Telomeric G4s ligand 2
Telomeric G4s ligand 2 is an orally active, selective ligand of telomeric G-quadruplex (G4), with an IC50 of 0.4 μM. Telomeric G4s ligand 2 binds to dimeric telomeric G4, inhibits the activities of DHX36 and BLM helicases. Telomeric G4s ligand 2 activates cGAS-STING and TERRA-ZBP1 pathways, inducing autophagy and G2/M cell cycle arrest, and exhibits antiproliferative effects across cancer cell lines. Telomeric G4s ligand 2 can be used for the study of colorectal cancer.
For research use only. We do not sell to patients.
- CAS No.: 3094716-52-3
- Formula: C25H32N6O
- Molecular Weight:432.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All DNA/RNA Synthesis Isoforms
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Biological Activity
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Helicase |
Telomeric G4s ligand 2 (CA11) binds selectively to dimeric telomeric G-quadruplex HTG57 with a Kd of 5.8 μM[1].
Telomeric G4s ligand 2 (1 μM; 2 min equilibration after each addition) binds with high affinity to dimeric telomeric DNA and RNA G4s (Kd = 0.4 μM and 0.1 μM, respectively) and shows no measurable binding to monomeric G4s, non-G4 nucleic acids, or promoter G4s[1].
Telomeric G4s ligand 2 (0-50 μM; 30 min at 37°C) inhibits the binding of G4-resolving helicases DHX36 and BLM to telomeric G4 DNA, with maximum inhibition rates of 80% and 50% at 50 μM, respectively[1].
Telomeric G4s ligand 2 (0-25 μM) potently inhibits the unwinding of telomeric G4 DNA by its complementary antisense strand, reaching 90% inhibition at 25 μM[1].
Telomeric G4s ligand 2 potently inhibits the proliferation of HCT116 colorectal cancer cells with an IC50 of 0.4 μM[1].
Telomeric G4s ligand 2 (0.25-0.5 μM; 48 h) dose-dependently induces telomere-specific DNA damage and dysfunction in both HCT116 and U2OS cancer cells, activates dual innate immune sensing pathways (TERRA-ZBP1 and cGAS-STING), induces autophagy[1].
Telomeric G4s ligand 2 (0-100 nM; 9 days) potently inhibits long-term colony formation of U2OS, MC38, HCT116, and HeLa cancer cells
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 (TERT+) and U2OS (ALT+) cancer cells
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Concentration:0.25-0.5 μM
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Incubation Time:48 h
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Result:Induced a dose-dependent increase in intracellular G4 foci, with >50% of foci colocalizing with telomeric protein TRF2 in both cell lines.
Induced a dose-dependent increase in γ-H2AX foci, with a substantial fraction colocalizing with TRF2 to form telomere dysfunction-induced foci (TIFs).
| Species | Dose | Route | Bioavailability | T1/2 |
|---|---|---|---|---|
| Rat[1] | 6 mg/kg | o.a. | 11.1 % | 12.2 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 5 weeks old; injected subcutaneously with 3×105 MC38 colorectal cancer cells)[1]
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Dosage:20 mg/kg; 40 mg/kg
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Administration:p.o.; every other day; 26 days
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Result:Reduced final tumor weight to a mean of 0.5 g (20 mg/kg) and 0.6 g (40 mg/kg).
Increased percentage of CD8+ T cells in CD3+ T cells to 4.5% (20 mg/kg) and 5% (40 mg/kg).
Increased percentage of CD4+ T cells in CD3+ T cells to 4.5% (40 mg/kg).
Increased percentage of MHC-II+ and CD86+ cells in tumor-associated macrophages (both doses).
Elevated serum levels of pro-inflammatory cytokines IFN-γ, TNF-α, and IL-6 (both doses).
Chemical Information
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CAS No. 3094716-52-3
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Molecular Weight 432.56
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Formula C25H32N6O
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SMILES
O=C(NC1=CC=C(NC2=NC(N3CCCC3)=NC4=CC=CC=C42)C=C1)CCN(CC)CC
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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)