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PX 12

In stock
Catalog No.
A4509
Trx-1 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$50.00
In stock
10mg
$136.00
In stock
50mg
$536.00
In stock

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Background

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.

Chemical Properties

StorageStore at 4°C
M.Wt188.31
Cas No.141400-58-0
FormulaC7H12N2S2
Solubility≥8.75mg/mL in DMSO, ≥99 mg/mL in EtOH, <2.5 mg/mL in H2O
Chemical Name2-(butan-2-yldisulfanyl)-1H-imidazole
SDFDownload SDF
Canonical SMILESCCC(C)SSC1=NC=CN1
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

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