ARE Activator, BTZO-1

A cell-permeable benzothiazinone that is shown to interact with MIF homotrimer (K_d = 68.6 nM and 157 nM toward human and rat MIF, respectively, at pH 7.3) via the N-terminal proline of each subunit in a pH-dependent manner, limiting its inhibitory capability against MIF tautomerase activity at acidic pH (13% inhibition at pH 6.0; [BTZO-1] = 30 µM) due to reduced MIF binding at acidic pH. Shown to prevent primary rat cardiomyocyte apoptotic death upon serum deprivation (2.38-fold of no-drug control survival rate after 4 days; [BTZO-1] = 330 nM) or DOX (200 nM; Cat. No. 324380) treatment (95% vs. 40% viability after 18 h, respectively, with or without 330 nM BTZO-1) via activation of ARE- (antioxidant response element) mediated cytoprotective genes transcription (5.3- and 3.6-fold, respectively, of control STS Ya and HO-1 mRNA after 24 h; [BTZO-1] = 1 µM) in a MIF-dependent manner.

Following reconstitution, aliquot and freez e(-20°C). Stock solutions are stable for up to 6 months at -20°C.

Kimura, H., et al. 2010. Chem. Biol.17, 1282.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Regulatory Review (Z)