CAA-0225
CAA-0225 is a tissue protease L inhibitor that inhibits rat liver tissue protease L with a IC50 value of 1.9 nM. CAA-0225 can participate in the degradation of autophagosome membrane markers LC3-II and GABARAP (HY-P72639), improve cardiac function in mice with reperfusion injury, and kill and eliminate Trypanosoma brucei parasites[1][2][3].
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- CAS 番号: 244072-26-2
- 分子式: C28H29N3O5
- 分子量:487.55
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Cathepsin アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
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cathepsin L |
体外実験
CAA-0225 (10 mg/mL, 4 h) acts as a probe for autophagic protein hydrolysis by specifically inhibiting the involvement of protease L in the degradation of autophagosome membrane markers LC3-II and GABARAP[1]. CAA-0225 (0-100 μM, 48 h) kills Trypanosoma brucei parasite by inhibiting tissue protease L[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HeLa、Huh-7 cells
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Concentration:10 mg/mL
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Incubation Time:4 h
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Result:Inhibited the degradation of microtubule associated protein IA/IB light chain 3-II (LC3-II) and gamma aminobutyric acid (A) receptor associated protein (GABARAP)-II
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Cell Line:Bloodstream forms of T. brucei clone 427–221a
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Concentration:0-100 μM
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Incubation Time:48 h
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Result:Inhibited the growth of trypanosomes in a dose-dependent manner with GI50 values of 0.33 μM, respectively
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Model of reperfusion injury involved male C57Bl/6 mice aged 9–12 weeks[2].
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Dosage:0.25 mg
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Administration:Intravenous injection (i.v.)
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Result:Reduced infarct size, improved systolic and diastolic cardiac function.
化学情報
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CAS 番号 244072-26-2
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分子量 487.55
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分子式 C28H29N3O5
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SMILES
O=C([C@H]1O[C@@H]1C(N[C@@H](CC2=CC=CC=C2)C(NCC3=CC=CC=C3)=O)=O)NCCC4=CC=C(O)C=C4
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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.
プロトコル
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Autophagy
Autophagy is a process in which eukaryotic cells use lysosomes to degrade their own cytoplasmic proteins and damaged organelles under the regulation of autophagy related gene (Atg). Microtubule-associated proteins light chain 3 (LC3) is recognized as autophagy marker, which transfers from cytoplasmic LC3 (LC3-I) to membrane type (LC3-II). LC3-II/I ratio could be detected by Western Blot and fluorescence microscopy.
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Macroautophagy Solutions
Macroautophagy is a conserved lysosome-dependent degradation pathway in which cytoplasmic material is sequestered into double-membrane autophagosomes and delivered to lysosomes for degradation and recycling. The pathway supports cellular homeostasis during nutrient limitation, organelle stress, protein-aggregate accumulation, infection, differentiation, and tissue remodeling by coupling cargo sequestration, autophagosome maturation, lysosomal fusion, and degradation of cargo-derived macromolecules. The core molecular sequence includes initiation by nutrient- and stress-regulated autophagy machinery, autophagosome nucleation, LC3/ATG8-family conjugation to autophagosomal membranes, cargo selection through receptors such as SQSTM1/p62, autophagosome-lysosome fusion, and lysosomal degradation. LC3 was identified as a mammalian homolog of yeast Atg8 that localizes to autophagosomal membranes after processing, and p62/SQSTM1 was shown to connect ubiquitinated cargo with autophagic degradati
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)