MCT1-IN-3

MCT1-IN-3 is a monocarboxylate transporter 1 (MCT1) inhibitor with an IC50 value of 81.0 nM. MCT1-IN-3 has also significant inhibitivity against the multidrug transporter ABCB1. MCT1-IN-3 can be used for the research of cancer[1].

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

Research Areas >> Cancer

Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein

IC50: 81.0 nM (MCT1)[1] GI50: 20 μM (A-549); 15.1 μM (MCF-7)[1]

MCT1-IN-3 (compound 24) 对 MCT1 具有抑制活性，IC50 值为 81.0 nM[1]。 MCT1-IN-3 对表达 MCT1 的癌细胞系 A-549 和 MCF-7 具有很强的抗增殖活性，GI50 值分别为 20 μM 和 15.1 μM[1]< /sup>. MCT1-IN-3（5 μM；24 h）导致癌细胞周期停滞和细胞凋亡[1]。 MCT1-IN-3（1.0、2.0、3.5 和 5.0 μM）显示可使这些癌细胞对抗肿瘤药物敏感[1]。 MCT1-IN-3 还对多药转运蛋白 ABCB1 具有显著的抑制作用，并显示可逆转 ABCB1 介导的多药耐药性 (MDR) [1]。 Cell Cycle Analysis[1] Cell Line: A-549 cells Concentration: 5 μM Incubation Time: 24 h Result: Caused a disruption of the cell cycle of A-549 cancer cells, indicated by a shift from the predominant Go/G, phase. Apoptosis Analysis[1] Cell Line: A-549 cells Concentration: 5 μM Incubation Time: 24 h Result: Increased the percentage of total apoptotic cells by a factor of 13 from 0.51 to 6.68%.

[1]. Sachin Puri, et al. Indole Derivatives as New Structural Class of Potent and Antiproliferative Inhibitors of Monocarboxylate Transporter 1 (MCT1; SLC16A1). J Med Chem. 2023 Jan 12;66(1):657-676.