Bestatin (Ubenimex)

製品コードS1591 バッチS159109

化学情報

	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
* <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.

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生物活性

製品説明	Bestatin (Ubenimex) is a potent aminopeptidase-B and leukotriene (LT) A4 hydrolase inhibitor, used in the treatment of acute myelocytic leukemia.
in vitro	Bestatin inhibits proliferation of all the human leukemic cell lines except KG1. Bestatin induces DNA fragmentation quantitatively and DNA ladder and enhances caspase-3 activity in U937 cells. Bestatin dose-dependently induces DNA fragmentation in human leukemic cell lines. ^[1] Bestatin 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. Bestatin inhibits hydrolysing activities towards substrates of aminopeptidases in SN12M cells. ^[2] Bestatin inhibits the tube-like formation of human umbilical vein endothelial cells (HUVECs) in vitro. ^[3] Bestatin 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. ^[4]
in vivo	Bestatin significantly inhibits the melanoma cell-induced angiogenesis in a mouse dorsal air sac assay. Bestatin reduces the number of vessels oriented towards the established primary tumor mass on the dorsal side of mice implantated of B16-BL6 melanoma cells. ^[3] Bestatin statistically significantly inhibits leukotriene B4 biosynthesis in the esophageal tissues of EGDA rats and reduces the incidence of EAC in the EGDA rats from 57.7% (15 of 26 rats) to 26.1% (6 of 23 rats). ^[5]

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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：

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。

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