compound C108

Compound C108 is a small molecule inhibitor of Ras-GTPase-activating protein SH3-domain-binding protein 2 (G3BP2). It is being investigated as a potential therapeutic agent for acute myeloid leukemia (AML), particularly to overcome resistance to the BCL2 inhibitor venetoclax. G3BP2 is an RNA-binding protein that is frequently overexpressed in AML and is associated with poor prognosis. C108 works by inhibiting G3BP2, which disrupts the stability of ELF1 mRNA. Because ELF1 is a transcription factor that facilitates the expression of the anti-apoptotic protein MCL1, its reduction leads to decreased MCL1 levels. This downregulation of MCL1 sensitizes AML cells to venetoclax-induced apoptosis. Preclinical studies have demonstrated that C108, in combination with venetoclax, reduces leukemic cell viability and tumor burden in xenograft models.

Other names

G3BP2 inhibitor C108G-3BP2 inhibitor C108G 3BP2 inhibitor C108