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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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Lys05, CAS 1391426-24-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 48.00
5 mg	In stock	$ 80.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 222.00
50 mg	In stock	$ 372.00
100 mg	In stock	$ 538.00
500 mg	In stock	$ 1,150.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 99.23%

Purity: 99.13%

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	HT29 cells:7.9 μM, LN229:6μM, 1205Lu:3.6μM, C8161 cells:3.8μM
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].

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 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), Sonification is recommended

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：

Inhibitor Library Anti-Cancer Active Compound Library NO PAINS Compound Library Anti-Cancer Compound Library Autophagy Compound Library Anti-COVID-19 Compound Library Bioactive Compounds Library Max Bioactive Compound Library Anti-Aging Compound Library

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Keywords

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

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