Lys05

Catalog No.S8369

Lys05 Chemical Structure

Molecular Weight(MW): 549.75

Lys05 is a new lysosomal autophagy inhibitor which potently accumulates within and deacidifies the lysosome of both cells and tumors, resulting in sustained inhibition of autophagy and tumor growth.

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Biological Activity

Description Lys05 is a new lysosomal autophagy inhibitor which potently accumulates within and deacidifies the lysosome of both cells and tumors, resulting in sustained inhibition of autophagy and tumor growth.
Targets
Autophagy [1]
()
In vitro

Lys05 is water soluble salt of Lys01. Lys05 shows potent antitumor activity as a single agent both in vitro and in vivo in multiple human cancer cell lines and xenograft models[1]. Lys01 and Lys05 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[2].

In vivo While lower doses of Lys05 are well tolerated and associated with antitumor activity, at the highest dose tested, Lys05 produces Paneth cell dysfunction and intestinal toxicity, similar to what can be observed in mice and humans with genetic defects in the autophagy gene ATG16L1. In two melanoma xenograft models and a colon cancer xenograft model, intermittent high dose Lys05 or chronic daily dosing of Lys05 at lower doses produces significant early blockade of autophagy in vivo, and has single-agent antitumor activity at doses as low as 10 mg/kg i.p. daily[1].

Protocol

Animal Research:

[1]

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  • Animal Models: Nu/Nu nude mice
  • Formulation: PBS
  • Dosages: 10 mg/kg, 40 mg/kg, or 80 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 9 mg/mL warmed (16.37 mM)
Water 3 mg/mL warmed (5.45 mM)
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 549.75
Formula

C23H23Cl2N5.3HCl

CAS No. 1391426-24-6
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Autophagy Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID