Application

Inhibitor of mastermind recruitment-1 (IMR-1) has been used as an inhibitor of Notch transcription activation complex to downregulate the expression of Notch and downstream protein in pheochromocytoma (PC -12) cells.

Biochem/physiol Actions

IMR-1 is a cell penetrant and potent inhibitor of Notch transcriptional activation complex that disrupted the recruitment of Mastermind-like 1 (Maml1) to the Notch transcriptional activation complex on chromatin. IMR-1 potently inhibits the growth of Notch-dependent cancer cell lines, and inhibits growth of patient-derived tumor xenografts. IMR-1 is hydrolyzed in vivo to acid metabolite IMR-1A.

Packaging

5, 25 mg in glass bottle