Nrf2 Activator IV, VSC2-Calbiochem

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一般描述

A cell-permeable vinylsulfone that acts as a more potent Nrf-2 activator than the chalcones (e.g. Cat. No. 492040) in stimulating HO-1 expression in murine microglial BV-2 cultures (3.82-fold of control in 24 h; 20 ?M). Shown to induce overall Nrf2 cellular accumulation & nuclear translocation (1 to10 ?M) in murine dopaminergic CATH.a cultures, presumably by freeing Nrf2 from its negative regulator keap1, with concomitant upregulation of Nrf2-regulated antioxidant enzymes expression, effectively protecting CATH.a against BH4 toxicity (effective conc. 0.1 to 1.0 ?M against 200 ?M BH4; 24 h)in vitroand preventing MPTP- (Cat. No. 506382) induced motor dysfunctions and neurodegeneration in a murine PD modelin vivo(3X 10 mg drug/kg/d p.o.; 4X 20 mg MPTP/kg/2 h i.p.).
A cell-permeable vinylsulfone compound that acts as a more potent Nrf-2 activator than the analogous α,β-unsaturated ketone-based chalcones (e.g. Cat. No. 492040) in stimulating HO-1 expression in murine microglial BV-2 cultures (382% of control protein level in 24 h; 20 ?M). Drug treatment in murine dopaminergic (DAergic) CATH.a cultures likewise effectively induces Nrf2 nuclear translocation (Fold of control in 3 h/dose = 1.4/1 ?M, 2.3/5 ?M, 3.4/10 ?M) and overall Nrf2 cellular accumulation (Fold of control in 24 h/dose = 1.5/0.5 ?M, 2.0/1 ?M, 2.8/2 ?M, 4.3/5 ?M), presumably by freeing Nrf2 from its negative regulator keap1, with concomitant upregulation of Nrf2-regulated antioxidant enzymes expression, including heme oxygenase-1/OH-1, NAD(P)H quinone oxidoreductase 1/NQO1, glutamate-cysteine ligase modifier & catalytic subunits, QCLM & GCLC. Shown to protect CATH.a against BH4 toxicity (effective conc. 0.1 to 1.0 ?M against 200 ?M BH4 for 24 h)in vitroand prevent MPTP- (Cat. No. 506382) induced motor deficits/dysfunctions (by vertical grid test 6 d post MPTP injection) and neurodegeneration (by TH staining 7 d post MPTP injection) in a murine PD modelin vivo(3 X 10 mg drug/kg/d oral dosages; 4X 20 mg MPTP/kg/2 h i.p. dosages starting 24 h post the 1st drug dosage).

生化/生理作用

Cell permeable: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Use only fresh DMSO for reconstitution.

其他说明

Lee, J.A., et al. 2015.Br. J. Pharmacol.172,1087.
Woo, S.Y., et al. 2014.J. Med. Chem.57,1473.

法律信息

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

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