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 autophagicflux 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 autophagicflux 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 autophagicflux and synergistically enhancing the anticancer activity of chemotherapeutic agents against HeLa cells. Pulsatilla saponin D has strong haemolytic activity.