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SML2097

Sigma-Aldrich

Lys05

≥98% (HPLC)

Synonym(s):

Lys-01 3HCl, Lys-05, Lys01 3HCl, N-(7-Chloroquinolin-4-yl)-N′-[2-[(7-chloroquinolin-4-yl)amino]ethyl]-N′-methylethane-1,2-diamine trihydrochloride, N1-(7-Chloroquinolin-4-yl)-N2-[2-[(7-chloroquinolin-4-yl)amino]ethyl]-N2-methylethane-1,2-diamine trihydrochloride, PS-1001, PS1001

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About This Item

Empirical Formula (Hill Notation):
C23H23Cl2N5 · 3HCl
CAS Number:
1391426-24-6
Molecular Weight:
549.75
UNSPSC Code:
12352200
NACRES:
NA.77

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

Application

Lys05 has been used as an autophagy inhibitor to study its interactions with piperazine. It has also been used as a lysosomal inhibitor to study its effects on myogenesis in Gallus gallus.

Biochem/physiol Actions

Lys05 (Lys01 trihydrochloride) is a dimeric chloroquine (CQ) that deacidifies the lysosome and causes impairment of lysosomal enzymes, exhibiting more than 10-fold higher autophagy inhibitory potency than hydroxychloroquine (HCQ) and CQ (LC3II/LC3I ratio = 15.4 post 4 hr 10 μM treatment in LN229 glioblastoma cells vs. <6.4 with 100 μM CQ or HCQ). Lys05 also shows higher anticancer activity both in vitro (IC50 3.6-6.0 μM vs. 15.6-23.8 μM with HCQ in 1205Lu, c8161, LN229, HT-29 cultures) and in mice in vivo (EC50 in reducing tumor growth rate ∼10 mg/kg/day i.p.; HT29 xenografts) with toxicity observed only at high doses (≥80 mg/kg) as a result of significant lysozyme reduction.

Storage Class Code

11 - Combustible Solids

WGK

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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Kayo M Bagri et al.
BioMed research international, 2020, 6404230-6404230 (2020-07-21)
Lysosomes and acidic compartments are involved in breaking down of macromolecules, membrane recycling, and regulation of signaling pathways. Here, we analyzed the role of acidic compartments during muscle differentiation and the involvement of the Wnt/beta-catenin pathway in lysosomal function during
Valentina Sica et al.
Cell reports, 27(3), 820-834 (2019-04-18)
Inhibition of oxidative phosphorylation (OXPHOS) by 1-cyclopropyl-4-(4-[(5-methyl-3-(3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl)-1H-pyrazol-1-yl)methyl]pyridin-2-yl)piperazine (BAY87-2243, abbreviated as B87), a complex I inhibitor, fails to kill human cancer cells in vitro. Driven by this consideration, we attempted to identify agents that engage in synthetically lethal interactions with B87. Here, we

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