1. Autophagy
  2. Autophagy
  3. Lys05

Lys05 (Synonyms: Lys01 trihydrochloride)

Cat. No.: HY-12855A Purity: 98.06%
Handling Instructions

Lys05 (Lys01 trihydrochloride) is a novel lysosomal autophagy inhibitor with IC50 values of 3.6, 3.8, 6 and 7.9 μM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay.

For research use only. We do not sell to patients.

Lys05 Chemical Structure

Lys05 Chemical Structure

CAS No. : 1391426-24-6

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10 mM * 1 mL in DMSO USD 121 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Lys05 (Lys01 trihydrochloride) is a novel lysosomal autophagy inhibitor with IC50 values of 3.6, 3.8, 6 and 7.9 μM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay.

IC50 & Target

IC50: 3.6 μM (1205Lu), 3.8 μM (c8161), 6 μM (LN229), 7.9 μM (HT-29)[1]

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 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

With this high-dose, short-term treatment, no mice die, but after 2 d of dosing, mice treated with Lys05 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 Lys05-treated tumors. Tumor growth is significantly impaired in Lys05-treated tumors compared with controls. Lys05 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 Lys05-treated tumors, respectively, compared with control-treated tumors[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

549.75

Formula

C₂₃H₂₆Cl₅N₅

CAS No.

1391426-24-6

SMILES

CN(CCNC1=CC=NC2=C1C=CC(Cl)=C2)CCNC3=CC=NC4=CC(Cl)=CC=C43.[H]Cl.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (45.48 mM; ultrasonic and adjust pH to 2 with HCl)

H2O : 6.4 mg/mL (11.64 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8190 mL 9.0950 mL 18.1901 mL
5 mM 0.3638 mL 1.8190 mL 3.6380 mL
10 mM 0.1819 mL 0.9095 mL 1.8190 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 4.17 mg/mL (7.59 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.55 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 7.5 mg/mL (13.64 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

1205Lu, c8161, LN229 and HT-29 cells are treated with Lys05 (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: To investigate the safety of Lys05 and its in vivo effects on autophagy, c8161 xenografts matched for tumor size are treated with i.p. daily PBS, or equimolar doses of HCQ or Lys05 [HCQ 60 mg/kg (138 nM/g), Lys05 76 mg/kg (138 nM/g)] for 48 h[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 98.06%

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Keywords:

Lys05Lys01 trihydrochlorideLys 05Lys-05AutophagyInhibitorinhibitorinhibit

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