3.5.1.2 (2R)-1-(2-formyl-3,6-dihydroxy-5-methoxycyclohexa-1,4-dien-1-yl)tridecan-2-yl acetate - 204515 3.5.1.2 (2R)-1-(2-hydroxy-5-methoxy-3,6-dioxocyclohexa-1,4-dien-1-yl)pentadecan-2-yl acetate - 204516 3.5.1.2 (2R)-1-(2-hydroxy-5-methoxy-3,6-dioxocyclohexa-1,4-dien-1-yl)tridecan-2-yl acetate - 204517 3.5.1.2 (2R)-1-(3,6-dihydroxy-5-methoxycyclohexa-1,4-dien-1-yl)tridecan-2-yl acetate - 204518 3.5.1.2 (2R)-1-(5-methoxy-3,6-dioxocyclohexa-1,4-dien-1-yl)pentadecan-2-yl acetate - 204519 3.5.1.2 (2R)-1-(5-methoxy-3,6-dioxocyclohexa-1,4-dien-1-yl)tridecan-2-yl acetate - 204520 3.5.1.2 (2R)-1-[3-(acetyloxy)-6-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl]pentadecan-2-yl acetate - 204521 3.5.1.2 (2R)-1-[3-(acetyloxy)-6-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl]tridecan-2-yl acetate - 204522 3.5.1.2 (2S)-1-(5-methoxycyclohexa-1,4-dien-1-yl)heptan-2-ol - 204534 3.5.1.2 (2S)-2-amino-6-imino-5-oxohexanoic acid - 204536 3.5.1.2 1,2-naphthoquinone 4-sulfonate - 104160 3.5.1.2 1,4-Naphthoquinone - 1083 3.5.1.2 1-amino-8-naphthol-2,4-disulfonic acid weak 104208 3.5.1.2 2,2-dimethyl-5-[4-(methylsulfanyl)phenyl]-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one 97% inhibition at 0.05 mM 204866 3.5.1.2 2,2-dimethyl-5-[4-(naphthalen-1-yl)phenyl]-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one 97% inhibition at 0.05 mM 204867 3.5.1.2 2,2-dimethyl-5-[4-(propan-2-yl)phenyl]-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one 91% inhibition at 0.05 mM 204868 3.5.1.2 2,4-dinitro-1-naphthol-7-sulfonic acid i.e. flavianic acid 104454 3.5.1.2 2-bromo-4-(2,2-dimethyl-4-oxo-1,2,3,4,5,6-hexahydrobenzo[a]phenanthridin-5-yl)-6-methoxyphenyl acetate 84% inhibition at 0.05 mM 204954 3.5.1.2 2-hydroxy-5-methoxy-3-tridecylcyclohexa-2,5-diene-1,4-dione - 204964 3.5.1.2 2-methoxy-6-pentadecylcyclohexa-2,5-diene-1,4-dione - 204966 3.5.1.2 2-methoxy-6-tridecylcyclohexa-2,5-diene-1,4-dione - 204967 3.5.1.2 2-methyl-5-[(7Z)-pentadec-7-en-1-yl]cyclohexa-1,4-diene-1,3-diol - 204969 3.5.1.2 2-methyl-5-[(7Z)-tridec-7-en-1-yl]cyclohexa-1,4-diene-1,3-diol - 204970 3.5.1.2 2-oxoglutarate enzyme from mesenteric lymph nodes 34 3.5.1.2 2-oxoglutarate competitive inhibition 34 3.5.1.2 2-phenyl isoindolin-1-one - 206473 3.5.1.2 2-phenylbenzo[d] isoxazol-3(2H)-one - 206472 3.5.1.2 2-phenylbenzo[d]isothiazol-3(2H)-one - 206471 3.5.1.2 3-[(2S)-2-hydroxypentadecyl]-5-methoxycyclohexa-2,5-dien-1-ol - 205084 3.5.1.2 4-hydroxy-2-methoxy-6-(2-oxopentadecyl)cyclohexa-2,5-dien-1-yl acetate - 205178 3.5.1.2 5,5'-(sulfanediyldiethane-2,1-diyl)bis(1,3,4-thiadiazol-2-amine) - 205229 3.5.1.2 5-(3-bromo-4,5-dimethoxyphenyl)-2,2-dimethyl-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one complete inhibition at 0.05 mM 205248 3.5.1.2 5-(3-bromo-4-(dimethylamino)phenyl)-2,2-dimethyl-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one - 206478 3.5.1.2 