Nagstatin 

Nagstatin is a naturally derived competitive inhibitor of N-acetyl-β-D-glucosaminidase (NAG-ase), with an IC₅₀ of 0.0012 μg/mL and a K_i of 1.7×10^-8 M against porcine-derived enzyme. Nagstatin enhances cellular immune responses in normal mice and reactivates suppressed cellular immune responses in tumor-bearing mice. Nagstatin can be used in the research of various diseases such as diabetes and leukemia^[1].

Nagstatin potently and specifically inhibits partially purified porcine kidney N-acetyl-β-D-glucosaminidase in a competitive manner, with an IC₅₀ of 0.0012 μg/mL and a K_i of 1.7×10^-8 M^[1].
Nagstatin inhibits N-acetyl-β-D-glucosaminidase, with an IC₅₀ of 5.85 nM and a K_i of 1.10 nM against the enzyme from Spodoptera litura, an IC₅₀ of 10.6 nM and a K_i of 9.69 nM against the enzyme from Aspergillus oryzae, an IC₅₀ of 60.6 nM and a K_i of 8.11 nM against the enzyme from Penicillium oxalicum, an IC₅₀ of 1.83 nM and a K_i of 0.952 nM against the enzyme from human placenta, an IC₅₀ of 1.71 nM and a K_i of 1.64 nM against the enzyme from bovine kidney, and an IC₅₀ of 1.87 nM and a K_i of 1.41 nM against the enzyme from jack bean^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Nagstatin (250 mg/kg; i.p.; single dose) exhibits low acute toxicity in mice, with no mortality seen at a single intraperitoneal dose of 250 mg/kg^[1].
Nagstatin potentiates cellular immune response in normal mice at a potency comparable to bestatin^[1].
Nagstatin reactivates depressed cellular immune response in tumor-bearing mice at a potency comparable to bestatin^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

299.28

C₁₂H₁₇N₃O₆

126844-81-3

N(C(C)=O)[C@H]1C=2N([C@H](CO)[C@H](O)[C@@H]1O)C=C(CC(O)=O)N2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Aoyagi T, et al. Nagstatin, a new inhibitor of N-acetyl-beta-D-glucosaminidase, produced by Streptomyces amakusaensis MG846-fF3. Taxonomy, production, isolation, physico-chemical properties and biological activities. J Antibiot (Tokyo). 1992 Sep;45(9):1404-8.

  [2]. Usuki H, et al. Pochonicine, a polyhydroxylated pyrrolizidine alkaloid from fungus Pochonia suchlasporia var. suchlasporia TAMA 87 as a potent beta-N-acetylglucosaminidase inhibitor. Bioorg Med Chem. 2009;17(20):7248-7253.