GSK2879552
LSD1 inhibitor / GSK289552 is potent, selective, and irreversible inhibitor of Lysine Demethylase 1 (LSD1) via covalent modification of the LSD1 cofactor FAD (Ki = 1.7 µM). It is selective for LSD1 over the closely related LSD2, MAO-A, MAO-B, and the FAD dependent enzymes D-amino acid oxidase and glutathione reductase. Tested against a panel of 165 cancer cell lines, GSK2879552 inhibited the proliferation of 9 small cell lung carcinoma lines and 20 AML cell lines.
Biochemicals & reagents
1401966-69-5
1) Mohammad et al. (2015), A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC; Cancer Cell 28 57
-20°C
TARGET: Protein demethylase -- PATHWAY: Chromatin; Posttranslational modification; Proliferation -- RESEARCH AREA: Epigenetics -- DISEASE AREA: Cancer