LYN-1604 dihydrochloride 是一种有效的 UNC-51 样激酶 1 (ULK1) 激活剂，EC₅₀ 值为 18.94 nM。LYN-1604 可用于三阴性乳腺癌 (TNBC) 的研究。

LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC 50 =18.94 nM) for the research of triple negative breast cancer (TNBC).

Solid

ULK1 18.94 nM (EC50)

LYN-1604 is a potential ULK1 agonist (enzymatic activity=195.7% at 100 nM and IC50=1.66 μM against MDA-MB-231 cells) .
LYN-1604 binds to wild-type ULK1 with a binding affinity in the nanomole range (KD=291.4 nM) .
LYN-1604 (0.5, 1.0 and 2.0 μM) induces cell death via the ULK complex in MDA-MB-231 cells.
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.
LYN-1604 induces ATG5-dependent autophagy via the ULK complex.
LYN-1604 can also increase cleavage of caspase3 and induce apoptosis. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.

In Vitro: H₂O : 50 mg/mL (76.04 mM; Need ultrasonic)DMSO : 50 mg/mL (76.04 mM; Need ultrasonic)配制储备液