3.1.1.32 2-mercaptoethanol weak inhibition 63 3.1.1.32 2-mercaptoethanol 2 mM, 43% inhibition 63 3.1.1.32 Al3+ inhibition of phospholipase A1 activity and lysophospholipase activity 264 3.1.1.32 arachidonyl trifluoromethyl ketone analogue - 138719 3.1.1.32 Ca2+ slight inhibition at 2 mM 15 3.1.1.32 Ca2+ up to 0.1 mM 15 3.1.1.32 Ca2+ 200 mM, 77% inhibition 15 3.1.1.32 Ca2+ CaCl2, slight 15 3.1.1.32 Ca2+ - 15 3.1.1.32 Ca2+ 10 mM CaCl2, 50-60% inhibition of lysosomal enzyme 15 3.1.1.32 Ca2+ 10 mM, 20-60% increase in activity 15 3.1.1.32 Cationic amphiphilic drugs - 98982 3.1.1.32 Cd2+ complete inhibition at 2 mM 52 3.1.1.32 CHAPS - 1137 3.1.1.32 chlorpromazine 1 mM, 50% inhibition 727 3.1.1.32 choline plasmalogen inhibits hydrolysis of phosphatidylethanolamine 12474 3.1.1.32 Co2+ 43% inhibition at 2 mM 23 3.1.1.32 cocaine 10 mM, below 10% residual activity 1231 3.1.1.32 Cr3+ 51.4% relative activity at 5 mM 895 3.1.1.32 Cu2+ complete inhibition at 2 mM 19 3.1.1.32 Cu2+ 56.8% relative activity at 5 mM 19 3.1.1.32 DFP - 923 3.1.1.32 di-isopropyl fluorophosphate TbPLA1 possesses an active-site serine residue, but is relatively insensitive to serine-modifying reagents such as di-isopropyl fluorophosphate and PMSF 35850 3.1.1.32 diethyl-p-nitrophenyl phosphate - 20240 3.1.1.32 diisopropyl fluorophosphate IC50: 8 mM 244 3.1.1.32 dithiothreitol 1 mM, complete inhibition 45 3.1.1.32 DNA containing thymine glycol 0.05 mM, 50% inhibition 33417 3.1.1.32 DNA containing thymine glycol - 33417 3.1.1.32 E-600 - 58859 3.1.1.32 EDTA no activity in the presence of EDTA 21 3.1.1.32 EDTA - 21 3.1.1.32 EDTA complete inhibition at 5 mM 21 3.1.1.32 EDTA 10 mM, 30-40% inhibition 21 3.1.1.32 ethanolamine plasmalogen inhibits hydrolysis of phosphatidylethanolamine 31450 3.1.1.32 Fe2+ complete inhibition at 2 mM 25 3.1.1.32 Fe2+ 89.2% relative activity at 5 mM 25 3.1.1.32 Fe2+ - 25 3.1.1.32 Fe2+ inhibition of phospholipase A1 activity and lysophospholipase activity 25 3.1.1.32 Fe2+ 5 mM 25 3.1.1.32 Fe3+ - 70 3.1.1.32 Fe3+ 10 mM, 79% inhibition 70 3.1.1.32 Fe3+ inhibition of phospholipase A1 activity and lysophospholipase activity 70 3.1.1.32 Fe3+ 1 mM, almost complete inhibition 70 3.1.1.32 gentamycin the inhibition by aminoglycosides appears to be due to substrate depletion caused by binding of aminoglycosides to the negatively charged phospholipid and can be overcome by raising the substrate concentration 8318 3.1.1.32 GSK264220A - 147041 3.1.1.32 guanosine 5'-[gamma-thio]triphosphate - 31492 3.1.1.32 Hg2+ 5 mM 33 3.1.1.32 Insulin significantly reduces endothelial lipase mRNA and protein expression in a dose dependent manner 524 3.1.1.32 iodoacetic acid - 213 3.1.1.32 KCl 2 M, inactivation of the soluble enzyme, no inactivation of the membrane-bound enzyme 79 3.1.1.32 lauryldimethylbenzyl ammonium chloride - 100829 3.1.1.32 liponox DCH 