1. Cell Cycle/DNA Damage Apoptosis
  2. G-quadruplex DNA/RNA Synthesis Apoptosis
  3. Telomeric G4s ligand 1

Telomeric G4s ligand 1 is a telomeric G-quadruplex ligand that stabilizes telomeric G4 and induces R-loop formation, leading to DNA damage responses. Telomeric G4s ligand 1 induces apoptosis and evokes immunogenic cell death (ICD) in tumor cells.

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Telomeric G4s ligand 1 Chemical Structure

Telomeric G4s ligand 1 Chemical Structure

CAS No. : 3047091-81-3

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Description

Telomeric G4s ligand 1 is a telomeric G-quadruplex ligand that stabilizes telomeric G4 and induces R-loop formation, leading to DNA damage responses. Telomeric G4s ligand 1 induces apoptosis and evokes immunogenic cell death (ICD) in tumor cells[1].

In Vitro

Telomeric G4s ligand 1 (compound R1; 1-4 μM; 24 h) could stabilize G4 and induce R-loop structures in the telomeric regions of MDA-MB-231 cells, which triggered DNA damage responses, cell cycle arrest in G2/M phase, apoptosis and antiproliferation[1].
Telomeric G4s ligand 1 evokes immunogenic cell death (ICD) in tumor cells, which promoted the maturation of bone marrow derived dendritic cells (BMDCs)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 1 μM, 2 μM, 4 μM
Incubation Time: 24 h
Result: Induced cell cycle arrest in G2/M phase and apoptosis.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 1 μM, 2 μM, 4 μM
Incubation Time: 24 h
Result: Increased the levels of DNA damage-related proteins, such as γH2AX and replication protein A subunit.
In Vivo

Telomeric G4s ligand 1 (compound R1; 10 mg/kg; ip; every other day for 14 days) exhibits a significant decrease in tumor burden through the immunomodulatory effects, including the increase of CD4+ and CD8+ T cells in tumors and cytokine levels in sera in breast cancer mouse model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 4-week-old female BALB/c mice injected 4T1 cells[1]
Dosage: 10 mg/kg
Administration: ip; every other day for 14 days
Result: Exhibited the ability to lengthen the survival time of tumor-bearing mice, and resulted in DNA damage and apoptosis in vivo.
Molecular Weight

550.66

Formula

C31H37F3N6

CAS No.
SMILES

CN(CCN(C)C)C1=CC=C(C2=C(C3=CC=C(N(C)CCN(C)C)C=C3)N=C(C=CC(C(F)(F)F)=C4)C4=N2)C=C1

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    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.

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Telomeric G4s ligand 1
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HY-161693
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