Notch transcriptional activation inhibitor / 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 uM (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 uM (in vitro assay). Binding of IMR-1 to NTC is non-covalent and reversible.1
Biochemicals & reagents
310456-65-6
1) Austudilo et al. (2016), The Small Molecule IMR-1 Inhibits the Notch Transcriptional Activation Complex to Suppress Tumorigenesis; Cancer Res., 76 3593
-20°C
TARGET: Transcription factor -- PATHWAY: Notch; Transcription -- RESEARCH AREA: Cancer Stem Cells -- DISEASE AREA: Cancer