ISR activator-5
ISR activator-5 is an eIF2B modulator and integrated stress response (ISR) activator. ISR activator-5 stabilises the inactive I-state of eIF2B, inhibits protein synthesis, and activates canonical ISR pathways without inducing eIF2α phosphorylation. ISR activator-5 can be used for the research of cancer, neurologic and metabolic disorders.
For research use only. We do not sell to patients.
- Formula: C52H60F6N4O6
- Molecular Weight:951.05
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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eIF2-β |
ISR activator-5 (Compound B) (20 μM; 16 h) activates the CHOP::Luciferase ISR reporter in CHO-K1 cells with an EC50 of 13 μM[1].
ISR activator-5 (20 μM; 60 min) inhibits protein synthesis in CHO-K1 cells with an IC50 of 11.74 μM[1].
ISR activator-5 (30 μM; 1 h) inhibits translation initiation in HEK cells[1].
ISR activator-5 (6 h) activates a canonical, PERK-specific ISR gene expression program in CHO cells, with significant induction of pathways linked to ISR-mediated stress adaptation[1].
ISR activator-5 (20 μM; 1-24 h) induces endogenous ISR marker proteins (GADD34, ATF4, CHOP) in CHO parental cells starting at 1 hour, with peak induction at 6 hours, and this activity requires eIF2α phosphorylation at Ser51[1].
ISR activator-5 (20 μM; 18 h) activates the CHOP::GFP ISR reporter in CHO cells with an EC50 of 15 μM, and this activation is partially attenuated by co-treatment with 1 μM ISRIB[1].
ISR activator-5 (escalating concentrations; 18 h) activates the CHOP::GFP ISR reporter in EIF2B4L180F mutant CHO cells with an EC50 of 22.63 μM, showing modestly reduced potency compared to wildtype CHO cells, and ISRIB cannot attenuate this activity[1].
ISR activator-5 does not significantly activate the IRE1/XBP1 axis in CHO cells, demonstrating specificity for the ISR pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CHO parental cells
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Concentration:20 μM
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Incubation Time:1 h; 3 h; 6 h; 9 h; 12 h; 24 h
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Result:Induced expression of GADD34, ATF4, and CHOP beginning at 1 hour, with induction peaking at 6 hours, similar to thapsigargin-treated cells.
Showed no induction of these markers in eIF2α-S51A mutant cells treated with Compound B.
Chemical Information
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Molecular Weight 951.05
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Formula C52H60F6N4O6
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SMILES
O=C(C)N(C)CC1=CC=CC(C2=CC3=C(C(C(F)(F)F)=C2)CCCC3N(C)C(CCOCCOCCC(N(C)C4C(C=C(C5=CC=CC(CN(C)C(C)=O)=C5)C=C6C(F)(F)F)=C6CCC4)=O)=O)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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