LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) agonist with an EC50 of 18.94 nM.
CAS：2088939-99-3
分子式：C33H43Cl2N3O2
分子量：584.62
纯度：98%
存储：Store at -20°C

Background:

LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) agonist with an EC50 of 18.94 nM.

LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) agonist with an EC50 of 18.94 nM in ADP-Glo™ kinase assay. The in vitro kinase assay reveals that the LYN-1604 increases the phosphorylation of mATG13 at ser318 in wild-type ULK1 transfected HEK-293T cells. It is found that LYN-1604-treated cells display a remarkable green fluorescence with MDC staining and the autophagy ratio is increased in a dose-dependent manne. It is also found that LYN-1604 induces remarkable up-regulation of Beclin-1 and degradation of p62, as well as transformation of LC3-I to LC3-II[1].

Based on the results of tumor volume and weight, it is found that LYN-1604 can significantly inhibit the growth of xenograft MDA-MB-231 cells. The body weights of mice are stable, with no obvious distinctions between LYN-1604-treated and control mice. It also reveals that LYN-1604 induces remarkable autophagy in vivo[1].

参考文献:
[1]. Zhang L, et al. Discovery of a small molecule targeting ULK1-modulated cell death of triple negative breast cancer in vitro and in vivo. Chem Sci. 2017 Apr 1;8(4):2687-2701.