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SML2921

Sigma-Aldrich

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:
2088939-99-3
Molecular Weight:
584.62 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

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.

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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
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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