LYN-1604 hydrochloride |
カタログ番号GC36517 |
LYN-1604 塩酸塩は、トリプルネガティブ乳がん (TNBC) の研究のための強力な UNC-51 様キナーゼ 1 (ULK1) 活性化剤 (EC50=18.94 nM) です。
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Cas No.: 2216753-86-3
Sample solution is provided at 25 µL, 10mM.
LYN-1604 hydrochloride is a potent ULK1 activator with an EC50 of 18.94 nM. EC50: 18.94 nM (ULK1)[1]
LYN-1604 is found as a potential ULK1 activator with enzymatic activity of 195.7% at 100 nM and IC50 of 1.66 μM against MDA-MB-231 cells. LYN-1604 displays a good effect on ULK1 activation with an EC50 of 18.94 nM. LYS50, LEU53, and TYR89 are key to the activation site of LYN-1604. LYN-1604 induces cell death in MDA-MB-231 cells. LYN-1604 could modulate ATF3 and RAD21 through ULK1 in MDA-MB-231 cells. LYN-1604 can also increase cleavage of caspase3 and induce apoptosis. LYN-1604 induces cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis[1].
LYN-1604 could significantly inhibit the growth of xenograft MDA-MB-231 cells. The body weights of mice are stable. LYN-1604 induces remarkable autophagy in vivo. LYN-1604 has good therapeutic potential by targeting ULK1-modulated cell death of TNBC, thus making a ULK1 agonist that can be utilized as a new drug for triple negative breast cancer therapy[1].
[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.
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