1%, i.e. polyoxyethylene alkylether 12984 3.1.1.32 methyl arachidonyl fluorophosphonate blocks phospholipase A1 as well as phospholipase A2 activity 2443 3.1.1.32 Mg2+ 13.5% relative activity at 5 mM 6 3.1.1.32 MgCl2 slight 196 3.1.1.32 Mn2+ slight inhibition at 2 mM 11 3.1.1.32 Mn2+ complete inhibition at 5 mM 11 3.1.1.32 additional information PLA1 is not affected by Mg2+, Cs2+, and EDTA 2 3.1.1.32 additional information inhibition of RP534 PLA2 activity by nanomolar amounts of the potent, irreversible inhibitor methyl arachidonoyl fluorophosphonate and by the reversible inhibitor arachidonoyl trifluoromethylketone 2 3.1.1.32 additional information the enzyme is not inhibited by EDTA and DTT 2 3.1.1.32 additional information not inhibitory: 0.1% Triton X-100 2 3.1.1.32 additional information naturally occuring inhibitors of lysosomal phospholipase A are present in two of the lysosomal-soluble protein fractions obtained in the purification 2 3.1.1.32 additional information a protein found in Bacillus subtilis specifically inhibits the phospholipase 2 3.1.1.32 additional information protease inhibitors, e.g. pepstatin, E 64, leupeptin or chymostatin reduce lysosomal acid phospholipase A1 activity in cultured rat hepatocytes 2 3.1.1.32 N-bromosuccinimide - 208 3.1.1.32 Na+ 54.7% relative activity at 5 mM 59 3.1.1.32 NaCl 10 mM, 50% inhibition 42 3.1.1.32 NaCl 100 mM, 20-30% inhibition of lysosomal enzyme 42 3.1.1.32 Ni2+ 57% inhibition at 2 mM 38 3.1.1.32 octyl-beta-glucoside - 30299 3.1.1.32 p-Diazobenzenesulfonic acid - 44646 3.1.1.32 palmitoyl trifluoromethyl ketone analogue - 138718 3.1.1.32 PMSF TbPLA1 possesses an active-site serine residue, but is relatively insensitive to serine-modifying reagents such as di-isopropyl fluorophosphate and PMSF 248 3.1.1.32 PMSF weak inhibition 248 3.1.1.32 rabbit anti-phospholipase A antibodies - 101416 3.1.1.32 Rosenthal's inhibitor - 138720 3.1.1.32 SDS - 124 3.1.1.32 SDS 20.9% relative activity at 5 mM 124 3.1.1.32 SDS 2 mM, 85% inhibition 124 3.1.1.32 SDS Triton enhances the inhibitory effect 124 3.1.1.32 sodium deoxycholate - 549 3.1.1.32 Sodium vanadate 0.01 mM, 50% inhibition 4598 3.1.1.32 taurodeoxycholate - 1833 3.1.1.32 tetrahydrolipstatin - 5351 3.1.1.32 thiol reagents protected by 2-mercaptoethanol 3246 3.1.1.32 tobramycin the inhibition by aminoglycosides appears to be due to substrate depletion caused by binding of aminoglycosides to the negatively charged phospholipid and can be overcome by raising the substrate concentration 939 3.1.1.32 Triton X-100 - 61 3.1.1.32 Triton X-100 complete inhibition at 5 mM 61 3.1.1.32 Triton X-100 weak inhibition at up to 0.23% w/v 61 3.1.1.32 Triton X-100 at high concentration 61 3.1.1.32 Tween 20 - 555 3.1.1.32 Zn2+ 66% inhibition at 2 mM 14 3.1.1.32 Zn2+ 52% relative activity at 5 mM 14 3.1.1.32 Zn2+ 10 mM, 44% inhibition 14