Molecular structure of L-685,458, CAS Number: 292632-98-5
L-685,458 (CAS 292632-98-5)
See product citations (4)
Alternate Names:
(5S)-(t-Butoxycarbonylamino)-6-phenyl-(4R)hydroxy-(2R)benzylhexanoyl)-L-leu-L-phe-amide
Application:
L-685,458 is a potent and selective γ-secretase inhibitor
CAS Number:
292632-98-5
Molecular Weight:
672.85
Molecular Formula:
C39H52N4O6
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Potent and selective γ-secretase inhibitor (IC50 = 17 nM) that displays > 50-fold selectivity over a range of aspartyl, serine and cysteine proteases. Exhibits equal potency for inhibition of Aβ40 and Aβ42 peptides (IC50 values are 48 and 67 nM respectively in human neuroblastoma cells). Also regulates CXCR4 and VEGFR2 expression through inhibition of Notch signaling in vitro.
L-685,458 (CAS 292632-98-5) References
- L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of amyloid beta-protein precursor gamma-secretase activity. | Shearman, MS., et al. 2000. Biochemistry. 39: 8698-704. PMID: 10913280
- Overexpression of calsenilin enhances gamma-secretase activity. | Jo, DG., et al. 2005. Neurosci Lett. 378: 59-64. PMID: 15763173
- Up-regulation of the Notch ligand Delta-like 4 inhibits VEGF-induced endothelial cell function. | Williams, CK., et al. 2006. Blood. 107: 931-9. PMID: 16219802
- Gamma-secretase inhibitors exerts antitumor activity via down-regulation of Notch and Nuclear factor kappa B in human tongue carcinoma cells. | Yao, J., et al. 2007. Oral Dis. 13: 555-63. PMID: 17944672
- Regulation of CXCR4 by the Notch ligand delta-like 4 in endothelial cells. | Williams, CK., et al. 2008. Cancer Res. 68: 1889-95. PMID: 18339870
- Calcium/calmodulin-dependent kinase II regulates notch-1 signaling in prostate cancer cells. | Mamaeva, OA., et al. 2009. J Cell Biochem. 106: 25-32. PMID: 19021144
- Contribution of gamma-secretase to calcium-mediated cell death. | Choi, YH., et al. 2010. Neurosci Lett. 469: 425-8. PMID: 20035833
- MUC5AC expression through bidirectional communication of Notch and epidermal growth factor receptor pathways. | Kang, JH., et al. 2011. J Immunol. 187: 222-9. PMID: 21622856
- Specificity of presenilin-1- and presenilin-2-dependent γ-secretases towards substrate processing. | Stanga, S., et al. 2018. J Cell Mol Med. 22: 823-833. PMID: 28994238
- Uncovering the Binding Mode of γ -Secretase Inhibitors. | Hitzenberger, M. and Zacharias, M. 2019. ACS Chem Neurosci. 10: 3398-3403. PMID: 31244051
Inhibitor of:
Aph-1c, beta-Amyloid, Csl, ENHO, FKBP51, fringe, Gamma-secretase, HES4, HES7, HoxA5, ILT-7, Jagged, KIAA1024L_A730017C20Rik, LOC441052, NET-7, NUMB, PPIAL4, PPIAL4F, Ppil3, pS2, Radical Fringe, SPPase2, SPPL3, TLE5, and X11α.Activator of:
achaete, Aph-1b, Aph-1c, C14orf135, Contactin 4, Delta, Dengue Virus, FKBP6, Hairless, Notch 2, NRIP3, and SPPL3.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
L-685,458, 1 mg | sc-204042 | 1 mg | $337.00 | |||
L-685,458, 5 mg | sc-204042A | 5 mg | $1000.00 |