LYN-1604 Chemical Properties

Boiling point:

670.9±55.0 °C(Predicted)

Density 

1.168±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMF: 30 mg/ml; DMSO: 20 mg/ml; Ethanol: 30 mg/ml; Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml

form 

A crystalline solid

pka

8.03±0.50(Predicted)

color 

white to beige

LYN-1604 Usage And Synthesis

Description

LYN-1604 is an activator of unc-51-like kinase 1 (ULK1; EC₅₀ = 18.94 nM). It increases Beclin 1, LC3-II, and total LC3 protein levels and reduces levels of p62 in human MDA-MB-231 triple-negative breast cancer (TNBC) cells in a concentration-dependent manner, indicating an increase in autophagy. It also increases the cleavage of the pro-apoptotic protein caspase-3. LYN-1604 decreases the viability of MDA-MB-231 cells in vitro (IC₅₀ = 1.66 μM), an effect that can be reversed by the autophagy inhibitor 3-methyladenine (3-MA; ). LYN-1604 (25, 50, and 100 mg/kg) reduces tumor growth in an MDA-MB-231 mouse xenograft model.

Uses

LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC)[1].

in vivo

IC 50

ULK1: 18.94 nM (EC₅₀)

References

[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. DOI:10.1039/c6sc05368h