research use only

Lys05 Autophagy inhibitor

Name: Lys05
Brand: Selleck Chemicals
SKU: S8369
Availability: InStock
Rating: 5 (14 reviews)

Cat.No.S8369

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.

Chemical Structure

Molecular Weight: 549.75

Jump to

Quality Control

Batch: Purity: 99.93%

99.93

Related Targets	CXCR Nrf2 Mitophagy LRRK2 ULK FKBP Heme Oxygenase LC3 cGAS Cell wall
Other Autophagy Products	Resveratrol (trans-Resveratrol) Spautin-1 PIK-III DC661 Autophinib SMER28 EAD1 Flubendazole EN6 ROC-325

Solubility

In vitro
Batch:

DMSO : 9 mg/mL (16.37 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 3 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.000mg/ml (7.28mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	549.75	Formula	C₂₃H₂₃Cl₂N₅.3HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1391426-24-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CN(CCNC1=C2C=CC(=CC2=NC=C1)Cl)CCNC3=C4C=CC(=CC4=NC=C3)Cl.Cl.Cl.Cl

Mechanism of Action

Targets/IC₅₀/Ki	Autophagy
In vitro	Lys05 is water soluble salt of Lys01. This compound shows potent antitumor activity as a single agent both in vitro and in vivo in multiple human cancer cell lines and xenograft models. Lys01 and this chemical 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.
In vivo	While lower doses of Lys05 are well tolerated and associated with antitumor activity, at the highest dose tested, this compound 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 or chronic daily dosing of this chemical 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/22878685/ [2] https://pubmed.ncbi.nlm.nih.gov/22566612/ [3] https://pubmed.ncbi.nlm.nih.gov/34099621/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):