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1179347-65-9

中文名稱(chēng) 5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile
英文名稱(chēng) 5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile
CAS 1179347-65-9
分子式 C21H14N2O2
分子量 326.35
MOL 文件 1179347-65-9.mol
1179347-65-9 結(jié)構(gòu)式 1179347-65-9 結(jié)構(gòu)式

基本信息

中文別名
化合物MT 63-78
英文別名
MT 63-78
5-{2',6'-dihydroxy-[1,1'-biphenyl]-4-yl}-1H-indole-3-carbonitrile
1H-Indole-3-carbonitrile, 5-(2',6'-dihydroxy[1,1'-biphenyl]-4-yl)-

物理化學(xué)性質(zhì)

儲(chǔ)存條件4°C, protect from light
形態(tài)Solid
顏色Light yellow to brown

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
防范說(shuō)明P261-P280-P305+P351+P338

常見(jiàn)問(wèn)題列表

生物活性
MT 63-78 是一種有效的直接 AMPK 激活劑,EC50 為 25 μM。M 63-78 還誘導(dǎo)細(xì)胞有絲分裂阻滯和細(xì)胞凋亡 (apoptosis)。MT 63-78 通過(guò)抑制脂肪生成和 mTORC1 途徑來(lái)阻止前列腺癌的生長(zhǎng)。MT 63-78 具有抗腫瘤作用。
靶點(diǎn)

AMPK

25 μM (EC 50 )

mTORC1

體外研究

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.
體內(nèi)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.
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