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SI-2

Chemical Structure : SI-2

CAS No.: 223788-33-8

SI-2 (EPH-116, EPH116)

Catalog No.: PC-70313Not For Human Use, Lab Use Only.

SI-2 (EPH-116) is a potent small-molecule inhibitor of steroid receptor coactivator-3 (SRC-3 or AIB1) that can selectively inhibit the intrinsic transcriptional activities of SRC-3, also inhibits SRC-1 and SRC-2.

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Biological Activity

SI-2 (EPH-116) is a potent small-molecule inhibitor of steroid receptor coactivator-3 (SRC-3 or AIB1) that can selectively inhibit the intrinsic transcriptional activities of SRC-3, also inhibits SRC-1 and SRC-2.
SI-2 (EPH-116) selectively reduces cellular protein levels of SRC-3, but not that of CARM-1, blocks MDA-MB-468 cell growth with an IC50 value of 3.4 nM, but spares normal cells.
SI-2 (EPH-116)  significantly inhibit primary tumor growth and reduce SRC-3 protein levels in a breast cancer mouse model.
SI-2 (EPH-116)  is a "first-in-class" compound that targets oncogenic coactivator.

Physicochemical Properties

M.Wt 265.3
Formula C15H15N5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(1E)-1-(2-pyridinyl)-ethanone-2-(1-methyl-1H-benzimidazol-2-yl)hydrazone

References

1. Song X, et al. Proc Natl Acad Sci U S A. 2016 May 3;113(18):4970-5.

2. Rohira AD, et al. Cancer Res. 2017 Aug 15;77(16):4293-4304.

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