MT 63-78 是一种有效的直接AMPK激活剂,EC50为 25 μM。它诱导细胞有丝分裂阻滞和细胞凋亡,通过抑制脂肪生成和mTORC1途径来阻止前列腺癌的生长,具有抗肿瘤作用。
产品描述
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.
体外活性
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 .
体内活性
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.
Cas No.
1179347-65-9
分子式
C21H14N2O2
分子量
326.35
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years