PX 12
Catalogue Number: A4509-APE
| Manufacturer: | Apexbio |
| Type: | Other Inhibitors |
| Shipping Condition: | Blue Ice |
| Storage Condition: | 2-8°C |
| Unit(s): | 10 mg, 10 mM (in 1mL DMSO), 50 mg |
Description
Description: 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-1α 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.
Additional Text
Storage Note
Store at 4°C
Short Description
Trx-1 inhibitor
Reagent:Smile String
CCC(C)SSC1=NC=CN1
Solubility
insoluble in H2O; ≥8.75 mg/mL in DMSO; ≥99 mg/mL in EtOH
A4509 Datasheet
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