Name | 5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile |
Synonyms | MT 63-78 5-[4-(2,6-dihydroxyphenyl)phenyl]-1H-indole-3-carbonitrile 5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile 1H-Indole-3-carbonitrile, 5-(2',6'-dihydroxy[1,1'-biphenyl]-4-yl)- |
CAS | 1179347-65-9 |
Molecular Formula | C21H14N2O2 |
Molar Mass | 326.35 |
biological activity | MT 63-78 is a potent direct AMPK activator with an EC50 of 25 μm. M 63-78 also induces mitotic arrest and apoptosis. MT 63-78 prevents the growth of prostate cancer by inhibiting adipogenesis and the mTORC1 pathway. MT 63-78 has anti-tumor effect. |
Cell Line: | LNCaP and PC3 cells LNCaP and CRPC cells LNCaP, PC3, C4-4, C4-2B, CL1and 22RV1cells LNCaP and PC3 cells |
Concentration: | 0 μM, 1 μM, 5 μM, 10 μM, 25 μM, 50 μM 25 μM 0 μM, 10 μM, 25 μM, 50 μM 0 μM, 0.25 μM, 0.5 μM, 1 μM, 5 μM, 25 μM, 50 μM |
Incubation Time: | 4 days 24 hours 24 hours 30 minutes |
Result: | A dose-dependent decrease in cell number, concomitant to the activation of AMPK signaling was observed. Induced a significant enrichement in the G2/M population in both androgen sensitive and CRPC cell models. Induced reduction of anti-apoptotic Mcl-1 in concert with accumulation of the pro-apoptotic BH3-only protein Puma in all PCa cells. Observed a dose-dependent phosphorylation of the two major AMPK targets Acetyl-CoA Carboxylase (ACC) on Ser79 and of Raptor on Ser792. A corresponding increase in Thr172 phosphorylation on the AMPK α subunit was also observed. Led to a 33% inhibition of tumor growth. |
Animal Model: | C57 BL/6 male mice bearing LNCaP tumors |
Dosage: | 30 mg/kg |
Administration: | Intraperitoneal injection; daily; for 14 days |