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PX 12 (CAS 141400-58-0) LS-H94

Thioredoxin 1 inhibitor
LS-H94-1 / 1 mg / $175
LS-H94-5 / 5 mg / $205
LS-H94-10 / 10 mg / $225
USA Shipment Only
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Description: PX 12 is a competitive, irreversible inhibitor of thioredoxin 1 (Trx1), acting by binding to Cys73 of this enzyme. As Trx1 is overexpressed in certain cancers, PX 12 is effective in suppressing the growth of cancer cells, with growth inhibition in a panel of 60 human tumors significantly correlated with expression of Trx1 mRNA. Through its effects on Trx1, PX 12 reduces hypoxia-induced HIF-1 alpha protein levels (IC50 = 7.2 µM), as well as expression of VEGF (IC50 = 10.4 µM) and iNOS (IC50 = 18.1 µM), culminating in attenuation of the proliferation of MCF-7 cells (IC50 = 1.9 µM) and HT-29 cells (IC50 = 2.9 µM) as well as reduced microvessel density in MCF-7 tumor xenografts. PX 12 also blocks Trx-mediated activation of extracellular transglutaminase 2 (IC50 = ~3 µM) and Trx-1-increased expression and translation of CYP1B1. H94_ChemicalStructureImage.png
2-[(1-methylpropyl)dithio]-1H-imidazole
 
biochemical, chemical, inhibitor
LS-H94
141400-58-0
C7H12N2S2
≥98%
A crystalline solid
 
CC(CC)SSC1=NC=CN1
InChI=1S/C7H12N2S2/c1-3-6(2)10-11-7-8-4-5-9-7/h4-6H,3H2,1-2H3,(H,8,9)
BPBPYQWMFCTCNG-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: TXN / Thioredoxin / TRX related products

Usage Information

PX 12 is supplied as a crystalline solid. A stock solution may be made by dissolving the PX 12 in the solvent of choice. PX 12 is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide, which should be purged with an inert gas. The solubility of PX 12 in these solvents is approximately 20, 14, and 16 mg/ml, respectively. PX 12 is sparingly soluble in aqueous solutions. To enhance aqueous solubility, dilute the organic solvent solution into aqueous buffers or isotonic saline. If performing biological experiments, ensure the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Oblong, J.E., Chantler, E.L., Gallegos, A., et al. Reversible inhibition of human thioredoxin reductase activity by cytotoxic alkyl 2-imidazolyl disulfide analogues. Cancer Chemother. Pharmacol. 34, 434-438 (1994).
  2. Powis, G. and Montfort, W.R. Properties and biological activities of thioredoxins. Annu. Rev. Biophys. Biomol. Struct. 30, 421-455 (2001).
  3. Mukherjee, A. and Martin, S.G. The thioredoxin system: A key target in tumour and endothelial cells. Br. J. Radiol. 81, S57-S68 (2008).
  4. Welsh, S.J., Williams, R.R., Birmingham, A., et al. The thioredoxin redox inhibitors 1-methylpropyl 2-imidazolyl disulfide and pleurotin inhibit hypoxia-induced factor 1α and vascular endothelial growth factor formation. Mol. Cancer Ther. 2(3), 235-243 (2003).
  5. Jin, X., Stamnaes, J., Klöck, C., et al. Activation of extracellular transglutaminase 2 by thioredoxin. J. Biol. Chem. 286(43), 37866-37873 (2011).

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