Topoisomerase I-IN-21
Topoisomerase I-IN-21 is a promising topoisomerase I inhibitor with an IC50 of 18.79 μM. Topoisomerase I-IN-21 shows higher selectivity toward cancer cells over normal CD8+ cells. Topoisomerase I-IN-21 induces G0/G1 cell cycle arrest and apoptosis. Topoisomerase I-IN-21 activates the cGAS-STING pathway, leading to enhanced immune gene expression. Topoisomerase I-IN-21 can be used for research on leukemia, non-small-cell lung, colon, central nervous system, melanoma, ovarian, renal, prostate, and breast cancers.
For research use only. We do not sell to patients.
- Formula: C29H23ClN2O4S
- Molecular Weight:531.02
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Topoisomerase Isoforms
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Biological Activity
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Topoisomerase I 18.79 μM (IC50) |
Topoisomerase I-IN-21 (compound 5c) (0.01-100 μM) exhibits IC50s ranged from 0.01 μM to 100 μM and mean graph midpoint values for growth inhibition of 0.04 in NCI-60 human cancer cell lines[1].
Topoisomerase I-IN-21 (0.01-100 μM) exhibits IC50s of 1.397 μM and 70.58 μM in SR leukemia cells and PCS-800-017 normal cell line, respectively[1].
Topoisomerase I-IN-21 (1-100 μM; 45 min) exhibits Topo I inhibitory activity in a concentration-dependent manner[1].
Topoisomerase I-IN-21 (18.79 μM; 24 h) induces cell cycle arrest and induces apoptosis in SR Leukemia cells[1].
Topoisomerase I-IN-21 (10 μg/mL; 24 h) significantly elevates the concentration levels of STING, INF-β, TNF-α, Bax and CASP3 in SR leukemia cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SR leukemia cells
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Concentration:10 μg/mL
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Incubation Time:24 h
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Result:Increased the expression of cGAS and IRF-3 compared to control cells.
Downregulated XIAP and IκB-α levels compared to control cells.
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Cell Line:SR leukemia cells
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Concentration:18.79 μM
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Incubation Time:24 h
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Result:Arrested cell cycle at the G0/G1 phase.
Chemical Information
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Molecular Weight 531.02
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Formula C29H23ClN2O4S
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SMILES
N#CC1=C(/N=C/C2=CC=C(Cl)C=C2)OC(C3=CC=CC(C)=C3S4)=C4C1C5=CC(OC)=C(OC)C(OC)=C5
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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)