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Description: γ-secretase inhibitor; attenuates amyloid plaque deposition
Chemical Name: N-[cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide
Purity: ≥99% (HPLC)
Biological Activity for MRK 560
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.
Licensing Information
Manufactured 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).
Extrernal Portal Information for MRK 560
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.
Compound Libraries for MRK 560
MRK 560 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for MRK 560
| M. Wt | 517.92 |
| Formula | C19H17ClF5NO4S2 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 677772-84-8 |
| PubChem ID | 11577204 |
| InChI Key | WDZVWDXOIGQJIO-UJKQEGAGSA-N |
| Smiles | FC1=CC(=C(F)C=C1)[C@]1(CC[C@@H](CC1)N[S](=O)(=O)C(F)(F)F)[S](=O)(=O)C1=CC=C(Cl)C=C1 |
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.
Solubility Data for MRK 560
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 51.79 | 100 | |
| ethanol | 25.9 | 50 |
Preparing Stock Solutions for MRK 560
The following data is based on the product molecular weight 517.92. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.93 mL | 9.65 mL | 19.31 mL |
| 5 mM | 0.39 mL | 1.93 mL | 3.86 mL |
| 10 mM | 0.19 mL | 0.97 mL | 1.93 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
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Product Datasheets for MRK 560
References for MRK 560
References are publications that support the biological activity of the product.
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) J.Pharm.Exp.Ther. 317 786 PMID: 16443723
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 T J.Pharm.Exp.Ther. 320 552 PMID: 17099072
If you know of a relevant reference for MRK 560, please let us know.
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Keywords: MRK 560, MRK 560 supplier, MRK560, gamma-secretase, inhibitor, g-secretase, inhibitors, inhibits, secretases, amyloidbeta, amyloidb, amyloidβ, Gamma-Secretase, Amyloid, Beta, Peptides, 4000, Tocris Bioscience
3 Citations for MRK 560
Citations are publications that use Tocris products. Selected citations for MRK 560 include:
Lariosa-Willingham et al (2016) Development of a central nervous system axonal myelination assay for high throughput screening. BMC Neurosci 17 16 PMID: 27103572
Singh et al (2014) GSI promotes vincristine-induced apoptosis by enhancing multi-polar spindle formation. Cell Cycle 13 157 PMID: 24200971
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
Do you know of a great paper that uses MRK 560 from Tocris? Please let us know.
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