| Biological Activity | px 12 is an inhibitor of thioredoxin-1 [1].thioredoxin-1 (trx-1) is a small redox protein with a conserved catalytic site and plays an important role in cells that includes the regulation of trans-activating activity and the dna binding of redox-sensitive transcription factors [1].in ht-29 human colon carcinoma cells and mcf-7 human breast cancer, px 12 prevented the hypoxia-induced increase in hif-1 protein. also, px 12 decreased inducible nitric oxide synthase, hif-1-trans-activating activity and vegf formation [2].in immunodeficient mice bearing ht-29 human colon xenografts, px 12 decreased the average tumor blood vessel permeability by 63% within 2 hours and returned to pretreatment values after 48 hours. px 12 reduced tumor-derived vegf and tumor after 24 hours. also, trx-1 showed a rapid decrease within 2 hours and maintained for 24 hours [1]. in mice bearing mcf-7 tumor xenografts, px 12 reduced hif-1ɑ and vegf protein levels [2]. in cancer patients, px-12 treatment significantly reduced the levels of trx-1 and vegf in plasma [3]. |
| references | [1]. jordan bf, runquist m, raghunand n, et al. the thioredoxin-1 inhibitor 1-methylpropyl 2-imidazolyl disulfide (px-12) decreases vascular permeability in tumor xenografts monitored by dynamic contrast enhanced magnetic resonance imaging. clin cancer res, 2005, 11(2 pt 1): 529-536.[2]. welsh sj, williams rr, birmingham a, et al. the thioredoxin redox inhibitors 1-methylpropyl 2-imidazolyl disulfide and pleurotin inhibit hypoxia-induced factor 1alpha and vascular endothelial growth factor formation. mol cancer ther, 2003, 2(3): 235-243.[3]. baker af, dragovich t, tate wr, et al. the antitumor thioredoxin-1 inhibitor px-12 (1-methylpropyl 2-imidazolyl disulfide) decreases thioredoxin-1 and vegf levels in cancer patient plasma. j lab clin med, 2006, 147(2): 83-90. |
![2-[(1-Methylpropyl)dithio]-1H-imidazole](/img/141400-58-0.jpg "2-[(1-Methylpropyl)dithio]-1H-imidazole")
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