2. Cell Cycle/DNA Damage Apoptosis
  3. G-quadruplex DNA/RNA Synthesis Apoptosis
  4. 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

Telomeric G4s ligand 1 Chemical Structure

CAS No. : 3047091-81-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Telomeric G4s ligand 1 Related Antibodies

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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].

Cellular Effect
Cell Line Type Value Description References
4T1 IC50
4.6 μM
Compound: R1
Cytotoxicity against mouse 4T1 cells incubated for 24 hrs by CCK-8 reagent based spectrophotometric analysis
Cytotoxicity against mouse 4T1 cells incubated for 24 hrs by CCK-8 reagent based spectrophotometric analysis
[PMID: 38805936]
MCF-10A IC50
5.8 μM
Compound: R1
Cytotoxicity against human MCF-10A cells incubated for 24 hrs by CCK-8 reagent based spectrophotometric analysis
Cytotoxicity against human MCF-10A cells incubated for 24 hrs by CCK-8 reagent based spectrophotometric analysis
[PMID: 38805936]
MCF7 IC50
3.6 μM
Compound: R1
Cytotoxicity against human MCF7 cells incubated for 24 hrs by CCK-8 reagent based spectrophotometric analysis
Cytotoxicity against human MCF7 cells incubated for 24 hrs by CCK-8 reagent based spectrophotometric analysis
[PMID: 38805936]
MDA-MB-231 IC50
1.7 μM
Compound: R1
Cytotoxicity against human MDA-MB-231 cells incubated for 24 hrs by CCK-8 reagent based spectrophotometric analysis
Cytotoxicity against human MDA-MB-231 cells incubated for 24 hrs by CCK-8 reagent based spectrophotometric analysis
[PMID: 38805936]
U2OS IC50
3 μM
Compound: R1
Cytotoxicity against human U2OS cells incubated for 24 hrs by CCK-8 reagent based spectrophotometric analysis
Cytotoxicity against human U2OS cells incubated for 24 hrs by CCK-8 reagent based spectrophotometric analysis
[PMID: 38805936]
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.

Telomeric G4s ligand 1 Related Antibodies

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.
Appearance

Solid

Color

Orange to red

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (30.27 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8160 mL 9.0800 mL 18.1600 mL
5 mM 0.3632 mL 1.8160 mL 3.6320 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8160 mL 9.0800 mL 18.1600 mL 45.4001 mL
5 mM 0.3632 mL 1.8160 mL 3.6320 mL 9.0800 mL
10 mM 0.1816 mL 0.9080 mL 1.8160 mL 4.5400 mL
15 mM 0.1211 mL 0.6053 mL 1.2107 mL 3.0267 mL
20 mM 0.0908 mL 0.4540 mL 0.9080 mL 2.2700 mL
25 mM 0.0726 mL 0.3632 mL 0.7264 mL 1.8160 mL
30 mM 0.0605 mL 0.3027 mL 0.6053 mL 1.5133 mL
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Telomeric G4s ligand 1 Related Classifications

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:

Telomeric G4s ligand 13047091-81-3G-quadruplexDNA/RNA SynthesisApoptosistelomeric G-quadruplex ligandDNA damageR-loop formationapoptosiscell cycle arrest in G2/M phaseInhibitorinhibitorinhibit

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