TrxR inhibitor D9
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.
For research use only. We do not sell to patients.
- CAS No.: 1527513-89-8
- Formula: C25H20AuOPS
- Molecular Weight:596.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
EC50: 2.8 nM (TrxR)[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 and HT-29 cells
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Concentration:0.1, 0.5, 1 μM
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Incubation Time:72 hours
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Result:Killed 70% MCF-7 cells and 50% HT-29 cells with the concentration as low as 0.1 μM.
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Cell Line:MCF-7 cells
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Concentration:0.8 μM
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Incubation Time:4 and 8 hours
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (17-18 g) bearing a MCF-7 tumor[1]
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Dosage:5 mg/kg
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Administration:I.v. once every 2 days for 15 days
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Result:Inhibited tumor growth with IR (inhibition ratio) of 91.5% and was well tolerated.
Chemical Information
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CAS No. 1527513-89-8
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Molecular Weight 596.43
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Formula C25H20AuOPS
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SMILES
COC1=CC=C(C=C1)C#[C-][Au+][P](C2=CC=CC=C2)(C3=CC=CC=C3)C4=CC=CS4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TrxR inhibitor D9 Related Classifications
HY-136279 Related Classifications
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