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.
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- Formule: C30H32F3N3O4S
- Masse moléculaire:587.65
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
ATG4B 18.01 nM (Kd) |
In Vitro
Atg4B-IN-3 (compound a25) (2.5-10 μM; 24 h) inhibits EBSS-induced autophagy in ECA-109 and TE-1 ESCC cells, as shown by reduced LC3 puncta formation, restored p62 levels, and decreased LC3-II conversion[1].
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
Atg4B-IN-3 (5-20 mg/kg; i.p.; once every two days) dose-dependently inhibits hematogenous metastasis of esophageal squamous cell carcinoma in BALB/c nude mice, as evidenced by reduced systemic tumor burden, decreased number of lung metastatic foci, and downregulated expression levels of epithelial-mesenchymal transition markers N-cadherin and MMP-2[1].
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.
Chemical Information
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Masse moléculaire 587.65
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Atg4B-IN-3 Related Classifications
HY-184717 Related Classifications
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