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    Salubrinal
    Salubrinal

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0058
    CAS #: 405060-95-9Purity ≥98%

    Description: Salubrinal is a novel, potent, cell-permeable and selective inhibitor of eIF2α (eukaryotic translation initiation factor 2 subunit α) dephosphorylation and inhibits ER stress-mediated apoptosis with EC50 of ~15 μM in a cell-free assay. A cell-permeable and selective inhibitor of eIF2α dephosphorylation with an IC50 of 15 M. The eukaryotic translation initiation factor 2 subunit α (eIF2α) is crucial in protein synthesis. eIF2α phosphorylation played an important role in protecting cells from apoptosis. Salubrinal selectively suppresses the phosphatase complexes that dephosphorylate eIF-2α. Salubrinal inhibits eIF2α dephosphorylation by inhibiting the PP1/GADD34 complex. Salubrinal inhibits HSV replication with IC50 of ~ 3μM by inhibiting eIF2α dephosphorylation.

    References: Science, 2005, 307(5711), 935-939.Am J Physiol Regul Integr Comp Physiol, 2009, 296(1), 178-184.


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    Molecular Weight (MW)479.81
    FormulaC21H17Cl3N4OS
    CAS No.405060-95-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 96 mg/mL (200.07 mM)
    Water: <1 mg/mL (slightly soluble or insoluble)
    Ethanol: 2 mg/mL (4.16 mM) 
    Other info

    InChi Key: LCOIAYJMPKXARU-VAWYXSNFSA-N

    InChi Code: InChI=1S/C21H17Cl3N4OS/c22-21(23,24)19(27-17(29)12-11-14-6-2-1-3-7-14)28-20(30)26-16-10-4-8-15-9-5-13-25-18(15)16/h1-13,19H,(H,27,29)(H2,26,28,30)/b12-11+

    SMILES Code: O=C(NC(NC(NC1=C2N=CC=CC2=CC=C1)=S)C(Cl)(Cl)Cl)/C=C/C3=CC=CC=C3

    Chemical Name(E)-3-phenyl-N-[2,2,2-trichloro-1-(quinolin-8-ylcarbamothioylamino)ethyl]prop-2-enamide


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    In VitroSalubrinal is a selective inhibitor of cellular complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit α (eIF2α). Salubrinal inhibited ER stress-mediated apoptosis induced by the protein glycosylation inhibitor tunicamycin (Tm) in a dose-dependent manner, with a median effective concentration (EC50) ∼ 15 μM. Salubrinal also suppressed Tm-induced DNA fragmentation the processing of caspase-7, a caspase activated by ER stress.
    In VivoSalubrinal inhibits HSV replication in a mouse cornea infection model. Compared to vehicle control, topical Salubrinal treatment significantly reduced the viral titer recovered from eye swabs of infected animals. I.C.V. administration of Salubrinal significantly modified the homeostatic sleep response.
    Animal modelEight-week-old male CD-1 outbred mice
    Formulation & DosageDMEM; 75μM; On cornea
    References[1] Boyce M, et al. Science, 2005, 307(5711), 935-939.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Salubrinal

    Am J Physiol Regul Integr Comp Physiol, 2009, 296(1), 178-184.
     

    Salubrinal

     

    Salubrinal


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