3.1.1.53 2,3-Butanedione irreversibly inactivated 1001 3.1.1.53 2,3-Butanedione inhibited by this arginine-modifying reagents, an essential arginine residue in the active site is important for substrate recognition 1001 3.1.1.53 2-alpha-thiomethylmercuryl 9-acetamido-9-deoxy sialoside competitive inhibition, Ki: 4.2 mM; the inhibitor is used to prepare heavy atom derivatives of the crystals 31297 3.1.1.53 3,4-dichloroisocoumarin - 1040 3.1.1.53 9-acetamido-N-acetyl-O-acetylneuraminate no effect up to 5 mM 47004 3.1.1.53 9-acetamido-N-acetyl-O-acetylneuraminate little effect at 5 mM 47004 3.1.1.53 Alpha-naphthyl acetate competitive inhibitor 1254 3.1.1.53 ammonium (allyl 5-acetamido-3,5-dideoxy-4-O-methyl-D-glycero-alpha-D-galacto-2-nonulopyranosidonate) - 85072 3.1.1.53 ammonium (allyl 5-acetamido-9-O-methyl-3,5-dideoxy-D-glycero-alpha-D-galacto-2-nonulopyranosidonate) - 85070 3.1.1.53 bis-p-nitrophenyl phosphate little effect on the activity 918 3.1.1.53 CHAPS lowers the activity by 40% 1137 3.1.1.53 Cu2+ complete inhibition at 1 mM 19 3.1.1.53 Cu2+ 5 mM, 30% residual activity 19 3.1.1.53 Cu2+ - 19 3.1.1.53 deoxycholate 75-80% loss of activity at 2% concentration 441 3.1.1.53 diammonium (allyl 5-acetamido-3,5-dideoxy-4-O-(P-methylphosphonyl)-D-glycero-alpha-D-galacto-2-nonulopyranosidonate) - 85073 3.1.1.53 diammonium (allyl 5-acetamido-3,5-dideoxy-9-O-(P-methylphosphonyl)-D-glycero-alpha-D-galacto-2-nonulopyranosidonate) - 85071 3.1.1.53 Diethyl-4-nitrophenylphosphate 50% inhibition at 0.0024 mM 9149 3.1.1.53 Diethyl-4-nitrophenylphosphate - 9149 3.1.1.53 Diethyl-4-nitrophenylphosphate 50% inhibition at 0.24 mM 9149 3.1.1.53 Diethyl-4-nitrophenylphosphate irreversibly inactivated 9149 3.1.1.53 diisopropyl fluorophosphate DFP strong inhibition 244 3.1.1.53 diisopropyl fluorophosphate 50% inhibition at 0.35 mM 244 3.1.1.53 diisopropyl fluorophosphate - 244 3.1.1.53 diisopropyl fluorophosphate 50% inhibition at 0.01 mM 244 3.1.1.53 diisopropyl fluorophosphate irreversibly inactivated 244 3.1.1.53 diisopropyl fluorophosphates complete inhibition at 1 mM 11341 3.1.1.53 diisopropylfluorophosphate 1 mM, 25°C, 15 min, total loss of activity 299 3.1.1.53 F- little effect on the activity 174 3.1.1.53 Hg2+ complete inhibition at 1 mM 33 3.1.1.53 Hg2+ 50% inhibition at 0.0035 mM 33 3.1.1.53 Hg2+ - 33 3.1.1.53 Hg2+ little effect on the activity 33 3.1.1.53 additional information no inhibition by PMSF 2 3.1.1.53 additional information bis-(4-nitrophenyl)phosphate, 1 mM Ca2+, 1 mM ethylene diaminotetraacetate (EDTA) without influence on activity 2 3.1.1.53 additional information synthesis and evaluation of a series of sialosides modified at the 4- and 9-hydroxy group for inhibition of the viral haemagglutinin-esterase activity from various Orthomyxoviruses and Coronaviruses, overview. While no inhibition of the sialate-4-O-acetylesterases from Mouse hepatitis virus strain S or Sialodacryoadenitis virus is found, a 9-O-methyl derivative displays inhibitory activity against recombinant sialate-9-O-acetylesterase from Influenza C virus. No inhibition of Bovine coronavirus by ammonium (allyl 5-acetamido-3,5-dideoxy-4-O-methyl-D-glycero-alpha-D-galacto-2-nonulopyranosidonate) and diammonium (allyl 5-acetamido-3,5-dideoxy-4-O-(P-methylphosphonyl)-D-glycero-alpha-D-galacto-2-nonulopyranosidonate) 