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Lys05

Lys05
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Purity:99.23%
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Lys05

Catalog No. T3437Cas No. 1391426-24-6
Lys05, or Lys01 trihydrochloride, is a potent, water soluble lysosomal autophagy inhibitor. Lys05 is a previously undescribed dimeric chloroquine which more potently accumulates in the lysosome and blocks autophagy compared with HCQ. Lys05 produced more potent antitumor activity as a single agent both in vitro and in vivo in multiple human cancer cell lines and xenograft models compared with HCQ. Lys05 is therefore a new lysosomal autophagy inhibitor that has potential to be developed further into a drug for cancer and other medical applications.
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Pack SizePrice/USDAvailabilityQuantity
1 mg$34In Stock
2 mg$48In Stock
5 mg$80In Stock
10 mg$122In Stock
25 mg$222In Stock
50 mg$372In Stock
100 mg$538In Stock
500 mg$1,150In Stock
1 mL x 10 mM (in DMSO)$98In Stock
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Product Introduction

Bioactivity
Description
Lys05, or Lys01 trihydrochloride, is a potent, water soluble lysosomal autophagy inhibitor. Lys05 is a previously undescribed dimeric chloroquine which more potently accumulates in the lysosome and blocks autophagy compared with HCQ. Lys05 produced more p
In vitro
Lys01 is an autophagy inhibitor significantly (10-fold) more potent than hydroxychloroquine (HCQ). Its water-soluble derivative, Lys05, demonstrates enhanced potency by more effectively accumulating in and deacidifying lysosomes compared to HCQ. Both Lys01 and its trihydrochloride version induce similar dose-dependent effects, such as an increase in the LC3II/LC3I ratio, p62 protein accumulation, and identical half-maximal inhibitory concentrations (IC50) in the MTT assay[1].
In vivo
In a study utilizing high-dose, short-term administration of lys01 trihydrochloride at 76 mg/kg intraperitoneally (i.p.), no mortality was observed in mice. However, symptoms such as arched backs and lethargy became apparent after two days of treatment. Electron microscopy (EM) revealed that in lys01 trihydrochloride-treated tumors, cells maintained intact nuclear and cytoplasmic membranes but demonstrated a significant presence of large autophagic vacuoles (AVs). This treatment markedly inhibited tumor growth, showing a substantial 53% decrease in the average daily tumor growth rate compared to tumors in vehicle-treated control mice. Furthermore, a pronounced increase in AV accumulation was noted in treated tumors—three-fold in HCQ-treated and six-fold in lys01 trihydrochloride-treated tumors—after 14 days of treatment, when compared to control-treated tumors.
Cell Research
1205Lu, c8161, LN229 and HT-29 cells are treated with lys01 trihydrochloride (0, 0.01, 0.1, 1, and 10 μM) or Lys01 (0, 0.01, 0.1, 1, and 10 μM) in five replicates for 72 h. The Acid Phsophatase Assay kit is used for the MTT assay[1].
AliasLys01 trihydrochloride
Chemical Properties
Molecular Weight549.75
FormulaC23H26Cl5N5
Cas No.1391426-24-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: 3 mg/mL(5.5 mM)
DMSO: 5.5 mg/mL (10 mM)
Solution Preparation Table
DMSO/H2O
1mg5mg10mg50mg
1 mM1.8190 mL9.0950 mL18.1901 mL90.9504 mL
5 mM0.3638 mL1.8190 mL3.6380 mL18.1901 mL
DMSO
1mg5mg10mg50mg
10 mM0.1819 mL0.9095 mL1.8190 mL9.0950 mL
20 mM0.0910 mL0.4548 mL0.9095 mL4.5475 mL
50 mM0.0364 mL0.1819 mL0.3638 mL1.8190 mL
100 mM0.0182 mL0.0910 mL0.1819 mL0.9095 mL

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