中文名称:

UK 5099

中文同义词:

2-氰基-3-(1-苯基-1H-吲哚-3-基)-2-丙烯酸;线粒体丙酮酸转运蛋白抑制剂(UK-5099);化合物UK5099

英文名称:

2-cyano-3-(1-phenylindol-3-yl)acrylate

英文同义词:

2-cyano-3-(1-phenylindol-3-yl)acrylate;PF-06340678;PF-1005023;2-Cyano-3-(1-phenyl-1H-indol-3-yl)-2-propenoicacid;UK 5099;(E)-2-cyano-3-(1-phenyl-1H-indol-3-yl)acrylic acid;BIZNHCWFGNKBBZ-JLHYYAGUSA-N;Mitochondrial Pyruvate Carrier Inhibitor, UK5099

CAS号:

56396-35-1

分子式:

C18H12N2O2

分子量:

288.3

EINECS号:

相关类别:

细胞生物学试剂;离子通道;膜转运;化工原料;Aromatics;Heterocycles;Inhibitors;Intermediates Fine Chemicals;Pfizer Compounds;Pharmaceuticals

Mol文件:

56396-35-1.mol

沸点 

448.6±45.0 °C(Predicted)

密度 

1.20

储存条件 

2-8°C

溶解度 

DMSO: >20mg/mL

酸度系数(pKa)

1.49±0.19(Predicted)

形态

powder

颜色

yellow to tan

InChIKey

BIZNHCWFGNKBBZ-JLHYYAGUSA-M

生物活性

UK-5099 (PF-1005023) 是线粒体丙酮酸转运蛋白 (MPC) 的有效抑制剂， 抑制丙酮酸依赖性O2消耗的 IC50 值为50 nM。

靶点

Target Value mitochondrial pyruvate carrier () 49 μM(Ki)

Target

Value

mitochondrial pyruvate carrier ()

49 μM(Ki)

体外研究

The trypanosomal pyruvate carrier is found to be rather insensitive to inhibition by alpha-cyano-4-hydroxycinnamate (K i =17 mM) but can be completely blocked by UK-5099 (K i =49 microM). UK-5099 also inhibits the monocarboxylate transporter (MCT) . UK5099 significantly inhibits the glucose-stimulated rise in oxygen consumption in a dose-dependent manner and at 150 μM reduced oxygen consumption below basal levels. UK5099 reduces ATP levels and increases ADP and AMP levels in 832/13 cells. The UK5099 treated cells show significantly higher proportion of side population fraction and express higher levels of stemness markers Oct3/4 and Nanog. UK5099 application may be an ideal model for Warburg effect studies.

体内研究

The MPC inhibitor UK5099 increases the glucose excursion seen during an intraperitoneal glucose tolerance test in C57BLK mice.

WGK Germany 

3