LYN-1604 dihydrochlorideLYN-1604 dihydrochloride
MedChemExpress (MCE)
HY-101923B
2310109-38-5
99.55%
4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months
-20°C, 1 month (sealed storage, away from moisture)
Room temperature in continental US
may vary elsewhere.
LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC).
LYN-1604 is a potential ULK1 agonist (enzymatic activity=195.7% at 100 nM and IC50=1.66 μM against MDA-MB-231 cells) [1]. LYN-1604 binds to wild-type ULK1 with a binding affinity in the nanomole range (KD=291.4 nM) [1]. LYN-1604 (0.5, 1.0 and 2.0 μM) induces cell death via the ULK complex in MDA-MB-231 cells[1]. LYN-1604 (0.5-2 μM, 24 hours) induces remarkable up-regulation of Beclin-1 and degradation of p62, as well as transformation of LC3-I to LC3-II in MDA-MB-231 cells[1]. LYN-1604 induces ATG5-dependent autophagy via the ULK complex[1]. LYN-1604 can also increase cleavage of caspase3 and induce apoptosis[1].
LYN-1604 (low dose, 25 mg/kg
median dose, 50 mg/kg
high dose, 100 mg/kg
intragastric administration once a day for 14 days) inhibits the growth of xenograft TNBC by targeting ULK1-modulated cell death[1].
ULK1 18.94 nM (EC50)
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[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. [Content Brief]