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General description
The 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; 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).
Biochem/physiol Actions
Cell permeable: yes
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Sidrauski, C., et al. 2013 Elife2, e00498.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| assay | ≥93% (HPLC) |
| Quality Segment | 100 |
| form | powder |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | light beige |
| solubility | DMSO: 10 mg/mL |
| web metadata keyword.default | ISR Inhibitor ISRIB 25 nM,ISRIB chemical structure 1597403-47-8,ISRIB for ER stress studies,ISRIB for apoptosis research,ISRIB for cell culture applications,ISRIB trans-diastereomer Sigma-Aldrich,ISRIB with Thapsigargin treatment,ISRIB,Integrated Stress Response Inhibitor ISRIB,Sigma-Aldrich ISRIB,UPR inhibitor ISRIB 200 nM,eIF2α signaling inhibitor ISRIB,eIF2S1 Ser51 phosphorylation inhibitor ISRIB,purity ISRIB 99% or greater,trans-2-(4-Chlorophenoxy)-N-(4-(2-(4-chlorophenoxy)acetylamino)cyclohexyl)acetamide |
| storage temp. | 2-8°C |
| SMILES string | C1CC(CCC1NC(=O)COC2=CC=C(C=C2)Cl)NC(=O)COC3=CC=C(C=C3)Cl |
| InChI | 1S/C22H24Cl2N2O4/c23-15-1-9-19(10-2-15)29-13-21(27)25-17-5-7-18(8-6-17)26-22(28)14-30-20-11-3-16(24)4-12-20/h1-4,9-12,17-18H,5-8,13-14H2,(H,25,27)(H,26,28) |
| InChI key | HJGMCDHQPXTGAV-UHFFFAOYSA-N |
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NALGENE 180透明塑料管，透明，柔软，多用，经济，内径 x 外径x壁厚，1/8 x 1/4 x 1/16，英寸，每箱数量50，50/箱，8000-0020，Thermofisher，赛默飞世尔
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