Lys05

**Lys05** is a potent, water-soluble small molecule autophagy inhibitor and dimeric chloroquine analogue. It accumulates in lysosomes and impairs their acidification, leading to inhibition of autophagy. Mechanistically, Lys05 blocks autophagic flux more potently than hydroxychloroquine (HCQ) or chloroquine (CQ), resulting in cytotoxicity and antitumor activity both in vitro and in vivo. Structural features responsible for activity include two aminoquinoline rings, a triamine linker, and C7 chlorine. Lys05 has shown antitumor effects against multiple cancer cell lines, drives leukemic stem cells out of quiescence, and induces their maturation. It also inhibits potassium inwardly rectifying channel subfamily J member 10 (Kir4.1). At high doses, Lys05 produces Paneth cell dysfunction and intestinal toxicity similar to phenotypes of genetic autophagy deficiency. Lys05 is being investigated for indications including neoplasms, nervous system diseases, and depressive disorders, with studies most advanced in preclinical cancer research[1][2][3][4][5][7][8][9].

Brand names

Lys05Lys-05Lys 05

Other names

dimeric chloroquine derivativebisaminoquinoline autophagy inhibitor