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.
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- CAS No.: 19086-75-0
- Formule: C27H20O18
- Masse moléculaire:632.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Activité biologique
Description
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.
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41009002 |
| MCF7 | IC50 |
16.1 μg/mL
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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.
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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.
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41009002 |
In Vitro
Castalin (0.5-124 µg/mL; 72 h) induces dose-dependent cytotoxicity in HeLa, MCF-7 and MDA-MB-231 cancer cell lines, with IC50 values of 25.13 µg/mL, 16.1 µg/mL and 5.2 µg/mL, respectively[2].
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].
Castalin (31-124 μg/mL; 1-3 h) induces phosphorylation of CHK1 kinase at Ser345, triggers reactive oxygen species (ROS) production, significantly increases the number of 53BP1 and RIF1 foci, upregulates phosphorylation of DNA-PKcs at S2056, and does not induce phosphorylation of RPA32 protein[2].
Combination treatment with Castalin (7.7 μg/mL; 6-72 h) and 1 μM SRA737 (HY-18958) synergistically enhances the cytotoxicity of CHK1 inhibitors and induces mitotic arrest in HeLa, MCF-7 and MDA-MB-231 cells.
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.
Chemical Information
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CAS No. 19086-75-0
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Masse moléculaire 632.44
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Castalin Related Classifications
HY-N21945 Related Classifications
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