EC Number |
Inhibitors |
Structure |
---|
2.4.1.133 | 1,4-diamino-2,3-dicyano-1,4-bis-(2-aminophenylthio)butadiene |
0-10 microM of specific inhibitor U0126 of MAP kinase cascade inhibits beta-1,4-GalT I mRNA production induced by lipopolysaccharide |
|
2.4.1.133 | 2-(6-hydroxynaphthyl) beta-D-xylopyranoside |
- |
|
2.4.1.133 | 3-acetamido-propyl beta-D-xylopyranoside |
- |
|
2.4.1.133 | 3-benzamido-propyl beta-D-xylopyranoside |
- |
|
2.4.1.133 | 3-hexanamido-propyl beta-D-xylopyranoside |
- |
|
2.4.1.133 | 4-methylumbelliferyl 4-deoxy-beta-D-fluoroxylose |
- |
|
2.4.1.133 | 4-methylumbelliferyl 4-deoxy-beta-D-xylopyranoside |
- |
|
2.4.1.133 | 4-methylumbelliferyl 4-deoxy-beta-D-xyloside |
- |
|
2.4.1.133 | 4-methylumbelliferyl 4-fluoro-beta-D-xylopyranoside |
50% inhibition at 2 mM. The strategic position of Tyr194 forming stacking interactions with the aglycone, and the hydrogen bond between the His195 nitrogen backbone and the carbonyl group of the coumarinyl molecule to develop a tight binder of the enzyme. This leads to the synthesis of 4-deoxy-4-fluoroxylose linked to 4-methylumbelliferone that inhibits enzyme activity in vitro with a Ki 10 times lower than the Km value and efficiently impairs glycosaminoglycan synthesis in a cell assay |
|
2.4.1.133 | 4-[4-(4-fluorophenyl)-5-(4-pyridinyl)-1H-imidazol-2-yl] phenol |
10-30 microM of specific inhibitor SB202190 of MAP kinase cascade inhibits beta-1,4-GalT I mRNA production induced by lipopolysaccharide |
|