Biochem/physiol Actions

Reversible: no

Primary TargetKeap1

Cell permeable: yes

General description

A cell-permeable chloro-quinolinone compound that selectively and covalently modifies Kelch-like ECH-associated protein 1 (Keap1)-Cys¹⁵¹ and represses Keap1 function and reduces Nrf2 (Nuclear factor erythroid 2-related factor 2)-Keap1 interaction. Shown to stabilize Nrf2 by inhibiting the Keap1-driven ubiquitination of Nrf2 and thereby activating the Nrf2-ARE (antioxidant response element) pathway (EC₅₀ = 2.7 µM in neuroblastoma IMR-32 cells). Offers protection against H₂O₂ induced oxidative stress, but unlike tert-butylhydroquinone (Cat. No. 286888). AI-1 does not act as a free radical scavenger. Its anti-oxidant effects are mediated via Nrf2 induced antioxidant response. Does not affect mutant ARE where GC are substituted with AT within the core ARE sequence.

A cell-permeable chloro-quinolinone compound that selectively and covalently modifies Kelch-like ECH-associated protein 1 (Keap1)-Cys¹⁵¹ and represses Keap1 function and reduces Nrf2 (Nuclear factor E2-related factor 2)-Keap1 interaction. Shown to stabilize Nrf2 by inhibiting the Keap1-driven ubiquitination of Nrf2 and thereby activating the Nrf2-ARE (antioxidant response element) pathway (EC₅₀ = 2.7 µM in neuroblastoma IMR-32 cells). Offers protection against H₂O₂ induced oxidative stress, but unlike tert-butylhydroquinone (Cat. No. 286888) AI-1 does not act as a free radical scavenger. Its anti-oxidant effects are mediated via Nrf2 induced antioxidant response. Does not affect mutant ARE where GC are substituted with AT within the core ARE sequence.

Legal Information

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

Other Notes

Hur, W., et al. 2010. Chem. Biol.17, 537.

Packaging

25 mg in Glass bottle

Packaged under inert gas

Reconstitution

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

Use only fresh DMSO for reconstitution.

Warning

Toxicity: Standard Handling (A)