56396-35-1
56396-35-1 結(jié)構(gòu)式
基本信息
線粒體丙酮酸轉(zhuǎn)運蛋白抑制劑(UK-5099)
2-氰基-3-(1-苯基-1H-吲哚-3-基)-2-丙烯酸
UK 5099
PF-1005023
PF-06340678
BIZNHCWFGNKBBZ-JLHYYAGUSA-N
2-cyano-3-(1-phenylindol-3-yl)acrylate
Mitochondrial Pyruvate Carrier Inhibitor, UK5099
PF-1005023
UK5099
UK 5099
PF1005023
PF 1005023
(E)-2-cyano-3-(1-phenyl-1H-indol-3-yl)acrylic acid
2-Cyano-3-(1-phenyl-1H-indol-3-yl)-2-propenoicacid
物理化學(xué)性質(zhì)
常見問題列表
| Target | Value |
|
mitochondrial pyruvate carrier
() | 49 μM(Ki) |
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.
The MPC inhibitor UK5099 increases the glucose excursion seen during an intraperitoneal glucose tolerance test in C57BLK mice.