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CAS No.: 56396-35-1

UK-5099 Catalog No. CSN13884

Synonyms: PF-1005023

UK-5099 is a potent is MPC (mitochondrial pyruvate carrier) inhibitor with IC50 value of 50 nM.

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描述The mitochondrial pyruvate carriers (MPC) mediate pyruvate import into the mitochondria, which is key to the sustenance of the tricarboxylic cycle and oxidative phosphorylation^[3]. In two distinct CRC mouse models, loss of Mpc1 prior to a tumorigenic stimulus doubled the frequency of adenoma formation and produced higher grade tumors. MPC loss was associated with a glycolytic metabolic phenotype and increased expression of stem cell markers. UK-5099 (PF-1005023) is a potent inhibitor of MPC^[4]. UK-5099 (PF-1005023) inhibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.^[5]. The trypanosomal pyruvate carrier is found to be rather insensitive to inhibition by alpha-cyano-4-hydroxycinnamate (Ki=17 mM) but can be completely blocked by UK-5099 (Ki=49 mM)^[6]. UK-5099 also inhibits the monocarboxylate transporter (MCT)^[7]. 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^[8]. 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^[9].
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实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.4686 mL
- 17.3430 mL
- 34.6861 mL
- 5 mM
- 0.6937 mL
- 3.4686 mL
- 6.9372 mL
- 10 mM
- 0.3469 mL
- 1.7343 mL
- 3.4686 mL

技术信息

CAS号

56396-35-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H12N2O2

运输

蓝冰

分子量

288.30

别名

PF-1005023

溶解度

DMSO	290.0 mg/mL (1005.9 mM)
Water	insoluble

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