CBB1007 (trihydrochloride)

CBB1007 trihydrochloride is a reversible and selective LSD1 inhibitor with an IC₅₀ of 5.27 µM for human LSD1. CBB1007 trihydrochloride significantly blocks the demethylase activity of LSD1 on H3K4Me2 and H3K4Me. CBB1007 trihydrochloride shows selectivity for LSD1 over LSD2 or JARID1A, and induces differentiation-related genes in pluripotent cells. CBB1007 trihydrochloride is studied in non-pluripotent cancer research, targeting teratocarcinoma, embryonic carcinoma, and seminoma^[1][2]. In Vitro:CBB1007 (0-100 μM; 30 h; F9) trihydrochloride inhibits F9 cell growth^[2].
CBB1007 (5-20 μM; 14 days; hESCs) trihydrochloride increases lipid droplet formation in hESCs during adipogenesis^[1].
CBB1007 (5-20 μM; 14 days; hESCs) trihydrochloride reduces LSD1 and histone H3 levels while increasing H3K4me2 in human embryonic stem cells (hESCs)^[1].
CBB1007 (5-20 μM; 14 days; hESCs) trihydrochloride upregulates adipocyte marker genes PPARγ-2 and C/EBPα in hESCs^[1].
CBB1007 (0.5-20 μM; 24 h; F9) trihydrochloride activates the expression of CHRM4 and SCN3A genes^[2].
CBB1007 (10 μM) trihydrochloride significantly blocks the demethylase activity of LSD1 on mono- and di-methylated H3K4, but not tri-methylated H3K4 or di-methylated H3K9^[2].