SR 13800

MCT1-IN-2 is a potent monocarboxylate transporter 1 (MCT1) inhibitor. MCT1-IN-2 has anti-cancer activity[1][2].

Signaling Pathways >> Membrane Transporter/Ion Channel >> Monocarboxylate Transporter

Research Areas >> Cancer

MCT1-IN-2 (compound 3) has a pKi of 9.48 for Jurkat T-cells and inhibits human peripheral blood mononuclear cells (PBMC) proliferation (pIC50=8.61)[1]. MCT1-IN-2 (compound 1) has an EC50 of 5.5 nM (MTT assay) and an IC50 of 105 nM (lactate transport inhibition assay) in human Raji lymphoma cell proliferation[2].

[1]. Clare M Murray, et al. Monocarboxylate transporter MCT1 is a target for immunosuppression. Nat Chem Biol. 2005 Dec;1(7):371-6.

[2]. Hui Wang, et al. Synthesis and structure-activity relationships of pteridine dione and trione monocarboxylate transporter 1 inhibitors. J Med Chem. 2014 Sep 11;57(17):7317-24.