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ChemicalBook CAS数据库列表 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

生物活性靶点体外研究体内研究 5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile 试剂级价格

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

5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile化学性质

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。
靶点

AMPK

25 μM (EC ₅₀ )

mTORC1

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.