Lss-11
Lss-11 is a topoisomerase inhibitor. LSS-11 enhances cell death in cancer cells by inducing apoptosis through increasing the DR5 protein level and PARP1 cleavage. LSS-11 dose-dependently reduces STAT3 phosphorylation, downregulates its target genes MDR1 and MRP1, reduces P-gp protein expressionwithout affecting P-gp transport function. Lss-11 is a chemosensitizer and shows synergistic anticancer effect with Paclitaxel (HY-B0015). Lss-11 can be used for the research of paclitaxel-resistant lung cancer.
For research use only. We do not sell to patients.
- CAS No.: 1392014-36-6
- Formula: C21H27N7O2
- Molecular Weight:409.48
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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
All Topoisomerase Isoforms
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Biological Activity
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STAT3 |
PARP1 |
Lss-11 (0.5-2 μM; 72 h) has an IC50 of 6.87 μM in Paclitaxel (HY-B0015)-resistant A549/T lung cancer cells and >10 μM in Paclitaxel-sensitive A549 lung cancer cells, and synergizes with Paclitaxel to reduce A549/T cell viability[1].
Lss-11 (0.5 μM; 6-24 h) increases the percentage of apoptotic Paclitaxel-resistant A549/T lung cancer cells in a time-dependent manner, reaching 16.50% after 24 h of treatment[1].
Lss-11 (0.5-2 μM; 24 h) increases DR5 and cleaved PARP1 protein levels without altering Bax or Bcl2 levels, and reduces MRP1 protein levels, in Paclitaxel-resistant A549/T lung cancer cells[1].
Lss-11 (0.5-2 μM; 24 h) reduces phosphorylated STAT3 protein levels while increasing total STAT3 protein levels in Paclitaxel-resistant A549/T lung cancer cells, with p-STAT3 reduction strongly correlated with MDR1 and MRP1 downregulation[1].
Lss-11 (0.5-2 μM; 24 h) significantly downregulates MDR1 and MRP1 mRNA levels in Paclitaxel-resistant A549/T lung cancer cells[1].
Lss-11 (0.5-2 μM; 24 h) reduces P-gp protein expression in Paclitaxel-resistant A549/T lung cancer cells[1].
Lss-11 (24 h) hinders the binding of STAT3 to the MDR1 and MRP1 promoters in paclitaxel-resistant A549/T lung cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:paclitaxel-resistant A549/T lung cancer cells
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Concentration:0.5 μM
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Incubation Time:6 h, 24 h
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Result:Increased the percentage of Annexin V+/PI+ apoptotic A549/T cells from 3.87% (untreated) to 11.23% after 6 h and 16.50% after 24 h.
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Cell Line:paclitaxel-resistant A549/T lung cancer cells
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Concentration:0.5 μM, 2 μM
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Incubation Time:24 h
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Result:Dose-dependently increased protein levels of DR5 and cleaved PARP1 in A549/T cells relative to vehicle-treated controls.
Had no significant effect on Bax or Bcl2 protein levels.
Reduced MRP1 protein levels to 0.7 relative to the vehicle control (set at 1.0) at 2 μM.\nSignificantly reduced phosphorylated STAT3 (p-STAT3) protein levels in A549/T cells relative to vehicle-treated controls, while increasing total STAT3 protein levels.
Showed a strong positive correlation between reduction in p-STAT3 and downregulation of MDR1 (r=0.94) and MRP1 (r=0.89) mRNA levels.
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Cell Line:paclitaxel-resistant A549/T lung cancer cells
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Concentration:0.5 μM, 2 μM
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Incubation Time:24 h
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Result:Downregulated MDR1 mRNA levels by 9-fold and MRP1 mRNA levels by 26-fold in A549/T cells relative to vehicle-treated controls at 0.5 μM.
Significantly downregulated MDR1 and MRP1 mRNA levels at 2 μM.
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Cell Line:paclitaxel-resistant A549/T lung cancer cells
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Concentration:0.5 μM, 2 μM
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Incubation Time:24 h
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Result:Reduced P-gp protein abundance in A549/T cells treated with 0.5 μM or 2 μM LSS-11 relative to vehicle-treated controls.
Chemical Information
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CAS No. 1392014-36-6
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Molecular Weight 409.48
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Formula C21H27N7O2
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SMILES
O=C1C2=CC3=C(C4=C2C(C(N1CCN(C)C)=O)=CC(N)=C4)N(CCCN(C)C)N=N3
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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)
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