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TrxR inhibitor D9
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。
TrxR inhibitor D9 Chemical Structure
CAS No. : 1527513-89-8
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
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].
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IC50 & Target |
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体外研究
(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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
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体内研究
(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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Zhang D, et, al. Synthesis and molecular recognition studies on small-molecule inhibitors for thioredoxin reductase. J Med Chem. 2014 Oct 9;57(19):8132-9.
[2]. Lin YX, et, al. pH-Sensitive Polymeric Nanoparticles with Gold(I) Compound Payloads Synergistically Induce Cancer Cell Death through Modulation of Autophagy. Mol Pharm. 2015 Aug 3;12(8):2869-78.
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