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.

Product information

CAS Number: 1527513-89-8

Molecular Weight: 597.44

Formula: C25H21AuOPS

Chemical Name: 1-ethynyl-4-methoxybenzene diphenyl(thiophen-2-yl)phosphane gold

Smiles: [Au].COC1C=CC(=CC=1)C#C.C1=CC=C(S1)P(C1C=CC=CC=1)C1C=CC=CC=1

InChiKey: HWIUTLSXZCXKKH-UHFFFAOYSA-N

InChi: InChI=1S/C16H13PS.C9H8O.Au/c1-3-8-14(9-4-1)17(16-12-7-13-18-16)15-10-5-2-6-11-15;1-3-8-4-6-9(10-2)7-5-8;/h1-13H;1,4-7H,2H3;

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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 significantly affects 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 significantly 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) effectively inhibits the growth of tumors in mice.

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.
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.

Products are for research use only. Not for human use.