Atg4B activator-1
Atg4B activator-1 (Compound 16a) is an allosteric, selective, and orally active ATG4B activator with a Kd of 0.2199 μM. Atg4B activator-1 binds to the allosteric pocket of ATG4B and induces conformational changes. Atg4B activator-1 induces Autophagy. Atg4B activator-1 inhibits the proliferation and migration of triple-negative breast cancer cells. Atg4B activator-1 can be used in studies related to triple-negative breast cancer.
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- CAS 番号: 3126601-01-9
- 分子式: C25H22ClFN2O2
- 分子量:436.91
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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ATG4B 0.2199 μM (Kd) |
Atg4B activator-1 activates the activity of recombinant human ATG4B protease in a concentration-dependent manner in in vitro assays, with a Kd of 2.199×10-7 M[1].
Atg4B activator-1 (24 h) potently inhibits the viability of various triple-negative breast cancer cell lines, and exhibits the strongest activity against MDA-MB-231 cells after 24 h of treatment (IC50 = 1.81 ± 0.95 μM)[1].
Atg4B activator-1 (1-2 μM; 0-48 h) inhibits the migratory wound healing of MDA-MB-231 cells within 48 h in a concentration-dependent manner[1].
Atg4B activator-1 (1-4 μM) induces autophagy in a concentration-dependent manner in MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231
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Concentration:1, 2, 4 μM
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Incubation Time:24 h for Immunofluorescence assay
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Result:Increased LC3 puncta intensity.
Increased LC3-II protein levels.
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, 5-6 weeks old, triple-negative breast cancer model via subcutaneous inoculation of MDA-MB-231 cells)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:i.p.; once every two days; 14 days
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Result:Achieved 49.2% tumor growth inhibition at 5 mg/kg, 72.2% at 10 mg/kg, and 86.3% at 20 mg/kg relative to control.
Significantly reduced tumor weight in all treatment groups, with the greatest reduction in the 20 mg/kg group.
Showed no significant changes in mouse body weight across treatment groups.
Upregulated E-cadherin, downregulated MMP-2, and increased LC3-II levels in tumor tissue.
Caused no pathological lesions in heart, liver, spleen, lung, and kidney via hematoxylin-eosin staining.
Markedly reduced Ki-67 positive nuclei in the 20 mg/kg group, indicating suppressed tumor cell proliferation.
化学情報
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CAS 番号 3126601-01-9
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分子量 436.91
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分子式 C25H22ClFN2O2
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SMILES
FC1=CC(Cl)=C(COC2=C(OC)C=C(CNCC3=CC=CC4=C3N=CC=C4)C=C2)C=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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 activator-1 関連分類
HY-181936 関連分類
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