For research use only. Not for therapeutic Use.
2BAct is a highly selective, and orally active eIF2B (eukaryotic initiation factor 2B) activator with an EC50 of 33 nM. 2BAct prevents neurological defects caused by a chronic integrated stress response. 2BAct is able to penetrate the central nervous system (CNS). 2BAct displays improved solubility and pharmacokinetics relative to eIF2B activator ISRIB trans-isomer (HY-12495)[1].
Primary fibroblast lysates from R191H embryos has lower GEF activity than WT lysates, and 2BAct enhances this activity threefold (EC50=7.3 nM)[1].
2BAct (300 μg 2BAct/g of meal; 21 weeks) normalizes body weight gain in VWM mice[1].
2BAct prevents the appearance of motor deficits, myelin loss and reactive gliosis in VWM mice[1].
2BAct stimulates the remaining activity of mutant eIF2B complex in vivo, abrogating the maladaptive stress response[1].
| Catalog Number | I020808 |
| CAS Number | 2143542-28-1 |
| Synonyms | N-[3-[[2-(4-chloro-3-fluorophenoxy)acetyl]amino]-1-bicyclo[1.1.1]pentanyl]-5-(difluoromethyl)pyrazine-2-carboxamide |
| Molecular Formula | C19H16ClF3N4O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C19H16ClF3N4O3/c20-11-2-1-10(3-12(11)21)30-6-15(28)26-18-7-19(8-18,9-18)27-17(29)14-5-24-13(4-25-14)16(22)23/h1-5,16H,6-9H2,(H,26,28)(H,27,29) |
| InChIKey | HYQJXXCYOYRNMP-UHFFFAOYSA-N |
| SMILES | C1C2(CC1(C2)NC(=O)C3=NC=C(N=C3)C(F)F)NC(=O)COC4=CC(=C(C=C4)Cl)F |
| Reference | [1]. Wong YL, et al. eIF2B activator prevents neurological defects caused by a chronic integrated stress response. Elife. 2019;8:e42940. Published 2019 Jan 9. |
