1. Apoptosis
  2. Apoptosis
  3. TrxR inhibitor D9

TrxR inhibitor D9 

目录号: HY-136279

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。

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TrxR inhibitor D9 Chemical Structure

TrxR inhibitor D9 Chemical Structure

CAS No. : 1527513-89-8

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TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo[1][2].

IC50 & Target

EC50: 2.8 nM (TrxR)[1]

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[1].
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 significantly affects normal cells viability[1].
TrxR inhibitor D9 (0.8 μM; 4 and 8 h) induces HT-29 cells necrosis/apoptosis[1].
TrxR inhibitor D9 (2-20 nM; 1-60 s) inhibits TrxR activity in a concentration-dependent manner[1].
TrxR inhibitor D9 (1-1000 nM) does not significantly inhibits the catalytic activity of glutathione reductase (GR) even when the concentration increases to more than 1000 nM[1].
TrxR inhibitor D9 (0.4 μM) could effectively avoid the ligand exchange with albumin[1].

Cell Proliferation Assay[1]

Cell Line: MCF-7 and HT-29 cells
Concentration: 0.1, 0.5, 1 μM
Incubation Time: 72 hours
Result: Killed 70% MCF-7 cells and 50% HT-29 cells with the concentration as low as 0.1 μM.

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.8 μM
Incubation Time: 4 and 8 hours
Result: Led to more than 50% necrosis/apoptosis of cells compared to control after 4 h of treatment.
Induced all cells necrosis/apoptosis after 8 h of incubation.
In Vivo

TrxR inhibitor D9 (5 mg/kg; i.v. once every 2 d for 15 d) effectively inhibits the growth of tumors in mice[1].

Animal Model: BALB/c nude mice (17-18 g) bearing a MCF-7 tumor[1]
Dosage: 5 mg/kg
Administration: I.v. once every 2 days for 15 days
Result: Inhibited tumor growth with IR (inhibition ratio) of 91.5% and was well tolerated.
Molecular Weight









Room temperature in continental US; may vary elsewhere.


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