Apoptosis inducer 56
Apoptosis inducer 56 is an apoptosis inducer. Apoptosis inducer 56 induces DNA damage (upregulation of γH2AX and p-ATM expression) by minor groove binding. Apoptosis inducer 56 induces intrinsic apoptosis (upregulation of p53 and Bax/Bcl-2 ratio, cleaved caspase-7) via S-phase cell cycle arrest. Apoptosis inducer 56 shows selectivity for cancer cells over normal breast epithelial cells. Apoptosis inducer 56 can be used for the research of breast cancer.
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- CAS 番号: 952306-31-9
- 分子式: C11H17N3O3S
- 分子量:271.34
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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Caspase-7 |
Bax |
Bcl-2 |
Apoptosis inducer 56 (compound 1) (5-60 μM; 24 h) selectively induces cytotoxicity in MCF-7 human breast cancer cells with an IC50 of 21.18 μM and does not exhibit notable cytotoxicity in non-malignant MCF-10A breast epithelial cells[1].
Apoptosis inducer 56 (21.18 μM; 24 h) inhibits proliferation and colony formation, and induces S-phase cell cycle arrest in MCF-7 human breast cancer cells[1].
Apoptosis inducer 56 (21.18 μM; 24 h) induces 45% apoptosis in MCF-7 human breast cancer cells and does not induce apoptosis in non-malignant MCF-10A breast epithelial cells[1].
Apoptosis inducer 56 (21.18 μM; 24 h) induces DNA damage-mediated apoptosis, and induces mitochondrial membrane depolarization in 75.8% of MCF-7 human breast cancer cells[1].
Apoptosis inducer 56 (21.18 μM) activates the DNA damage response (upregulates γ-H2AX, p-ATM, p-Chk2) and suppresses DNA repair (downregulates p-BRCA1) in MCF-7 human breast cancer cells[1].
Apoptosis inducer 56 (21.18 μM; 24 h) induces mitochondria-dependent apoptosis in MCF-7 human breast cancer cells via upregulation of pro-apoptotic proteins, cytochrome c release, caspase activation, and PARP cleavage[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 human breast cancer cells, MCF-10A non-malignant breast epithelial cells
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Concentration:5, 10, 20, 40, 60 μM
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Incubation Time:24 h
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Result:Induced cytotoxicity in MCF-7 cells with an IC₅₀ of 21.18 ± 2.01 μM; maintained >70% viability in MCF-10A cells across 5, 10, 20, 40, 60 μM.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:21.18 μM
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Incubation Time:24 h
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Result:Reduced cell proliferation from 83.1% (control) to 66.3%.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:21.18 μM
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Incubation Time:24 h
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Result:Increased S-phase cell accumulation from 17.4% (control) to 30.1%.
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Cell Line:MCF-7 human breast cancer cells, MCF-10A non-malignant breast epithelial cells
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Concentration:21.18 μM
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Incubation Time:24 h
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Result:Induced 45% apoptosis in MCF-7 cells compared to 2.62% in the control group; maintained 95.8% viability in MCF-10A cells after 24 h treatment.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:21.18 μM
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Incubation Time:24 h
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Result:Caused a substantial increase in TUNEL-positive cells (green fluorescence) compared to the untreated group.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:21.18 μM
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Incubation Time:24 h
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Result:Upregulated pro-apoptotic Bim and Bax; downregulated anti-apoptotic Bcl2 and Bcl-xL; elevated p53; suppressed survivin; induced cytochrome c release from mitochondria to cytoplasm; upregulated Apaf-1; activated caspase-7 and caspase-9 via cleavage; induced PARP cleavage.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice (adult female, 25-28 g)[1]
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Dosage:1, 2.5, 5, 10 mg/kg
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Administration:p.o.; daily; 28 days
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Result:Detected no significant adverse effects on liver, renal, biochemical, or hematological parameters; observed no treatment-related behavioral deviations; maintained stable body weights across all dose groups; showed no structural abnormalities in liver and kidney tissues via histopathological analysis.
化学情報
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CAS 番号 952306-31-9
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分子量 271.34
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分子式 C11H17N3O3S
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SMILES
O=C(CCCCCCC(NO)=O)NC1=NC=CS1
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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)