Topoisomerase ll/ME-1-IN-1
Topoisomerase ll/ME-1-IN-1 (Compound 7a) is a Topoisomerase ll and ME-1 inhibitor with an IC50 of 5.03 μM against Topoisomerase ll. Topoisomerase ll/ME-1-IN-1 functionally inhibits the activity of Topoisomerase II and functionally blocks the activity of ME-1. Topoisomerase ll/ME-1-IN-1 induces Autophagy by upregulating the expression of Beclin-1 and LC3-II. Topoisomerase ll/ME-1-IN-1 promotes Apoptosis. Topoisomerase ll/ME-1-IN-1 exhibits antiproliferative activity against breast cancer cells and shows no toxicity to normal mammary epithelial cells. Topoisomerase ll/ME-1-IN-1 can be used in studies related to breast cancer (including triple-negative breast cancer).
For research use only. We do not sell to patients.
- Formula: C20H19N3OS
- Molecular Weight:349.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
Topoisomerase II 5.03 μM (IC50) |
In Vitro
Topoisomerase II/ME-1-IN-1 (48 h) potently inhibits the proliferation of MCF-7 and MDA-MB-231 breast cancer cells, with IC50 values of 3.1 ± 0.17 μM and 1.04 ± 0.07 μM, respectively, while exhibits low activity against normal MCF-10A cells[1].
Topoisomerase II/ME-1-IN-1 induces autophagy in MCF-7 and MDA-MB-231 cells by upregulating the expression of Beclin-1 and LC3-II, with the level of LC3-II in MDA-MB-231 cells reaching 1852.448 ± 48.193 ng/mg proteins[1].
Topoisomerase II/ME-1-IN-1 (at IC50 concentration) induces apoptosis in MCF-7 and MDA-MB-231 cells via the mitochondrial pathway, upregulates the expression of Bax, cleaved PARP-1 and caspase-9, downregulates the expression of Bcl-2, and causes cell cycle arrest; among these cells, the early apoptosis rate of MCF-7 cells is 24.61%, and that of MDA-MB-231 cells is 18.28%[1].
Topoisomerase II/ME-1-IN-1 potently inhibits topoisomerase II with an IC50 of 5.03 ± 0.163 μM[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, MDA-MB-231 human breast cancer cells
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Concentration:IC50 concentration
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Incubation Time:No specific explanation
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Result:Induced early apoptosis in 24.61% of MCF-7 cells.
Induced early apoptosis in 18.28% of MDA-MB-231 cells.
Increased Bax protein to 21.04 ± 0.918 ng/mg proteins in MCF-7 cells.
Increased Bax protein to 19.75 ± 0.725 ng/mg proteins in MDA-MB-231 cells.
Decreased Bcl-2 protein to 39.85 ± 1.76 ng/mg proteins in MCF-7 cells.
Decreased Bcl-2 protein to 46.51 ± 1.62 ng/mg proteins in MDA-MB-231 cells.
Increased cleaved PARP-1 to 9.517 ± 1.995 ng/mg proteins in MDA-MB-231 cells.
Increased caspase-9 to 10.26 ± 0.607 ng/mg proteins in MCF-7 cells.
Increased caspase-9 to 8.42 ± 0.583 ng/mg proteins in MDA-MB-231 cells.
Caused G0-G1 and S phase cell cycle arrest in MCF-7 cells.
Caused S phase arrest in MDA-MB-231 cells.
Chemical Information
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Molecular Weight 349.45
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Formula C20H19N3OS
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SMILES
O=C(CS/1)NC1=N/N=C/C2=C3C=CC(CCC4=CC=C(CC3)C=C4)=C2
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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)
Topoisomerase ll/ME-1-IN-1 Related Classifications
HY-182054 Related Classifications
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