Lys05 (Synonyms: Lys01 trihydrochloride)

Name: Lys05
Brand: MedChemExpress
SKU: HY-12855A
Rating: 5.0 (4 reviews)

Cat. No.: HY-12855A Purity: 99.74%: Data Sheet
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Handling Instructions
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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.

CAS No. : 1391426-24-6

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Lys05:

Lys01 Get quote

4 Publications Citing Use of MCE Lys05

ELISA

In Vivo Efficacy Study

RT-PCR

: Lys05 purchased from MedChemExpress. Usage Cited in: FASEB J. 2025 May 15;39(9):e70605. [Abstract]; Lys05 (2-5 μM; 48 h) decreased the levels of LC3 and increased the levels of p62 in senescent RCTE cells induced by IR.

: Lys05 purchased from MedChemExpress. Usage Cited in: Nat Microbiol. 2023 May;8(5):958-972. [Abstract]; Lys05 (16 mg/kg; i.c) increased the production of inflammatory cytokines in WT and Shisa9^-/- mice.

: Lys05 purchased from MedChemExpress. Usage Cited in: Nat Microbiol. 2023 May;8(5):958-972. [Abstract]; Lys05 (16 mg/kg; i.c.) increased the mortality of both WT and Shisa9^-/- mice.

: Lys05 purchased from MedChemExpress. Usage Cited in: Nat Microbiol. 2023 May;8(5):958-972. [Abstract]; Lys05 (16 mg/kg; i.c.) increased the disease score of both WT and Shisa9^-/- mice.

: Lys05 purchased from MedChemExpress. Usage Cited in: Nat Microbiol. 2023 May;8(5):958-972. [Abstract]; Lys05 (16 mg/kg; i.c.) abolished Shisa9's function in regulating the expression of IKKi-dependent genes in WT and Shisa9^-/- mice.

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Biological Activity
Protocol
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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].

MedChemExpress (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].

MedChemExpress (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

Appearance

Solid

Color

Light brown to gray

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 5.83 mg/mL (10.60 mM; Need ultrasonic)

DMSO : 5.41 mg/mL (9.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 7.5 mg/mL (13.64 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 2

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

This protocol yields a clear solution of ≥ 4.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (41.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.74%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (249 KB) HNMR (279 KB) RP-HPLC (244 KB) MS (229 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

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	[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	1.8190 mL	9.0950 mL	18.1901 mL	45.4752 mL
DMSO / H₂O	5 mM	0.3638 mL	1.8190 mL	3.6380 mL	9.0950 mL
H₂O	10 mM	0.1819 mL	0.9095 mL	1.8190 mL	4.5475 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Lys05 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lys051391426-24-6Lys01 trihydrochlorideLys 05Lys-05AutophagyInhibitorinhibitorinhibit

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Lys05 (Synonyms: Lys01 trihydrochloride)

Customer Review

Other Forms of Lys05:

Lys05 Related Antibodies

4 Publications Citing Use of MCE Lys05

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Lys05 Related Antibodies

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Complete Stock Solution Preparation Table

Lys05 Related Classifications

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