ML 239

An inhibitor of breast cancer stem cells

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Background

ML239 is the best-in-class inhibitor of the breast cancer stem cells with an IC₅₀?= 1.16 μM. [1]

ML239 was a selective inhibitor an IC₅₀= 1.18 μM against HMLE_sh_ECad, demonstrated a >23-fold selectivity over the control line, and was toxic to another CSC-like line, HMLE_shTwist, and a breast carcinoma cell line, MDA-MB-231. Five genes (ATP6V0C, PKM2, PPDPF, RPL23, and?SERINC2) were differentially regulated in HMLE_sh_GFP after treatment with ML239. Gene expression studies conducted with ML239-treated cells showed altered gene expression in the NF-κB pathway in the HMLE_sh_ECad line but not in the isogenic control line. ML239 was selectively toxic toward another CSC-like cell line, HMLE_Twist, and the breast cancer line, MDA-MB-231. Similar to the results observed in the HMLE_sh_ECad cell line, ML239 was potently toxic, inhibiting HMLE_Twist with an IC₅₀?~0.1 μM. ML239 displayed potent toxicity (IC₅₀?= 2.81 μM) to the breast carcinoma cell line, MDA-MB-231 [1]. ML239 also alters the expression of genes in the NF-κB, MAPK and inflammatory cytokine pathways.

Reference:

1.Phenotypic high-throughput screening elucidates target pathway in breast cancer stem cell-like cells. J Biomol Screen. 2012 Oct;17(9):1204-10. Epub 2012 Aug 30.

Protocol

Cell experiment:

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].

参考文献:

[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.