292632-98-5

292632-98-5 structure

Name: L-685,458
Chemical Name: L-685,458,(5S)-(tert-Butoxycarbonylamino)-6-phenyl-(4R)-hydroxy-(2R)-benzylhexanoyl)-L-leucy-L-phenylalaninamide
CAS Number: 292632-98-5
Molecular Formula: C₃₉H₅₂N₄O₆
Molecular Weight: 672.85300
Catalog: Signaling Pathways Neuronal Signaling γ-secretase
Create Date: 2017-08-24 21:20:53
Modify Date: 2024-01-03 07:25:52
L-685458 is a potent inhibitor of Amyloid β-Protein precursor γ-secretase activity with IC50 of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested.IC50 value: 17 nMTarget: γ-secretasein vitro: L-685458 is a Notch inhibitor. L-685458 blocks Notch activation in the two cell lines in terms of reduced cytoplasmic distribution and almost diminished nuclear labelling of Hes1 proteins. [2] L-685458 is a γ-secretase inhibitor. [3]

Name	L-685,458,(5S)-(tert-Butoxycarbonylamino)-6-phenyl-(4R)-hydroxy-(2R)-benzylhexanoyl)-L-leucy-L-phenylalaninamide
Synonyms	(5S)-(t-Butoxycarbonylamino)-6-phenyl-(4R)hydroxy-(2R)benzylhexanoyl)-L-leu-L-phe-amide L-685458

Description	L-685458 is a potent inhibitor of Amyloid β-Protein precursor γ-secretase activity with IC50 of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested.IC50 value: 17 nMTarget: γ-secretasein vitro: L-685458 is a Notch inhibitor. L-685458 blocks Notch activation in the two cell lines in terms of reduced cytoplasmic distribution and almost diminished nuclear labelling of Hes1 proteins. [2] L-685458 is a γ-secretase inhibitor. [3]
Related Catalog	Signaling Pathways >> Neuronal Signaling >> γ-secretase Signaling Pathways >> Stem Cell/Wnt >> γ-secretase Research Areas >> Neurological Disease
References	[1]. Shearman MS, et al. L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of amyloid beta-protein precursor gamma-secretase activity. Biochemistry. 2000 Aug 1;39(30):8698-8704. [2]. Zhang P, et al. Biological significance and therapeutic implication of resveratrol-inhibited Wnt, Notch and STAT3 signaling in cervical cancer cells. Genes Cancer. 2014 May;5(5-6):154-164. [3]. Jeon JH, et al. Glucosamine-induced OGT activation mediates glucose production through cleaved Notch1 and FoxO1, which coordinately contributed to the regulation of maintenance of self-renewal in mouse embryonic stem cells. Stem Cells Dev. 2014 Sep 1;23(1

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