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ESI1
- Development stage
- Preclinical
- Lead developer
- Cincinnati Children's Hospital Medical Center
- Modality
- Small Molecules
- Administration
- Intraperitoneal, Oral
01
Overview
ESI1 (also known as PT3) is a brain-penetrant, selective small-molecule inhibitor of histone deacetylase 3 (HDAC3) with an IC50 of approximately 250 nM. Originally developed as a memory enhancer and anticancer agent, ESI1 has been shown to promote central nervous system (CNS) myelin regeneration and repair. It acts by reversing epigenetic silencing in mature oligodendrocytes, reducing repressive chromatin marks (such as H3K27me3 and H3K9me3) and increasing activating marks (H3K27ac). Additionally, ESI1 triggers the nuclear condensate formation of master lipid-metabolic regulators SREBP1 and SREBP2, driving the lipid and cholesterol biosynthesis necessary for myelin sheath assembly. Preclinical studies have demonstrated its efficacy in animal models of multiple sclerosis (such as experimental autoimmune encephalomyelitis) and age-related cognitive decline.
- Other names
- ESI-1ESI1ESI 1N-(2-aminophenyl)-5-(benzylamino)pyrazine-2-carboxamideepigenetic-silencing-inhibitor-1epigenetic-silencing-inhibitor1epigenetic-silencing-inhibitor 1
02
Targets
HDAC3 (Histone Deacetylase 3)
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