5-(3-chloro-4,5-dimethoxyphenyl)-2,2-dimethyl-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one 88% inhibition at 0.05 mM 205249 3.5.1.2 5-(4-tert-butylphenyl)-2,2-dimethyl-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one 99% inhibition at 0.05 mM 205277 3.5.1.2 5-[(6Z)-13-(3,5-dihydroxy-4-methylcyclohexa-1,4-dien-1-yl)tridec-6-en-1-yl]-2-methylbenzene-1,3-diol - 205319 3.5.1.2 5-[(6Z)-13-(3,5-dihydroxy-4-methylcyclohexa-1,4-dien-1-yl)tridec-6-en-1-yl]benzene-1,3-diol - 205320 3.5.1.2 5-[(6Z)-13-(3-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl)tridec-6-en-1-yl]benzene-1,3-diol - 205321 3.5.1.2 5-[(7Z)-13-(3-hydroxy-5-methoxyphenyl)tridec-7-en-1-yl]-2-methylcyclohexa-1,4-diene-1,3-diol - 205322 3.5.1.2 5-[(7Z)-15-(3-hydroxy-5-methoxyphenyl)pentadec-7-en-1-yl]-2-methylcyclohexa-1,4-diene-1,3-diol - 205323 3.5.1.2 5-[(7Z)-pentadec-7-en-1-yl]cyclohexa-1,4-diene-1,3-diol - 205324 3.5.1.2 5-[(7Z)-tridec-7-en-1-yl]cyclohexa-1,4-diene-1,3-diol - 205325 3.5.1.2 5-[(8Z)-15-(3,5-dihydroxy-4-methylcyclohexa-1,4-dien-1-yl)pentadec-8-en-1-yl]-2-methylbenzene-1,3-diol - 205326 3.5.1.2 5-[(8Z)-15-(3,5-dihydroxy-4-methylcyclohexa-1,4-dien-1-yl)pentadec-8-en-1-yl]benzene-1,3-diol - 205327 3.5.1.2 5-[(8Z)-15-(3-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl)pentadec-8-en-1-yl]benzene-1,3-diol - 205328 3.5.1.2 5-[14-(3-hydroxy-5-methoxycyclohexa-1,4-dien-1-yl)tetradecyl]benzene-1,3-diol - 205330 3.5.1.2 5-[3-bromo-4-(dimethylamino)phenyl]-2,2-dimethyl-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one - 205331 3.5.1.2 5-[3-bromo-4-(dimethylamino)phenyl]-2,2-dimethyl-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one 95% inhibition at 0.05 mM 205331 3.5.1.2 5-[4-(diethylamino)phenyl]-2,2-dimethyl-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one 96% inhibition at 0.05 mM 205333 3.5.1.2 5-[4-(dimethylamino)phenyl]-2,2-dimethyl-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one 59% inhibition at 0.05 mM 205334 3.5.1.2 5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]-N-[2-(4-phenylpiperidin-1-yl)ethyl]pentanamide - 205336 3.5.1.2 5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]-N-[2-(piperidin-1-yl)ethyl]pentanamide - 205337 3.5.1.2 5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]-N-[2-(pyrrolidin-1-yl)ethyl]pentanamide - 205338 3.5.1.2 5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]-N-[4-(trifluoromethyl)benzyl]pentanamide - 205339 3.5.1.2 6-diazo-5-oxo-L-norleucine - 839 3.5.1.2 6-diazo-5-oxo-L-norleucine blockade of PAG, avoids the toxic effects of Gln accumulation in the brain 839 3.5.1.2 6-diazo-5-oxo-L-norleucine 10 mM, strongly inhibited, 80% inhibition, especially more strongly with a progress of purification steps 839 3.5.1.2 6-diazo-5-oxo-L-norleucine active site inhibitor, about 53% inhibition at about 1 mM 839 3.5.1.2 6-diazo-5-oxo-Lnorleucine time-dependent inhibition 206470 3.5.1.2 