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 NFkappaB pathway1 and support activation of fatty acid desaturase 2 (FADS2) as a potential mechanism of action for ML239.3
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