SI-2

SI-2 (also known as EPH 116) is a first-in-class, potent small-molecule inhibitor of steroid receptor coactivator-3 (SRC-3, also known as NCOA3 or AIB1) and other members of the p160 family of steroid receptor coactivators (SRC-1 and SRC-2). Developed by researchers at Baylor College of Medicine and licensed to Coregon, SI-2 directly binds to SRC-3 to promote its degradation, thereby reducing its transcriptional activity and cellular protein levels. In preclinical studies, SI-2 has demonstrated high potency in selectively killing various breast cancer cells (including endocrine-sensitive, endocrine-resistant, and triple-negative breast cancer cells) and lymphoma cells in the low nanomolar range, while sparing normal cells. It has also shown efficacy in inhibiting primary tumor growth in breast cancer and lymphoma mouse models with minimal toxicity.

Other names

(1E)-1-(2-pyridinyl)-ethanone-2-(1-methyl-1H-benzimidazol-2-yl)hydrazone(1E)-1-(2-pyridinyl)ethanone 2-(1-methyl-1H-benzimidazol-2-yl)hydrazone(E)-EPH 116(E)-SI-2EPH 116 hydrochlorideEPH116 hydrochlorideEPH-116 hydrochlorideSI-2 hydrochlorideSI2 hydrochlorideSI 2 hydrochloride