CBB1007

CBB1007 is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).IC50 Value: 5.27 uMTarget: hLSD1CBB1007 efficiently can block LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC50 ≤ 5 μM) with no effect on H3K4Me3 and H3K9Me2, and LSD2 and JARID1A activities. Increases H3K4Me2 and H3K4Me contents (IC50 ≤ 5 μM), and causes activation of epigenetically suppressed CHRM4/M4-ArchR and SCN3A genes in F9 cells (IC50 ≤ 3.74 μM). CBB1007 was Shown to preferentially arrest the growth of pluripotent tumors with minimal effect on non-pluripotent cancer or normal somatic cells (IC50 ≥ 100 μM).

Signaling Pathways >> Epigenetics >> Histone Demethylase

Research Areas >> Cancer

[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.

GSK-J4 | QC6352 | GSK2879552 | SP-2509 | CPI-455 | trans-2-Phenylcyclopropylamine hemisulfate salt | 5-Carboxy-8-hydroxyquinoline | ML324 | GSK-LSD1 Dihydrochloride | NCGC00244536 | Daminozide | ORY-1001(trans) | JIB-04 | AS 8351 | KDM5-IN-1