UK 5099

製品コードS5317 バッチS531706

印刷

化学情報

Chemical Structure Synonyms PF-1005023 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C18H12N2O2
分子量 288.30 CAS No. 56396-35-1
Solubility (25°C)* 体外 DMSO 100 mg/mL (346.86 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 1.250mg/ml (4.34mM) Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 UK5099 (PF-1005023) is a potent inhibitor of the mitochondrial pyruvate carrier, inhibiting pyruvate transport across the plasma membrane of trypanosomes with Ki value of 49 μM.
in vitro UK5099 covalently binds to Mpc and blocks pyruvate transport[2]. UK5099 enhances aerobic glycolysis and decreases mitochondrial oxidative phosphorylation in LnCap cell in vitro, which is accompanied by increasing proportion of side population (SP) fraction, higher level of stemness markers expression and exhibiting high resistance to chemotherapy. UK5099 enhances stem-like phenotype of prostatic cancer cell through metabolic shift from oxidative phosphorylation to aerobic glycolysis. UK5099 suppresses proliferation and arrested LnCap cell cycle at G1/G0[3].
in vivo UK-5099 slows the growth of patient-derived xenograft (PDX) tumors in mice without severe loss of animal body weight[4].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 C2C12 cells
濃度 10 μM
反応時間 24 hr
実験の流れ --
動物実験 動物モデル Female C.B-17-Icr-scid-scidJcl mice implanted subcutaneously with patient-derived grafts
投薬量 10 or 100 mg/kg/day
投与方法 p.o.

参考

  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1136287/
  • https://www.sciencedirect.com/science/article/pii/S1097276514007813
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4741963/
  • https://pubmed.ncbi.nlm.nih.gov/28408240/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Integrated molecular-phenotypic profiling reveals metabolic control of morphological variation in a stem-cell-based embryo model [ Cell Stem Cell, 2025, 32(5):759-777.e13] PubMed: 40245869
Hexokinase detachment from mitochondria drives the Warburg effect to support compartmentalized ATP production [ bioRxiv, 2025, 2025.02.07.637120] PubMed: 39975027
Hypoxia promotes metastasis by relieving miR-598-3p-restricted glycolysis in gastric cancer [ J Transl Med, 2024, 22(1):283] PubMed: 38491378
Inhibition of the mitochondrial pyruvate carrier simultaneously mitigates hyperinflammation and hyperglycemia in COVID-19 [ Sci Immunol, 2023, eadf0348] PubMed: 36821695
PASK links cellular energy metabolism with a mitotic self-renewal network to establish differentiation competence [ Elife, 2023, 12e81717] PubMed: 37052079
The mitochondrial pyruvate carrier complex potentiates the efficacy of proteasome inhibitors in multiple myeloma [ Blood Adv, 2023, 7(14):3485-3500] PubMed: 36920785
The mitochondrial pyruvate carrier complex potentiates the efficacy of proteasome inhibitors in multiple myeloma [ Blood Adv, 2023, 7(14):3485-3500] PubMed: 36920785
Perturbation of Copper Homeostasis Sensitizes Cancer Cells to Elevated Temperature [ Int J Mol Sci, 2023, 25(1)423] PubMed: 38203594
Generación de una plataforma para la producción de células CAR-T alogénicas: estudios de eficacia y seguridad [ University of Granada, 2023, ] PubMed: None
Copper induces cell death by targeting lipoylated TCA cycle proteins [ Science, 2022, 375(6586):1254-1261] PubMed: 35298263

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。