MRK 560
Biological Activity
γ-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 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).
Compound Libraries
MRK 560 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| 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-UHFFFAOYSA-N |
| Smiles | ClC(C=C3)=CC=C3[S@]([C@@]1([C@]2=C(F)C=CC(F)=C2)CC[C@@H](NS(=O)(C(F)(F)F)=O)CC1)(=O)=O |
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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 51.79 | 100 | |
| ethanol | 25.9 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 517.92. Batch specific molecular weights may vary from batch to batch due to solvent 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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References
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:
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
Lariosa-Willingham et al (2016) Development of a central nervous system axonal myelination assay for high throughput screening. BMC Neurosci 17 16 PMID: 27103572
Do you know of a great paper that uses MRK 560 from Tocris? Please let us know.
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