8-[3-bromo-4-(diethylamino)phenyl]-11,11-dimethyl-8,10,11,12-tetrahydrobenzo[a][4,7]phenanthrolin-9(7H)-one 96% inhibition at 0.05 mM 205394 3.5.1.2 8-[3-bromo-4-(dimethylamino)phenyl]-11,11-dimethyl-8,10,11,12-tetrahydrobenzo[a][4,7]phenanthrolin-9(7H)-one 91% inhibition at 0.05 mM 205395 3.5.1.2 Ag+ - 75 3.5.1.2 Al3+ 46% residual activity at 1 mM 264 3.5.1.2 ampicillin - 191 3.5.1.2 anthraquinone-1,8-disulfonate - 105447 3.5.1.2 apomorphine competitive inhibition, i.e. 5,6,6a,7-tetrahydro-6-methyl-4H-dibenzo[de,g]quinoline-10,11-diol 92466 3.5.1.2 arsenate 0.5 M, 74% inhibition 255 3.5.1.2 azaserine about 19% inhibition at about 1 mM 1861 3.5.1.2 BaCl2 inhibition to a variable extent 1275 3.5.1.2 Berberine - 1612 3.5.1.2 bicarbonate 0.5 M, complete inhibition 1136 3.5.1.2 bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl) ethyl sulfide i.e. BPTES, binds to an allosteric pocket at the dimer interface of kidney-type glutaminase, triggering a dramatic conformational change of the key loop (Glu312-Pro329) near the catalytic site and rendering it inactive, allosteric inhibition. Binding of BPTES stabilizes the inactive tetramers of the catalytic domain of kidney-type glutaminase. The binding mode of BPTES on the hydrophobic pocket determines its specificity to the kidney-type glutaminase isoform KGA 169823 3.5.1.2 bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide a potent inhibitor of kidney-type glutaminase, but not of the liver-type glutaminase, glutamate dehydrogenase or gamma-glutamyl transpeptidase. The potent inhibitor causes the formation of a stable, but inactive, tetramer 69210 3.5.1.2 bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide - 69210 3.5.1.2 bis-2-(5-phenylacetimido-1,2,4,thiadiazol-2-yl)ethyl sulfide inhibits specifically GLS1 and its splice variant GAC, two inhibitor molecules bind at an interface region of the GAC tetramer in a manner that appears to lock the GAC tetramer into a nonproductive conformation, binding structure and mechanism of glutaminase inhibition, overview; inhibits specifically GLS1 splice variant GAC, two inhibitor molecules bind at an interface region of the GAC tetramer in a manner that appears to lock the GAC tetramer into a nonproductive conformation, binding structure and mechanism of glutaminase inhibition, overview 12199 3.5.1.2 bis-2-(5-phenylacetimido-1,2,4-thiadiazol-2-yl) ethyl sulfide glutaminase-1-selective inhibitor 206467 3.5.1.2 bis-2-(5-phenylacetimido-1,2,4-thiadiazol-2-yl)ethyl sulfide uncompetitive inhibition 206469 3.5.1.2 Bromocresol green - 6493 3.5.1.2 bromocresol purple - 32161 3.5.1.2 Ca2+ 0.5-1.0 mM, NEM-sensitive enzyme 15 3.5.1.2 Ca2+ 72.59% residual activity at 100 mM 15 3.5.1.2 Ca2+ 10 mM, 80% of initial activity 15 3.5.1.2 CaCl2 inhibition to a variable extent 218 3.5.1.2 CB-839 i.e. N-[5-[4-[6-[[2-[3-(trifluoromethoxy)phenyl]acetyl]amino]-3-pyridazinyl]butyl]-1,3,4-thiadiazol-2-yl]-2-pyridineacetamide, is