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

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TS-IN-8

TS-IN-8 Chemical Structure

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TS-IN-8 Related Antibodies

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Description

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].

In Vitro

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.

TS-IN-8 Related Antibodies

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 %.
Molecular Weight

389.44

Formula

C19H20FN3O3S
SMILES

FC1=CC=C(C(N=C(SCCCCCC(OCC)=O)N2)=C(C#N)C2=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TS-IN-8 Related Classifications

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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:

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

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