compound introduction
DMU2105 is a potent and specific CYP1B1 inhibitor, with IC 50 s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively. In Vitro DMU2105 (Compound 7k) shows 74 and 120-fold selectivity for CYP1B1 over CYP1A1 and CYP1A2. In the presence of DMU2105 however, the EC 50 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×IC 50 ) do not show any perceptible decrease of cisplatin EC 50 (8.5 μM ± 0.9). MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:CYP1B1 10 nM (IC 50 ) CYP1A1 742 nM (IC 50 )
