| Bioactivity | TRi-1 is a potent, specific and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1), with an IC50 of 12 nM. TRi-1 has little mitochondrial toxicity for anticancer therapy[1]. |
| Target | IC50: 12 nM (TXNRD1). |
| Invitro | TRi-1 (0.679 and 6.79 μM; 6 h) has no effect on cellular glutathione (GSH) concentrations in FaDu cells, efficiently activates JNK and p38 phosphorylation[1].TRi-1 (2 μM) irreversibly inhibit TXNRD1 in an NADPH-dependent manner[1].TRi-1 (0.1-10 μM; 0-10 h) increases cellular H2O2 production in cultured FaDu cells in a concentration- and time-dependent manner[1].TRi-1 (10 nM-100 μM; 48 h) shows cytotoxicity toward cancer cells[1]. Western Blot Analysis[1] Cell Line: |
| In Vivo | TRi-1 (10 mg/kg; i.v.; twice a day for 4 days or 5 mg/kg; i.p.; twice a week for 3 weeks) impaires growth and viability of human tumor xenografts and syngeneic mouse tumors[1]. Animal Model: |
| Name | TRi-1 |
| CAS | 246020-68-8 |
| Formula | C12H9ClN2O5S |
| Molar Mass | 328.73 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [1]. Stafford WC, et al. Irreversible inhibition of cytosolic thioredoxin reductase 1 as a mechanistic basis for anticancer therapy. Sci Transl Med. 2018 Feb 14;10(428). pii: eaaf7444. |