Bestatin (NK421)

For research use only.

Catalog No.S1591 Synonyms: Ubenimex

5 publications

Bestatin (NK421) Chemical Structure

CAS No. 58970-76-6

Bestatin (NK421, Ubenimex) is a potent aminopeptidase-B and leukotriene (LT) A4 hydrolase inhibitor, used in the treatment of acute myelocytic leukemia.

Selleck's Bestatin (NK421) has been cited by 5 publications

1 Customer Review

  • The aminopeptidase-N inhibitor, bestatin (C), showed an inhibitory effect on cell proliferation that predominated in mixed-IHCCA. *p< 0.05 mucin vs mixed, N experiments = 5-7.

    PLoS One, 2015, 10(11):e0142124.. Bestatin (NK421) purchased from Selleck.

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Biological Activity

Description Bestatin (NK421, Ubenimex) is a potent aminopeptidase-B and leukotriene (LT) A4 hydrolase inhibitor, used in the treatment of acute myelocytic leukemia.
Targets
Aminopeptidase-N [6]
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]

Protocol

Solubility (25°C)

In vitro DMSO 0.4 mg/mL (1.29 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 308.37
Formula

C16H24N2O4

CAS No. 58970-76-6
Storage powder
in solvent
Synonyms Ubenimex
Smiles CC(C)CC(C(=O)O)NC(=O)C(C(CC1=CC=CC=C1)N)O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID