CBB3001

CBB3001 is an inhibitor of LSD1/KDM1A. CBB3001 exerts its effect by inhibiting Histone Demethylase activity, with an IC₅₀ of 21.25 μM. It downregulates the expression of pluripotency-related proteins and genes such as SOX2 and OCT4, and induces cell differentiation, growth arrest, and apoptosis. CBB3001 can be used for research on testicular germ cell tumors, teratomas, and embryonal carcinomas^{[1][2][3][4][5][6][7]}. In Vitro:CBB3001 (1-100 μM) potently inhibits the demethylase activity of purified recombinant GST-LSD1 protein in vitro, with an IC₅₀ of 21.25 μM^[2].
CBB3001 (20 μM; 16 h) inhibits LSD1 histone demethylase activity in human colorectal cancer HCT116 cells and human ovarian teratocarcinoma PA-1 cells, thereby increasing the levels of monomethylated and dimethylated H3K4, but does not affect the level of trimethylated H3K4^[2].
CBB3001 (20-40 μM; 16-30 h) downregulates the expression of the pluripotent stem cell proteins SOX2 and OCT4 in human ovarian teratocarcinoma PA-1 cells and mouse embryonal carcinoma F9 cells^[2].
CBB3001 (20 μM; 20 h) reduces EZH2 protein levels in wild-type mouse embryonic fibroblasts^[4].
CBB3001 (10 h treatment) reduces the protein levels of mSWI/SNF complex subunits in CAGGCre-ER/LSD1^fl/fl mouse embryonic fibroblasts (MEFs) within 10 h^[5].
CBB3001 (1-40 μM; 12-30 h) selectively inhibits the growth of human ovarian teratocarcinoma PA-1 cells and mouse embryonal carcinoma F9 cells, but exerts no significant effect on the growth of human colorectal cancer HCT116 cells or mouse fibroblast NIH3T3 cells^[2].
CBB3001 (20-40 μM) potently inhibits the growth of human ovarian teratocarcinoma (PA-1) cells and mouse embryonal carcinoma (F9) cells, with an IC₅₀ of approximately 20 μM. It also reduces the expression of pluripotency markers and exerts no effect on non-pluripotent tumor cells^[3].
CBB3001, a histone demethylase inhibitor, inhibits cell growth, downregulates pluripotency, and upregulates differentiation in testicular germ cell tumor cell lines^[7].