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3-Phenyl-N-[2,2,2-trichloro-1-[[(8-quinolinylamino)thioxomethyl]amino]ethyl]-2-propenamide
Cell-permeable, selective inhibitor of cellular phosphatase complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit á (eIF2á).
Protects cells from endoplasmic reticulum stress-induced apoptosis (EC50 ~ 15 ìM)
Chemical Formula: C21H17Cl3N4OS
Molecular Weight: 479.8
OTAVAchemicals Catalogue Number: 7119987003
CAS Registry Number: 405060-95-9
Purity: 98% (HPLC)
Ref. : Yuan et al. A Selective Inhibitor of eIF2á Dephosphorylation Protects Cells from ER Stress. Science (2005), 307, 935-939
Abstract: Most protein phosphatases have little intrinsic substrate specificity, making selective pharmacological inhibition of specific dephosphorylation reactions a challenging problem. In a screen for small molecules that protect cells from endoplasmic reticulum (ER) stress, we identified salubrinal, a selective inhibitor of cellular complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit alpha (eIF2alpha). Salubrinal also blocks eIF2alpha dephosphorylation mediated by a herpes simplex virus protein and inhibits viral replication. These results suggest that selective chemical inhibitors of eIF2alpha dephosphorylation may be useful in diseases involving ER stress or viral infection. More broadly, salubrinal demonstrates the feasibility of selective pharmacological targeting of cellular dephosphorylation events.
DOI: 10.1126/science.1101902
Price info:
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1 MG |
30 EUR |
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5 MG |
90 EUR |
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10 MG |
130 EUR |
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300uL of 10mM solution |
50 EUR
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