CBB1003 is a new inhibitor of histone demethylase LSD1 (IC50: 10.54 μM).

In mouse embryonic teratocarcinoma F9 cells, treatment of CBB1003 led to significant growth inhibition and the activation of CHRM4 and SCN3A expression. Treatment of mouse ES cells with CBB1003 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].