MK-0752

MK-0752 is a synthetic small molecule that acts as a potent and reversible inhibitor of gamma-secretase. By inhibiting gamma-secretase activity, it blocks the cleavage of several integral membrane proteins including Notch receptors and amyloid precursor protein (APP), thereby suppressing the Notch signaling pathway. This mechanism may result in antineoplastic effects by inducing growth arrest and apoptosis in tumor cells dependent on Notch signaling. It was developed primarily for oncology indications (such as CNS cancer, breast cancer, hematological malignancies, pancreatic cancer) and Alzheimer's disease but has been discontinued for all these indications[1][5][7]. The drug was originally developed by Merck & Co., with Cancer Research UK also involved in development efforts[5].

Other names

3-[4-(4-chlorophenyl)sulfonyl-4-(2,5-difluorophenyl)cyclohexyl]propanoic acidCyclohexanepropanoic acid, 4-((4-chlorophenyl)sulfonyl)-4-(2,5-difluorophenyl)-, cis-NOTCH SIGNALING PATHWAY INHIBITOR MK0752