Pyrimidinone 8 is a reversible linear non-competitive inhibitor of divalent metal transporter 1 ( DMT1 ), with a K i of 20 μM ( hDMT1 ). Pyrimidinone 8 does not affect hDMT1 cell surface expression and shows no dependence with the extracellular pH. Pyrimidinone 8 can inhibit hDMT1 -mediated iron uptake, with an IC50 of 13.8 μM [1].
References:
[1]. Montalbetti N, et al. Discovery and characterization of a novel non-competitive inhibitor of the divalent metal transporter DMT1/SLC11A2. Biochem Pharmacol. 2015 Aug 1;96(3):216-24.
References:
[1]. Montalbetti N, et al. Discovery and characterization of a novel non-competitive inhibitor of the divalent metal transporter DMT1/SLC11A2. Biochem Pharmacol. 2015 Aug 1;96(3):216-24.