TS-IN-8
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C19H20FN3O3S
- 分子量:389.44
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Caspase アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
体外実験
TS-IN-8 (Compound 4d) (1-80 μM, 24 h) shows 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)[1].
TS-IN-8 (1-5 μM, 24 h) induces apoptosis in MCF-7 cells in a dose-dependent manner and causes cell cycle arrest at the G2/M phase[1].
TS-IN-8 (1-5 μM, 24 h) induces dose-dependent nuclear morphological changes in MCF-7 cells, including chromatin condensation at 1 μM (apoptotic nuclear index 4.12%) and nuclear fragmentation with apoptotic bodies at 5 μM (apoptotic nuclear index 8.97%), significantly increases intracellular reactive oxygen species (ROS) levels, and activates intrinsic apoptosis pathways by regulating apoptosis-related proteins such as bax/bcl-2 ratio and Caspase activation[1].
TS-IN-8 (1-5 μM, 6 h) significantly reduces TS protein expression in MCF cells[1].
TS-IN-8 (1-5 μM, 24 h) inhibits MCF-7 cell migration in a dose-dependent manner[1].
TS-IN-8 (1-5 μM, 24 h) disrupts the structural integrity of 3D tumor spheres and reduces the number of live cells while increasing the proportion of dead cells in 3D spheres[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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).
-
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 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 %.
-
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.
-
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 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 %.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- ROS/oxidative-stress fluorescent staining
- Apoptosis Solutions
- Protocol for Cell Cycle
- Breast Cancer Modeling
化学情報
-
分子量 389.44
-
分子式 C19H20FN3O3S
-
SMILES
FC1=CC=C(C(N=C(SCCCCCC(OCC)=O)N2)=C(C#N)C2=O)C=C1
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)