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PZ0160

Sigma-Aldrich

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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About This Item

经验公式（希尔记法）:
C18H12N2O2
CAS号:
56396-35-1
分子量:
288.30
MDL號碼:
MFCD19443867
分類程式碼代碼:
12352200
PubChem物質ID:
329823742
NACRES:
NA.77

product name

UK-5099, ≥98% (HPLC)

品質等級

100

化驗

≥98% (HPLC)

形狀

powder

顏色

yellow to tan

溶解度

DMSO: >20 mg/mL

儲存溫度

2-8°C

SMILES 字串

OC(=O)\C(=C\c1cn(-c2ccccc2)c3ccccc13)C#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+

InChI 密鑰

BIZNHCWFGNKBBZ-JLHYYAGUSA-N

應用

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

生化／生理作用

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。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。

特點和優勢

该化合物是细胞凋亡研究的推荐产品。点击此处，了解更多精选的细胞凋亡产品。了解更多有关用于其他研究领域的生物活性小分子的信息，请访问sigma.com/discover-bsm。

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

分析证书(COA)

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M S Shearman et al.
The Biochemical journal, 223(3), 673-676 (1984-11-01)
alpha-Cyano-beta-(1-phenylindol-3-yl)acrylate inhibited pyruvate transport into both liver and heart mitochondria approximately linearly with respect to its concentration until 65% inhibition was achieved. The extent of inhibition was dependent on the mitochondrial protein concentration. By extrapolation of plots of inhibition versus
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
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
A P Halestrap et al.
The Biochemical journal, 223(3), 677-685 (1984-11-01)
The inhibitor of mitochondrial pyruvate transport alpha-cyano-beta-(1-phenylindol-3-yl)-acrylate was used to inhibit progressively pyruvate carboxylation by liver mitochondria from control and glucagon-treated rats. The data showed that, contrary to our previous conclusions [Halestrap (1978) Biochem. J. 172, 389-398], pyruvate transport could
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)
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