2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
CAS NO.:1179347-65-9 Product Name:5-[4-(2,6-dihydroxyphenyl)phenyl]-1H-indole-3-carbonitrile Synonyms: EINEC: Molecular Formula:C21H14N2O2 Molecular Weight:326.348064899445
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.
Kinase Assay
Cell Assay
Animal Administration
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.
Return Policy
If you are in any way unsatisfied with your purchase, you may return any item(s) within 365 days of its original purchase date.
Please provide your Order Number in the email. We strive to reply to all email inquiries within one business day.