Cat. No. 4000
Chemical Name: N-[cis-4-[(4-Chlorophenyl)sulfonyl]
Biological Activityγ-secretase inhibitor; inhibits proteolytic cleavage of amyloid precursor protein (APP) over the Notch pathway. Reduces levels of Aβ in the brain (inhibits Aβ40 and Aβ42 in SH-SY5Y neuroblastoma cells with an IC50 of 0.65 nM); attenuates plaque deposition. Orally bioavailable.
Licensing InformationManufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans).
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
Best et al (2007) The novel γ-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) reduces amyloid plaque deposition without evidence of Notch-related pathology in the Tg2576 mouse. J.Pharm.Exp.Ther. 320 552. PMID: 17099072.
Best et al (2006) In vivo characterization of Aβ(40) changes in brain and cerebrospinal fluid using the novel γ-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) in the rat. J.Pharm.Exp.Ther. 317 786. PMID: 16443723.
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Citations are publications that use Tocris products. Selected citations for MRK 560 include:
Qi et al (2014) Longitudinal testing of hippocampal plasticity reveals the onset and maintenance of endogenous human Aβ-induced synaptic dysfunction in individual freely behaving pre-plaque transgenic rats: rapid reversal by anti-Aβ agents. Acta Neuropathol Commun 2 175. PMID: 25540024.
Singh et al (2014) GSI promotes vincristine-induced apoptosis by enhancing multi-polar spindle formation. Cell Cycle 13 157. PMID: 24200971.
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Keywords: MRK 560, supplier, MRK560, gamma-secretase, inhibitor, g-secretase, inhibitors, inhibits, secretases, amyloidbeta, amyloidb, amyloidβ, Tocris Bioscience, γ-Secretase Inhibitor products
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