PZ0160
UK-5099
≥98% (HPLC), powder, mitochondrial pyruvate carrier inhibitor
别名:
2-氰基-3-(1-苯基-1H-吲哚-3-基)-2-丙烯酸, PF-1005023
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关于此项目
经验公式（希尔记法）:
C18H12N2O2
化学文摘社编号:
分子量:
288.30
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
UK-5099, ≥98% (HPLC)
SMILES string
OC(=O)\C(=C\c1cn(-c2ccccc2)c3ccccc13)C#N
InChI key
BIZNHCWFGNKBBZ-JLHYYAGUSA-N
InChI
1S/C18H12N2O2/c19-11-13(18(21)22)10-14-12-20(15-6-2-1-3-7-15)17-9-5-4-8-16(14)17/h1-10,12H,(H,21,22)/b13-10+
assay
≥98% (HPLC)
form
powder
color
yellow to tan
solubility
DMSO: >20 mg/mL
storage temp.
2-8°C
Quality Level
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Application
UK-5099已用于：
- 在用于前列腺癌细胞系培养的Roswell公园纪念研究所（RPMI）1640培养基中用作线粒体丙酮酸阻滞剂，以减少丙酮酸向线粒体的运输
- 二甲基亚砜（DMSO）的储备液中， 以研究抑制丙酮酸转运入线粒体对脂多糖激活的巨噬细胞促炎反应的影响
- 局部处理，以用于研究其对实验小鼠毛发周期诱导的作用
Biochem/physiol Actions
UK-5099可诱导产生乳酸。
UK-5099是线粒体丙酮酸转运蛋白的有效抑制剂。
UK-5099是线粒体丙酮酸转运蛋白的有效抑制剂。n大鼠心脏线粒体，UK-5099可抑制丙酮酸依赖性O2消耗，IC50 为50 nM。
Features and Benefits
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存储类别
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
M O Proudlove et al.
The Biochemical journal, 247(2), 441-447 (1987-10-15)
1. Mitochondria isolated from the thermogenic spadices of Arum maculatum and Sauromatum guttatum plants oxidized external NADH, succinate, citrate, malate, 2-oxoglutarate and pyruvate without the need to add exogenous cofactors. 2. Oxidation of substrates was virtually all via the alternative
Ajit S Divakaruni et al.
Proceedings of the National Academy of Sciences of the United States of America, 110(14), 5422-5427 (2013-03-21)
Facilitated pyruvate transport across the mitochondrial inner membrane is a critical step in carbohydrate, amino acid, and lipid metabolism. We report that clinically relevant concentrations of thiazolidinediones (TZDs), a widely used class of insulin sensitizers, acutely and specifically inhibit mitochondrial
Oleic acid stimulates glucagon-like peptide-1 release from enteroendocrine cells by modulating cell respiration and glycolysis
Clara R, et al.
Metabolism and Disease, 65(3), 8-17 (2016)
B J Dezube et al.
Journal of acquired immune deficiency syndromes and human retrovirology : official publication of the International Retrovirology Association, 14(1), 13-17 (1997-01-01)
Interleukin-6 (IL-6) may be important in the pathogenesis of HIV-1 because of its ability to induce HIV-1 expression in infected cells in vitro. Tenidap, a structurally and functionally novel antirheumatic drug affecting diverse biologic processes, has been shown to reduce
Interleukin-1beta secretion is impaired by inhibitors of the Atp binding cassette transporter, ABC1.
Y Hamon et al.
Blood, 90(8), 2911-2915 (1997-10-24)
The production of interleukin-1beta (IL-1beta), a powerful mediator of inflammation, is tightly regulated at several levels. However, in some pathologic conditions, a pharmacologic treatment is required to control the toxicity of excessive extracellular IL-1beta. Because of the heavy side effects
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