Castalin
Castalin is a polyphenolic anticancer compound isolated and identified from the bark or nut shells of Castanea sativa Mill. Castalin induces DNA damage by increasing ROS to activate CHK1, while recruiting 53BP1/RIF1 and activating DNA-PKcs to initiate the NHEJ pathway for DNA repair. Castalin can be used in research related to cervical cancer and breast cancer.
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。
- CAS 番号: 19086-75-0
- 分子式: C27H20O18
- 分子量:632.44
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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
製品説明
IC50 & Target
[1]|
Chk1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
25.13 μg/mL
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Cytotoxicity against human cervix adenocarcinoma HeLa cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay.
Cytotoxicity against human cervix adenocarcinoma HeLa cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay.
|
41009002 |
| MCF7 | IC50 |
16.1 μg/mL
|
Cytotoxicity against hormone-dependent human breast carcinoma MCF-7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay.
Cytotoxicity against hormone-dependent human breast carcinoma MCF-7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay.
|
41009002 |
| MDA-MB-231 | IC50 |
5.2 μg/mL
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Cytotoxicity against triple-negative human breast cancer MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay.
Cytotoxicity against triple-negative human breast cancer MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay.
|
41009002 |
体外実験
Castalin (62-124 µg/mL; 1-6 h) induces dose- and time-dependent DNA double-strand breaks in HeLa cells, and this effect is detectable via γH2AX foci[2].
Castalin (124 μg/mL; 3 h, followed by elution and recovery for 12-24 h) exerts an effect in HeLa cells that reduces γH2AX foci over time after elution, indicating the initiation of DNA repair[2].
Castalin (31-124 μg/mL; 3 h) modulates transcriptional programs, downregulates homologous recombination-related genes, and upregulates tumor microenvironment-related pathways in HeLa cells. When combined with SRA737 (1 μM), it exerts a stronger effect on upregulating the phosphorylation level of CHK1 S345 than either agent used alone[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa, MCF-7 cells
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Concentration:7.7, 15.5, 31, 62, 124 μg/mL
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Incubation Time:72 h
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Result:Decreased the viability of tumor cells in a dose-dependent manner.
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Cell Line:MDA-MB-231 cells
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Concentration:0.5, 1, 2, 4, 8 μg/mL
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Incubation Time:72 h
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Result:Strongly decreased the viability of the triple-negative breast cancer cell line in a dose-dependent manner.
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Cell Line:HeLa cells
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Concentration:62, 84, 124 μg/mL
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Incubation Time:1, 3, 6 h
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Result:Increased the formation of intracellular γH2AX foci in a dose- and time-dependent manner, inducing DNA damage.
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Cell Line:HeLa cells
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Concentration:31, 62, 124 μg/mL
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Incubation Time:3 h
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Result:Dose-dependently increased the phosphorylation activation of the key checkpoint kinase CHK1 at Ser345.
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Cell Line:HeLa cells
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Concentration:124 µg/mL
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Incubation Time:3 h
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Result:Significantly increased the number of 53BP1 and RIF1 foci involved in the Non-Homologous End Joining (NHEJ) repair pathway, and significantly up-regulated the phosphorylation of DNA-PKcs at S2056.
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Cell Line:HeLa cells
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Concentration:124 μg/mL
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Incubation Time:1, 2, 3 h
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Result:Failed to induce the phosphorylation of RPA32, a marker of the Homologous Recombination (HR) repair pathway.
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Cell Line:HeLa, MCF-7, MDA-MB-231 cells
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Concentration:7.7 μg/mL (combined with SRA737: 0.06, 0.125, 0.25, 0.5, 1 μM)
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Incubation Time:72 h
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Result:Significantly enhanced the cytotoxic effect of the CHK1 inhibitor SRA737, synergistically decreasing the survival rate of the three cancer cell lines compared to monotherapy.
化学情報
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CAS 番号 19086-75-0
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分子量 632.44
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分子式 C27H20O18
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SMILES
OC(C(O1)C2[C@@]([H])(O)C3=C(O)C(O)=C(O)C4=C3C(O2)=O)C(CO)OC(C5=CC(O)=C(O)C(O)=C5C6=C(O)C(O)=C(O)C4=C6C1=O)=O
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Structure Classification
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Initial Source
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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)