Creatine transporter-IN-1 is a synthetic creatine transporter ( CT1/SLC6A8 ) inhibitor. Creatine transporter-IN-1 inhibits creatine uptake and shows anticancer activity against cancer cells [1].
In Vitro, Creatine transporter-IN-1 (Compound 4) (500 μM) weakly inhibits creatine uptake in CT1-expressing HEK293 cells[1]. Creatine transporter-IN-1 (0.1-100 μM; 24-48 h) reduces the viability of DLD-1 human colorectal adenocarcinoma cells in a concentration-dependent manner[1]. Creatine transporter-IN-1 (0.1-100 μM; 24-72 h) reduces the viability of HT-29 human colorectal adenocarcinoma cells in a concentration-dependent manner[1]. Creatine transporter-IN-1 (0.1-1 mM; 48 h) reduces the viability of MDA-MB-231 human breast adenocarcinoma cells in a concentration-dependent manner at millimolar concentrations[1].
References:
[1]. Stary, Dorota, et al. Structure-Based Search for Novel Creatine Transporter Inhibitors. ACS Medicinal Chemistry Letters (2026).
In Vitro, Creatine transporter-IN-1 (Compound 4) (500 μM) weakly inhibits creatine uptake in CT1-expressing HEK293 cells[1]. Creatine transporter-IN-1 (0.1-100 μM; 24-48 h) reduces the viability of DLD-1 human colorectal adenocarcinoma cells in a concentration-dependent manner[1]. Creatine transporter-IN-1 (0.1-100 μM; 24-72 h) reduces the viability of HT-29 human colorectal adenocarcinoma cells in a concentration-dependent manner[1]. Creatine transporter-IN-1 (0.1-1 mM; 48 h) reduces the viability of MDA-MB-231 human breast adenocarcinoma cells in a concentration-dependent manner at millimolar concentrations[1].
References:
[1]. Stary, Dorota, et al. Structure-Based Search for Novel Creatine Transporter Inhibitors. ACS Medicinal Chemistry Letters (2026).