L-685,458

Modify Date: 2024-01-03 07:25:52

L-685,458 Structure
L-685,458 structure
Common Name L-685,458
CAS Number 292632-98-5 Molecular Weight 672.85300
Density N/A Boiling Point N/A
Molecular Formula C39H52N4O6 Melting Point N/A
MSDS USA Flash Point N/A

 Use of L-685,458


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]

 Names

Name L-685,458,(5S)-(tert-Butoxycarbonylamino)-6-phenyl-(4R)-hydroxy-(2R)-benzylhexanoyl)-L-leucy-L-phenylalaninamide
Synonym More Synonyms

 L-685,458 Biological Activity

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
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

 Chemical & Physical Properties

Molecular Formula C39H52N4O6
Molecular Weight 672.85300
Exact Mass 672.38900
PSA 159.85000
LogP 6.34900
Storage condition -20℃

 Safety Information

Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Safety Phrases 22-24/25
RIDADR NONH for all modes of transport
WGK Germany 3

 Articles3

More Articles
RAGE inhibition in microglia prevents ischemia-dependent synaptic dysfunction in an amyloid-enriched environment.

J. Neurosci. 34(26) , 8749-60, (2014)

Ischemia is known to increase the deleterious effect of β-amyloid (Aβ), contributing to early cognitive impairment in Alzheimer's disease. Here, we investigated whether transient ischemia may function...

Suppression of Notch signaling in the neonatal mouse ovary decreases primordial follicle formation.

Endocrinology 150 , 1014-24, (2009)

Notch signaling directs cell fate during embryogenesis by influencing cell proliferation, differentiation, and apoptosis. Notch genes are expressed in the adult mouse ovary, and roles for Notch in reg...

L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of amyloid beta-protein precursor gamma-secretase activity.

Biochemistry 39 , 8698, (2000)

Progressive cerebral amyloid beta-protein (A beta) deposition is believed to play a central role in the pathogenesis of Alzheimer's disease (AD). Elevated levels of A beta(42) peptide formation have b...

 Synonyms

(5S)-(t-Butoxycarbonylamino)-6-phenyl-(4R)hydroxy-(2R)benzylhexanoyl)-L-leu-L-phe-amide
L-685458