6.3.4.2 additional information - additional information xanthine and related compounds inhibit CTPS activity with IC50 = 0.16-0.58 mM. The presence of an 8-oxo function enhances the inhibition to IC50 = 0.060-0.121 mM. Raising the pH from 8.0 to 8.5 results in slightly increased inhibition of NH3-dependent CTP formation by the xanthines 702613 6.3.4.2 0.04 - CTP wild-type, pH 8.1, 37°C 715549 6.3.4.2 0.042 - CTP wild-type, pH 8.1, 37°C 715549 6.3.4.2 0.045 - CTP mutant S571A, pH 8.1, 37°C 715549 6.3.4.2 0.05 - CTP IC50: 0.05 mM 649000 6.3.4.2 0.057 - CTP C-terminal deletion mutant, pH 8.1, 37°C 715549 6.3.4.2 0.06 - uric acid pH 8.0, Gln-dependent CTP formation 702613 6.3.4.2 0.063 - 3,7-dimethyluric acid pH 8.0, Gln-dependent CTP formation 702613 6.3.4.2 0.067 - 1,3,7-trimethyluric acid pH 8.0, Gln-dependent CTP formation 702613 6.3.4.2 0.07 - 1,3,7-trimethyluric acid pH 8.0, NH3-dependent CTP formation 702613 6.3.4.2 0.072 - 1,3-dimethyluric acid pH 8.0, NH3-dependent CTP formation 702613 6.3.4.2 0.072 - CTP mutant S568A, pH 8.1, 37°C 715549 6.3.4.2 0.079 - 1,3,7,9-tetramethyluric pH 8.0, Gln-dependent CTP formation 702613 6.3.4.2 0.08 - 8-oxoguanosine - 674909 6.3.4.2 0.08 - 8-oxoguanosine IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.087 - uric acid pH 8.0, NH3-dependent CTP formation 702613 6.3.4.2 0.088 - 1,3-dimethyluric acid pH 8.0, Gln-dependent CTP formation 702613 6.3.4.2 0.09 - 3,7-dimethyluric acid pH 8.0, NH3-dependent CTP formation 702613 6.3.4.2 0.096 - 1-methyluric acid pH 8.0, NH3-dependent CTP formation 702613 6.3.4.2 0.1 - uric acid in HEPES buffer (70 mM, pH 7.3), at 37°C 727139 6.3.4.2 0.101 - 1-methyluric acid pH 8.0, Gln-dependent CTP formation 702613 6.3.4.2 0.11 - 2,6-diaminopurine riboside IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.11 - 8-oxoguanosine 5'-triphosphate IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.113 - 1,7-dimethyluric acid pH 8.0, Gln-dependent CTP formation 702613 6.3.4.2 0.119 - 1,7-dimethyluric acid pH 8.0, NH3-dependent CTP formation 702613 6.3.4.2 0.121 - 1,3,7,9-tetramethyluric pH 8.0, NH3-dependent CTP formation 702613 6.3.4.2 0.13 - 8-oxoguanosine IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.15 - 8-oxoguanosine 5'-triphosphate IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.15 - CTP IC50: 0.15 mM 649000 6.3.4.2 0.15 - O-methylguanosine 0.30 mM Gln, IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.16 - O-methylguanosine 10 mM Gln, IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.16 - O-methylguanosine 2.5 mM Gln, IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.16 - O-methylguanosine IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.17 - N-methylguanosine IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.17 - O-methylguanosine 0.75 mM Gln, IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.18 - 2,6-diaminopurine riboside IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.21 - CTP IC50 for the native enzyme: 0.12 in presence of 0.5 mM ATP, 0.22 mM in presence of 1 mM ATP. IC50 for the phosphorylated enzyme: 0.21 mM in presence of 0.5 mM ATP, 0.31 mM in presence of 1 mM ATP 648994 6.3.4.2 0.22 - 2-aminopurine riboside IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.22 - guanosine 5.44 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.22 - Xanthosine IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.23 - 6-thioguanosine IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.23 - GMP 5.44 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.23 - N-methylguanosine IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.23 - xanthine pH 8.0, Gln-dependent CTP formation 702613 6.3.4.2 0.25 - GMP 2.72 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.25 - O-methylguanosine IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.26 - 2-aminopurine riboside IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.26 - GMP IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.26 - guanosine 1.36 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.26 - guanosine 2.72 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.28 - GMP 1.36 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.29 - dideoxy-GTP IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.29 - GDP 2.72 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.29 - GDP 5.44 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.29 - GDP IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.29 - GMP 8.16 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.29 - GTP 5.44 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.29 - guanosine 8.16 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.29 - guanosine IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.29 - Xanthosine IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.3 - CTP IC50: 0.3 mM 648973 6.3.4.2 0.3 - GDP 1.36 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.3 - GTP 2.72 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.3 - GTP 8.16 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.3 - GTP IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.3 - guanosine 0.30 mM Gln, IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.31 - acycloguanosine monophosphate IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.31 - GTP 1.36 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.32 - CTP IC50: 0.32 mM 648978 6.3.4.2 0.32 - guanosine 10 mM Gln, IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.32 - guanosine 2.5 mM Gln, IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.32 - guanosine IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.33 - 2'-deoxy-GTP IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.33 - 2'-deoxy-guanosine IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.33 - acycloguanosine IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.33 - GDP IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.33 - GMP IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.33 - guanosine 5'-tetraphosphate IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.34 - 3'-deoxy-guanosine IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.35 - guanosine 0.75 mM Gln, IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.37 - xanthine pH 8.0, NH3-dependent CTP formation 702613 6.3.4.2 0.38 - guanosine in HEPES buffer (70 mM, pH 7.3), at 37°C 727139 6.3.4.2 0.39 - 6-thioguanine IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 0.39 - Caffeine pH 8.0, Gln-dependent CTP formation 702613 6.3.4.2 0.4 - 3'-deoxy-guanosine IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.4 - 6-thioguanosine IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.41 - acycloguanosine monophosphate IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.41 - dideoxy-GTP IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.42 - 2'-deoxy-GTP IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.42 - guanosine 5'-tetraphosphate IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.42 - Theobromine pH 8.0, Gln-dependent CTP formation 702613 6.3.4.2 0.43 - theophylline pH 8.0, Gln-dependent CTP formation 702613 6.3.4.2 0.44 - paraxanthine pH 8.0, Gln-dependent CTP formation 702613 6.3.4.2 0.45 - 2'-deoxy-guanosine IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.45 - acycloguanosine 8.16 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.45 - acycloguanosine IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.46 - GTP in HEPES buffer (70 mM, pH 7.3), at 37°C 727139 6.3.4.2 0.47 - acycloguanosine 5.44 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.48 - acycloguanosine 2.72 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.48 - Caffeine in HEPES buffer (70 mM, pH 7.3), at 37°C 727139 6.3.4.2 0.48 - paraxanthine pH 8.0, NH3-dependent CTP formation 702613 6.3.4.2 0.49 - acycloguanosine 1.36 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 0.51 - Caffeine pH 8.0, NH3-dependent CTP formation 702613 6.3.4.2 0.55 - theophylline pH 8.0, NH3-dependent CTP formation 702613 6.3.4.2 0.58 - Theobromine pH 8.0, NH3-dependent CTP formation 702613 6.3.4.2 0.61 - 6-thioguanine IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 2.6 - uracil-4-acetic acid pH 8.0, Gln-dependent CTP formation 702613 6.3.4.2 2.9 - ITP 8.16 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 3 - ITP 2.72 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 3.1 - ITP 5.44 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 3.1 - uridine pH 8.0, Gln-dependent CTP formation 702613 6.3.4.2 3.2 - uracil-4-acetic acid pH 8.0, NH3-dependent CTP formation 702613 6.3.4.2 3.3 - ITP 1.36 mM NH3, IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 3.5 - Inosine IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 3.7 - ITP IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 4.1 - ITP IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 4.2 - Uracil pH 8.0, Gln-dependent CTP formation 702613 6.3.4.2 4.6 - uridine pH 8.0, NH3-dependent CTP formation 702613 6.3.4.2 4.7 - Uracil pH 8.0, NH3-dependent CTP formation 702613 6.3.4.2 5.2 - Inosine IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 11 - adenosine IC50 for inhibition of Gln-dependent CTP formation 674909 6.3.4.2 12 - adenosine IC50 for inhibition of NH3-dependent CTP formation 674909 6.3.4.2 12.9 - adenine pH 8.0, NH3-dependent CTP formation 702613 6.3.4.2 15.8 - adenine pH 8.0, Gln-dependent CTP formation 702613