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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C30H32F3N3O4S
- 分子量:587.65
-
保管条件:
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]
-
生物活性
-
化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
ATG4B 18.01 nM (Kd) |
体外実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:ECA-109; TE-1
-
Concentration:2.5 μM, 5 μM, 10 μM
-
Incubation Time:24 h
-
Result:Did not significantly alter ATG4B protein levels, increased p62 accumulation, and decreased LC3-II levels in a concentration-dependent manner.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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]
-
Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
-
Administration:i.p.; every two days; 3 weeks
-
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.
-
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]
-
Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
-
Administration:i.p.; every two days
-
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
化学情報
-
分子量 587.65
-
分子式 C30H32F3N3O4S
-
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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Atg4B-IN-3 関連分類
HY-184717 関連分類
Powered by Bioz