2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. Eukaryotic Initiation Factor (eIF) Mitogen- and Stress-Activated Protein Kinase (MSK)
  4. ISR activator-4

ISR activator-4 is an eIF2B modulator and integrated stress response (ISR) activator with a human eIF2B EC50 of 2.2 μM. ISR activator-4 stabilises the inactive I-state of eIF2B, favours formation of the inhibitory eIF2B-eIF2(αP) complex, and attenuates eIF2B's guanine nucleotide exchange factor activity. ISR activator-4 can be used for the research of cancer, neurologic and metabolic disorders.

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ISR activator-4

ISR activator-4 Chemical Structure

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ISR activator-4 Related Antibodies

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Description

ISR activator-4 is an eIF2B modulator and integrated stress response (ISR) activator with a human eIF2B EC50 of 2.2 μM. ISR activator-4 stabilises the inactive I-state of eIF2B, favours formation of the inhibitory eIF2B-eIF2(αP) complex, and attenuates eIF2B's guanine nucleotide exchange factor activity. ISR activator-4 can be used for the research of cancer, neurologic and metabolic disorders[1].

IC50 & Target[1]

eIF2-β

 

In Vitro

ISR activator-4 (Compound A-(S)) stabilises the inhibitory complex between recombinant human eIF2B and phosphorylated eIF2α-NTD with an EC50 of 2.2 μM, reducing the fast-phase dissociation contribution by 82%[1].
ISR activator-4 binds recombinant human eIF2B with a K1/2max of 6.4 μM, showing positive cooperative binding with eIF2(αP) (alpha = 0.16) and displacing the ISRIB (HY-12495A) probe ~30-fold more potently than its diastereomer[1].
ISR activator-4 inhibits the GEF activity of recombinant human eIF2B in an eIF2(αP)-dependent manner, increasing the half-life of GDP-BODIPY bound to eIF2 to 76.42 s[1].
ISR activator-4 (1 h) binds to the ISRIB-binding site of recombinant human eIF2B, stabilising the complex in the inactive I-state and forming specific interactions with residues across the eIF2B β-δ subunit interface[1].
ISR activator-4 (18 h) activates the CHOP::GFP ISR reporter in CHO cells with an EC50 of 12.47 μM[1].
ISR activator-4 (20 μM) inhibits translation initiation in U-2 OS cells, reducing the polysome/monosome ratio, and this effect is reversed by co-treatment with 2 μM ISRIB[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ISR activator-4 Related Antibodies
Molecular Weight

563.63

Formula

C30H37F4N3O3
SMILES

CC(N(C)CC1=CC=CC(C2=CC([C@@H](N(C)C(COC[C@H]3[C@@H](F)CNCC3)=O)CCC4)=C4C(C(F)(F)F)=C2)=C1)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ISR activator-4 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ISR activator-4ISR activator4ISR activator 4Eukaryotic Initiation Factor (eIF)Mitogen- and Stress-Activated Protein Kinase (MSK)Mitogen- and Stress-Activated Protein KinaseeIF2(αP)CHOP::GFP ISR reporterISRIBU-2 OS cellsIntegrated Stress ResponseeIF2BeIF2α-NTDeIF2B β-δ subunit interfaceguanine nucleotide exchange factorCHO cellsInhibitorinhibitorinhibit

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