NEO214, an autophagy inhibitor and a covalent conjugate of the PDE4 inhibitor Rolipram and perillyl alcohol, exhibits anti-cancer activity and blood-brain barrier (BBB) permeability. It prevents autophagy-lysosome fusion, blocking autophagic flux and triggering glioma cell death via mTOR activation and TFEB (Transcription Factor EB) aggregation. NEO214 inhibition of Macroautophagy/autophagy in glioblastoma cells may overcome chemotherapy resistance in glioblastoma [1].
Nur77 modulator 3 (9e) binds to Nur77 and inhibits TGF-β1-induced α-SMA and COLA1 expression in a Nur77-dependent manner. It induces Nur77 expression and enhances autophagic flux by inhibiting the mTORC1 signaling pathway in vitro and in vivo. Nur77 modulator 3 blocks the progression of hepatic fibrosis [1].
Lup-20(29)-en-28-oic acid exhibits anticancer activities in various cancer types, inhibiting autophagic flux and synergistically enhancing the anticancer activity of chemotherapeutic agents against HeLa cells. Pulsatilla saponin D has strong haemolytic activity.