MT 63-78

MT 63-78 is a specific and effective direct AMPK activator (EC50: 25 μM) . MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects. MT 63–78 also causes cell mitotic arrest and apoptosis.MT 63-78 (0-50 μM; 24 hours; LNCaP, PC3, C4-4, C4-2B, CL1and 22RV1cells) treatment induces reduction of anti-apoptotic Mcl-1 in concert with an accumulation of the pro-apoptotic BH3-only protein Puma. MT 63-78 (0-50 μM; 4 days; LNCaP and PC3 cells) treatment displays a dose-dependent decrease in cell number and concomitant to the activation of AMPK signaling. MT 63-78 (0-50 μM; 30 minutes; LNCaP and PC3 cells) treatment shows dose-dependent phosphorylation of the two major AMPK targets Acetyl-CoA Carboxylase (ACC) on Ser79 and of Raptor on Ser792. And also increases Thr172 phosphorylation on the AMPK α subunit. MT 63-78 (25 μM; 24 hours; LNCaP and CRPC cells) treatment causes a significant enrichment in the G2/M population .MT 63-78 (30 mg/kg; intraperitoneal injection; daily; for 14 days; C57 BL/6 male mice) treatment causes a 33% inhibition of tumor growth.