2. Cell Cycle/DNA Damage Immunology/Inflammation Autophagy
  3. G-quadruplex DNA/RNA Synthesis Cyclic GMP-AMP Synthase STING Autophagy
  4. 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.

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Telomeric G4s ligand 2

Telomeric G4s ligand 2 Chemical Structure

CAS No. : 3094716-52-3

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Telomeric G4s ligand 2 Related Antibodies

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Description

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[1].

IC50 & Target

Helicase

 

In Vitro

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.

Telomeric G4s ligand 2 Related Antibodies

Immunofluorescence[1]

Cell Line: HCT116 (TERT+) and U2OS (ALT+) cancer cells
Concentration: 0.25-0.5 μM
Incubation Time: 48 h
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).
Parmacokinetics
Species Dose Route Bioavailability T1/2
Rat[1] 6 mg/kg o.a. 11.1 % 12.2 h
In Vivo

Telomeric G4s ligand 2 (20-40 mg/kg; p.o.; every other day; 26 days) significantly suppresses MC38 colorectal tumor growth in mice, activates antitumor immunity, and is well tolerated systemically[1].

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

Animal Model: C57BL/6 (male, 5 weeks old; injected subcutaneously with 3×105 MC38 colorectal cancer cells)[1]
Dosage: 20 mg/kg; 40 mg/kg
Administration: p.o.; every other day; 26 days
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).
Molecular Weight

432.56

Formula

C25H32N6O
CAS No.
SMILES

O=C(NC1=CC=C(NC2=NC(N3CCCC3)=NC4=CC=CC=C42)C=C1)CCN(CC)CC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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Purity & Documentation
References
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Telomeric G4s ligand 2 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:

Telomeric G4s ligand 23094716-52-3G-quadruplexDNA/RNA SynthesisCyclic GMP-AMP SynthaseSTINGAutophagycGASStimulator of Interferon GenesTMEM173MITAERISMPYStelomeric G-quadruplexcolorectal cancerTERRA-ZBP1HeLaMC38cGAS-STINGU2OSHCT116DHX36BLMInhibitorinhibitorinhibit

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