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.
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.