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IMR-1 is an inhibitor of mastermind-like 1 (Maml1) recruitment to chromatin.1 It binds to the intracellular domain of Notch (KD = 11 µM) and prevents transcription of Notch target genes by inhibiting the recruitment of Maml1, but not Notch1, to chromatin. It inhibits colony formation in the Notch-dependent cell lines SUM149, SUM159, and HT-1080, but not the Notch-independent cell lines T47D, MCF-7, and H23 when used at concentrations of 15 and 45 µM. IMR-1 (15 mg/kg) decreases the expression of the Notch target genes HES1, HEYL, and NOTCH3 and reduces tumor growth in a patient-derived esophageal adenocarcinoma mouse xenograft model.
WARNING This product is not for human or veterinary use.
1. The small molecule IMR-