A competitive

PX 12 – 1 mg

Brand:
Cayman
CAS:
141400-58-0
Storage:
-20
UN-No:
Non-Hazardous - /

PX 12 is a competitive, irreversible inhibitor of thioredoxin 1 (Trx1), acting by binding to Cys73 of this enzyme.{22315} 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.{22325,22314} 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.{22317} PX 12 also blocks Trx-mediated activation of extracellular transglutaminase 2 (IC50 = ~3 μM) and Trx-1-increased expression and translation of CYP1B1.{22313,22312}  

 

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Description

A competitive, irreversible inhibitor of Trx1; effective in suppressing the growth of cancer cells, with inhibition correlated with expression of Trx1 mRNA; reduces hypoxia-induced HIF-1α protein levels (IC50 = 7.2 μM) and expression of VEGF and iNOS; reduces microvessel density in MCF-7 tumor xenografts

Formal name: 2-[(1-methylpropyl)dithio]-1H-imidazole

Synonyms: 

Molecular weight: 188.3

CAS: 141400-58-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Transcription Factors|HIF-1α||Research Area|Cancer|Tumor Microenvironment

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