2. Cell Cycle/DNA Damage Apoptosis Epigenetics JAK/STAT Signaling Stem Cell/Wnt Membrane Transporter/Ion Channel
  3. Topoisomerase Apoptosis TNF Receptor PARP STAT P-glycoprotein
  4. 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.

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Lss-11

Lss-11 Chemical Structure

CAS No. : 1392014-36-6

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Lss-11 Related Antibodies

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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STAT3 STAT5 STAT6 STAT1

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Description

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[1].

IC50 & Target[1][3]

STAT3

 

PARP1

 

In Vitro

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.

Lss-11 Related Antibodies

Apoptosis Analysis[1]

Cell Line: paclitaxel-resistant A549/T lung cancer cells
Concentration: 0.5 μM
Incubation Time: 6 h, 24 h
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.

Western Blot Analysis[1]

Cell Line: paclitaxel-resistant A549/T lung cancer cells
Concentration: 0.5 μM, 2 μM
Incubation Time: 24 h
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.

Real Time qPCR[1]

Cell Line: paclitaxel-resistant A549/T lung cancer cells
Concentration: 0.5 μM, 2 μM
Incubation Time: 24 h
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.

Immunofluorescence[1]

Cell Line: paclitaxel-resistant A549/T lung cancer cells
Concentration: 0.5 μM, 2 μM
Incubation Time: 24 h
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.
Molecular Weight

409.48

Formula

C21H27N7O2
CAS No.
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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Purity & Documentation
References
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Lss-11 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lss-111392014-36-6Lss11Lss 11TopoisomeraseApoptosisTNF ReceptorPARPSTATP-glycoproteinTumor Necrosis Factor ReceptorTNFRpoly ADP ribose polymerase P-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243apoptosistopoisomeraseMRP1paclitaxel-resistant lung cancerA549/T lung cancer cellsSTAT3DR5PARP1DNA minor grooveInhibitorinhibitorinhibit

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