181315-M

ARE Activator, BTZO-1

The ARE Activator, BTZO-1 modulates the biological activity of ARE. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): ARE Activator, BTZO-1, 2-Pyridin-2-yl-4H-1,3-benzothiazin-4-one, Antioxidant Response Element Activator, Macrophage Migration Inhibitory Factor Antagonist II, MIF Antagonist II, Macrophage Migration Inhibitory Factor Antagonist II, MIF Antagonist II, 2-Pyridin-2-yl-4H-1,3-benzothiazin-4-one, Antioxidant Response Element Activator
• Empirical Formula (Hill Notation): C₁₃H₈N₂OS
• Molecular Weight: 240.28
• UNSPSC Code: 12352200

Properties

• Assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 50 mg/mL
• storage temp.: 2-8°C

Description

General description

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.

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.

Warning

Toxicity: Regulatory Review (Z)

Reconstitution

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

Other Notes

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

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable