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 是一种具有口服活性的选择性端粒 G-quadruplex (G4) 配体，其 IC50 为 0.4 μM。Telomeric G4s ligand 2 可结合二聚体端粒 G4，抑制 DHX36 和 BLM 解旋酶的活性。Telomeric G4s ligand 2 可激活 cGAS-STING 和 TERRA-ZBP1 通路，诱导自噬 (autophagy) 和 G2/M 期细胞周期阻滞，并在多种癌细胞系中表现出抗增殖作用。Telomeric G4s ligand 2 可用于结直肠癌的研究。

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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 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

Telomeric G4s ligand 2 (CA11) 选择性地与二聚体端粒 G-quadruplex HTG57结合，其解离常数 Kd 为 5.8 μM[1]。
Telomeric G4s ligand 2 (1 μM; 每次加入后平衡 2 min) 与二聚体端粒 DNA 和 RNA G4s 具有高亲和力结合 (Kd 分别为 0.4 μM 和 0.1 μM)[1]。
Telomeric G4s ligand 2 (0-50 μM; 37°C下孵育 30 min) 抑制 G4 解旋酶 DHX36 和 BLM 与端粒 G4 的结合，在 50 μM 浓度下分别达到 80% 和 50% 的最大抑制率[1]。
Telomeric G4s ligand 2 (0-25 μM) 能有效抑制其互补反义链介导的端粒 G4 DNA 解旋，在 25 μM 浓度下抑制率达 90%[1]。
Telomeric G4s ligand 2 能有效抑制 HCT116 结直肠癌细胞的增殖，IC50 为 0.4 μM[1]。
Telomeric G4s ligand 2 (0.25-0.5 μM; 48 h) 能剂量依赖性地诱导 HCT116 和 U2OS 癌细胞中端粒特异性 DNA 损伤和功能障碍，并激活双重固有免疫感应。 TERRA-ZBP1 和 cGAS-STING 通路可诱导自噬[1]。
Telomeric G4s ligand 2 (0-100 nM; 9 天) 可有效抑制 U2OS、MC38、HCT116 和 HeLa 癌细胞的长期克隆形成[1]。

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

Telomeric G4s ligand 2 相关抗体:

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).
药代动力学
(Parmacokinetics)
Species Dose Route Bioavailability T1/2
Species Dose Route Bioavailability T1/2
Rat[1] 6 mg/kg o.a. 11.1 % 12.2 h
Rat[1] 6 mg/kg o.a. 11.1 % 12.2 h
体内研究
(In Vivo)

Telomeric G4s ligand 2 (灌胃，每隔 1 天给药 1 次，持续 26 天，剂量 20-40 mg/kg) 可显著抑制小鼠体内 MC38 结直肠肿瘤的生长，激活抗肿瘤免疫，且具有良好的全身耐受性[1]。

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).
分子量

432.56

Formula

C25H32N6O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Telomeric G4s ligand 2 相关分类

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  • Do most proteins show cross-species activity?

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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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