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Lys05

Catalog No. T3437   CAS 1391426-24-6
Synonyms: Lys01 trihydrochloride

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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Lys05, CAS 1391426-24-6
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
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 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.
Targets&IC50 HT-29:7.9 μM, c8161:3.8μM, LN229:6μM, 1205Lu:3.6μM
In vitro Lys01, is a 10-fold more potent autophagy inhibitor than HCQ. Compared with HCQ, Lys05, a water-soluble salt of Lys01, more potently accumulates within and deacidifies the lysosome. Lys01 and lys01 trihydrochloride produce equivalent dose-dependent increases in the LC3II/LC3I ratio, accumulation of the autophagy cargo protein p62, and identical IC50 values in the MTT assay[1].
In vivo With this high-dose, short-term treatment, no mice die, but after 2 d of dosing, mice treated with lys01 trihydrochloride 76 mg/kg i.p. are observed to have arched backs and lethargy. Morphologically, EM show that cells with intact nuclear and cytoplasmic membranes contain large AVs in lys01 trihydrochloride-treated tumors. Tumor growth is significantly impaired in lys01 trihydrochloride-treated tumors compared with controls. Lys01 trihydrochloride treatment results in a 53% reduction in the average daily tumor growth rate compared with vehicle-treated controls. A significant three- and six-fold accumulation of AV is observed at the end of 14 d of treatment in HCQ- and lys01 trihydrochloride-treated tumors, respectively, compared with control-treated tumors[1].
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].
Synonyms Lys01 trihydrochloride
Molecular Weight 549.75
Formula C23H26Cl5N5
CAS No. 1391426-24-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: <1 mg/mL

H2O: 3 mg/mL(5.5 mM)

DMSO: 6.4 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. McAfee Q, et al. Autophagy inhibitor Lys05 has single-agent antitumor activity and reproduces the phenotype of a genetic autophagy deficiency. Proc Natl Acad Sci U S A. 2012 May 22;109(21):8253-8.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Autophagy Compound Library Inhibitor Library Anti-Cancer Active Compound Library Anti-COVID-19 Compound Library Anti-Aging Compound Library Bioactive Compound Library

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Keywords

Lys05 1391426-24-6 自噬 Autophagy lysosomal autophagy Inhibitor Lys-05 inhibit Lys 05 Lys01 trihydrochloride inhibitor