ML 239

ML239 is a potent and selective inhibitor of breast cancer stem cells, with an IC50 of 1.16 μM.

Signaling Pathways >> Others >> Others

Research Areas >> Cancer

ML239 (Compound 7j) is a potent and selective inhibitor of breast cancer stem cells, with an IC50 of 1.16 μM, with ∼24-fold selectivity against the control cell line[1]. ML239 inhibits breast cancer stem-like cells, most likely through activation of fatty acid desaturase 2 (FADS2). ML239 is cytotoxic to NCIH661 cells, and FADS2 knockdown reduces ML239 cytotoxicity, and furthermore, FADS2 inhibitor SC-26196 also reduces ML239 cytotoxicity in cancer cell lines (CCLs)[2].

Cancer cell lines (CCLs) are plated at a density of 500 cells/well in white opaque tissue-culture-treated Aurora 1536-well MaKO plates in the provider-recommended growth media using a highly automated platform. Compounds (ML239) are added by acoustic transfer using a Labcyte Echo 555. 24 hours after plating. The effects of small molecules (ML239) are measured over a 16-point concentration range (two-fold dilution) in duplicate. DMSO is used at a constant concentration of 0.33%, including vehicle-only control wells. As a surrogate for viability, cellular ATP levels are assessed 72 hours after compound transfer by addition of CellTiterGlo followed by luminescence measurement using a ViewLux Microplate Imager. Duplicates are averaged and luminescence values normalized to vehicle (DMSO) treatment and background (media-only) wells[2].

[1]. Germain AR, et al. Identification of a selective small molecule inhibitor of breast cancer stem cells. Bioorg Med Chem Lett. 2012 May 15;22(10):3571-4.

[2]. Rees MG, et al. Correlating chemical sensitivity and basal gene expression reveals mechanism of action. Nat Chem Biol. 2016 Feb;12(2):109-16.

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