S 2101 is an inhibitor of lysine-specific demethylase 1 (LSD1)(IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s).

LSD1:(ki)0.61 μM , LSD1:0.99 μM

S 2101 is an inhibitor of lysine-specific demethylase 1 (LSD1)(IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s). S 2101 also displays much lower inhibition activity toward MAO-B with Ki of 17 μM and Kinact/Ki of 18 M/s and MAO-A (Ki=110 μM, Kinact/Ki=60 M/s). The treatment of HEK293T cells with S 2101 results in a dose-dependent increase in the level of H3K4me2, which must have accumulated by the inactivation of LSD1. During the course of S 2101 treatment, the amounts of histone H3 and LSD1 in the nuclear extracts remain essentially unaffected. Because the treatment with 1 μM S 2101 generates a level of H3K4me2 similar to that elicited by 50 μM 2-PCPA, In human cells, S 2101 is assumed to have approximately 50-fold stronger LSD1 inhibition activity than 2-PCPA .