Selective cancer stem cell killer / A novel inhibitor of the growth and proliferation of breast cancer stem cells (CSC) discovered in a phenotypic screen employing CSC-like cells produced by inducing human breast epithelial cells into an epithelial-to-mesenchymal transdifferentiated state (HMLE_sh_ECad). ML239 displayed an IC50=1.18 μM against HMLE_sh_ECad and demonstrated a >23-fold selectivity over control cells. It was also toxic to two other CSC-like lines1,2. Gene expression studies showed altered gene expression in the NFκB pathway1 and support activation of fatty acid desaturase 2 (FADS2) as a potential mechanism of action for ML239.3
Biochemicals & reagents
1378872-36-6
1) Carmody et al. (2012), Phenotypic high-throughput screening elucidates target pathway in breast cancer stem cell-like cells; J. Biomol. Screening, 17 1204 2) Germain et al. (2012), Identification of a selective small molecule inhibitor of breast cancer stem cells; Bioorg. Med. Chem., 22 3571 3) Rees et al. (2015), Correlating chemical sensitivity and basal gene expression reveals mechanism of action; Nat. Chem. Biol. 12 109
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PATHWAY: NFkappaB; Proliferation -- RESEARCH AREA: Cancer Stem Cells -- DISEASE AREA: Cancer