677772-84-8
Chemical Structure
MRK-560
- CAS No.: 677772-84-8
- Formula:C19H17ClF5NO4S2
- Molecular Weight:517.92
IUPAC Name: N-((1s,4s)-4-((4-chlorophenyl)sulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)-1,1,1-trifluoromethanesulfonamide
InChIKey: WDZVWDXOIGQJIO-UJKQEGAGSA-N
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
Biological Activity: 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].
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MRK-560 | 99.92% | 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). | ||||||||||||||||||||
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- [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. [Content Brief]
- [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.
Keywords