OLIG2 Inhibitor

CT-179 is a brain-penetrant and orally active OLIG2 inhibitor with a human IC₅₀ of 1250 nM. CT-179 disrupts OLIG2 dimerization, phosphorylation, and DNA binding, blocking OLIG2-driven transcription. CT-179 induces G₂/M phase arrest and increases G₀ population. CT-179 induces apoptosis by reducing anti-apoptotic proteins and increasing cleaved caspase-3 and cleaved PARP. CT-179 can be used for the research of subgroup medulloblastoma.

SKOG102 is a potent OLIG2 inhibitor that is directly engaging OLIG2 and interferes with the ability of OLIG2 to bind DNA. SKOG102 can be used for the research of glioblastoma (GBM).

OLIG2-IN-1 is a potent and selective oligodendrocyte transcription factor 2 (OLIG2) inhibitor. OLIG2-IN-1 directly and dose-dependently downregulates nuclear OLIG2 levels with an IC₅₀ value of 0.88 μM. OLIG2-IN-1 exhibits strong anti-proliferative activity in U87 and U251 cells with IC₅₀ values of 7.02 μM and 6.43 μM, respectively. OLIG2-IN-1 can be used for the research of cancer, such as glioblastoma multiforme.