412511 | IRE1 Inhibitor II - Calbiochem

412511
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₅H₁₃NO₄

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      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®
          Synonyms3ʹ-Formyl-4ʹ-hydroxy-5ʹ-methoxybiphenyl-3-carboxamide, ER-to-Nucleus Signaling 1 Inhibitor II, Inositol-Requiring Protein 1 Inhibitor II
          References
          ReferencesMahoney, D.J., et al. 2011. Cancer Cell 20, 443.
          Product Information
          FormTan solid
          Hill FormulaC₁₅H₁₃NO₄
          ReversibleY
          Structure formula ImageStructure formula Image
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          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
          Synonyms3ʹ-Formyl-4ʹ-hydroxy-5ʹ-methoxybiphenyl-3-carboxamide, ER-to-Nucleus Signaling 1 Inhibitor II, Inositol-Requiring Protein 1 Inhibitor II
          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
          Structure formulaStructure formula
          Purity≥97% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage +2°C to +8°C
          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.
          Toxicity Standard Handling
          ReferencesMahoney, D.J., et al. 2011. Cancer Cell 20, 443.