ASCT-456

ASCT-456 is an investigational peptide antagonist developed by Alcamena that targets the RE1 silencing transcription factor (REST). It is being evaluated for the treatment of glioblastoma (GBM). ASCT-456 is designed to inhibit REST, which acts as an oncogene in brain cancers by driving tumor progression, proliferation, and migration. To overcome the challenges of nuclear localization and cellular permeability, ASCT-456 is utilized in conjunction with ASCT-1, Alcamena's proprietary peptide-based permeability enhancer. In preclinical studies, the addition of ASCT-1 enhanced the REST antagonist activity of ASCT-456 from 64% to 100%, and increased ASCT-456-induced cell death in U87 glioblastoma cells (from 63% to 100%) and temozolomide (TMZ)-resistant U251 glioblastoma cells (from 0% to 76%).