623165-93-5

MRK 003 is a potent, selective and orally active γ-secretase inhibitor. MRK 003 reduce brain Aβ production in vivo. MRK 003 induces caspase-dependent apoptosis and inhibits tumor cell proliferation in vivo and in vitro[1][2][3].

[1] Lewis HD, et al. Apoptosis in T cell acute lymphoblastic leukemia cells after cell cycle arrest induced by pharmacological inhibition of notch signaling. Chem Biol. 2007;14(2):209-219. DOI:10.1016/j.chembiol.2006.12.010
[2] Sparey T, et al. Cyclic sulfamide gamma-secretase inhibitors. Bioorg Med Chem Lett. 2005;15(19):4212-4216. DOI:10.1016/j.bmcl.2005.06.084
[3] Mizuma M, et al. The gamma secretase inhibitor MRK-003 attenuates pancreatic cancer growth in preclinical models. Mol Cancer Ther. 2012;11(9):1999-2009. DOI:10.1158/1535-7163.MCT-12-0017