MRK 560
Chemical Name: N-[cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide
Purity: ≥99%
Biological Activity
MRK 560 is a γ-secretase inhibitor, which selectively inhibits proteolytic cleavage of amyloid precursor protein (APP) over the Notch pathway. MRK 560 reduces levels of Aβ in vitro (inhibits Aβ40 and Aβ42 in SH-SY5Y neuroblastoma cells with an IC50 of 0.65 nM) and attenuates plaque deposition. This compound is orally bioavailable.Extrernal Portal Information
The Chemical Probes webpages of the Structural Genomics Consortium are a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of MRK 560 is reviewed.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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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)
Best et al.
J.Pharm.Exp.Ther., 2006;317:786 -
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 T
Best et al.
J.Pharm.Exp.Ther., 2007;320:552
Product Datasheets
Citations for MRK 560
The citations listed below are publications that use Tocris products. Selected citations for MRK 560 include:
3 Citations: Showing 1 - 3
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Development of a central nervous system axonal myelination assay for high throughput screening.
Authors: Lariosa-Willingham Et al.
BMC Neurosci 2016;17:16
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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.
Authors: Qi Et al.
Acta Neuropathol Commun 2014;2:175
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GSI promotes vincristine-induced apoptosis by enhancing multi-polar spindle formation.
Authors: Singh Et al.
Cell Cycle 2014;13:157
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