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MT 63-78

  Cat. No.:  DC60143   Featured
Chemical Structure
1179347-65-9
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More than 5000 active chemicals with high quality for research!
Field of application
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.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1179347-65-9
Chemical Name: 5-[4-(2,6-dihydroxyphenyl)phenyl]-1H-indole-3-carbonitrile
SMILES: OC1C=CC=C(O)C=1C1C=CC(C2C=C3C(=CC=2)NC=C3C#N)=CC=1
Formula: C21H14N2O2
M.Wt: 326.348064899445
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: MT 63-78 is a specific and potent direct AMPK activator with an EC50 of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects[1].
Target: AMPK:25 μM (EC50) mTORC1
In Vivo: MT 63-78 (30 mg/kg; intraperitoneal injection; daily; for 14 days; C57 BL/6 male mice) treatment leads to a 33% inhibition of tumor growth[1]. Animal Model: C57 BL/6 male mice bearing LNCaP tumors[1] Dosage: 30 mg/kg Administration: Intraperitoneal injection; daily; for 14 days Result: Led to a 33% inhibition of tumor growth.
In Vitro: MT 63-78 (0-50 μM; 4 days; LNCaP and PC3 cells) treatment shows a dose-dependent decrease in cell number, and concomitant to the activation of AMPK signaling[1]. MT 63-78 (25 μM; 24 hours; LNCaP and CRPC cells) treatment induces a significant enrichement in the G2/M population[1]. 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 accumulation of the pro-apoptotic BH3-only protein Puma[1]. MT 63-78 (0-50 μM; 30 minutes; LNCaP and PC3 cells) treatment shows a 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[1]. Cell Viability Assay[1] Cell Line: LNCaP and PC3 cells Concentration: 0 μM, 1 μM, 5 μM, 10 μM, 25 μM, 50 μM Incubation Time: 4 days Result: A dose-dependent decrease in cell number, concomitant to the activation of AMPK signaling was observed. Cell Cycle Analysis[1] Cell Line: LNCaP and CRPC cells Concentration: 25 μM Incubation Time: 24 hours Result: Induced a significant enrichement in the G2/M population in both androgen sensitive and CRPC cell models. Apoptosis Analysis[1] Cell Line: LNCaP, PC3, C4-4, C4-2B, CL1and 22RV1cells Concentration: 0 μM, 10 μM, 25 μM, 50 μM Incubation Time: 24 hours Result: Induced reduction of anti-apoptotic Mcl-1 in concert with accumulation of the pro-apoptotic BH3-only protein Puma in all PCa cells. Western Blot Analysis[1] Cell Line: LNCaP and PC3 cells Concentration: 0 μM, 0.25 μM, 0.5 μM, 1 μM, 5 μM, 25 μM, 50 μM Incubation Time: 30 minutes Result: 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.
References: [1]. Zadra G, et al. A novel direct activator of AMPK inhibits prostate cancer growth by blocking lipogenesis. EMBO Mol Med. 2014 Apr;6(4):519-38.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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