CBB1003 is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.IC50 value: 10.54 uM [1]Target: LSD1 inhibitorin vitro: Treatment of F9 cells with CBB1003 led to the activation of CHRM4 and SCN3A expression. Treatment of CBB1003 led to significant growth inhibition of mouse embryonic teratocarcinoma F9 cells. Treatment of mouse ES cells with CBB1003 and 1007 also led to substantial inhibition of the spherical growth of ES cells [1]. CBB1003 inhibited CRC cell proliferation and colony formation. In cultured CRC cells, inhibiting LSD1 activity by CBB1003 caused a decrease in LGR5 levels while overexpression of LGR5 reduced CBB1003-induced cell death [2].
[1]. Wang J, et al. Novel histone demethylase LSD1 inhibitors selectively target cancer cells with pluripotent stem cell properties. Cancer Res. 2011 Dec 1;71(23):7238-49. [2]. Hsu HC, et al. CBB1003, a lysine-specific demethylase 1 inhibitor, suppresses colorectal cancer cells growth through down-regulation of leucine-rich repeat-containing G-protein-coupled receptor 5 expression. J Cancer Res Clin Oncol. 2014 Jul 25.