A cell-permeable benzothiazinone that is shown to interact with MIF homotrimer (=68.6nM and 157nM 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] = 30uM) due to reduced MIF binding at acidic pH. Shown to protect primary rat cardiomyocytes (330nM) from apoptotic death upon serum deprivation or DOX (200nM) treatment via activation of ARE- (antioxidant response element) mediated cytoprotective genes transcription in a MIF-dependent manner.
Molecular Formula:C₁₃H₈N₂OS
Molecular Weight:240.3
Solubility:DMSO (50mg/ml)
Storage and Stability:Store at -20°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
