Atg4B-IN-3
Atg4B-IN-3 (compound a25) is a ATG4B inhibitor with a Kd value of 18.01 nM against the human target. Atg4B-IN-3 stably regulates the closed conformation of the loop, prevents substrates from accessing the catalytic site Cys74, and thereby inhibits the proteolytic activity of ATG4B. Atg4B-IN-3 blocks autophagic flux, reduces LC3-II levels, promotes p62 accumulation, disrupts autophagy homeostasis and enhances cell death. Atg4B-IN-3 inhibits cell proliferation, migration and clonogenic survival capacity. Atg4B-IN-3 can be used in studies related to esophageal squamous cell carcinoma.
For research use only. We do not sell to patients.
- Formula: C30H32F3N3O4S
- Molecular Weight:587.65
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
ATG4B 18.01 nM (Kd) |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:ECA-109; TE-1
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Concentration:2.5 μM, 5 μM, 10 μM
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Incubation Time:24 h
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Result:Did not significantly alter ATG4B protein levels, increased p62 accumulation, and decreased LC3-II levels in a concentration-dependent manner.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 5 weeks old, subcutaneous xenograft model via implantation of 5×106 ECA-109 cells mixed with Matrigel into the right flank)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:i.p.; every two days; 3 weeks
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Result:Exhibited dose-dependent inhibition of tumor growth.
Reduced final tumor weight and volume significantly compared to vehicle control.
Showed no significant body weight loss or pathological damage to major organs (heart, liver, spleen, lung, kidney).
Decreased Ki67 expression in tumor tissues in a dose-dependent manner.
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Animal Model:BALB/c nude (female, 6-8 weeks old, 18-20 g, hematogenous metastasis model via tail vein injection of 2×106 ECA-109-luc cells)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:i.p.; every two days
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Result:Reduced systemic tumor burden in a pronounced, dose-dependent manner compared to vehicle control.
Inhibited metastatic lung nodule formation significantly.
Downregulated N-cadherin and MMP-2 expression substantially in lung tissues.
- Mammalian live/dead viability and cytotoxicity staining
- BrdU Incorporation Assay
- Cell migration
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- Cell Cytotoxicity Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Autophagy
- Apoptosis Solutions
- Lysosome and acidic-vesicle live-cell staining
- MTT Cell Proliferation Assay
- Macroautophagy Solutions
Chemical Information
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Molecular Weight 587.65
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Formula C30H32F3N3O4S
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SMILES
O=S(C(C=C1)=CC=C1CCNCC2=C(C(OCCCC)=O)N(C3=CC=CC=C32)CC4=CC=C(C(F)(F)F)C=C4)(N)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Atg4B-IN-3 Related Classifications
HY-184717 Related Classifications
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