the best inhibitor as designated by the binding free energy changes 235309 3.5.1.2 Cd2+ complete inhibition at 50 mM 52 3.5.1.2 chelerythrine competitive inhibition, i.e. 1,2-dimethoxy-N-methyl[1,3]benzodioxolo[5,6-c]phenanthridinium 9640 3.5.1.2 citrate enzyme from mesenteric lymph nodes 131 3.5.1.2 Cl- 0.5 M, complete inhibition 141 3.5.1.2 CN- 0.5 M, complete inhibition 159 3.5.1.2 Co2+ 70.53% residual activity at 100 mM 23 3.5.1.2 Co2+ 90% residual activity at 1 mM 23 3.5.1.2 Co2+ 5 mM, 81% of initial activity 23 3.5.1.2 CoCl2 14% inhibition at 1 mM 414 3.5.1.2 compound 968 i.e. 5-(3-bromo-4-(dimethylamino)phenyl)-2,2-dimethyl-2,3,5,6-tetrahydrobenzo[a]phenanthridin-4(1H)-one, combined with erlotinib down-regulates the glutamine and glycolysis metabolism in erlotinib-resistant non-small cell lung cancer cells 235307 3.5.1.2 Cu2+ - 19 3.5.1.2 Cu2+ CuCl2, inhibition of glutaminase II 19 3.5.1.2 Cu2+ complete inhibition at 50 mM 19 3.5.1.2 Cu2+ 10 mM, 44% of initial activity 19 3.5.1.2 Cu2+ 5 mM, 86% of initial activity 19 3.5.1.2 CuCl2 20% inhibition at 1 mM, 17% at 0.1 mM 347 3.5.1.2 CuSO4 inhibition to a variable extent 263 3.5.1.2 D-glucose negative influence in media with glucose as carbon source 35 3.5.1.2 diazo-5-oxo-L-norleucine enzyme from mesenteric lymph nodes 48984 3.5.1.2 diazo-5-oxo-L-norleucine inactivates dimeric enzyme form in presence or absence of phosphate 48984 3.5.1.2 diethyl dicarbonate - 463 3.5.1.2 dimethyl 2-[1-(4-tert-butylbenzoyl)-2,2,7-trimethyl-3-methylidene-2,3-dihydroquinolin-4(1H)-ylidene]-1,3-dithiole-4,5-dicarboxylate 97% inhibition at 0.05 mM 205425 3.5.1.2 diphenylarsinic acid the protein level of GAC significantly decrease in an concentration manner. The PAG activities are also decreased in parallel with the decrease in GAC 163463 3.5.1.2 diphosphate 0.1 M, 98% inhibition 17 3.5.1.2 dithiothreitol complete inhibition at 1 mM 45 3.5.1.2 dithiothreitol 5 mM, 82% of initial activity 45 3.5.1.2 ebselen mixed non-competitive inhibition, i.e. 2-phenyl-1,2-benzisoselenazol-3[2H]-one 2514 3.5.1.2 EDTA glutaminase I and II 21 3.5.1.2 EDTA - 21 3.5.1.2 EDTA 10% inhibition at 1 mM 21 3.5.1.2 EDTA 80% residual activity at 1 mM 21 3.5.1.2 Evans blue - 49046 3.5.1.2 Fe2+ 92% residual activity at 1 mM 25 3.5.1.2 Fe2+ 0.1 mM, 55% of initial activity 25 3.5.1.2 Fe2+ 5 mM, 83% of initial activity 25 3.5.1.2 Fe3+ 0.1 mM, 45% of initial activity 70 3.5.1.2 Fe3+ 5 mM, 84% of initial activity 70 3.5.1.2 FeCl3 glutaminase II 702 3.5.1.2 glufosinate ammonium about 23% inhibition at about 1 mM 206468 3.5.1.2 glutamate no inhibition 297 3.5.1.2 glutamate competitive with respect to Gln 297 3.5.1.2 glutamate - 297 3.5.1.2 glutamate inhibits the enzyme in vivo in tumor cells at 100 mM 297 3.5.1.2 Hg2+ 0.1 mM, complete inhibition 33 3.5.1.2 Hg2+ HgCl2 33 3.5.1.2 Hg2+ complete inhibition at 50 mM 33 3.5.1.2 Hg2+ 10 mM, 35% of initial activity 33 3.5.1.2 