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SML2921

Sigma-Aldrich

LYN-1604 hydrochloride

≥98% (HPLC)

Synonym(e):

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

Empirische Formel (Hill-System):
C33H43Cl2N3O2 · xHCl
CAS-Nummer:
2088939-99-3
Molekulargewicht:
584.62 (free base basis)
UNSPSC-Code:
12352200
NACRES:
NA.77

Qualitätsniveau

100

Assay

≥98% (HPLC)

Form

powder

Lagerbedingungen

desiccated

Farbe

white to beige

Löslichkeit

DMSO: 2 mg/mL, clear

Lagertemp.

2-8°C

Biochem./physiol. Wirkung

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.

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Analysenzertifikate (COA)

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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
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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