MRK-560

MRK-560, a chemical probe, is an orally active, brain barrier-penetrated γ-Secretase inhibitor, reducing Aβ peptide in rat brain and cerebrospinal fluid. MRK-560 decreases mutant NOTCH1 processing by selectively inhibiting PSEN1. MRK-560 can be used in studies of Alzheimer's disease and T-cell acute lymphoblastic leukaemia (T-ALL) [1][2].

Product Specifications

CAS Number

[677772-84-8]

UNSPSC

12352005

Hazard Statement

H315, H319

Target

γ-secretase

Type

Reference compound

Related Pathways

Neuronal Signaling; Stem Cell/Wnt

Applications

Neuroscience-Neurodegeneration

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/mrk-560.html

Purity

99.51

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=S([C@]1(C2=C(C=CC(F)=C2)F)CC[C@H](NS(C(F)(F)F)(=O)=O)CC1)(C3=CC=C(Cl)C=C3)=O

Molecular Formula

C19H17ClF5NO4S2

Molecular Weight

517.92

Precautions

H315, H319

References & Citations

[1]Habets RA, et al. Safe targeting of T cell acute lymphoblastic leukemia by pathology-specific NOTCH inhibition. Sci Transl Med. 2019 May 29;11 (494) :eaau6246. |[2]Best JD, et al. In vivo characterization of Abeta (40) changes in brain and cerebrospinal fluid using the novel gamma-secretase inhibitor N-[cis-4-[ (4-chlorophenyl) sulfonyl]-4- (2,5-difluorophenyl) cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) in the rat. J Pharmacol Exp Ther.2006 May;317 (2) :786-90.