ARE Activator, BTZO-1 - Calbiochem

General Description

A cell-permeable benzothiazinone that is shown to interact with MIF homotrimer (Kd = 68.6 nM and 157 nM toward human and rat MIF, respectively, at pH 7.3) via the N-terminal proline in a pH-dependent manner, limiting its inhibitory capability against MIF tautomerase activity (13% inhibition at pH 6.0; [BTZO-1] = 30 μM) due to reduced MIF binding at acidic pH. Shown to protect primary rat cardiomyocytes (330 nM) from apoptotic death upon serum deprivation or DOX (200 nM; Cat. No. 324380) treatment via activation of ARE- (antioxidant response element) mediated cytoprotective genes transcription in a MIF-dependent manner.