TRi-1 |
Katalog-Nr.GC65101 |
TRi-1 ist ein potenter, spezifischer und irreversibler Inhibitor der zytosolischen Thioredoxinreduktase 1 (TXNRD1) mit einem IC50 von 12 nM. TRi-1 hat eine geringe mitochondriale ToxizitÄt fÜr die Krebstherapie.
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Cas No.: 246020-68-8
Sample solution is provided at 25 µL, 10mM.
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.
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