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CS1
- Soluble in DMSO
- MF: C16H12O3
- MW: 252.26
Description
CS1 is a topoisomerase IIα inhibitor with broad in vitro antitumor activity and IC50 values of 4.3 μM, 11.5 μM and 4.6 μM for proliferation inhibition in MDA-MB-231, A549 and HeLa cells, respectively. It stabilizes the Topo II/DNA complex, causing DNA damage, G2/M cell-cycle arrest and apoptosis.
Topoisomerase IIα is essential for DNA topology control and chromosome segregation and is a validated anticancer target. CS1 is useful for studying Topo II poison mechanisms and DNA damage-induced apoptotic signaling.
Key Features
- Topoisomerase IIα inhibitor
- Stabilizes the Topo II/DNA cleavage complex
- Induces DNA damage and G2/M arrest
- Shows broad antitumor activity in vitro
Applications
- Topoisomerase II pharmacology
- DNA damage response assays
- Cell-cycle arrest studies
- Cancer apoptosis and proliferation models
More Information
| Parent CAS No. | 1448009-94-6 |
|---|---|
| Chemical Name | 4-(6-hydroxynaphthalen-2-yl)benzene-1,2-diol |
| SMILES | C1(O)=CC=C(C2=CC=C3C(=C2)C=CC(O)=C3)C=C1O |
| MFCD | N.A. |
| InChi | InChI=1S/C16H12O3/c17-14-5-3-11-7-10(1-2-12(11)8-14)13-4-6-15(18)16(19)9-13/h1-9,17-19H |
| InChiKey | LDFFDYWHCCDSBO-UHFFFAOYSA-N |
| CID | 57173257 |
| Short Description | TOPO IIα inhibitor |
References
- W. Chen et al. Design and synthesis of 2-phenylnaphthalenoids as inhibitors of DNA topoisomeraseIIα and antitumor agents. Eur J Med Chem. 2014 Oct 30;86:782-96.
- Y. Shen et al. CS1 is a novel topoisomerase IIα inhibitor with favorable drug resistance profiles. Biochem Biophys Res Commun. 2014 Oct 24;453(3):302-8.
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