EC Number |
Inhibitors |
Structure |
---|
3.5.4.10 | 2'-deoxy-AMP |
decreased IMP cyclohydrolase activity by 10-50% |
|
3.5.4.10 | 2,2-dioxo-1,5-dihydroimidazo[4,5-c][1,2,6]thiadiazin-4(3H)-one |
construction of 1,5-dihydroimidazo[4,5-c][1,2,6]thiadiazin-4(3H)-one 2,2-dioxide, the corresponding nucleoside, and the nucleoside monophosphate, as mimics of the tetrahedral intermediate in the cyclization reaction. All compounds are competitive inhibitors against IMPCH, but the simpler heterocycle has a completely different IMPCH binding mode, compared to the nucleosides, and is relocated to the phosphate binding pocket, the aromatic imidazole ring interacts with a helix dipole, inhibitor synthesis, binding structure, and mechanism of inhibition, overview |
|
3.5.4.10 | 2-chloroinosine 5'-monophosphate |
potent inhibitor |
|
3.5.4.10 | 2-flouroinosine 5'-monophosphate |
IC50-value in cell culture 0.0049 mM; potent inhibitor |
|
3.5.4.10 | 2-fluoroadenine arabinoside 5'-monophosphate |
IC50-value in cell culture 0.0002 mM; strong competitive inhibitor, derivative of anti-cancer drug |
|
3.5.4.10 | 2-fluoroadenine arabinoside 5'-monophosphate |
strong competitive inhibitor, derivative of anti-cancer drug |
|
3.5.4.10 | 2-mercaptoinosine 5'-monophosphate |
most potent competitive inhibitor, precursor of GMP in the purine pathway |
|
3.5.4.10 | 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside |
decreased IMP cyclohydrolase activity by 10-50% |
|
3.5.4.10 | 6-mercaptopurine riboside 5'-monophosphate |
IC50-value in cell culture 0.0075 mM; strong competitive inhibitor, derivative of anti-cancer drug |
|
3.5.4.10 | 6-mercaptopurine riboside 5'-monophosphate |
strong competitive inhibitor, derivative of anti-cancer drug |
|