UK-5099
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
UK-5099是一种强效的线粒体丙酮载体抑制剂[1]。
线粒体丙酮载体(MPC)协助丙酮酸盐穿过线粒体内膜转运,并在碳水化合物、脂质和氨基酸代谢中起关键作用。
UK-5099 (1 mM)完全阻断丙酮酸盐摄取,Ki值为49 μM。同时,UK-5099浓度依赖性地减少总的外流率[ 1 ]。在分离自S. Guttatum的线粒体中,UK-5099 (20 μM)抑制丙酮酸盐依赖型02的消耗[ 2 ]。
在大鼠心脏线粒体中,UK-5099 抑制丙酮酸氧化作用,其具有非线性的阻抑动力学[ 2 ]。在胰高血糖素处理过的大鼠中,UK-5099 呈线性关系地抑制丙酮酸羧化反应和全部丙酮酸代谢[ 3 ]。在大鼠肝脏和心脏线粒体中,UK-5099抑制丙酮酸盐依赖型02的消耗,IC50值为50 nM [4]。
参考文献:
[1]. Wiemer EA, Michels PA, Opperdoes FR. The inhibition of pyruvate transport across the plasma membrane of the bloodstream form of Trypanosoma brucei and its metabolic implications. Biochem J, 1995, 312 ( Pt 2): 479-484.
[2]. Halestrap AP. The mitochondrial pyruvate carrier. Kinetics and specificity for substrates and inhibitors. Biochem J, 1975, 148(1): 85-96.
[3]. Halestrap AP, Armston AE. A re-evaluation of the role of mitochondrial pyruvate transport in the hormonal control of rat liver mitochondrial pyruvate metabolism. Biochem J, 1984, 223(3): 677-685.
[4]. Proudlove MO, Beechey RB, Moore AL. Pyruvate transport by thermogenic-tissue mitochondria. Biochem J, 1987, 247(2): 441-447.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 288.3 |
Cas No. | 56396-35-1 |
Formula | C18H12N2O2 |
Synonyms | PF-1005023;UK5099;UK 5099;PF1005023;PF 1005023 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥28.8 mg/mL in DMSO |
Chemical Name | (E)-2-cyano-3-(1-phenylindol-3-yl)prop-2-enoic acid |
SDF | Download SDF |
Canonical SMILES | C1=CC=C(C=C1)N2C=C(C3=CC=CC=C32)C=C(C#N)C(=O)O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Cell experiment:[1] | |
Cell lines |
832/13 cells derived from INS-1 rat insulinoma cells |
Reaction Conditions |
50 ~ 150 μM UK-5099 for 30 ~ 65 min incubation |
Applications |
UK-5099 significantly inhibited the glucose-stimulated rise in oxygen consumption in a dose-dependent manner and at 150 μM reduced oxygen consumption below basal levels. Moreover, UK-5099 (150 μM) reduced ATP levels and increased ADP and AMP levels in 832/13 cells. |
Animal experiment:[1] | |
Animal models |
C57BLK mice |
Dosage form |
32 μmol/kg Injected intraperitoneally 30 min before the glucose challenge |
Applications |
UK-5099 caused a significantly greater glucose excursion at 30, 60, and 120 min as compared with DMSO control mice. The area under the curve was also significantly increased by UK-5099 as compared with DMSO control mice. Thus, UK-5099 resulted in impaired glucose tolerance in vivo. |
Note |
The technical data provided above is for reference only. |
References: 1. Patterson JN, Cousteils K, Lou JW, et al Mitochondrial metabolism of pyruvate is essential for regulating glucose-stimulated insulin secretion. Journal of Biological Chemistry, 2014, 289(19): 13335-13346. |
质量控制和MSDS
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