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Literature summary for 3.2.1.169 extracted from

  • Chen, W.; Shen, S.; Dong, L.; Zhang, J.; Yang, Q.
    Selective inhibition of beta-N-acetylhexosaminidases by thioglycosyl-naphthalimide hybrid molecules (2018), Bioorg. Med. Chem., 26, 394-400 .
    View publication on PubMed
Search for more literature for 3.2.1.169

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21(DE3) cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-amino-1H-benzo[de]isoquinoline-1,3(2H)-dione 22.2% inhibition at 0.1 mM Homo sapiens
2-[[1-[(2-acetamido-beta-D-glucopyranosylthiomethyl)-1H-1,2,3-triazol-4-yl]methyl]-1H-benzo[de]isoquinoline-1,3(2H)-dione 18.5% inhibition at 0.1 mM Homo sapiens
2-[[1-[2-[(2-acetamido-beta-D-glucopyranosyl)thio]ethyl]-1H-1,2,3-triazol-4-yl]methyl]-1H-benzo[de]isoquinoline-1,3(2H)-dione 27.8% inhibition at 0.1 mM Homo sapiens
2-[[1-[3-[(2-acetamido-beta-D-glucopyranosyl)thio]propyl]-1H-1,2,3-triazol-4-yl]methyl]-1H-benzo[de]isoquinoline-1,3(2H)-dione 22.7% inhibition at 0.1 mM Homo sapiens
2-[[1-[4-[(2-acetamido-beta-D-glucopyranosyl)thio]butyl]-1H-1,2,3-triazol-4-yl]methyl]-1H-benzo[de]isoquinoline-1,3(2H)-dione 25.1% inhibition at 0.1 mM Homo sapiens
2-[[1-[5-[(2-acetamido-beta-D-glucopyranosyl)thio]pentyl]-1H-1,2,3-triazol-4-yl]methyl]-1H-benzo[de]isoquinoline-1,3(2H)-dione 26% inhibition at 0.1 mM Homo sapiens
2-[[1-[6-[(2-acetamido-beta-D-glucopyranosyl)thio]hexyl]-1H-1,2,3-triazol-4-yl]methyl]-1H-benzo[de]isoquinoline-1,3(2H)-dione 25.7% inhibition at 0.1 mM Homo sapiens
LOGNAc i.e. 2-acetamido-2-deoxy-D-gluconhydroximo-1,5-lactone Homo sapiens
N-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)-2-[(2-acetamido-beta-D-glucopyranosyl)thio]acetamide 31.1% inhibition at 0.1 mM Homo sapiens
N-[2-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)ethyl]-2-[(2-acetamido-beta-D-glucopyranosyl) thio]acetamide 38.6% inhibition at 0.1 mM Homo sapiens
N-[2-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)ethyl]-3-[(2-acetamido-beta-D-glucopyranosyl)thio]propanamide 66.9% inhibition at 0.1 mM Homo sapiens
N-[3-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)propyl]-2-[(2-acetamido-beta-D-glucopyranosyl)thio]acetamide 97.6% inhibition at 0.1 mM Homo sapiens
N-[3-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)propyl]-3-[(2-acetamido-beta-D-glucopyranosyl)thio]propanamide 59.4% inhibition at 0.1 mM Homo sapiens
N-[4-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)butyl]-2-[(2-acetamido-beta-D-glucopyranosyl)thio]acetamide 50% inhibition at 0.1 mM Homo sapiens
N-[4-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)butyl]-3-[(2-acetamido-beta-D-glucopyranosyl)thio]propanamide 34.3% inhibition at 0.1 mM Homo sapiens
NAG-thiazoline
-
 Homo sapiens
naphthalimide
-
 Homo sapiens
PUGNAc i.e. O-(2-acetamido-2-deoxy-D-glucopyranosylidenamino) N-phenylcarbamate, 98.9% inhibition at 0.1 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens O60502
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-methylumbelliferyl N-acetyl-beta-D-glucosaminide + H2O
-
 Homo sapiens 4-methylumbelliferone + N-acetyl-beta-D-glucosamine
-
 ?

Synonyms

Synonyms Comment Organism
O-GlcNAcase
-
 Homo sapiens
OGA
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.1
-
 at pH 6.5 and 30°C Homo sapiens N-[4-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)butyl]-2-[(2-acetamido-beta-D-glucopyranosyl)thio]acetamide