SR-C-107 R

SR-C-107 R is an orally bioavailable small molecule inhibitor of the ENL (Eleven-Nineteen-Leukemia) YEATS domain, an epigenetic reader protein. Developed by researchers at Texas A&M University, it is designed to target acute myeloid leukemia (AML), particularly cases harboring oncogenic MLL rearrangements. The compound functions by competitively binding to the ENL YEATS domain, thereby disrupting its interaction with acetylated histones (such as H3K9ac and H3K27ac). This disruption prevents the recruitment of the super elongation complex (SEC) to oncogenic promoters, leading to the suppression of leukemia-essential gene expression programs. Preclinical studies have demonstrated that SR-C-107 R possesses high potency (IC50 of 40 nM), excellent metabolic stability, and significant in vivo efficacy in AML xenograft models, where it has shown tumor regression and improved survival.

Other names

(R)-N-(2-((2-Isopropylazetidin-1-yl)methyl)-1H-pyrrolo[3,2-c]pyridin-6-yl)-[1,2,4]triazolo[4,3-a]pyridine-6-carboxamide