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.
For research use only. We do not sell to patients.
- CAS No.: 19086-75-0
- Formula: C27H20O18
- Molecular Weight:632.44
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Chk1 |
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Cell Line
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Type | Value | Description | References |
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| 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 |
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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Molecular Weight 632.44
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Castalin Related Classifications
HY-N21945 Related Classifications
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