2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Cell Cycle/DNA Damage Apoptosis
  3. Phosphodiesterase (PDE) Reactive Oxygen Species (ROS) DNA/RNA Synthesis Apoptosis
  4. TDP1-IN-5

TDP1-IN-5 是一种酪氨酸-DNA 磷酸二酯酶 1 (TDP1) 抑制剂，其 IC50 为 2.2 μM。TDP1-IN-5 通过在细胞内外靶向 TDP1，抑制 NHEJ 修复途径，阻滞细胞周期于 G2/M 期，上调 PIG3 增强 ROS，最终显著增强电离辐射 (IR) 诱导的 DNA 损伤和细胞凋亡 (apoptosis)。TDP1-IN-5 可用于结直肠癌的研究。

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TDP1-IN-5

TDP1-IN-5 Chemical Structure

CAS No. : 3115524-78-9

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TDP1-IN-5 相关抗体

Top Publications Citing Use of Products

查看 Phosphodiesterase (PDE) 亚型特异性产品:

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TDP1-IN-5 is a tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitor with an IC50 of 2.2 μM. By targeting TDP1 both intracellularly and extracellularly, TDP1-IN-5 inhibits the NHEJ repair pathway, arrests the cell cycle at the G2/M phase, upregulates PIG3 to enhance ROS, and ultimately significantly potentiates ionizing radiation (IR)-induced DNA damage and apoptosis. TDP1-IN-5 can be used in the research of colorectal cancer[1].

体外研究
(In Vitro)

TDP1-IN-5 (Compound A6) (0.025-0.1 μM) 在 HCT116 细胞中表现出强放射增敏活性，在 0.1 μM 浓度下联合 2 GY IR 处理时可杀死 83% 的细胞，且具有协同活性，其 CI 值低至 0.20[1]。
TDP1-IN-5 (5-25 μM; 1 h) 靶向 HCT116 细胞中的细胞内 TDP1，以剂量依赖的方式稳定 TDP1-DNA 共价复合物，且与电离辐射联合使用时稳定作用增强[1]。
TDP1-IN-5 (1.25-5.0 μM) 可在体外以剂量依赖方式抑制 HCT116 细胞中的 NHEJ 修复活性，在 5.0 μM 浓度下修复率最高可降低 42%[1]。
TDP1-IN-5 (5 μM; 6 h) 可增强电离辐射诱导的 HCT116 细胞 DNA 损伤，当在 5 μM 浓度下联合 4 GY IR 处理时，可使 γH2AX 灶点增加至 4.2 倍[1]。
TDP1-IN-5 (1.25-2.5 μM) 可单独或联合 4 GY 电离辐射上调 HCT116 细胞中 PIG3 蛋白的表达[1]。
TDP1-IN-5 (10 μM) 在 10 μM 浓度下可增强电离辐射诱导的 HCT116 细胞内 ROS 生成，但自身不会诱导 ROS 生成[1]。
TDP1-IN-5 (5-10 μM; 24 h) 以剂量依赖的方式诱导 HCT116 细胞发生 G2/M 期细胞周期阻滞，与 4 GY 电离辐射联合使用时阻滞作用增强[1]。
TDP1-IN-5 (5-10 μM; 24 h) 以剂量依赖的方式诱导 HCT116 细胞发生凋亡，并显著增强电离辐射诱导的凋亡；在 10 μM 浓度下联合 4 GY IR 处理时，凋亡率可达 43.8%[1]。

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

TDP1-IN-5 相关抗体:

Immunofluorescence[1]

Cell Line: HCT116 human colorectal cancer cells
Concentration: 5 μM
Incubation Time: 6 h
Result: Increased γH2AX foci by 1.5-fold when used alone compared to untreated cells.
Increased γH2AX foci to 4.2-fold above untreated levels when combined with 4 GY ionizing radiation (IR).

Cell Cycle Analysis[1]

Cell Line: HCT116 human colorectal cancer cells
Concentration: 5 μM, 10 μM
Incubation Time: 24 h
Result: Increased the G2/M phase cell proportion from 27.9% (control) to 40.2% at 5 μM when used alone.
Increased the G2/M phase cell proportion from 27.9% (control) to 47.9% at 10 μM when used alone.
Increased the G2/M phase proportion from 40.4% (IR alone) to 53.1% at 5 μM when combined with 4 GY ionizing radiation (IR).
Increased the G2/M phase proportion from 40.4% (IR alone) to 59.0% at 10 μM when combined with 4 GY IR.

Apoptosis Analysis[1]

Cell Line: HCT116 human colorectal cancer cells
Concentration: 5 μM, 10 μM
Incubation Time: 24 h
Result: Increased the apoptotic ratio from 4.1% (control) to 8.3% at 5 μM when used alone.
Increased the apoptotic ratio from 4.1% (control) to 22.2% at 10 μM when used alone.
Increased the apoptotic ratio from 13.5% (IR alone) to 19.4% at 5 μM when combined with 4 GY ionizing radiation (IR).
Increased the apoptotic ratio from 13.5% (IR alone) to 43.8% at 10 μM when combined with 4 GY IR.
体内研究
(In Vivo)

TDP1-IN-5 (Compound A6) (10 mg/kg；腹腔注射；每日一次；连续 14 天) 在体内可作为有效放射增敏剂，当与每两天给药一次、连续 14 天的 1 GY IR 联用时，可使 HCT116 异种移植瘤的重量降低 79%[1]。

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

Animal Model: BALB/c nude (male, 4-5 weeks old, 15-18 g, subcutaneous xenograft model)[1]
Dosage: 10 mg/kg
Administration: i.p.; daily; 14 days
Result: Slightly inhibited tumor growth alone.
Reduced tumor weight by 79% when combined with 1 GY IR.
Caused slight body weight loss relative to controls alone.
Showed no obvious body weight difference compared to IR alone group when combined with IR.
Exhibited protective effect on liver and spleen weight against IR-induced reduction.
分子量

603.75

Formula

C34H45N5O5
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

TDP1-IN-5 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

TDP1-IN-53115524-78-9Phosphodiesterase (PDE)Reactive Oxygen Species (ROS)DNA/RNA SynthesisApoptosisHCT116 cellsTyrosyl-DNA phosphodiesterase 1 (TDP1)apoptosisG2/M cell cycle arrestNHEJ repair activityROS productionγH2AX fociSgTDP1-HCT116 cellscolorectal cancerPIG3Inhibitorinhibitorinhibit

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