Name: PX 12
Price: 193.00 USD

- Overview
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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].
    
    [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.
- Properties
  - Alternative Name
    
    2-(butan-2-yldisulfanyl)-1H-imidazole
    
    CAS Number
    
    141400-58-0
    
    Molecular Formula
    
    C7H12N2S2
    
    Molecular Weight
    
    188.31
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥8.75 mg/mL in DMSO; ≥99 mg/mL in EtOH
    
    Storage
    
    Store at 4°C
    
    * For Research Use Only
- Reference
  - 1. Yang J, Gong Y, et al. "Dysfunction of thioredoxin triggers inflammation through activation of autophagy in chicken cardiomyocytes." Biofactors. 2020;10.1002/biof.1625. PMID:32031748