Hg2+ 5 mM, 61% of initial activity 33 3.5.1.2 HgCl2 - 110 3.5.1.2 HgCl2 inhibition to a variable extent 110 3.5.1.2 iodoacetamide - 67 3.5.1.2 iodoacetamide complete inhibition at 50 mM 67 3.5.1.2 iodoacetamide 5 mM, 3% of initial activity 67 3.5.1.2 iodoacetate 50 mM, strongly inhibited, 80% inhibition, especially more strongly with a progress of purification steps 93 3.5.1.2 iodoacetate 10 mM, 23% of initial activity 93 3.5.1.2 L-glutamate - 41 3.5.1.2 L-glutamate strong product inhibition of isozyme KGA, no inhibition of isozyme LGA 41 3.5.1.2 L-glutamate product inhibition, competitive 41 3.5.1.2 L-Glutamic acid 5 mM, about a 40% inhibition 1163 3.5.1.2 L-glutamine above 0.3 mM 102 3.5.1.2 L-glutamine inhibition of enzyme activity in tumor tissue 102 3.5.1.2 L-glutamine product inhibition, strongly inhibits the membrane-associated enzyme, while the soluble form is not or weakly inhibited 102 3.5.1.2 L-methionine sulfoximine about 21% inhibition at about 1 mM 2748 3.5.1.2 Mersalyl enzyme from mesenteric lymph nodes 1982 3.5.1.2 Mersalyl 0.5 mM, almost complete inhibition 1982 3.5.1.2 metformin 68% inhibition at 100 mM 3021 3.5.1.2 methylene blue 0.005%, irreversible inactivation 512 3.5.1.2 Mg2+ - 6 3.5.1.2 Mg2+ 74.29% residual activity at 100 mM 6 3.5.1.2 Mg2+ 10 mM, 55% of initial activity 6 3.5.1.2 MgCl2 20% inhibition at 1 mM, 12% at 0.1 mM 196 3.5.1.2 Mn2+ - 11 3.5.1.2 Mn2+ 76.23% residual activity at 100 mM 11 3.5.1.2 Mn2+ 80% residual activity at 1 mM 11 3.5.1.2 Mn2+ 0.1 mM, 75% of initial activity 11 3.5.1.2 MnCl2 22% inhibition at 1 mM, 13% at 0.1 mM 307 3.5.1.2 additional information no inhibited by glutamate 2 3.5.1.2 additional information activity is not significantly impaired with 2-oxoglutarate, pyruvate, succinate and citrate, no inhibition with L-glutamate, NH4+ and L-aspartate 2 3.5.1.2 additional information no inhibition by HgCl2; no inhibition by p-chloromercuribenzoate 2 3.5.1.2 additional information no inhibition by 2-mercaptomethanol and iodoacetate 2 3.5.1.2 additional information bis(diphenylarsine)oxide causes no siginficant changes in GAC levels and PAG activities. Methylated inorganic arsenics dimethylarsinic acid, dimethylarsinous acid, and phenyldimethylarsine oxide show no effects on GAC levels and PAG activities. And both glutathione-conjugated diphenylarsinic acid and triphenylarsine had no significant suppressive effects on the GAC levels and PAG activity 2 3.5.1.2 additional information not inhibited by EDTA 2 3.5.1.2 additional information phenylmethylsulfonyl fluoride, sodium azide, ethylenediaminetetraacetic acid and N-acetylimidazole have no effect on enzyme 2 3.5.1.2 N'-[(E)-[3-bromo-4-(dimethylamino)phenyl]methylidene]-2-(9-oxoacridin-10(9H)-yl)acetohydrazide 93% inhibition at 0.05 mM 205475 3.5.1.2 N,N'-[sulfanediylbis(ethane-2,1-diyl-1,3,4-thiadiazole-5,2-diyl)]bis(2-phenylacetamide) - 191990 3.5.1.2 