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412512 IRE1 Inhibitor III, 4μ8C - CAS 14003-96-4 - Calbiochem

IRE1 Inhibitor III, , CAS 14003-96-4, is a cell-permeable. Covalent inhibitor of IRE1 RNase activity (IC₅₀ = 550 and 45 nM, respectively, with 0 & 16 min preincubation in RNA cleavage assays).

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Synonymes: ER-to-Nucleus Signaling 1 Inhibitor III, Inositol-Reguiring Protein 1 Inhibitor III, 8-Formyl-7-hydroxy-4-methylcoumarin, 7-Hydroxy-4-methyl-2-oxo-2H-chromene-8-carbaldehyde

Primary Target: IRE1
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412512
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Tableau de caractéristiques principal

CAS #Empirical Formula
14003-96-4C₁₁H₈O₄

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412512-25MG
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      Description
      OverviewA cell-permeable coumarin o-hydroxyaldehyde that inhibits IRE1 RNase activity in a time- and dose-dependent manner (IC50 = 550 and 45 nM, respectively, with 0 and 16 min drug preincubation in RNA cleavage assays) by covalently targeting IRE1 Lys907 via Schiff base formation, effectively preventing ER stress-induced site-specific mRNA splicing as well as RIDD (Regulated IRE1-Dependent Degradation) mRNA degradation (IC50 = 6.9 and 4.1 µM, respectively, against Xbp1 splicing and Scara3 degradation) in MEF cultures following Tunicamycin (Cat. No. 654380) treatment. Comparing to STF083010 (Cat. No. 412510), 4μ8C is also shown to inhibit IRE1 autophosphorylation in cell-free assays via Schiff base formation with IRE1 Lys599 in the absence of ADP, however cellular nucleotide prevents 4μ8C from targeting IRE1 Lys599 intracellularly.
      Catalogue Number412512
      Brand Family Calbiochem®
      SynonymsER-to-Nucleus Signaling 1 Inhibitor III, Inositol-Reguiring Protein 1 Inhibitor III, 8-Formyl-7-hydroxy-4-methylcoumarin, 7-Hydroxy-4-methyl-2-oxo-2H-chromene-8-carbaldehyde
      References
      ReferencesCross, B.C.S., et al. 2012. Proc. Natl. acad. Sci. USA 109, E869.
      Product Information
      CAS number14003-96-4
      FormYellow powder
      Hill FormulaC₁₁H₈O₄
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Primary TargetIRE1
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Référence GTIN
      412512-25MG 04055977188189