MRK 560

Name: MRK 560
Brand: Tocris Bioscience
SKU: 4000

Tocris Bioscience a Bio-Techne Brand

Catalog # 4000

Citations (3)

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Key Product Details

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)
Molecular Weight:	517.92

View Full Technical Details for MRK 560

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).

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.

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 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 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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References for MRK 560

References are publications that support the biological activity of the product.

Best 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. 2007 PMID: 17099072
Best 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. 2006 PMID: 16443723

Citations for MRK 560 (3)

Showing 1 - 3 of 3 citations Showing All

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Citations are publications that use Bio-Techne 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

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