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.
All Tocris products are intended for laboratory research use only.
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 |
Molarity Calculator
Reconstitution Calculator
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
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.
View Related Products by Target
View Related Products by Product Action
Keywords: MRK 560, supplier, MRK560, gamma-secretase, inhibitor, g-secretase, inhibitors, inhibits, secretases, amyloidbeta, amyloidb, amyloidβ, Gamma-Secretase, Tocris Bioscience
2 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
Do you know of a great paper that uses MRK 560 from Tocris? If so please let us know.
Literature in this Area
Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
- Cancer Metabolism
- Epigenetics in Cancer
- Receptor Signaling
- Cell Cycle and DNA Damage Repair
- Angiogenesis
- Invasion and Metastasis
Neurodegeneration Product Guide
A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:
- Alzheimer's disease
- Parkinson's disease
- Huntington's disease
Alzheimer's Poster
Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
