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Chemical Structure| 405060-95-9 Chemical Structure| 405060-95-9

Structure of Salubrinal
CAS No.: 405060-95-9

Chemical Structure| 405060-95-9

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Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation. It acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor, suppressing inflammation in anti-collagen antibody-induced arthritis, has antiviral activity against HSV-1, and inhibits the dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5.

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Product Details of Salubrinal

CAS No. :405060-95-9
Formula : C21H17Cl3N4OS
M.W : 479.81
SMILES Code : O=C(NC(NC(NC1=C2N=CC=CC2=CC=C1)=S)C(Cl)(Cl)Cl)/C=C/C3=CC=CC=C3
MDL No. :MFCD00548612
InChI Key :LCOIAYJMPKXARU-VAWYXSNFSA-N
Pubchem ID :5717801

Safety of Salubrinal

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • PERK

In Vitro:

Cell Line
Concentration Treated Time Description References
HepG2 cells 10-100 µM 24 hours To investigate the effects of salubrinal on eIF2α phosphorylation and CHOP expression, results showed that salubrinal dose-dependently induced eIF2α phosphorylation and upregulated CHOP expression. PMC3944242
BEL-7402 cells 25 µM 24 hours To investigate the effects of combination of salubrinal and TRAIL on eIF2α phosphorylation and CHOP expression, results showed that the combination significantly increased eIF2α phosphorylation and CHOP expression. PMC3944242
HepG2 cells 10 μM 2 days Salubrinal alleviated fatty degeneration and inhibited lipid deposition in HepG2 cells. PMC7736876
3T3-L1 cells 10 μM 3 days Salubrinal markedly inhibited lipid droplet formation in 3T3-L1 cells. PMC7736876
L6 skeletal muscle cells 30 µM 30 minutes Salubrinal attenuated iron-induced insulin resistance by elevating eIF2α phosphorylation and promoting the unfolded protein response (UPR). Salubrinal induced autophagy flux, and its beneficial effects on insulin sensitivity were not observed in autophagy-deficient cells generated by overexpressing a dominant-negative ATG5 mutant or via knockout of ATG7. PMC11027572
MC3T3-E1 cells 5 μM 48 hours Salubrinal significantly increased the autophagic puncta in MC3T3-E1 cells, indicating it promotes autophagy by regulating Atg7. PMC6892793
RAW264.7 cells 5, 10, 20 μM Salubrinal reduced RANKL-driven elevation of NFATc1 mRNA level in a dose-dependent manner, indicating it inhibits osteoclast differentiation. PMC6892793

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice High-fat diet-induced obesity model Subcutaneous injection 50 mg/kg Single injection, embryos harvested 1 hour post-injection Salubrinal alleviated obesity-induced hepatic steatosis and lipid metabolism disorder by inhibiting ER stress and promoting autophagy. PMC7736876
Rats Brain death model Intraperitoneal injection 1 mg 2 consecutive days per week for 5 weeks Salubrinal significantly reduced apoptosis in hepatic cells of BD rats, and the protective effect may be achieved via the PERK-eIF2α signaling pathway. PMC4733771
C57/BL6J male mice Systemic iron overload-induced skeletal muscle insulin resistance model Intraperitoneal injection 1 mg/kg Once a week for 8 weeks Salubrinal pretreatment promoted eIF2α phosphorylation, enhanced autophagic flux in skeletal muscle, and improved insulin responsiveness. PMC11027572
C57BL/6 female mice Ovariectomized (OVX) mouse model Subcutaneous injection 1 mg/kg Day 1, day 2, and day 3, once daily Salubrinal significantly alleviated the reduction of bone mineral density and bone volume fraction in OVX mice, and promoted autophagy of osteoblasts via regulation of eIF2α, Atg7, LC3, and p62. PMC6892793

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.42mL

2.08mL

1.04mL

20.84mL

4.17mL

2.08mL

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