Home Autophagy Autophagy inhibitor Lys05 For research use only.

Lys05

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.

Lys05 Chemical Structure

Lys05 Chemical Structure

CAS No. 1391426-24-6

Purity & Quality Control

Lys05 Related Products

Signaling Pathway

Autophagy Signaling Pathways

Autophagy Signaling Pathway

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
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
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].
Animal Research Animal Models Nu/Nu nude mice
Dosages 10 mg/kg, 40 mg/kg, or 80 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 549.75 Formula

C23H23Cl2N5.3HCl
CAS No. 1391426-24-6 SDF Download Lys05 SDF
Smiles CN(CCNC1=C2C=CC(=CC2=NC=C1)Cl)CCNC3=C4C=CC(=CC4=NC=C3)Cl.Cl.Cl.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 9 mg/mL ( (16.37 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 3 mg/mL

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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