OLIG2-IN-1 is a potent and selective inhibitor of the oligodendrocyte transcription factor 2 (OLIG2). It directly and dose-dependently reduces nuclear OLIG2 levels with an IC50 of 0.88 μM. In U87 and U251 cells, OLIG2-IN-1 exhibits significant antiproliferative activity with IC50 values of 7.02 μM and 6.43 μM, respectively. OLIG2-IN-1 is applicable in cancer research, particularly for studying glioblastoma multiforme.

OLIG2-IN-1 (Compound B01) at a concentration of 10 μM for 12 hours significantly reduces the nuclear OLIG2 protein levels in U87 cells by 75.87%. In addition, OLIG2-IN-1 exhibits antiproliferative activity in LN18 and C6 cells, with IC50 values of 8.88 μM and 6.02 μM, respectively. At 5 μM over a period of 10 days, OLIG2-IN-1 markedly inhibits colony formation in U87 cells. The compound also decreases nuclear OLIG2 protein levels in U87 and U251 cells in a dose-dependent manner when used at 0.02-10 μM for 12 hours. Furthermore, OLIG2-IN-1 offers protective effects against heat-induced denaturation of OLIG2 in U87 and U251 cells.

OLIG2-IN-1 (Compound B01), administered at 50 mg/kg via intraperitoneal injection every other day for 21 days, inhibits tumor growth in U87 xenograft mouse models when used in combination with Temozolomide.