An irreversible inhibitor of thioredoxin-1
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PX 12

Item No. 14192

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(1-methylpropyl)dithio]-1H-imidazole
CAS Number
141400-58-0
Molecular Formula
C7H12N2S2
Formula Weight
188.3
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 16 mg/mlDMSO: 14 mg/mlEthanol: 20 mg/ml
λmax
235 nm
SMILES
CC(CC)SSC1=NC=CN1
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)
InChi Key
BPBPYQWMFCTCNG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $77

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    10 mg

    $120

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    Cayman Chemical
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    Product Description

    PX 12 is a competitive, irreversible inhibitor of thioredoxin 1 (Trx1), acting by binding to Cys73 of this enzyme.1 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.2,3 Through its effects on Trx1, PX 12 reduces hypoxia-induced HIF-1α 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.4 PX 12 also blocks Trx-mediated activation of extracellular transglutaminase 2 (IC50 = ~3 μM) and Trx-1-increased expression and translation of CYP1B1.5,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description 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. The Journal of Biological Chemisty 286(43), 37866-37873 (2011).

    6. Husbeck, B., and Powis, G. The redox protein thioredoxin-1 regulates the constitutive and inducible expression of the estrogen metabolizing cytochromes P450 1B1 and 1A1 in MCF-7 human breast cancer cells. Carcinogenesis 23(10), 1625-1630 (2002).

    Product Citations

    Cao, W., Cho, C.-C.D., Geng, Z.Z., et al. Evaluation of SARS-CoV-2 main protease inhibitors using a novel cell-based assay. ACS Cent. Sci. 8(2), 192-204 (2022).