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492041 Nrf2 Activator II, AI-1 - CAS 75483-04-4 - Calbiochem

The Nrf2 Activator II, AI-1, also referenced under CAS 75483-04-4, modulates the biological activity of Nrf2. This small molecule/inhibitor is primarily used for Biochemicals applications.

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Synonyme: Ethyl-4-chloro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxylate

Primary Target: Keap1
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      Übersicht

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      75483-04-4C13H₁₂ClNO₃
      Description
      OverviewA 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.
      Catalogue Number492041
      Brand Family Calbiochem®
      SynonymsEthyl-4-chloro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxylate
      References
      ReferencesHur, W., et al. 2010. Chem. Biol. 17, 537.
      Product Information
      CAS number75483-04-4
      FormOff-white solid
      Hill FormulaC13H₁₂ClNO₃
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality SegmentMQ100
      Applications
      Biological Information
      Primary TargetKeap1
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Protect from Moisture Protect from moisture
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade ITEM Number
      Bestellnummer GTIN
      492041 0

      Documentation

      Nrf2 Activator II, AI-1 - CAS 75483-04-4 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Nrf2 Activator II, AI-1 - CAS 75483-04-4 - Calbiochem Analysenzertifikate

      TitelChargennummer
      492041

      Literatur

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

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision24-August-2012 JSW
      SynonymsEthyl-4-chloro-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxylate
      DescriptionA 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.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number75483-04-4
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
      Storage Protect from moisture
      Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesHur, W., et al. 2010. Chem. Biol. 17, 537.