| Bioactivity | 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 (HY-12495)[1]. |
| Target | EC50: 33 nM (eIF2B) |
| Invitro | Primary fibroblast lysates from R191H embryos has lower GEF activity than WT lysates, and 2BAct enhances this activity threefold (EC50=7.3 nM)[1]. |
| In Vivo | 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]. |
| Name | 2BAct |
| CAS | 2143542-28-1 |
| Formula | C19H16ClF3N4O3 |
| Molar Mass | 440.80 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 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. |