Salubrinal
Chemical Name: 3-Phenyl-N-[2,2,2-trichloro-1-[[(8-quinolinylamino)thioxomethyl]amino]ethyl]-2-propenamide
Purity: ≥99%
Biological Activity
Salubrinal is a cell-permeable, selective inhibitor of cellular phosphatase complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit α (eIF2α). Protects cells from endoplasmic reticulum stress-induced apoptosis (EC50 ~ 15 μM).Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Blockade of Smad signaling by 3'-deoxyadenosine: a mechanism for its anti-fibrotic potential.
Gu L, Johno H, Nakajima S, Kato H, Takahashi S, Katoh R, Kitamura M
Lab Invest, 2013;93(4):450-61. -
Inhibitory Effects of Dopamine Receptor D1 Agonist on Mammary Tumor and Bone Metastasis
K Minami, S Liu, Y Liu, A Chen, Q Wan, S Na, BY Li, N Matsuura, M Koizumi, Y Yin, L Gan, A Xu, J Li, H Nakshatri, H Yokota
Sci Rep, 2017;7(0):45686. -
Eukaryotic initiation factor 2 (eIF2) signaling regulates proinflammatory cytokine expression and bacterial invasion.
Shrestha N, Bahnan W, Wiley D, Barber G, Fields K, Schesser K
J Biol Chem, 2012;287(34):28738-44. -
Intestinal Epithelial TLR-4 Activation Is Required for the Development of Acute Lung Injury after Trauma/Hemorrhagic Shock via the Release of HMGB1 from the Gut.
Sodhi C, Jia H, Yamaguchi Y, Lu P, Good M, Egan C, Ozolek J, Zhu X, Billiar T, Hackam D
J Immunol, 2015;194(10):4931-9. -
A selective inhibitor of eIF2α dephosphorylation protects cells from ER stress.
Boyce et al.
Science, 2005;307:935 -
Structure-activity relationship studies of salubrinal lead to its active biotinylated derivative.
Long et al.
Bioorg.Med.Chem.Lett., 2005;15:3849
Product Datasheets
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Citations for Salubrinal
The citations listed below are publications that use Tocris products. Selected citations for Salubrinal include:
11 Citations: Showing 1 - 10
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Activated Integrated Stress Response Induced by Salubrinal Promotes CDDP Resistance in Human Gastric Cancer Cells via Enhanced xCT Expression and Glutathione Biosynthesis.
Authors: Wang Et al.
Int J Mol Sci 2018;19
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mTORC1 and CK2 coordinate ternary and eIF4F complex assembly.
Authors: Gandin Et al.
Nat Commun 2016;7:11127
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Modulation of the unfolded protein response impedes tumor cell adaptation to proteotoxic stress: a PERK for hepatocellular carcinoma therapy.
Authors: Vandewynckel Et al.
PLoS One 2015;9:93
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Chondroprotective effects of Salubrinal in a mouse model of osteoarthritis.
Authors: Hamamura Et al.
J Musculoskelet Neuronal Interact 2015;4:84
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Distinctive subcellular inhibition of cytokine-induced SRC by salubrinal and fluid flow.
Authors: Wan Et al.
PLoS One 2014;9:e105699
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Identification of small molecules that protect pancreatic β cells against endoplasmic reticulum stress-induced cell death.
Authors: Tran Et al.
ACS Chem Biol 2014;9:2796
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Inhibitors of eIF2α dephosphorylation slow replication and stabilize latency in Toxoplasma gondii.
Authors: Konrad Et al.
Antimicrob Agents Chemother 2013;57:1815
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Rac1 mediates load-driven attenuation of mRNA expression of nerve growth factor β in cartilage and chondrocytes.
Authors: Shim Et al.
Hepatol Int 2013;13:372
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Eukaryotic initiation factor 2α phosphorylation mediates fetal hemoglobin induction through a post-transcriptional mechanism.
Authors: Hahn and Lowrey
Blood 2013;122:477
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Synthesis, maturation, and trafficking of human Na+-dicarboxylate cotransporter NaDC1 requires the chaperone activity of cyclophilin B.
Authors: Bergeron Et al.
J Biol Chem 2011;286:11242
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Androgens modulate autophagy and cell death via regulation of the endoplasmic reticulum chaperone glucose-regulated protein 78/BiP in prostate cancer cells.
Authors: Bennett Et al.
Cell Death Dis 2011;1:e72
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