5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile
| 中文名称 | 5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile |
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| 中文同义词 | 化合物MT 63-78;5-{2',6'-二羟基-[1,1'-联苯基]-4-基}-1H-吲哚-3-甲腈;5-{2',6'-二羟基-[1,1'-二联苯]-4-基}-1H-吲哚-3-甲腈;5-{2',6'-二羟基-[1,1'-二联苯]-4-基}-1H-吲哚-3-甲腈 |
| 英文名称 | 5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile |
| 英文同义词 | 5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile;MT 63-78;1H-Indole-3-carbonitrile, 5-(2',6'-dihydroxy[1,1'-biphenyl]-4-yl)-;5-[4-(2,6-dihydroxyphenyl)phenyl]-1H-indole-3-carbonitrile;Raptor,mitotic,Mammalian target of Rapamycin,direct,antitumor,MT 63-78,mTOR,Thr172,arrest,dephosphorylation,Inhibitor,AMP-activated protein kinase,Mcl-1,mTORC1,Apoptosis,AMPK,MT 63 78,lipogenesis,BH3,MT 6378,p53,inhibit;5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile |
| CAS号 | 1179347-65-9 |
| 分子式 | C21H14N2O2 |
| 分子量 | 326.35 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1179347-65-9.mol |
| 结构式 | ![5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile 结构式](CAS/20180601/GIF/1179347-65-9.gif) |
5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile 性质
| 储存条件 | 4°C, protect from light |
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AMPK 25 μM (EC 50 ) |
mTORC1
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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.
MT 63-78 (25 μM; 24 hours; LNCaP and CRPC cells) treatment induces a significant enrichement in the G2/M population.
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.
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.
Cell Viability Assay
| 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
| 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
| 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
| 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. |
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.
| Animal Model: | C57 BL/6 male mice bearing LNCaP tumors |
| Dosage: | 30 mg/kg |
| Administration: | Intraperitoneal injection; daily; for 14 days |
| Result: | Led to a 33% inhibition of tumor growth. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-W058849 | MT 63-78 | 1 mg | 800元 | |
| 2024/04/30 | HY-W058849 | 5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile MT 63-78 | 1179347-65-9 | 5mg | 2100元 |