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.
别名:
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
方案
≥98% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
off-white
溶解性
DMSO: 50 mg/mL
储存温度
2-8°C
一般描述
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 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.
制备说明
Following reconstitution, aliquot and freez e(-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Kimura, H., et al. 2010. Chem. Biol.17, 1282.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Regulatory Review (Z)
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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