L-685,458

Description: L-685, 458 (also called L685458; L-685458) is a selective inhibitor of Aß PP gamma-secretase with potential anti-AD and anticancer activity. It inhibits Aß PP gamma-secretase with a Ki of 17 nM and shows more than 50-fold selectivity over a range of aspartyl, serine and cysteine proteases. L685458 is also equally potent in the inhibition of A beta 40 and A beta 42 peptides with IC50 values of 48 and 67 nM, respectively in human neuroblastoma cells. It regulates CXCR4 and VEGFR2 expression through blocking of Notch signaling in vitro as observed in the two cell lines in terms of reduced cytoplasmic distribution and almost diminished nuclear labelling of Hes1 proteins

References: Biochemistry. 2000 Aug 1; 39(30):8698-704; J Neurochem. 2001 Jan; 76(1):173-81; J Pharmacol Exp Ther. 2003 Jun; 305(3):864-71.

L685458; L685, 458; L-685, 458; L 685, 458; L-685458; L 685458;