|
Back to products
Browse products
Approved anticancer agents
Anticancer agents in trials
Anticancer agents
in preclinical trials
Anticancer molecular libraries
Other drug agents
Drug intermediates
Bio-reagents and biochemicals
|
MedKoo product information:
L685458
Description of
L685458:
L685458 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.
L685458 also 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.
|
MedKoo Code#: 500910
|
|
Name: L685458
|
|
CAS#: 292632-98-5
Synonym:
L685,458;
L-685458;
L 685458;
L-685,458
IUPAC/Chemical name:
tert-butyl
((2S,3R,5R)-6-(((S)-1-(((S)-1-amino-1-oxo-3-phenylpropan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)amino)-5-benzyl-3-hydroxy-6-oxo-1-phenylhexan-2-yl)carbamate.
|
|
Chemical structure
|
Theoretical analysis
|
|
|
MedKoo Code#: 500910
Name: L685458
CAS#: 292632-98-5
Chemical Formula: C39H52N4O6
Exact Mass: 672.38869
Molecular Weight: 672.85
Elemental Analysis: C, 69.62; H, 7.79; N,
8.33; O, 14.27
|
|
Availability and price:
This agent is available
through custom synthesis
To inquire quotation and lead time or to ask questions, please send email to
sales@medkoo.com to describe your needs. A representative
will respond your email shortly. We offer big discount for orders of bulk quantities.
|
|
Information about this agent
|
1: Singh CR, Bakhru P, Khan A, Li QB, Jagannath
C. Cutting edge: Nicastrin and related components of γ-secretase
generate a peptide epitope facilitating immune recognition of
intracellular mycobacteria, through MHC class II-dependent priming of T
cells. J Immunol. 2011 Dec 1;187(11):5495-9. Epub 2011 Oct 28. PubMed
PMID: 22039303; PubMed Central PMCID: PMC3221744.
2: Hiyama A, Skubutyte R, Markova D, Anderson DG, Yadla S, Sakai D,
Mochida J, Albert TJ, Shapiro IM, Risbud MV. Hypoxia activates the notch
signaling pathway in cells of the intervertebral disc: implications in
degenerative disc disease. Arthritis Rheum. 2011 May;63(5):1355-64. doi:
10.1002/art.30246. PubMed PMID: 21305512.
3: Knappenberger KS, Tian G, Ye X, Sobotka-Briner C, Ghanekar SV,
Greenberg BD, Scott CW. Mechanism of gamma-secretase cleavage
activation: is gamma-secretase regulated through autoinhibition
involving the presenilin-1 exon 9 loop? Biochemistry. 2004 May
25;43(20):6208-18. PubMed PMID: 15147205.
4: Tian G, Ghanekar SV, Aharony D, Shenvi AB, Jacobs RT, Liu X,
Greenberg BD. The mechanism of gamma-secretase: multiple inhibitor
binding sites for transition state analogs and small molecule
inhibitors. J Biol Chem. 2003 Aug 1;278(31):28968-75. Epub 2003 Apr 28.
PubMed PMID: 12719412.
5: Tian G, Sobotka-Briner CD, Zysk J, Liu X, Birr C, Sylvester MA,
Edwards PD, Scott CD, Greenberg BD. Linear non-competitive inhibition of
solubilized human gamma-secretase by pepstatin A methylester, L685458,
sulfonamides, and benzodiazepines. J Biol Chem. 2002 Aug
30;277(35):31499-505. Epub 2002 Jun 18. PubMed PMID: 12072428.
|
Contact MedKoo:
Email:
sales@medkoo.com
(Keyword; CAS#; MedKoo code#)
|
