Catalog No.: PC-43039Not For Human Use, Lab Use Only.
LY3039478 (Crenigacestat) is an exquisitely potent inhibitor of Notch-1 intracellular domain (N1ICD) cleavage with IC50 of 1 nM, also potently inhibits mutant Notch receptor activity.
LY3039478 (Crenigacestat) is an exquisitely potent inhibitor of Notch-1 intracellular domain (N1ICD) cleavage with IC50 of 1 nM, also potently inhibits mutant Notch receptor activity.
LY3039478 inhibits N1ICD cleavage and expression of Notch-regulated genes in the tumor microenvironment in xenograft tumor models.
LY3039478 significantly inhibits the growth of CCRCC cell lines in a concentration-dependent manne, decreases expression of Myc and cyclin A1, causes G0/G1 cell cycle arrest in CCRCC cells.
LY3039478 demonstrates in vivo efficacy in CCRCC in mice model.
1. Bhagat TD, et al. J Biol Chem. 2017 Jan 20;292(3):837-846.
2. Cancer Discov. 2017 Feb;7(2):OF3. doi: 10.1158/2159-8290.CD-NB2016-159.
3. Mark H. Bender, et al. Abstract 1131: Novel inhibitor of Notch signaling for the treatment of cancer. DOI: 10.1158/1538-7445.AM2013-1131 Published April 2013
