Biological Activity
Thioredoxin-1 (Trx-1) inhibitor; irreversibly inactivates Trx-1 as a substrate for reduction by thioredoxin reductase (TR); competitively inhibits the reduction of Trx-1 by TR (Ki = 30.8 μM). Attenuates expression of HIF-1α, VEGF and iNOS (IC50 values are 7.2, 10.4 and 18.1 μM respectively). Exhibits antitumor activity; directly inhibits tubulin in vitro and decreases tumor microvessel density in vivo.
Technical Data
| M. Wt | 188.31 |
| Formula | C7H12N2S2 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 141400-58-0 |
| PubChem ID | 219104 |
| InChI Key | BPBPYQWMFCTCNG-UHFFFAOYSA-N |
| Smiles | CC(CC)SSC1=NC=CN1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.83 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 188.31. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 5.31 mL | 26.55 mL | 53.1 mL |
| 5 mM | 1.06 mL | 5.31 mL | 10.62 mL |
| 10 mM | 0.53 mL | 2.66 mL | 5.31 mL |
| 50 mM | 0.11 mL | 0.53 mL | 1.06 mL |
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References
References are publications that support the products' biological activity.
Kirkpatrick et al (1998) Mechanisms of inhibition of the thioredoxin growth factor system by antitumor 2-imidazolyl disulfides. Biochem.Pharmacol. 55 987 PMID: 9605422
Welsh et al (2003) 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. 2 235 PMID: 12657718
Jordan et al (2005) 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. 11 529 PMID: 15701837
Keywords: PX 12, supplier, px12, thioredoxin-1, trx-1, inhibitors, inhibits, HIF-1alpha, HIF-1a, HIF-1α, IV-2, antiangiogenics, IV-2, Antiangiogenics, HIF, Hypoxia, Inducible, Factors, TrxR, TrxR, Tocris Bioscience
