A potent combination of small molecules YFSS (Y27632, Forskolin, SB431542, SP600125) that were screened through a neuronal‐specific promoter–reporter system TUBB3::mCherry effectively induces neuronal‐GBM conversion in vitro and in vivo, unveiling molecular mechanisms that offer a theoretical basis and a potential therapeutic strategy for treating GBM. Here, TUBB3 is linked to glioblastoma.