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    InvivoChem Cat #: V1865
    CAS #: 141400-58-0 Purity ≥98%

    Description: PX-12 is an investigational antitumor agent acting as a potent thioredoxin-1 (Trx-1) inhibitor by irreversibly thioalkylating Cys73 of Trx-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. 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. 

    References: Mol Cancer Ther. 2003 Mar;2(3):235-43; Cancer Chemother Pharmacol. 2011 Aug;68(2):405-13. 

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    Molecular Weight (MW)188.31 
    CAS No.141400-58-0 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 38 mg/mL (201.8 mM) 
    Water: <1 mg/mL
    Ethanol: 38 mg/mL (201.8 mM) 
    Other info

    Chemical Name: 2-(sec-butyldisulfanyl)-1H-imidazole.


    InChi Code: InChI=1S/C7H12N2S2/c1-3-6(2)10-11-7-8-4-5-9-7/h4-6H,3H2,1-2H3,(H,8,9)

    SMILES Code: CCC(SSC1=NC=CN1)C           

    SynonymsPX12; PX 12; PX-12

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    In Vitro

    In vitro activity: In MCF-7 and HT-29 cells, PX-12 prevents the hypoxia (1% oxygen)-induced increase in HIF-1alpha protein, and decreases HIF-1-trans-activating activity, VEGF formation, and inducible nitric oxide synthase. PX-12 also inhibits the growth of MCF-7 and HT-29 cells with IC50s of 1.9 μM and 2.9μM, respectively. PX-12 also inhibits HIF-1α protein levels through an Nrf2/PMF-1-mediated increase. In A549 cells, PX-12 inhibits cell growth via G2/M phase arrest, and Bax-mediated and ROS-dependent apoptosis. In hepatocelluar carcinoma cells, PX-12 exerts a synergistic effect with 5-FU to significantly suppress tumorigenicity.

    Cell Assay: Cell growth is measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Cells are exposed to a range of concentrations of PX-12 or pleurotin for 16 h in air or hypoxia (1% oxygen). The cells are then washed with warm drug-free medium and grown in air for the remainder of the 72-h incubation.

    In VivoIn mice bearing MCF-7 tumor xenografts, PX-12 (12 mg/kg, i.p.) decreases HIF-1α and VEGF protein levels and microvessel density. 
    Animal modelMice bearing MCF-7 tumor xenografts 
    Formulation & DosageDissolved in 0.01 N HCl, polyethylene glycol-400 (2.0 mg/ml); 12 mg/kg; i.p. 

    Mol Cancer Ther. 2003 Mar;2(3):235-43; Cancer Chemother Pharmacol. 2011 Aug;68(2):405-13.  

    These protocols are for reference only. InvivoChem does not independently validate these methods.


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