TRi-1 是有效的、特异性的、不可逆的胞质硫氧还蛋白还原酶1 (TXNRD1) 的抑制剂，其 IC50 值为 12 nM。TRi-1 有抗肿瘤活性，且线粒体毒性很小。
货号:ajcx38916
CAS:246020-68-8
分子式:C12H9ClN2O5S
分子量：328.73
溶解度:DMSO : 62.5 mg/mL (190.13 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

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].

[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.