TrxR-IN-10
TrxR-IN-10 is a thioredoxin reductase (TrxR) inhibitor. TrxR-IN-10 induces excessive intracellular ROS accumulation, mitochondrial membrane potential collapse, Apoptosis, and cell cycle arrest. TrxR-IN-10 exhibits in vivo antitumor activity in colorectal cancer xenograft models.
For research use only. We do not sell to patients.
- Formula: C32H43NO8Se
- Molecular Weight:648.65
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SW480 | IC50 |
23.37 μM
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Antiproliferative activity against human SW480 colorectal cancer cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human SW480 colorectal cancer cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42748746 |
| HCT-116 | IC50 |
6.00 μM
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Antiproliferative activity against human HCT116 colorectal cancer cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human HCT116 colorectal cancer cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42748746 |
| SW-620 | IC50 |
18.26 μM
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Antiproliferative activity against human SW620 colorectal cancer cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human SW620 colorectal cancer cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
42748746 |
| HT-29 | IC50 |
>50 μM
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Antiproliferative activity against human HT29 colorectal cancer cells assessed as viability reduction incubated 48 hrs by MTT assay; IC50 greater than 50 μM.
Antiproliferative activity against human HT29 colorectal cancer cells assessed as viability reduction incubated 48 hrs by MTT assay; IC50 greater than 50 μM.
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42748746 |
In Vitro
TrxR-IN-10 (1-12 μM; 8 h-2 weeks of culture) inhibits the long-term clonogenic growth of HCT116 cells in a dose-dependent manner[1].
TrxR-IN-10 (3-12 μM; 24 h) inhibits HCT116 cell migration in a dose-dependent manner[1].
TrxR-IN-10 (0.5-2 μM; 48 h) shows reproducible modulation of pro-apoptotic proteins in SW480 colorectal cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 cells
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Concentration:1, 3, 6, 9, 12 μM
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Incubation Time:8 h (compound exposure); 2 weeks (culture)
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Result:Suppressed long-term clonogenic growth of HCT116 cells in a dose-dependent manner.
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Cell Line:HCT116 cells
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Concentration:3, 6, 12 μM
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Incubation Time:48 h
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Result:Early apoptotic ratios of HCT116 cells were 19.1%, 22.8%, and 25.4%, with corresponding late apoptotic rates of 28.8%, 27.3%, and 28.0%, at 3, 6, and 12 μM compound 3e, respectively.
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Cell Line:HCT116 cells
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Concentration:3, 6, 12 μM
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Incubation Time:24 h
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Result:The proportion of cells in G0/G1 phase was 51.9%, 54.5%, and 56.9% upon exposure to 3, 6, and 12 μM compound 3e, respectively.
The percentage of S-phase cells decreased to 19.8%.
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Cell Line:HCT116 cells
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Concentration:3, 6, 12 μM
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Incubation Time:24 h
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Result:Cell migration rates in the 3, 6, and 12 μM 3e groups were 9.5%, 7.0%, and 5.5%, respectively.
Resulted in a concentration-dependent reduction in cell migration.
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Cell Line:SW480 cells
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Concentration:0.5, 1, 2 μM
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Incubation Time:48 h
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Result:Elevated Bax, cleaved-caspase-3, and cleaved-PARP, while decreasing procaspase-3 and Bcl-2 in SW480 cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (male and female; 5-week-old)[1]
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Dosage:25 mg/kg and 50 mg/kg
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Administration:once every two days; for 13 consecutive days
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Result:exhibited only moderate tumor-suppressive activity.
No significant body-weight loss was observed in mice, indicating acceptable general tolerability.
Robust in-vivo efficacy was not achieved under the current experimental conditions.
- Mitochondrial membrane-potential fluorescent assay
- Annexin V plus membrane-impermeant dye apoptosis staining
- ROS/oxidative-stress fluorescent staining
- BrdU Incorporation Assay
- Protocol for Cell Cycle
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Fluorescent plasma-membrane potential dye assay
- Mitochondrial membrane-potential and mitochondrial mass staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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Molecular Weight 648.65
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Formula C32H43NO8Se
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SMILES
O=C(O[C@@H]1O[C@@]2([H])[C@@]3(OO[C@](O2)(C)CC4)[C@]4([H])[C@H](C)CC[C@@]3([H])[C@H]1C)CCC(OCCCC[Se]C5=C(C)NC6=C5C=CC=C6)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TrxR-IN-10 Related Classifications
HY-189690 Related Classifications
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