EAD1 trihydrochloride

EAD1 trihydrochloride is a Chloroquine analog with anticancer activity. EAD1 trihydrochloride blocks autophagy, leading to the intracellular accumulation of autophagosome-related proteins LC3-II and p62. EAD1 trihydrochloride induces cancer cell apoptosis and inhibits cancer cell proliferation. EAD1 trihydrochloride can be used in the research of lung cancer and pancreatic cancer ^[1].

In Vitro, EAD1 (compound 3h) (72 h) trihydrochloride potently inhibits the proliferation of H460, HCC827 and BxPC3 cancer cells at 72 h, with IC₅₀ values of 11 μM, 7.6 μM and 5.8 μM, respectively^[1]. EAD1 (6.5-100 μM; 24 h) trihydrochloride potently inhibits colony formation of H460 non-small cell lung cancer cells^[1]. EAD1 (5-75 μM; 24 h) trihydrochloride induces concentration-dependent apoptosis in H460 non-small cell lung cancer (NSCLC) cells^[1]. EAD1 (25-50 μM; 6 h) trihydrochloride enhances the expression of punctate LC3 in H3122 non-small cell lung cancer cells^[1]. EAD1 (1-25 μM, 10 μM; 2-72 h, 24 h) trihydrochloride induces concentration- and time-dependent accumulation of autophagy-related proteins LC3-II and p62 in H460 non-small cell lung cancer (NSCLC) cells^[1].

References:
[1]. Lars Ulrik Nordstrøm, et al. Discovery of Autophagy Inhibitors With Antiproliferative Activity in Lung and Pancreatic Cancer Cells. ACS Med Chem Lett. 2015 Jan 8;6(2):134-9.