Home Autophagy Autophagy inhibitor IITZ-01 For research use only.

IITZ-01

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

IITZ-01 Chemical Structure

IITZ-01 Chemical Structure

CAS: 1807988-47-1

Selleck's IITZ-01 has been cited by 1 publication

Purity & Quality Control

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

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Biological Activity

Description IITZ-01 is a potent autophagy inhibitor, enhancing autophagosome accumulation but inhibiting autophagosomal degradation by impairing lysosomal function.
Targets
Autophagy [1]
In vitro
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. IITZ-01 enhances autophagosome accumulation but inhibit 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, IITZ-01 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 IITZ-01. IITZ-01 can trigger apoptosis via disrupting MMP and modulating Bcl-2 and IAP family proteins[1].
Cell Research Cell lines MDA-MB-231 cells
Concentrations 0.125-2 µM
Incubation Time 24 h
Method

MDA-MB-231 cells were treated with the designated concentrations (0.125-2 µM) of IITZ-01 and IITZ-02 for 24 h or 2 µM of IITZ-01 for specific time periods 3, 6, 12, 18, and 24 h. The protein expression levels of SQSTM1 were measured by western blotting experiment.
In Vivo
In vivo

IITZ-01 displays potent antitumor action in vivo through autophagy inhibition and apoptosis induction in MDA-MB-231 breast cancer xenograft model[1].
Animal Research Animal Models MDA-MB-231/green fluorescent protein (GFP) orthotropic breast cancer xenografts (developed in CrTac:NCr-Foxnnu BALB/c female nude mice)
Dosages 45 mg/kg every alternate day
Administration i.p.

Chemical Information & Solubility

Molecular Weight 482.51 Formula

C26H23FN8O
CAS No. 1807988-47-1 SDF --
Smiles C1COCCN1C2=NC(=NC(=N2)NC3=CC=C(C=C3)F)NC4=CC=C(C=C4)C5=NC6=CC=CC=C6N5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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