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TrxR inhibitor D9

CAS No. : 1527513-89-8

MCE 站：TrxR inhibitor D9

产品活性：TrxR inhibitor D9 是一种有效和选择性的硫氧还蛋白还原酶 (TrxR) 的抑制剂，EC₅₀ 值为 2.8 nM。TrxR inhibitor D9 具有在体外和体内抑制肿瘤增殖的能力。

研究领域：Apoptosis

作用靶点：Apoptosis

In Vitro: TrxR inhibitor D9 (0.1-1 μM; 72 h) inhibits the cell proliferation with IC₅₀s of 0.03 and 0.1 μM for MCF-7 and HT-29 cells, respectively.
TrxR inhibitor D9 (72 h) completely inhibits all cancer cells (A549, KB, MDA MB-231, HeLa, MCF-7 and HT-29) viability at the concentration of 0.60 μM, and the IC₅₀s of all cancer cells could be as low as 0.55 μM, and dose not signi?cantly a?ects normal cells viability.
TrxR inhibitor D9 (0.8 μM; 4 and 8 h) induces HT-29 cells necrosis/apoptosis.
TrxR inhibitor D9 (2-20 nM; 1-60 s) inhibits TrxR activity in a concentration-dependent manner.
TrxR inhibitor D9 (1-1000 nM) does not signi?cantly inhibits the catalytic activity of glutathione reductase (GR) even when the concentration increases to more than 1000 nM.
TrxR inhibitor D9 (0.4 μM) could effectively avoid the ligand exchange with albumin.

In Vivo: TrxR inhibitor D9 (5 mg/kg; i.v. once every 2 d for 15 d) e?ectively inhibits the growth of tumors in mice.

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