L-685,458 CAS: 292632-98-5
MF: C39H52N4O6
MW: 672.85
A potent and selective γ-secretase inhibitor.

L-685,458 (CAS 292632-98-5)

L-685,458 | CAS 292632-98-5 is rated 5.0 out of 5 by 1.
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Synonym: (5S)-(t-Butoxycarbonylamino)-6-phenyl-(4R)hydroxy-(2R)benzylhexanoyl)-L-leu-L-phe-amide
Application: A potent and selective γ-secretase inhibitor
CAS Number: 292632-98-5
Molecular Weight: 672.85
Molecular Formula: C39H52N4O6
* Refer to Certificate of Analysis for lot specific data (including water content).
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L-685,458 is a potent and selective γ-secretase inhibitor (IC50 = 17 nM) that displays > 50-fold selectivity over a range of aspartyl, serine and cysteine proteases. It exhibits equal potency for inhibition of Aβ40 and Aβ42 peptides.


References

1. Shearman, M S., et al., 2000. L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of amyloid beta-protein precursor gamma-secretase activity. Biochemistry. 39(30): 8698-704. PMID: 10913280
2. Williams, Cassin Kimmel., et al., 2006. Up-regulation of the Notch ligand Delta-like 4 inhibits VEGF-induced endothelial cell function. Blood. 107(3): 931-9. PMID: 16219802
3. Williams, Cassin Kimmel., et al., 2008. Regulation of CXCR4 by the Notch ligand delta-like 4 in endothelial cells. Cancer research. 68(6): 1889-95. PMID: 18339870

Physical State :
Solid
Solubility :
Soluble in DMSO (15 mM).
Storage :
Store at -20° C
IC50 :
γ-secretase: IC50 = 17 nM; Aβ40 peptide: IC50 = 48 nM (human neuroblastoma cells); Aβ42 peptide: IC50 = 67 nM (human neuroblastoma cells)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
456313
MDL Number :
MFCD03093402
SMILES :
CC(C)C[[email protected]@H](C(=O)N[[email protected]@H](CC1=CC=CC=C1)C(=O)N)NC(=O)[[email protected]@H](CC2=CC=CC=C2)C[[email protected]]([[email protected]](CC3=CC=CC=C3)NC(=O)OC(C)(C)C)O

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Certificate of Analysis

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L-685,458  Product Citations

See how others have used L-685,458. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 24861611  Yang, ZY. et al. 2014. Basic Clin. Pharmacol. Toxicol. 115: 518-26.

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from Shearman Shearman, MS. et al. (PubMed 10913280) reported that L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of amyloid beta-protein precursor gamma-secretase activity. -SCBT Publication Review
Date published: 2015-03-15
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