SML2921
LYN-1604 hydrochloride
≥98% (HPLC)
Synonym(s):
1-(4-(2-(2,4-Dichlorophenyl)-2-(naphthalen-2-ylmethoxy)ethyl)piperazin-1-yl)-2-(diisobutylamino)ethanone hydrochloride, 2-[bis(2-Methylpropyl)amino]-1-[4-[2-(2,4-dichlorophenyl)-2-(2-naphthalenylmethoxy)ethyl]-1-piperazinyl]-ethanone hydrochloride, UA3-02 hydrochloride
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About This Item
Empirical Formula (Hill Notation):
C33H43Cl2N3O2 · xHCl
CAS Number:
Molecular Weight:
584.62 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77
Quality Level
Assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Related Categories
Biochem/physiol Actions
LYN-1604 is a potent ULK1 (UNC-51-like kinase 1; Autophagy-related protein 1 homolog) activator (EC50 = 18.94 nM; 1.96-fold activation at 100 nM) that induces ULK complex (ULK1-mATG13-FIP200-ATG101)-dependent death in the triple-negative breast cancer (TNBC) MDA-MB-231 cultures (IC50 = 1.66 μM) involving both autophagy and apoptosis pathway effectors (e.g. ATF3, RAD21, and caspase-3). Intragastric administration is shown to suppress MDA-MB-231 xenograft tumor growth in mice in vivo (EC50 ~50 mg/kg/day on day 14). Mutagenesis and in silico docking studies identify Lys50, Leu53, and Tyr89 as important ULK1 residues that mediate LYN-1604 target site interaction.
Potent ULK1 (UNC-51-like kinase 1; hTAG1) activator with in vitro and in vivo anti-cancer efficacy against triple-negative breast cancer (TNBC) MDA-MB-231.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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Liang Ouyang et al.
Autophagy, 13(4), 777-778 (2017-02-07)
ULK1 (unc-51 like autophagy activating kinase 1) is well known to be required to initiate the macroautophagy/autophagy process, and thus activation of ULK1-modulating autophagy/autophagy-associated cell death (ACD) may be a possible therapeutic strategy in triple negative breast cancer (TNBC). Here
Shisi Ma et al.
Experimental eye research, 184, 126-134 (2019-04-25)
Dry eye disease (DED), a multifactorial ocular surface disorder affecting millions of individuals worldwide, is characterized by inflammation and damage to the ocular surface. It is unclear whether corneal autophagy participates in ocular surface inflammation observed in DED. To test
Lan Zhang et al.
Chemical science, 8(4), 2687-2701 (2017-05-30)
UNC-51-like kinase 1 (ULK1) is well-known to initiate autophagy, and the downregulation of ULK1 has been found in most breast cancer tissues. Thus, the activation of ULK1-modulated autophagy could be a promising strategy for breast cancer therapy. In this study
ULK1 and ULK2 Regulate Stress Granule Disassembly Through Phosphorylation and Activation of VCP/p97.
Bo Wang et al.
Molecular cell, 74(4), 742-757 (2019-04-14)
Disturbances in autophagy and stress granule dynamics have been implicated as potential mechanisms underlying inclusion body myopathy (IBM) and related disorders. Yet the roles of core autophagy proteins in IBM and stress granule dynamics remain poorly characterized. Here, we demonstrate
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