes down to 1 μM indicating that the cells have suffered from toxicity which may have been mediated by CYP1B1 inhibition. Un-transfected cells (HEK293: pcDNA3.1), when treated with cisplatin and DMU2105 (10×IC50) do not show any perceptible decrease of cisplatin EC50 (8.5 μM ± 0.9)[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

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