485842-97-5
Chemical Structure
PMX464
Synonym(s): AW 464
- CAS. Nr.: 485842-97-5
- Formula:C13H9NO2S
- Molecular Weight:243.28
IUPAC Name: 4-(benzo[d]thiazol-2-yl)-4-hydroxycyclohexa-2,5-dien-1-one
InChIKey: SDYBYKXWYDVVKP-UHFFFAOYSA-N
SMILES: O=C1C=CC(O)(C2=NC3=CC=CC=C3S2)C=C1
Biological Activity: PMX464 (AW 464) is a thiol-reactive quinol compound and an inhibitor of the thioredoxin-thioredoxin reductase (Trx/TrxR) system, with an IC50 value of 6.5 μM against TrxR. PMX464 acts by irreversibly inhibiting the thioredoxin (Trx-1) system, blocking HIF-1α transcriptional activation and the NF-κB inflammatory pathway, inducing apoptosis, attenuating platelet function and inhibiting thrombosis, and specifically disrupting the trypanothione antioxidant metabolic network in parasites. PMX464 is used in research concerning malignant tumors (colorectal cancer, breast cancer, renal cancer, and leukemia), pulmonary inflammation, African sleeping sickness, and antithrombotic applications[1][2][3][4][5][6][7].
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PMX464 | PMX464 (AW 464) is a thiol-reactive quinol compound and an inhibitor of the thioredoxin-thioredoxin reductase (Trx/TrxR) system, with an IC50 value of 6.5 μM against TrxR. PMX464 acts by irreversibly inhibiting the thioredoxin (Trx-1) system, blocking HIF-1α transcriptional activation and the NF-κB inflammatory pathway, inducing apoptosis, attenuating platelet function and inhibiting thrombosis, and specifically disrupting the trypanothione antioxidant metabolic network in parasites. PMX464 is used in research concerning malignant tumors (colorectal cancer, breast cancer, renal cancer, and leukemia), pulmonary inflammation, African sleeping sickness, and antithrombotic applications. | |||||||||||||||||||||
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- [1]. Jones DT, et al. Novel thioredoxin inhibitors paradoxically increase hypoxia-inducible factor-alpha expression but decrease functional transcriptional activity, DNA binding, and degradation. Clin Cancer Res. 2006 Sep 15;12(18):5384-94. [Content Brief]
- [2]. Pallis M, et al. Induction of apoptosis without redox catastrophe by thioredoxin-inhibitory compounds. Biochem Pharmacol. 2003 Nov 1;66(9):1695-705. [Content Brief]
- [3]. Mukherjee A, et al. A cellular and molecular investigation of the action of PMX464, a putative thioredoxin inhibitor, in normal and colorectal cancer cell lines. Br J Pharmacol. 2007 Aug;151(8):1167-75. [Content Brief]
- [4]. Callister ME, et al. PMX464, a thiol-reactive quinol and putative thioredoxin inhibitor, inhibits NF-kappaB-dependent proinflammatory activation of alveolar epithelial cells. Br J Pharmacol. 2008 Nov;155(5):661-72. [Content Brief]
- [5]. König J, et al. Antitumor quinol PMX464 is a cytocidal anti-trypanosomal inhibitor targeting trypanothione metabolism. J Biol Chem. 2011 Mar 11;286(10):8523-8533. [Content Brief]
- [6]. Chew EH, et al. Thioredoxin reductase inhibition by antitumor quinols: a quinol pharmacophore effect correlating to antiproliferative activity. FASEB J. 2008 Jun;22(6):2072-83. [Content Brief]
- [7]. Metcalfe C,et al. Thioredoxin Inhibitors Attenuate Platelet Function and Thrombus Formation. PLoS One. 2016 Oct 7;11(10):e0163006. [Content Brief]
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