steroid receptor coactivator-3

SI-2 is an inhibitor (SMI) of steroid receptor coactivator-3 (SRC-3 or AIB1). SI-2 can selectively reduce the transcriptional activities and the protein concentrations of SRC-3 in cells, and selectively induce breast cancer cell death with IC50 values in the low nanomolar range (3-20 nM), but not affect normal cell viability.

SRC-3-IN-2 (SI-12 6c) is an orally active inhibitor of steroid receptor coactivator 3 (SRC-3) with antitumor properties.

SRC-3-IN-1 (compound SI-10) is an inhibitor of steroid receptor coactivator 3 (SRC-3) with an IC50 of 3.3 μM. It features good water solubility, oral bioavailability, and selectivity. SRC-3-IN-1 is applicable for prostate cancer research.

(E)-SI-2 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. It 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.