509584 | ISR Inhibitor, ISRIB - Calbiochem

509584
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₂H₂₄Cl₂N₂O₄

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.09584.0001
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          Glass bottle 10 mg
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          Description
          OverviewThe cell-permeable trans diastereomer of a bis-glycolamide compound that acts as a potent and selective blocker of eIF2α/eIF2S1 Ser51 phosphorylation-initiated unfold protein response/UPR (Effec. conc. 25 to 200 nM in HEK293T, HeLa, MEF, U2OS cultures) upon ER stress induction. Although noncytotoxic in the absence of ER stress, ISRIB does cause enhanced apoptotic cell death upon ER stress induction by Thapsigargin/Tg (100 to 500 nM; Cat. Nos. 586005 & 586006) or Tunicamycin/Tm (2 to 5 µg/mL; Cat. No. 654380) treatment. Reported to exhibit good pharmacokinetics with blood-brain permeability in mice and significantly enhance learning and long-term memory in mice (0.25 mg/kg/d i.p.) and rats (25 ng/0.5 µL/275-350 g rat; amygdala administration via cannulation) in vivo. Although the exact molecular target is not yet established, ISRIB most likely exerts its effect by modulating the interaction between the guanine nucleotide exchange factor eIF2B and the phosphorylated eIF2α (pS51).
          Catalogue Number509584
          Brand Family Calbiochem®
          Synonymstrans-2-(4-Chlorophenoxy)-N-(4-(2-(4-chlorophenoxy)acetylamino)cyclohexyl)acetamide, Integrated Stress Response Inhibitor, UPR Inhibitor, eIF2α (pS51) Signaling Inhibitor, eIF2S1 (pS51) Signaling Inhibitor
          References
          ReferencesSidrauski, C., et al. 2013 Elife 2, e00498.
          Product Information
          FormLight beige powder
          Hill FormulaC₂₂H₂₄Cl₂N₂O₄
          Chemical formulaC₂₂H₂₄Cl₂N₂O₄
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥93% 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.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Sidrauski, C., et al. 2013 Elife 2, e00498.
          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.

          Revision21-February-2014 JSW
          Synonymstrans-2-(4-Chlorophenoxy)-N-(4-(2-(4-chlorophenoxy)acetylamino)cyclohexyl)acetamide, Integrated Stress Response Inhibitor, UPR Inhibitor, eIF2α (pS51) Signaling Inhibitor, eIF2S1 (pS51) Signaling Inhibitor
          DescriptionThe cell-permeable trans-diastereomer of a bis-glycolamide compound that acts as a potent and selective blocker ofeIF2α/eIF2S1-Ser51 phosphorylation-initiated unfold protein response/UPR (Effec. conc. 25 to 200 nM in HEK293T, HeLa, MEF, U2OS cultures) upon ER stress induction by Cys/Met starvation, HRI activation (6 µM KM09748), Thapsigargin/Tg (100 to 500 nM; Cat. Nos. 586005 & 586006) or Tunicamycin/Tm (2 to 5 µg/mL; Cat. No. 654380) treatment without affecting UPR responses independent of eIF2α (pS51), including ATF6 cleavage and IRE1-initiated XBP1s production. Although noncytotoxic in the absence of ER stress, ISRIB does prevent URP from properly restoring ER homeostasis following ER stress induction, causing enhanced apoptotic cell death in Tg- or Tm-treated HEK293T (2 µg/mL Tm & 200 nM ISRIB) and HeLa (25 nM ISRIB and 5 µg/mL Tm or 500 nM Tg) cultures. Reported to exhibit good pharmacokinetics with blood-brain permeability (plasma/brain Tmax ≈ 6/6 h; Cmax ≈ 180/100 ng/mL; C24 h ≈ 55/33 ng/mL; 2.5 mg/kg i.p.) in mice and significantly enhance hippocampus-dependent learning of mice subjected to Morris water maze (0.25 mg/kg/d i.p.) in vivo. Likewise, single amygdala administration via cannulation (25 ng/0.5 µL/275-350 g rat) immediately following auditory fear conditioning significantly enhances long-term, but not short-term, post-conditioning auditory response (% response above basal at 4 h/24 post conditioning = 27/33 vs. 27/22 among vehicle-treated control rats) in rats in vivo. Although the exact molecular target is not yet established, ISRIB most likely exerts its effect by modulating the interaction between the guanine nucleotide exchange factor eIF2B and the phosphorylated eIF2α (pS51).
          FormLight beige powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₂H₂₄Cl₂N₂O₄
          Structure formulaStructure formula
          Purity≥93% by HPLC
          SolubilityDMSO (10 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.
          Toxicity Standard Handling
          ReferencesSidrauski, C., et al. 2013 Elife 2, e00498.