PMX 464 - CAS 485842-97-5
Category: Inhibitor
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PMX 464, a thiol-reactive quinol and putative thioredoxin inhibitor, is a putative inhibitor of the thioredoxin-thioredoxin reductase (Trx-TrxR) system, which shown to inhibit Trx and induce a G1/S block in HT29 cells, and inhibits cell proliferation in various colorectal cancer cell lines and MCF7 cells.
≥98% by HPLC
PMX464; PMX-464; PMX 464; 4-(2-Benzothiazolyl)-4-hydroxy-2,5-cyclohexadien-1-one
Store in a cool and dry place (or refer to the Certificate of Analysis).
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1.Targeting airway inflammation: PMX464 and the epithelial bulls eye.
Sexton DW Br J Pharmacol. 2008 Nov;155(5):620-2. doi: 10.1038/bjp.2008.290. Epub 2008 Jul 7.
Increasing evidence places the epithelial cell at the centre of inflammatory processes in human airways. Crucial to this function and the maintenance of inflammatory homoeostasis is a balanced oxidant-antioxidant status in the airway, in part controlled by thioredoxin and thioredoxin reductase, which together can alter the NF-kappaB pathway. PMX464, a thiol-reactive quinol and putative thioredoxin inhibitor, has been investigated in endothelial cells, fibroblasts and colorectal cancer cell lines but in the present issue of the BJP, these investigations were extended to A549 airway epithelial cells. Thioredoxin inhibition was confirmed as was NF-kappaB and IKK suppression but siRNA knockdown of thioredoxin did not alter inflammatory marker expression or activity, suggesting that PMX464 has targets other than thioredoxin. Future consolidation of this evidence will involve concomitant knockdown of thioredoxin reductase, the use of primary airway epithelial cells and, potentially, the employment of three-dimensional (3D) culture systems for both A549 and primary cells.
2.Heteroaromatic 4-arylquinols are novel inducers of nuclear factor-erythroid 2-related factor 2 (Nrf2).
Wong DP;Wells G;Hagen T Eur J Pharmacol. 2010 Sep 25;643(2-3):188-94. doi: 10.1016/j.ejphar.2010.06.040. Epub 2010 Jun 30.
The induction of phase 2 and antioxidant enzymes via the transcription factor Nuclear factor-erythroid 2-related factor 2 (Nrf2) is an important chemopreventive strategy in cancer and neurodegenerative diseases. Nrf2 is mainly regulated at the level of its protein stability by the cytosolic protein Keap1, which functions as a substrate recruiting subunit of a Cullin3 E3 ubiquitin ligase to target Nrf2 for ubiquitination and subsequent degradation. Phase 2 inducing agents usually covalently modify cysteine residues in Keap1, leading to inhibition of Nrf2 ubiquitination. Quinols, which due to their Michael acceptor moiety react readily with cysteine residues in selective cellular proteins, are good candidates for potential Nrf2 inducing chemopreventive agents. Indeed, we found that similar to the known phase II inducer sulforaphane, the heteroaromatic 4-arylquinols PMX290 and PMX464 increase both Nrf2 protein concentrations and transcriptional activity. Interestingly, PMX290 had a much stronger effect on the Nrf2 protein concentration, but a weaker effect on Nrf2 transcriptional activity compared to PMX464. Given the marked effect of PMX290 on the Nrf2 protein concentration, we examined its effect on the interaction of Keap1 with its binding partners.
3.PMX464, a thiol-reactive quinol and putative thioredoxin inhibitor, inhibits NF-kappaB-dependent proinflammatory activation of alveolar epithelial cells.
Callister ME;Pinhu L;Catley MC;Westwell AD;Newton R;Leaver SK;Quinlan GJ;Evans TW;Griffiths MJ;Burke-Gaffney A Br J Pharmacol. 2008 Nov;155(5):661-72. doi: 10.1038/bjp.2008.258. Epub 2008 Jun 30.
BACKGROUND AND PURPOSE: ;Subtle changes in the intracellular reduction-oxidation (redox) state can modulate nuclear factor-kappaB (NF-kappaB) activity. Thioredoxin-1 (Trx) is a small, ubiquitous, redox-active thiol (-SH) protein that, with thioredoxin reductase-1 (TrxR), modifies the redox status of NF-kappaB pathway components. PMX464 is a novel thiol-reactive quinol thought to inhibit the Trx/TrxR system. The aim of this work was to investigate whether PMX464 inhibited NF-kappaB-mediated proinflammatory activation of human type II alveolar epithelial cells (A549).;EXPERIMENTAL APPROACH: ;Intercellular adhesion molecule-1 (ICAM-1), granulocyte-macrophage colony-stimulating factor (GM-CSF) and CXCL8, NF-kappaB DNA binding, nuclear translocation of NF-kappaB p65 subunit, IkappaBalpha degradation, IkappaB phosphorylation and IkappaB kinase (IKK) activity were assessed in A549 cells stimulated with IL-1beta with or without PMX464 pretreatment. Effects of PMX464 on ICAM-1 expression in human lung microvascular endothelial cells (HLMVEC) were also investigated. For comparison, selected measurements (ICAM-1 and IkappaB-alpha phospho-IkappaB-alpha) were made on A549 cells after RNA interference-mediated silencing (siRNA) of Trx.
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CAS 485842-97-5 PMX 464

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