TrxR inhibitor D9

CAS: 1527513-89-8 F: C25H20AuOPS W: 596.43

TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhi

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Bioactivity	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].
Target	EC50: 2.8 nM (TrxR)
Invitro	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:
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:
Name	TrxR inhibitor D9
CAS	1527513-89-8
Formula	C25H20AuOPS
Molar Mass	596.43
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

Antitumor agent-76