HsClpP activator-2
HsClpP activator-2 is an orally active HsClpP agonist with a KD of 40 nM. HsClpP activator-2 potently inhibits SCLC cells including H69 (IC50 = 0.17 μM) and H82 (IC50 = 0.19 μM). HsClpP activator-2 disrupts mitochondrial membrane potential (MMP), as well as induces apoptosis and ROS in H82 cells. HsClpP activator-2 significantly inhibits tumor growth in non-SMC xenograft models with a tumor growth inhibition. HsClpP activator-2 can be used for the study of small cell lung carcinoma (SCLC).
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- 分子式: C29H26F3N3O2
- 分子量:505.53
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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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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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HsClpP 40 nM (Kd) |
HsClpP activator-2 (Compound 8o) (0.02-10 μM, 72 h) shows potent antiproliferative activity against H69, H82, and non-SMC cells, with IC50 values of 0.17 μM, 0.19 μM, and 0.1 μM, respectively[1].
HsClpP activator-2 (100-400 nM, 72 h) induces dose-dependent degradation of mitochondrial OXPHOS complex proteins (NDUFB8, SDHB, UQCRC2, MTCO1, ATP5A) in H82 cells[1].
HsClpP activator-2 (100-400 nM, 72 h) significantly reduces intracellular ATP levels and increases ROS levels in H82 cells in a dose-dependent manner[1].
HsClpP activator-2 (100-400 nM, 48-72 h) disrupts mitochondrial membrane potential (MMP) and induces apoptosis in H82 cells[1].
HsClpP activator-2 (100-400 nM, 24-48 h) inhibits colony formation and migration of non-SMC cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H82 cells
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Concentration:100, 200, 400 nM
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Incubation Time:72 h
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Result:Induced dose-dependent degradation of mitochondrial OXPHOS complex proteins (NDUFB8, SDHB, UQCRC2, MTCO1, ATP5A) in H82 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Non-SMC cells (1×106 cells) were subcutaneously implanted into the flanks of 6-8-week-old male BALB/c nude mice (18-22 g)[1]
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Dosage:1.3, 2.5, 5 mg/kg
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Administration:i.p., twice weekly, 20 days
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Result:Achieved tumor growth inhibition (TGI) rates of 37.03%, 49.12%, and 60.44% for tumor weight, as well as 41.93%, 50.08%, and 63.01% for tumor volume at doses of 1.3, 2.5, and 5 mg/kg, respectively.
Showed no significant changes in body weight and no pathological damage in major organs (heart, liver, spleen, lung, kidney).
Reduced the Ki67 expression.
Increased the Caspase 3 expression in tumor.
化学情報
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分子量 505.53
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分子式 C29H26F3N3O2
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SMILES
O=C(C1=C(C2=CC=C(CO)C=C2)CCN(CC3=CC=CC(C#N)=C3)C1)NCC4=CC=C(C(F)(F)F)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.
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)
HsClpP activator-2 関連分類
HY-175757 関連分類
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