TRi-1 |
Catalog No.GC65101
One-Click Copy Product Info
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TRi-1 is a potent, specific, and irreversible inhibitor of TXNRD1 and TXNRD2 with IC50 values of 18nM and 44nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 246020-68-8
Sample solution is provided at 25 µL, 10mM.
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TRi-1 is a potent, specific, and irreversible inhibitor of TXNRD1 and TXNRD2 with IC50 values of 18nM and 44nM [1]. TRi-1 can enhance the activation of Nrf2 by increasing the intracellular ROS level, leading to a compensatory increase in the relative mRNA expression levels of the classic activated genes downstream of Nrf2 [2]. TRi-1 has been widely used to reduce the senescence-associated secretory phenotype (SASP), inhibit the proliferation of cancer stem cells (CSCs) and impede tumor growth[3].
In vitro, TRi-1 treatment for 48 hours significantly inhibited the proliferation of B16-F10 cells and LLC cells with IC50 values of 20µM and 25µM, respectively[4]. Treatment of LN229TAZ(4SA) cells with 1.25μM TRi-1 for 48h significantly induced cell death in the absence of glucose[5].
In vivo, TRi-1 treatment via intraperitoneal injection at a dose of 10mg/kg daily for 5 consecutive days, followed by a 2-day drug-free period, and subsequently administered three times per week for two weeks, resulted in significant suppression of tumor volume in mouse MDA-MB-231 xenograft models without affecting body weight [6]. TRi-1 (10mg/kg), administered intraperitoneally every three days for 21 days, significantly reduced TXNRD1 levels and decreased the expression of IL-1β and C-X-C motif chemokine 15 (CXCL15) in ovarian tissues of 22-month-old mice[7].
References:
[1] Jović M, Gencheva R, Scholzen K C, et al. Development of novel analogs of the TRi-1 and TRi-2 selenoprotein thioredoxin reductase inhibitors with initial assessment of their cytotoxicity profiles[J]. Free Radical Biology and Medicine, 2025.
[2] Bonner M Y, Vancsik T, Oliveira-Coelho A, et al. Anti-Tumoral Treatment with Thioredoxin Reductase 1 Inhibitor Auranofin Fosters Regulatory T Cell and B16F10 Expansion in Mice[J]. Antioxidants, 2025, 14(11): 1351.
[3] Towers M, Hao X, Sriramkumar S, et al. Abstract B029: Targeting non-canonical function of TXNRD1 to overcome platinum resistance by eradicating ovarian cancer stem-like cells[J]. Cancer Research, 2024, 84(5_Supplement_2): B029-B029.
[4] Sabatier P, Beusch C M, Gencheva R, et al. Comprehensive chemical proteomics analyses reveal that the new TRi-1 and TRi-2 compounds are more specific thioredoxin reductase 1 inhibitors than auranofin[J]. Redox Biology, 2021, 48: 102184.
[5] Tang M, Dirks K, Kim S Y, et al. Inhibition of thioredoxin reductase 1 sensitizes glucose-starved glioblastoma cells to disulfidptosis[J]. Cell Death & Differentiation, 2025, 32(4): 598-612.
[6] Stafford W C, Peng X, Olofsson M H, et al. Irreversible inhibition of cytosolic thioredoxin reductase 1 as a mechanistic basis for anticancer therapy[J]. Science translational medicine, 2018, 10(428): eaaf7444.
[7] Hao X, Zhao B, Towers M, et al. TXNRD1 drives the innate immune response in senescent cells with implications for age-associated inflammation[J]. Nature aging, 2024, 4(2): 185-197.
| Cell experiment [1]: | |
Cell lines | B16-F10 cells |
Preparation Method | B16-F10 cells were cultured in Dulbecco's Modified Eagle's medium containing 10% fetal bovine serum, 2mM l-glutamine, and 150nM Na2SeO3 at 37℃ in the presence of 5% CO2. B16-F10 cells were seeded at a density of 3×103 cells/well in 96-well flat-bottom plates and cultured for 24 hours. Cells were treated with different concentrations of TRi-1 (0.005, 0.05, 0.5, 1, 5, 10, 25, and 50μM) for 48h, and cell viability was measured. |
Reaction Conditions | 0.005, 0.05, 0.5, 1, 5, 10, 25, and 50μM; 48h |
Applications | TRi-1 treatment reduced the cell viability of B16-F10 cells in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female C56BL/6 mice |
Preparation Method | Female C56BL/6 mice (aged 22 months) were housed in a room with controlled humidity (50±10%) and temperature (25±3°C) under a 12/12h light/dark cycle. Mice were randomly divided into three groups: injected intraperitoneally once every 3 days with 10mg/kg TRi-1 in solvent (10% DMSO+90% corn oil), 5mg/kg auranofin in solvent, or solvent alone in a 100μl volume for 21 days. The mice were killed, and the ovarian tissues were collected for analysis. |
Dosage form | 10mg/kg; every 3 days for 21 days; i.p. |
Applications | TRi-1 treatment significantly reduced TXNRD1 levels and decreased the expression of IL-1β and CXCL15 in ovarian tissues of mice. |
References: | |
| Cas No. | 246020-68-8 | SDF | |
| Formula | C12H9ClN2O5S | M.Wt | 328.73 |
| Solubility | DMSO : 62.5 mg/mL (190.13 mM; Need ultrasonic) | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.042 mL | 15.2101 mL | 30.4201 mL |
| 5 mM | 608.4 μL | 3.042 mL | 6.084 mL |
| 10 mM | 304.2 μL | 1.521 mL | 3.042 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)