TRi-1是一种强效、特异且不可逆的TXNRD1和TXNRD2抑制剂，IC50值分别为18nM和44nM。
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.
TRi-1是一种强效、特异且不可逆的TXNRD1和TXNRD2抑制剂，IC50值分别为18nM和44nM[1]。TRi-1能通过增加细胞内活性氧（ROS）水平来增强Nrf2的激活，导致Nrf2下游经典激活基因的相对mRNA表达水平代偿性升高[2]。TRi-1已被广泛用于减少衰老相关分泌表型（SASP）、抑制癌症干细胞（CSCs）增殖和阻碍肿瘤生长[3]。
在体外，TRi-1处理48小时显著抑制了B16-F10细胞和LLC细胞的增殖，IC50值分别为20µM和25µM[4]。使用1.25µM TRi-1处理LN229TAZ(4SA)细胞48小时，在无葡萄糖条件下显著诱导了细胞死亡[5]。
在体内，每日腹腔注射10mg/kg剂量的TRi-1，连续5天，随后停药2天，接着每周三次给药，持续两周，显著抑制了小鼠MDA-MB-231异种移植模型中的肿瘤体积，且未影响体重[6]。每三天腹腔注射一次TRi-1（10mg/kg），持续21天，显著降低了22月龄小鼠卵巢组织中的TXNRD1水平，并减少了IL-1β和C-X-C motif chemokine 15 (CXCL15)的表达[7]。
| 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 | Download SDF |
| 分子式 | C12H9ClN2O5S | 分子量 | 328.73 |
| 溶解度 | DMSO : 62.5 mg/mL (190.13 mM; Need ultrasonic) | 储存条件 | 4°C, protect from light |
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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 |
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2.
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