SI-2 | Potent inhibitor of steroid receptor coactivator-3 (SRC-3)
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $70.00 | ||
| 25 mg | $230.00 |
SI-2 (380537-35-9) 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
References/Citations:
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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
SI-2 (380537-35-9) 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
References/Citations:
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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