2. Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. Thymidylate Synthase Apoptosis Reactive Oxygen Species (ROS) Bcl-2 Family Caspase
  4. TS-IN-8

TS-IN-8 是一种强效的胸苷酸合成酶 (TS) 抑制剂。TS-IN-8 可诱导 MCF-7 细胞凋亡 (apoptosis)，并导致细胞周期停滞于 G2/M 期。TS-IN-8 可诱导细胞核形态改变。TS-IN-8 可增加细胞内活性氧 (ROS) 水平。TS-IN-8 可通过调节凋亡相关蛋白 (如 bax/bcl-2 比值和 caspase 活化) 激活内源性凋亡通路。TS-IN-8 可用于乳腺癌的研究。

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TS-IN-8

TS-IN-8 Chemical Structure

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TS-IN-8 相关抗体

Top Publications Citing Use of Products

查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TS-IN-8 is a potent thymidylate synthase (TS) inhibitor. TS-IN-8 can induce apoptosis and cause cell cycle arrest at the G2/M in MCF-7 cells. TS-IN-8 can induce nuclear morphological changes. TS-IN-8 can increase intracellular reactive oxygen species (ROS) levels. TS-IN-8 can activate intrinsic apoptosis pathways by regulating apoptosis-related proteins such as the bax/bcl-2 ratio and caspase activation. TS-IN-8 can be used for the study of breast cancer[1].

体外研究
(In Vitro)

TS-IN-8 (Compound 4d) (1-80 μM，24 小时) 对 MCF-7 细胞 (IC50 = 10.11 μM) 和 A549 细胞 (IC50 = 22.49 μM) 表现出强烈的抑制作用，对 HepG2 细胞的抑制作用较弱，且对正常 McCoy 细胞的毒性较低 (IC50 = 115.86 μM)[1]。
TS-IN-8 (1-5 μM，24 小时) 以剂量依赖的方式诱导 MCF-7 细胞凋亡，并导致细胞周期阻滞于 G2/M 期[1]。
TS-IN-8 (1-5 μM，24 小时) 可诱导 MCF-7 细胞发生剂量依赖性的核形态学改变，包括 1 μM 浓度下的染色质浓缩 (凋亡核指数 4.12 %) 和 5 μM 浓度下的核碎裂并伴有凋亡小体形成 (凋亡核指数 8.97 %) 。此外，化合物 TS-IN-8 还显著提高细胞内活性氧 (ROS) 水平，并通过调节 bax/bcl-2 比值和 Caspase 激活等凋亡相关蛋白来激活内源性凋亡通路[1]。
TS-IN-8 (1-5 μM，6 小时) 可显著降低 MCF 细胞中 TS 蛋白的表达[1]。
TS-IN-8 (1-5 μM，24 小时) 以剂量依赖的方式抑制 MCF-7 细胞的迁移[1]。
TS-IN-8 (1-5 μM，24 小时) 破坏 3D 肿瘤球的结构完整性，减少 3D 球中活细胞的数量，同时增加死细胞的比例[1]。

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

TS-IN-8 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: MCF-7 cells, A549 cells, HepG2 cells, McCoy cells
Concentration: 1 μM, 5 μM, 10 μM, 20 μM, 40 μM, 60 μM, 80 μM
Incubation Time: 24 h
Result: Showed strong inhibitory effects on MCF-7 cells (IC50 = 10.11 μM) and A549 cells (IC50 = 22.49 μM), weaker inhibitory effects on HepG2 cells, and low toxicity to normal McCoy cells (IC50 = 115.86 μM).

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 1 μM, 5 μM
Incubation Time: 24 h
Result: At 1 μM, the proportion of apoptotic cells increased to 3.27 %; at 5 μM, the proportion of apoptotic cells increased to 6.49 %.

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 1 μM, 5 μM
Incubation Time: 24 h
Result: At 1 μM, the percentage of cells in the G2/M phase increased to 34.8 %; at 5 μM, the percentage of cells in the G2/M phase increased to 39.8 %.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 1 μM, 5 μM
Incubation Time: 24 h
Result: Pro-apoptotic protein Bax expression was upregulated, while anti-apoptotic proteins Bcl-2 and Survivin expression were downregulated.
The cleavage patterns of Caspase-3, Caspase-9, and PARP-1 were increased.
An elevated Bax/Bcl-2 ratio indicates activation of the mitochondrial pathway for apoptosis.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 1 μM, 5 μM
Incubation Time: 24 h
Result: TS protein expression levels were reduced (0.8-fold compared to the control at 1 μM and 0.6-fold compared to the control at 5 μM).

Cell Migration Assay [1]

Cell Line: MCF-7 cells
Concentration: 1 μM, 5 μM
Incubation Time: 24 h
Result: At 1 μM, reduced the wound closure rate to 68.4 %; at 5 μM, reduced the wound closure rate to 55.6 %.
分子量

389.44

Formula

C19H20FN3O3S
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

TS-IN-8 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

TS-IN-8Thymidylate SynthaseApoptosisReactive Oxygen Species (ROS)Bcl-2 FamilyCaspaseThiopyrimidineCyanopyrimidineROS productionInhibitorinhibitorinhibit

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