Potent inhibitor of steroid receptor coactivator-3 (SRC-3) / Si-2 is a potent inhibitor of steroid receptor coactivator-3 (SRC-3).1 It blocks MDA-MB-468 cell growth with an IC50 = 3.4 nM without effecting normal cells.1 It significantly inhibited breast cancer cell growth in an orthotopic MDA-MD-468 mouse model. Treatment of MCF-7 or triple negative MDA-MB-231 cells with SI-2 resulted in inhibition of proliferation and breast cancer stem cell (CSC) tumorsphere formation.2 CSC markers CD44+/CD24-/1o and aldehyde dehydrogenase (ALDH) were also reduced indicating that SI-2 can selectively interfere with the TIC/CSC state in breast cancer cells.2,3
Biochemicals & reagents
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1) Song et al. (2016), Development of potent small-molecule inhibitors to drug the undruggable steroid receptor coactivator-3; Proc. Natl. Acad. Sci. USA 113 4970 2) Rohira et al. (2017), Targeting SRC Coactivators Blocks the Tumor-Initiating Capacity of Cancer Stem-like Cells; Cancer Res. 77 4293 3) Truong et al. (2018), Cancer Stem Cell Phenotypes in ER+ Breast Cancer Models are Promoted by PELP/AIB1 Complexes; Mol. Cancer Res. 16 707
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TARGET: Transcription factor -- PATHWAY: Proliferation; Transcription -- RESEARCH AREA: Cancer stem cells -- DISEASE AREA: Cancer