2 3.1.1.53 additional information synthesis and evaluation of a series of sialosides modified at the 4- and 9-hydroxy group for inhibition of the viral haemagglutinin-esterase activity from various Orthomyxoviruses and Coronaviruses, overview. While no inhibition of the sialate-4-O-acetylesterases from Mouse hepatitis virus strain S or Sialodacryoadenitis virus is found, a 9-O-methyl derivative displays inhibitory activity against recombinant sialate-9-Oacetylesterase from Influenza C virus. No inhibition of Influenza C virus by ammonium (allyl 5-acetamido-3,5-dideoxy-4-O-methyl-D-glycero-a-D-galacto-2-nonulopyranosidonate) and diammonium (allyl 5-acetamido-3,5-dideoxy-4-O-(P-methylphosphonyl)-D-glycero-a-d-galacto-2-nonulopyranosidonate) 2 3.1.1.53 additional information synthesis and evaluation of a series of sialosides modified at the 4- and 9-hydroxy group for inhibition of the viral haemagglutinin-esterase activity from various Orthomyxoviruses and Coronaviruses, overview. While no inhibition of the sialate-4-O-acetylesterases from Mouse hepatitis virus strain S or Sialodacryoadenitis virus is found, a 9-O-methyl derivative displays inhibitory activity against recombinant sialate-9-O-acetylesterase from Influenza C virus. No inhibition of Mouse hepatitis virus strain S by ammonium (allyl 5-acetamido-9-O-methyl-3,5-dideoxy-D-glycero-alpha-D-galacto-2-nonulopyranosidonate) and diammonium (allyl 5-acetamido-3,5-dideoxy-9-O-(P-methylphosphonyl)-D-glycero-alpha-D-galacto-2-nonulopyranosidonate) 2 3.1.1.53 additional information synthesis and evaluation of a series of sialosides modified at the 4- and 9-hydroxy group for inhibition of the viral haemagglutinin-esterase activity from various Orthomyxoviruses and Coronaviruses, overview. While no inhibition of the sialate-4-O-acetylesterases from Mouse hepatitis virus strain S or Sialodacryoadenitis virus is found, a 9-O-methyl derivative displays inhibitory activity against recombinant sialate-9-O-acetylesterase from Influenza C virus. No inhibition of Rat sialoadacryoadenitis coronavirus by ammonium (allyl 5-acetamido-9-O-methyl-3,5-dideoxy-dglycero-alpha-D-galacto-2-nonulopyranosidonate) and diammonium (allyl 5-acetamido-3,5-dideoxy-9-O-(P-methylphosphonyl)-D-glycero-alpha-D-galacto-2-nonulopyranosidonate) 2 3.1.1.53 additional information not inhibitory: Ca2+, Zn2+, Co2+, Mn2+ and Mg2+ or EDTA 2 3.1.1.53 additional information not affected by detergents, i.e. Triton X-100, Triton CF-54, saponin; not affected by EDTA 2 3.1.1.53 additional information not affected by detergents, i.e. Triton X-100, Triton CF-54, saponin 2 3.1.1.53 N-acetyl-9-O-acetylneuraminate substrate inhibition above 2 mM 31551 3.1.1.53 p-chloromercuribenzoate little effect on the activity 43 3.1.1.53 paraoxon diethyl-4-nitrohenylphosphate (E600), 1 mM at 25°C within 15 min leads to total loss of activity 228 3.1.1.53 Phenylglyoxal irreversibly inactivated 301 3.1.1.53 Phenylglyoxal inhibited by this arginine-modifying reagents, an essential arginine residue in the active site is important for substrate recognition 301 3.1.1.53 phenylmethylsulfonyl fluoride complete inhibition at 10 mM 257 3.1.1.53 physostigmine 25% inhibition at 10 mM 1207 3.1.1.53 PMSF 45% inhibition at 1 mM 248 3.1.1.53 Zn2+ - 14