N-(2-aminoethyl)-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide - 205498 3.5.1.2 N-(5-[2-[2-(5-amino-[1,3,4]thiadiazol-2-yl)-ethylsulfanyl]-ethyl]-[1,3,4]thiadiazol-2-yl)-2-phenyl-acetamide - 206477 3.5.1.2 N-benzyl-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide - 205567 3.5.1.2 N-bromosuccinimide 5 mM, 19% of initial activity 208 3.5.1.2 N-ethylmaleimide 10 mM, 60% of initial activity 49 3.5.1.2 N-ethylmaleimide 5 mM, 8% of initial activity 49 3.5.1.2 N-methyl-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]-N-[2-(pyrrolidin-1-yl)ethyl]pentanamide - 205641 3.5.1.2 N-tert-butyl-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide - 205652 3.5.1.2 N-tert-butyl-N-methyl-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide - 205653 3.5.1.2 N-[2-(1-methylpyrrolidin-2-yl)ethyl]-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide - 205738 3.5.1.2 N-[2-(4-hydroxypiperidin-1-yl)ethyl]-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide - 205743 3.5.1.2 N-[2-(diethylamino)ethyl]-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide - 205747 3.5.1.2 N-[4-(dimethylamino)benzyl]-5-[5-[(phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]pentanamide - 205765 3.5.1.2 N-[4-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3-thiazol-2-yl]-2-phenylacetamide - 205770 3.5.1.2 N-[5-(2-[[2-(5-amino-1,3,4-thiadiazol-2-yl)ethyl]sulfinyl]ethyl)-1,3,4-thiadiazol-2-yl]-2-phenylacetamide - 205771 3.5.1.2 N-[5-[2-(5-amino-1,3,4-thiadiazol-2-yl)ethyl]-1,3,4-thiadiazol-2-yl]-2-phenylacetamide - 205776 3.5.1.2 N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]-2-(4-fluorophenyl)acetamide - 205777 3.5.1.2 N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]-2-(4-methylphenyl)acetamide - 205778 3.5.1.2 N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]-2-cyclohexylacetamide - 205779 3.5.1.2 N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]-2-phenylacetamide - 205780 3.5.1.2 N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]-2-phenylpropanamide - 205781 3.5.1.2 N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]-3-phenylpropanamide - 205782 3.5.1.2 N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3,4-thiadiazol-2-yl]benzamide - 205783 3.5.1.2 N-[5-[4-(5-amino-1,3,4-thiadiazol-2-yl)butyl]-1,3-thiazol-2-yl]-2-phenylacetamide - 205784 3.5.1.2 Na2SO4 glutaminase I and II 733 3.5.1.2 NaCIO4 0.3 M, 25% inhibition 106821 3.5.1.2 NaCl - 42 3.5.1.2 NaCl 15%, remains 90% of the initial activity 42 3.5.1.2 NaCl inhibits the enzyme slightly at 2.6 M, the enzyme is salt-tolerant, the C-terminally serine protease-cleaved enzyme fragment shows higher salt tolerance than the full-length enzyme, the N-terminal domain has abundant glutamic acid residues on its surface, which may explain its salt-tolerant mechanism 42 3.5.1.2 NaCl 40% inhibition of the enzyme from strain RIB40 and 90% of the enzyme from strain MA-27-IM at 2.9 M, reduces the