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412511 IRE1 Inhibitor II - CAS 1093118-73-0 - Calbiochem

Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1093118-73-0C₁₅H₁₃NO₄

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412511-25MG
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      Glass bottle 25 mg
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      Description
      OverviewA cell-permeable salicylaldehyde compound that is shown to inhibit ER stress-induced Xbp1 mRNA splicing (100% inhibition by ≤25 µM in Tunicamycin-treated U373 cultures) in a reversible manner, presumably due to IRE1 inhibition via the same mechanism as 4µ8C (Cat. No. 412512) and STF083010 (Cat. No. 412510). IRE1 inhibition is shown to initiate signaling events leading to increased CRADD/RAIDD protein level (36 hrs post IRE1 inhibition in U373 cells), an important adaptor protein for caspase-2-mediated apoptosis response. Also shown to synergize with Maraba oncolytic therapy in mice (250 mg/kg/12 h via i.p. for 6 days before viral therapy) bearing Ovcar-4 or EMT6 in vivo.
      Catalogue Number412511
      Brand Family Calbiochem®
      SynonymsER-to-Nucleus Signaling 1 Inhibitor II, Inositol-Requiring Protein 1 Inhibitor II, 3ʹ-Formyl-4ʹ-hydroxy-5ʹ-methoxybiphenyl-3-carboxamide
      References
      ReferencesMahoney, D.J., et al. 2011. Cancer Cell 20, 443.
      Product Information
      CAS number1093118-73-0
      FormTan solid
      Hill FormulaC₁₅H₁₃NO₄
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetIRE1
      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
      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. Use only fresh DMSO.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      412511-25MG 04055977188172

      Documentation

      IRE1 Inhibitor II - CAS 1093118-73-0 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      IRE1 Inhibitor II - CAS 1093118-73-0 - Calbiochem Certificates of Analysis

      TitleLot Number
      412511

      References

      Reference overview
      Mahoney, D.J., et al. 2011. Cancer Cell 20, 443.
      Data Sheet

      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.

      Revision22-November-2012 JSW
      SynonymsER-to-Nucleus Signaling 1 Inhibitor II, Inositol-Requiring Protein 1 Inhibitor II, 3ʹ-Formyl-4ʹ-hydroxy-5ʹ-methoxybiphenyl-3-carboxamide
      DescriptionA cell-permeable salicylaldehyde compound that is shown to inhibit ER stress-induced Xbp1 mRNA splicing (100% inhibition by ≤25 µM in Tunicamycin-treated U373 cultures) in a reversible manner, presumably due to IRE1 inhibition via the same molecular/chemical mechanism as 4µ8C (Cat. No. 412512) and STF083010 (Cat. No. 412510). Shown to effectively precondition/sensitize cancer cell lines (by 10,000- and 1,000-fold with 48 hrs 50 µM inhibitor pre-treatment of EMT6 and U373 cells, respectively) as well as primary cancer cultures from glioblastoma multiform patients (by ~15- to 55-fold with 48 hrs 15 µM inhibitor pre-treatment) for enhanced apoptosis upon Maraba virus infection. IRE1 inhibition is shown to initiate signaling events that eventually leads to increased CRADD/RAIDD protein level (36 hrs after initial IRE1 inhibition in U373 cells), an adaptor protein important for caspase-2-mediated apoptosis response. It is the cellular RAIDD upregulation, but not IRE1 inactivation, that is a prerequisite for the enhancing effect of rhabdovirus-mediated cancer killing. Also shown to synergize with Maraba oncolytic therapy in mice (twice daily i.p. dosing at 250 mg/kg for 6 days before viral therapy) bearing Ovcar-4 (87%, 60%, and 17% of control tumor size on day 30, respectively, with virus alone, drug alone, or combined treatment) or EMT6 (0% survival on day 20 vs. day 14, respectively, with or without combined treatment) in vivo.
      FormTan solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1093118-73-0
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage 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. Use only fresh DMSO.
      Toxicity Standard Handling
      ReferencesMahoney, D.J., et al. 2011. Cancer Cell 20, 443.