MK-0752

gamma-Secretase is a protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors and beta-amyloid precursor protein (APP), within the transmembrane domain. MK-0752 is a potent, reversible inhibitor of gamma-secretase, reducing the cleavage of APP to Abeta40 in human neuroblastoma SH-SY5Y cells with an IC50 value of 5 nM. It is orally bioavailable and crosses the blood-brain barrier, as orally administered MK-0752 dose-dependently reduces the generation of new amyloid beta protein in the brain of rhesus monkeys. Through its effects on the Notch pathway, MK-0752 reduces the number of breast cancer stem cells in tumorgrafts, enhancing the efficacy of the chemotherapy drug docetaxel (Cay-11637) in mice with breast cancer tumors.Formal Name: cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)-cyclohexanepropanoic acid. CAS Number: 471905-41-6. Molecular Formula: C21H21ClF2O4S. Formula Weight: 442.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 50 mg/ml, DMSO: 10 mg/ml, DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml, Ethanol: 5 mg/ml. lambdamax: 230, 275 nm. SMILES: O=C(O)CC[C@H]1CC[C@](S(C2=CC=C(Cl)C=C2)(=O)=O)(C3=C(F)C=CC(F)=C3)CC1. InChi Code: InChI=1S/C21H21ClF2O4S/c22-15-2-5-17(6-3-15)29(27,28)21(18-13-16(23)4-7-19(18)24)11-9-14(10-12-21)1-8-20(25)26/h2-7,13-14H,1,8-12H2,(H,25,26)/t14-,21+. InChi Key: XCGJIFAKUZNNOR-QCKZDCLWSA-N.