Back to your search result

Description

A cell-permeable VAS2870 (Cat No. 492000) analogue that displays improved solubility and effectively blocks ROS production in DMSO-differentiated HL-60 cultures upon oxidative burst induction by PMA (IC50 = 1 µ,M by Cytochrome C reduction & 2 µ,M by L012 chemiluminescence, Drug added 30 min prior to 100 nM PMA/500582 & 524400) via NADPH oxidases/NOX inhibition, while displaying no potency against eNOS or xanthine oxidase/XOD enzymatic activity in cell-free assays even at a high concentration of 100 µ,M. Reported to suppress the high ROS level in isolated thoracis aortas sections from spontaneously hypertensive rats (SHRs) in situ (by 66% with 10 µ,M) and synergize with Imatinib (Cat. No. 504595) against the proliferation of p210 Bcr-abl-expressing murine Boff 210 cultures. A commonly employed NOX inhibitor Apocynin (Cat. No. 178385), in comparison, is shown to interfere with L012-based assays and exhibit little potency against NOX-mediated ROS production in DMSO-differentiated HL-60 cultures (by Cytochrome C reduction) or in cell-free assays using A7r5 & CaCo-2 homogenates (IC50 >1 mM), while another NOX inhibitor DPI (Cat. No. 300260) is shown to inhibit both eNOS & XOD activities., A cell-permeable triazolo-pyrimidine derivative of VAS2870 (Cat. No. 492000) that displays enhanced solubility and acts as a selective inhibitor NOX family of NADPH oxidase. Shown to inhibit NOX activity in CaCo-2 cells (expressing NOX 1, 2, 4, and 5, IC50 = 12 µ,M), HL-60 cells (mainly expressing NOX2, IC50 = 2 µ,M), and A7r5 cells (mainly expressing NOX3 and 4, IC50 = 13 µ,M). Does not affect the activities of xanthine oxidase and endothelial nitric oxide synthase (eNOS) even at higher concentrations (~100 µ,M). Acts synergistically with Imatinib (Cat. No. 504595) to reduce the proliferation of chronic myeloid leukemia (CML) cells.Please note that the molecular weight for this compound is batch-specific due to variable water content.