temperature stability of the enzyme 42 3.5.1.2 NaCl enhances activity at 1-20% w/v, but reduces activity by 30% at 25% w/v, at 25% NaCl concentration, the enzyme retains 60% of its activity after 4 h 42 3.5.1.2 NaCl the enzyme activity is inhibited by approximately 95% in the presence of 18% (w/v) NaCl 42 3.5.1.2 NaF inhibition to a variable extent 235 3.5.1.2 NaH2PO4 0.3 M, complete inhibition 3482 3.5.1.2 NaI above 0.3 M 3483 3.5.1.2 NaN3 complete inhibition at 1 mM 238 3.5.1.2 NaNO3 0.3 M, 15% inhibition 2149 3.5.1.2 NEM enzyme from mesenteric lymph nodes 89 3.5.1.2 NEM enzyme exists as an NEM-sensitive form and an NEM-insensitive form 89 3.5.1.2 NEM - 89 3.5.1.2 NEM 1 mM, almost completely blocks activity 89 3.5.1.2 Ngamma,Ngamma-diethyl-L-glutamine - 41259 3.5.1.2 Ngamma,Ngamma-dimethyl-L-glutamine - 41260 3.5.1.2 Ngamma-ethyl-L-glutamine - 41257 3.5.1.2 Ngamma-methyl-L-glutamine - 41258 3.5.1.2 NH3 product inhibition, 10 mM inhibits the enzyme activity about 30% 27 3.5.1.2 NH3 product inhibition 27 3.5.1.2 NH4+ enzyme from mesenteric lymph nodes 54 3.5.1.2 NH4+ - 54 3.5.1.2 NH4+ no effect 54 3.5.1.2 NH4+ 0.01 M, 50% inhibition 54 3.5.1.2 nitidine - 166052 3.5.1.2 nitrite 0.5 M, complete inhibition 168 3.5.1.2 norsanguinarine - 206476 3.5.1.2 O-(diazoacetyl)-L-serine - 59049 3.5.1.2 p-benzoquinone - 2350 3.5.1.2 p-chloromercuribenzoate - 43 3.5.1.2 p-chloromercuribenzoic acid complete inhibition at 10 mM 614 3.5.1.2 p-mercuribenzoate 0.1 mM, complete inhibition, presence of Gln prevents inhibition 686 3.5.1.2 p-mercuribenzoate - 686 3.5.1.2 Pb2+ 69.27% residual activity at 100 mM 139 3.5.1.2 PCMB inhibition of glutaminase I but not glutaminase II 78 3.5.1.2 PCMB - 78 3.5.1.2 penicillin - 2664 3.5.1.2 phenylarsonic acid causes a decrease in GAC levels 7724 3.5.1.2 phenylmethylarsinic acid causes a decrease in GAC levels 163464 3.5.1.2 PO43- - 867 3.5.1.2 protein BNIP-H i.e. Caytaxin or brain-specific BNIP-2-homology protein, encoded by gene ATCAY, important in neuromal function, inhibits the enzyme and alters its steady-state kinetics, relocalises glutaminase to neurite terminals and reduces glutamate levels in vivo, effects on glutamate levels in overexpressing cell lines, e.g. murine Neuro2A cells or rat PC-12 cells, or in female rat brain, detailed overview 132653 3.5.1.2 pyruvate 0.5 M, complete inhibition 31 3.5.1.2 pyruvate mixed inhibition 31 3.5.1.2 R(-)-apocodeine - 206475 3.5.1.2 R(-)-propylnorapomorphine - 206474 3.5.1.2 Rose bengal 0.01%, irreversible inactivation 1331 3.5.1.2 sanguinarine - 10778 3.5.1.2 succinate enzyme from mesenteric lymph nodes 58 3.5.1.2 TLCK 5 mM, 12% of initial activity 4621 3.5.1.2 Tris 0.5 M, complete inhibition 317 3.5.1.2 Triton X-100 - 61 3.5.1.2 Zn2+ 82.12% residual activity at 100 mM 14 3.5.1.2 Zn2+ 10 mM, 30% of initial activity 14 3.5.1.2 Zn2+ 5 mM, 79% of initial activity 14 3.5.1.2 ZnCl2 7% inhibition at 1 mM 271