Topoisomerase I/II-IN-1
Topoisomerase I/II-IN-1 is a dual inhibitor of topoisomerase I/II. Topoisomerase I/II-IN-1 induces G2/M arrest and apoptosis in cancer cells by upregulating p53, p21, and Bax mRNA levels, caspase-3 protein levels, and the Bax/Bcl-2 ratio, while downregulating Bcl-2. Topoisomerase I/II-IN-1 is useful in the study of various cancers, including melanoma, renal cancer, colorectal cancer, and breast cancer.
For research use only. We do not sell to patients.
- Formula: C33H31FN4O7
- Molecular Weight:614.62
-
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]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
Topoisomerase I |
Topoisomerase II |
Caspase 3 |
In Vitro
Topoisomerase I/II-IN-1 (Compound 5j) (10 μM) shows inhibitory effects on a variety of cancer cells: the growth inhibition rate (GI) of melanoma LOX IMVI cells was -93.46%, the GI of colorectal cancer HCT-116, HCT-15 and SW-620 cells were -59.51%, -40.12% and -43.01%, respectively, the GI of breast cancer MDA-MB-468 cells was -24.45%, and the GI of renal cancer cells 786-0, RXF 393 and UO-31 cells were -11.21%, -12.44% and -29.74%, respectively[1].
Topoisomerase I/II-IN-1 inhibits Topo I/Topo IIβ enzyme activity by 61.58%/75.51% in LOX IMVI cell lines and 56.42%/76.39% in HCT-116 colon cancer cells, respectively[1].
Topoisomerase I/II-IN-1 (24 hours) induces G2/M arrest and apoptosis in cancer cells by upregulating p53, p21, and Bax mRNA levels, cleaved caspase-3 protein levels, and the Bax/Bcl-2 ratio, and downregulating Bcl-2 in HCT-116 and LOX IMVI cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HCT-116 and LOX IMVI cells
-
Concentration:/
-
Incubation Time:24 h
-
Result:Increased the percentage of cells in pre-G1 phase to 34.27%, upregulated the percentage of cells in G2/M phase to 33.32%, and decreased the percentage of cells in S phase to 29.17% in HCT116 cells.
Increased the proportion of cells in the G2/M phase to 27.54%, and decreased the percentage of cells in the S phase to 28.58% in LOX IMVI cells.
-
Cell Line:HCT-116 and LOX IMVI cells
-
Concentration:/
-
Incubation Time:24 h
-
Result:Decreased the survival rate, which was 0.43% and 0.42%, respectively, and increased the number of necrotic cells, which was 9.22% and 4.88%, respectively, but the number of apoptotic cells was still higher than that of necrotic cells, which was 34.27% and 36.85%, respectively.
Chemical Information
-
Molecular Weight 614.62
-
Formula C33H31FN4O7
-
SMILES
O=C(C1CC=C(C(CN2CCN(CC2)C3=C(C=C4C(C(C(O)=O)=CN(C4=C3)C5CC5)=O)F)=C1)O)/C=C/C6=CC=CC([N+]([O-])=O)=C6
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
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)
Topoisomerase I/II-IN-1 Related Classifications
HY-175034 Related Classifications
Powered by Bioz