2.4.1.212 2-deoxyglucose - 6423 2.4.1.212 4-methylesculetin - 34881 2.4.1.212 4-Methylumbelliferone changes the localization of the enzyme by preventing its association with the plasma membrane 319 2.4.1.212 4-Methylumbelliferone - 319 2.4.1.212 4-Methylumbelliferone inhibits HAS because it depletes UDPGlcUA in cells; inhibits HAS because it depletes UDPGlcUA in cells; inhibits HAS because it depletes UDPGlcUA in cells 319 2.4.1.212 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside modulates aortic smooth muscle cell motility and adhesive properties through AMP-activated protein kinase, AMPK 6097 2.4.1.212 AG825 ErbB2 inhibitor, blocks the heregulin-mediated HAS isozyme phosphorylation/activation; ErbB2 inhibitor, blocks the heregulin-mediated HAS isozyme phosphorylation/activation; ErbB2 inhibitor, blocks the heregulin-mediated HAS isozyme phosphorylation/activation 38150 2.4.1.212 brefeldin A - 5284 2.4.1.212 ceramide - 726 2.4.1.212 DTNB 52% inhibition at 0.5 mM 554 2.4.1.212 EDTA - 21 2.4.1.212 ethylene glycol - 1410 2.4.1.212 glycerol - 135 2.4.1.212 HAS1 siRNA - 146778 2.4.1.212 iodoacetamide 15% inhibition at 5 mM, biphasic inhibition 67 2.4.1.212 iodoacetamide 13% inhibition at 5 mM, biphasic inhibition 67 2.4.1.212 mannose inhibits HAS because it depletes UDP-GlcNAc in cells; inhibits HAS because it depletes UDP-GlcNAc in cells; inhibits HAS because it depletes UDP-GlcNAc in cells 988 2.4.1.212 metformin modulates aortic smooth muscle cell motility and adhesive properties through AMP-activated protein kinase, AMPK 3021 2.4.1.212 methylmethanethiosulfonate 93% reduced activity at 0.05 mM 20380 2.4.1.212 methylmethanethiosulfonate 89% reduced activity at 0.05 mM 20380 2.4.1.212 additional information interleukin-1beta augmented the expression of all 3 isozymes in the uterine cervix of pregnant mice, progesterone inhibited expression of isozymes HAS1 and HAS2 2 2.4.1.212 additional information enzyme is more active in 25 mM phosphate buffer than in 50 mM, enzyme is inhibited by increasing viscosity via addition of PEG, glycerol, sucrose or ethylene glycol 2 2.4.1.212 additional information using inhibitors for MEK1/2, U0126, and for PI3K, LY294002, and the SN50 inhibitor, a complete inhibition of HAS2 transcriptional activity and hyaluronan sythesis is observed 2 2.4.1.212 additional information not inhibitory: 4-methylumbeliferone 2 2.4.1.212 additional information heating, oxidization or cysteine modification with N-ethylmaleimide inhibit the enzyme 2 2.4.1.212 additional information HA product size is decreased by increasing concentrations of glycerol 2 2.4.1.212 additional information AMP-activated protein kinase, AMPK, phosphorylates HAS2 at Thr110, which inhibits its enzymatic activity, and is itself inhibit by Compound C. Isoenzymes HAS1 and HAS3 are not modified by the kinase 2 2.4.1.212 N-ethylmaleimide - 49 2.4.1.212 N-ethylmaleimide reacts with the Cys residues C226, C262, and C281, but not with C367, binding of substrates UDP-N-acetyl-D-glucosamine, UDP-D-glucuronate, or of product UDP protects the enzyme from inhibition by NEM, level of inhibition of wild-type and mutant enzymes, overview 49 2.4.1.212 N-ethylmaleimide biphasic inhibition, about 50% reduced reaction velocity, unaltered Km-value, 70% inhibition at 5 mM 49 2.4.1.212 N-ethylmaleimide 60% inhibition at 5 mM, biphasic inhibition 49 2.4.1.212 N-ethylmaleimide inhibits wild-type and mutant enzymes by about 90% at 0.2 mM, UDP-N-acetyl-D-glucosamine protects the enzyme best against inactivation by NEM compared to diverse other nucleotide compounds, overview 49 2.4.1.212 PEG increasing MW increases the inhibitory effect on the enzyme, overview 34904 2.4.1.212 PEG 20000 - 23378 2.4.1.212 siRNA - 772 2.4.1.212 sodium arsenite inhibition of wild-type and mutant enzymes, no inhibition of C262 deletion mutant, overview 2419 2.4.1.212 sodium arsenite 40% inhibition at 10 mM 2419 2.4.1.212 sodium arsenite 46% inhibition at 10 mM 2419 2.4.1.212 sodium salicylate sodium salicylate is a potent suppressor of HAS1 activation 25215 2.4.1.212 sucrose - 55 2.4.1.212 sulfhydryl reagents enzyme is inhibited by sulfhydryl-modifying reagents, inhibition mode and mechanism 978 2.4.1.212 tetramyristoyl cardiolipin inactivating 125135 2.4.1.212 thiazolidinedione ERK inhibitor, blocks the heregulin-mediated HAS isozyme phosphorylation/activation; ERK inhibitor, blocks the heregulin-mediated HAS isozyme phosphorylation/activation; ERK inhibitor, blocks the heregulin-mediated HAS isozyme phosphorylation/activation 18785 2.4.1.212 UDP - 26 2.4.1.212 UDP-Gal - 1775 2.4.1.212 UDP-GalNAc - 550 2.4.1.212 UDP-GalUA - 125134 2.4.1.212 UDP-Glc - 7631 2.4.1.212 UDP-glucuronate The substrate UDP-GlcA inhibits pmHAS in concentrations above 8 mM 226 2.4.1.212 UMP - 133 2.4.1.212 UMP dead-end inhibitor 133 2.4.1.212 UTP - 65