Inhibitor of Mastermind Recruitment-1 (IMR-1) disrupts the recruitment of Mastermind-like 1 to the Notch transcriptional activation complex (NTC) on chromatin, which attenuates Notch target gene transcription1. IC50=26 M (in vitro assay). IMR-1 inhibits the growth of Notch-dependent cell lines and attenuates the growth of patient-derived tumor xenografts. The ethylester is hydrolyzed by intracellular esterases which produces the free acid compound (IMR-1A), IC50=0.5 M (in vitro assay). Binding of IMR-1 to NTC is non-covalent and reversible.1
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