Bestatin (Ubenimex)

製品コードS1591 バッチS159111

印刷

化学情報

Chemical Structure Synonyms NK421 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H24N2O4
分子量 308.37 CAS No. 58970-76-6
Solubility (25°C)* 体外 DMSO 4 mg/mL (12.97 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.
* <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 ベスタチン（Ubenimex）は、急性骨髄性白血病の治療に用いられる、強力なアミノペプチダーゼBおよびロイコトリエン（LT）A4加水分解酵素阻害剤です。
in vitro

Bestatin (Ubenimex) inhibits proliferation of all the human leukemic cell lines except KG1. It induces DNA fragmentation quantitatively and DNA ladder and enhances caspase-3 activity in U937 cells. This compound dose-dependently induces DNA fragmentation in human leukemic cell lines. It also dose-dependently inhibits the invasion of SN12M cells into reconstituted basement membrane (Matrigel). Bestatin inhibits the degradation of type IV collagen by tumor cells, but not by tumor-conditioned medium (TCM), in a concentration-dependent manner. It inhibits hydrolysing activities towards substrates of aminopeptidases in SN12M cells. The compound inhibits the tube-like formation of human umbilical vein endothelial cells (HUVECs) in vitro. It exerts a direct stimulating effect on lymphocytes (and monocytes) via its fixation on cell surface leucine-aminopeptidase, and an indirect effect on monocytes (and lymphocytes) via aminopeptidase B inhibition of tuftsin catabolism.

in vivo

Bestatin (Ubenimex) significantly inhibits melanoma cell-induced angiogenesis in a mouse dorsal air sac assay and reduces the number of vessels oriented towards the established primary tumor mass on the dorsal side of mice implanted with B16-BL6 melanoma cells. It also statistically significantly inhibits leukotriene B4 biosynthesis in the esophageal tissues of EGDA rats and reduces the incidence of EAC from 57.7% (15 of 26 rats) to 26.1% (6 of 23 rats).

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/10374877/
  • https://pubmed.ncbi.nlm.nih.gov/1733647/
  • https://pubmed.ncbi.nlm.nih.gov/15500947/
  • https://pubmed.ncbi.nlm.nih.gov/1912369/
  • https://pubmed.ncbi.nlm.nih.gov/12865451/
  • https://pubmed.ncbi.nlm.nih.gov/7913090/

カスタマーフィードバック

Data from [Data independently produced by , , PLoS One, 2015, 10(11):e0142124.]

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：

Targeting the GPI transamidase subunit GPAA1 abrogates the CD24 immune checkpoint in ovarian cancer [ Cell Rep, 2024, 43(4):114041] PubMed: 38573857
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Novel paired CD13-negative (MT-50.1) and CD13-positive (MT-50.4) HTLV-1-infected T-cell lines with differential regulatory T cell-like activity [ Sci Rep, 2024, 14(1):12549] PubMed: 38822041
Protocol for monitoring phagocytosis of cancer cells by TAM-like macrophages using imaging cytometry [ STAR Protoc, 2024, 5(4):103320] PubMed: 39298319
Cholesterol-induced leucine aminopeptidase 3 (LAP3) upregulation inhibits cell autophagy in pathogenesis of NAFLD [ Aging (Albany NY), 2022, 14(7):3259-3275] PubMed: 35404840
Sarsasapogenin ameliorates diabetes-associated memory impairment and neuroinflammation through down-regulation of PAR-1 receptor [ Phytother Res, 2021, 35(6):3167-3180] PubMed: 33885189
CD13 promotes hepatocellular carcinogenesis and sorafenib resistance by activating HDAC5-LSD1-NF-κB oncogenic signaling [ Clin Transl Med, 2020, 10(8):e233] PubMed: 33377659
Sarsasapogenin alleviates diabetic nephropathy through suppression of chronic inflammation by down-regulating PAR-1: In vivo and in vitro study [ Phytomedicine, 2020, 78:153314] PubMed: 32882582
Thrombin/PAR-1 activation induces endothelial damages via NLRP1 inflammasome in gestational diabetes [ Biochem Pharmacol, 2020, 175:113849] PubMed: 32059841
Sensitivity of Human Intrahepatic Cholangiocarcinoma Subtypes to Chemotherapeutics and Molecular Targeted Agents: A Study on Primary Cell Cultures [Fraveto A, et al. PLoS One, 2015, 10(11):e0142124] PubMed: 26571380

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。