Home Autophagy Autophagy inhibitor IITZ-01

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IITZ-01 Autophagy inhibitor

Cat.No.S8764

IITZ-01 is a potent autophagy inhibitor, enhancing autophagosome accumulation but inhibiting autophagosomal degradation by impairing lysosomal function.
IITZ-01 Autophagy inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 482.51

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S876401 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.52%
99.52

Chemical Information, Storage & Stability

Molecular Weight 482.51 Formula

C26H23FN8O

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1807988-47-1 -- Storage of Stock Solutions

Synonyms N/A Smiles C1COCCN1C2=NC(=NC(=N2)NC3=CC=C(C=C3)F)NC4=CC=C(C=C4)C5=NC6=CC=CC=C6N5

Solubility

In vitro
Batch:

DMSO : 100 mg/mL ( (207.24 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

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Mechanism of Action

Targets/IC50/Ki
Autophagy [1]
In vitro

Treatment with IITZ-01 results in the vacuolated appearance of cells due to its specific accumulation in lysosomes. It deacidifies lysosomes and inhibits maturation of lysosomal enzymes leading to lysosomal dysfunction. This compound enhances autophagosome accumulation but inhibits autophagosomal degradation by impairing lysosomal function, finally resulting in the inhibition of autophagy. It also abolishes mitochondrial membrane potential and triggered apoptosis through the mitochondria-mediated pathway. In in-vitro screening assays, this chemical shows negligible inhibition toward PI3K γ (IC50: 2.62 μM) and no significant inhibition at 10 μM against mTORC1. Immunoblotting experiment has revealed no significant decrease in p-AKT levels in breast cancer cells when treated with this agent. It can trigger apoptosis via disrupting MMP and modulating Bcl-2 and IAP family proteins[1].
In vivo

This compound displays potent antitumor action in vivo through autophagy inhibition and apoptosis induction in MDA-MB-231 breast cancer xenograft model[1].
References

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