2BAct is a highly selective, and orally active eIF2B (eukaryotic initiation factor 2B) activator with an EC 50 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 )
In Vitro
Primary fibroblast lysates from R191H embryos has lower GEF activity than WT lysates, and 2BAct enhances this activity threefold (EC 50 =7.3 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
2BAct (300 μg 2BAct/g of meal; 21 weeks) normalizes body weight gain in VWM mice . ?\n2BAct prevents the appearance of motor deficits, myelin loss and reactive gliosis in VWM mice . ?\n2BAct stimulates the remaining activity of mutant eIF2B complex in vivo, abrogating the maladaptive stress response . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
