5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile
![5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile,1179347-65-9,结构式](https://www.chemicalbook.com/CAS/20180601/GIF/1179347-65-9.gif)
- CAS号:1179347-65-9
- 英文名:5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile
- 中文名:5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile
- CBNumber:CB83358519
- 分子式:C21H14N2O2
- 分子量:326.35
- MOL File:1179347-65-9.mol
- 储存条件 :4°C, protect from light
- 形态 :Solid
- 颜色 :Light yellow to brown
5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile性质、用途与生产工艺
- 生物活性 MT 63-78 是一种有效的直接 AMPK 激活剂，EC50 为 25 μM。M 63-78 还诱导细胞有丝分裂阻滞和细胞凋亡 (apoptosis)。MT 63-78 通过抑制脂肪生成和 mTORC1 途径来阻止前列腺癌的生长。MT 63-78 具有抗肿瘤作用。
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靶点
AMPK
25 μM (EC 50 )
mTORC1
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体外研究
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. -
体内研究
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.
- 更新日期：2024/11/08
- 产品编号：HY-W058849
- 产品名称：MT 63-78
- CAS编号：
- 包装：1 mg
- 价格：800元
- 更新日期：2024/11/08
- 产品编号：HY-W058849
- 产品名称：5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile MT 63-78
- CAS编号：1179347-65-9
- 包装：5mg
- 价格：2100元
- 公司名称：TargetMol Chemicals Inc.
- 联系电话：+1-781-999-5354 +1-00000000000
- 电子邮件：marketing@targetmol.com
- 国家：美国
- 产品数：32161
- 优势度：58
- 公司名称：MedChemExpress
- 联系电话：--
- 电子邮件：sales@medchemexpress.com
- 国家：美国
- 产品数：6398
- 优势度：58
