PX 12

PX 12 is a competitive, irreversible inhibitor of thioredoxin 1 (Trx1), acting by binding to Cys73 of this enzyme. 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. Through its effects on Trx1, PX 12 reduces hypoxia-induced HIF-1alpha 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. PX 12 also blocks Trx-mediated activation of extracellular transglutaminase 2 (IC50 = ~3 µM) and Trx-1-increased expression and translation of CYP1B1.Formal Name: 2-[(1-methylpropyl)dithio]-1H-imidazole. CAS Number: 141400-58-0. Molecular Formula: C7H12N2S2. Formula Weight: 188.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 16 mg/ml, DMSO: 14 mg/ml, Ethanol: 20 mg/ml. lambdamax: 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.