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LYN-1604 hydrochloride

Catalog No. T39687 CAS 2216753-86-3

LYN-1604 hydrochloride, a powerful activator of UNC-51-like kinase 1 (ULK1) with an EC50 value of 18.94 nM, has significant implications in the study of triple-negative breast cancer (TNBC).

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LYN-1604 hydrochloride Chemical Structure

LYN-1604 hydrochloride, CAS 2216753-86-3

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50 mg	Inquiry	$ 1,152.00
100 mg	Inquiry	$ 2,117.00

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Description	LYN-1604 hydrochloride, a powerful activator of UNC-51-like kinase 1 (ULK1) with an EC50 value of 18.94 nM, has significant implications in the study of triple-negative breast cancer (TNBC).
Targets&IC50	ULK1:18.94 nM (EC50)
In vitro	LYN-1604, identified as a potential ULK1 agonist, demonstrates enhanced enzymatic activity (195.7% at 100 nM) and exhibits a half-maximal inhibitory concentration (IC50) of 1.66 μM against MDA-MB-231 cells. It binds to the wild-type ULK1 with a nanomolar affinity (KD = 291.4 nM). At varying concentrations (0.5, 1.0, and 2.0 μM), LYN-1604 triggers cell death through the ULK complex in MDA-MB-231 cells and induces dose-dependent autophagy, evidenced by a notable increase in Beclin-1 expression, p62 degradation, and conversion of LC3-I to LC3-II. Additionally, it promotes ATG5-dependent autophagy via the ULK complex and facilitates apoptosis through increased caspase-3 cleavage. Cell viability assays and Western blot analyses further confirm these effects, showing dose-dependent induced cell death and autophagy, alongside the up-regulation of Beclin-1, degradation of p62, and LC3-I to LC3-II transformation, after a 24-hour incubation with LYN-1604.
In vivo	LYN-1604, administered intragastrically at various doses (low dose, 25 mg/kg; median dose, 50 mg/kg; high dose, 100 mg/kg) once daily for 14 days, significantly inhibits the growth of xenograft triple-negative breast cancer (TNBC) by targeting ULK1-modulated cell death, as demonstrated in an animal model using 24 female nude mice (BALB/c, 6-8 weeks, 20-22 g). The study reports no change in the body weights of mice across all doses, indicating a lack of systemic toxicity. However, a slight increase in liver and spleen weight indexes was observed in some groups, while the kidney weight index remained unaffected across all dose groups.

Molecular Weight	621.08
Formula	C33H44Cl3N3O2
CAS No.	2216753-86-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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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Keywords

LYN-1604 hydrochloride 2216753-86-3 LYN1604 Hydrochloride LYN1604 hydrochloride LYN 1604 hydrochloride LYN-1604 Hydrochloride LYN 1604 Hydrochloride inhibitor inhibit

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