Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Integrated stress response (ISR) inhibitor; reverses the effects of eIF2α phosphorylation (IC50 = 5 nM) and restores cell translation capacity. Acts downstream of PERK, targeting interactions between eIF2α kinases and elF2B. Blocks ATF4 production without altering the IRE1 or ATF6 responses in vitro. Displays memory enhancement in hippocampus-dependent spatial and fear-associated learning in rodents. Brain penetrant.
Technical Data
M. Wt
|
451.34 |
Formula
|
C22H24Cl2N2O4 |
Storage
|
Store at +4°C |
Purity
|
≥99% (HPLC) |
CAS Number
|
1597403-47-8 |
PubChem ID
|
1011240 |
InChI Key
|
HJGMCDHQPXTGAV-UHFFFAOYSA-N |
Smiles
|
O=C(COC1=CC=C(Cl)C=C1)N[C@@H]2CC[C@@H](NC(COC3=CC=C(Cl)C=C3)=O)CC2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Preparing Stock Solutions
The following data is based on the product molecular weight 451.34. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
1 mM |
2.22 mL |
11.08 mL |
22.16 mL |
5 mM |
0.44 mL |
2.22 mL |
4.43 mL |
10 mM |
0.22 mL |
1.11 mL |
2.22 mL |
50 mM |
0.04 mL |
0.22 mL |
0.44 mL |
Reconstitution Calculator
References
References are publications that support the products' biological activity.
Sidrauski
et al (2013) Pharmacological brake-release of mRNA translation enhances cognitive memory. Elife 2 e00498 PMID: 23741617
Sekine
et al (2015) Stress responses. Mutations in a translation initiation factor identify the target of a memory-enhancing compound. Science 348 1027 PMID: 25858979
Hinnebusch
(2015) Cell biology. Blocking stress response for better memory? Science 348 967 PMID: 26023119
Keywords: trans-ISRIB, supplier, Potent, inhibitors, inhibits, of, PERK, signaling, UPR, unfolded, protein, response, endoplasmic, reticulum, ER, stress, memory, consolidation, eIF2, alpha, kinases, ISR, integrated, stress, response, DNA,, RNA, and, Protein, Synthesis, Miscellaneous, Compounds, PERK, Other, ER, stress/UPR, PERK, Tocris Bioscience