2. Epigenetics Cell Cycle/DNA Damage
  3. DNA Glycosylase DNA/RNA Synthesis
  4. TDG-IN-1

TDG-IN-1 是一种具有口服活性的选择性小分子胸腺嘧啶 DNA 糖基化酶 (TDG) 抑制剂，其 Ka 为 1.46 nM。TDG-IN-1 可破坏 TDG 与 DNA 结合能力，诱导 DHX9 表达下调、双链 RNA 积累以及 RIG-I/MDA5-MAVS 通路激活，同时发挥肿瘤抑制因子、先天免疫激活剂和免疫刺激剂的作用。TDG-IN-1 可抑制 p53 缺陷型肿瘤细胞和异种移植瘤的生长，并与 p53 存在合成致死效应。TDG-IN-1 可用于 p53 缺陷型癌症的研究。

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TDG-IN-1

TDG-IN-1 Chemical Structure

CAS No. : 3092641-80-7

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TDG-IN-1 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TDG-IN-1 is an orally active, selective small-molecule inhibitor of thymine DNA glycosylase (TDG) with a Ka of 1.46 nM. TDG-IN-1 impairs the DNA-binding ability of TDG, induces downregulated expression of DHX9, accumulation of double-stranded RNA, and activation of the RIG-I/MDA5-MAVS pathway, while acting as a tumor suppressor, innate immune activator and immunostimulant. TDG-IN-1 inhibits the growth of p53-deficient tumor cells and xenograft tumors, and exerts a synthetic lethal effect with p53. TDG-IN-1 is applicable to the research of p53-deficient cancers[1].

体外研究
(In Vitro)

TDG-IN-1 (Compound C-271) (0.16-0.25 μM; 1 h) 可强效抑制纯化的人源 TDG 在多种双链 DNA (dsDNA) 底物上的糖基化酶活性，其 IC50 值范围为 0.16 至 0.25 μM[1]。
TDG-IN-1 (0.11-0.19 μM; 过夜) 可阻断 TDG 结合多种底物类型 dsDNA 的能力，其 IC50 值范围为 0.11 至 0.19 μM[1]。
TDG-IN-1 (1.25 μM; 4 days) 以依赖于 TDG 的方式抑制 p53 缺陷型 KP 肺腺癌细胞的活力[1]。
TDG-IN-1 (0.04-30 μM; 144 h) 可选择性抑制 p53 缺陷型人类实体癌细胞系的活力，在 16 株受试的 p53 缺陷型细胞系中，其 IC50 值均低于 5 μM[1]。
TDG-IN-1 (1.25 μM; 4 days) 处理 p53 缺陷型 KP 肺腺癌细胞会导致细胞质 dsRNA的积累[1]。
TDG-IN-1 (0.625-2.5 μM; 4 days) 可在体外以剂量依赖的方式下调 p53 缺陷型 KP 肺腺癌细胞中 DHX9 蛋白的表达[1]。

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

TDG-IN-1 相关抗体:

Cell Viability Assay[1]

Cell Line: Mouse KP (Kras^{LSL-G12D/+}; Trp53^{flox/flox}) lung adenocarcinoma cells
Concentration: 1.25 μM (follow-up experiments); IC50 range tested
Incubation Time: 4 days (follow-up experiments)
Result: Selectively inhibited the viability of wild-type KP cells, with this effect attenuated in TDG-KO and TDG^{C287S} (mouse ortholog of human C276S) mutant KP cells.

Immunofluorescence[1]

Cell Line: Mouse KP lung adenocarcinoma cells
Concentration: 1.25 μM
Incubation Time: 4 days
Result: Induced a significant increase in cytoplasmic dsRNA accumulation in KP cells; this signal was abolished by RNase III treatment.

Western Blot Analysis[1]

Cell Line: Mouse KP lung adenocarcinoma cells
Concentration: 0.625, 1.25, 2.5 μM
Incubation Time: 4 days
Result: Dose-dependently reduced DHX9 protein levels in KP cells.
体内研究
(In Vivo)

TDG-IN-1 (Compound C-271) (50 mg/kg; i.g.; 每日一次共 14-25 天) 可在 p53-null NCI-H1299 和 p53 突变型 NCI-H446 异种移植模型中抑制肿瘤生长，且能延长小鼠生存期，无明显毒性[1]。
TDG-IN-1 (5 mg/kg; i.g.; 每日一次共 30-50 天) 与抗 CTLA4 抗体协同作用，增强对肿瘤生长的抑制效果，并延长 p53 缺陷型 KP 同种异体移植瘤模型小鼠的生存期[1]。
TDG-IN-1 (5 mg/kg; i.g.; 每日一次共 25-50 天) 与抗 CTLA4 抗体协同作用，增强对肿瘤生长的抑制效果，并在 p53 基因缺失的 4T1 乳腺癌异种移植模型中延长生存期[1]。

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

Animal Model: Nude mice (female, 6-8 weeks old)[1]
Dosage: 50 mg/kg
Administration: i.g.; once daily for 14-25 days
Result: Suppressed p53-deficient tumors growth and induced
cytoplasmic dsRNA accumulation.
Animal Model: C57BL/6 mice (female, 6-8 weeks old)[1]
Dosage: 5 mg/kg
Administration: i.g.; once daily for 30-50 days
Result: Produced enhanced tumor growth inhibition compared to either agent alone when combined with anti-CTLA4 antibody.
Prolonged mouse survival.
Animal Model: BALB/c mice (female, 6-8 weeks old)[1]
Dosage: 5 mg/kg
Administration: i.g.; once daily for 25-50 days
Result: Produced enhanced tumor growth inhibition compared to either agent alone when combined with anti-CTLA4 antibody.
Prolonged mouse survival.
分子量

234.25

Formula

C13H14O4
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

TDG-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

TDG-IN-13092641-80-7DNA GlycosylaseDNA/RNA SynthesisG?U dsDNA substratesNCI-H1299 cellsp53-deficient tumor cellsTDGG?5caC dsDNA substratesG?5fC dsDNA substratesDHX9thymine DNA glycosylaseC276RIG-I/MDA5-MAVS pathwayInhibitorinhibitorinhibit

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