Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
(3S,4S)-1-[(4-chlorophenyl)sulfonyl]-3-methyl-4-phenylazetidin-2-one
(3S,4S)-3-butyl-4-(pent-4-yn-1-yl)oxetan-2-one
-
-
(3S,4S)-3-methyl-1-[(4-methylphenyl)sulfonyl]-4-phenylazetidin-2-one
-
-
1,2-dihexanoyl-sn-glycero-3-phosphocholine
-
1,2-dimyristoyl-sn-glycero-3-phosphocholine additionally added, paGlpG purified in detergent causes 37% reduction in activity
1,2-dimyristoyl-sn-glycero-3-phosphocholine
-
paGlpG purified in detergent causes 5% reduction in activity
1-(2,3-dihydro-4H-1,4-benzoxazin-4-yl)-3,3,3-trifluoro-2-(trifluoromethyl)propan-1-one
1-(biphenyl-3-ylsulfonyl)-4-phenylazetidin-2-one
1-(biphenyl-4-ylsulfonyl)-4-phenylazetidin-2-one
1-myristoyl-sn-glycero-3-phosphocholine
-
paGlpG purified in detergent causes 10% reduction in activity
1-palmitoyl-sn-glycero-3-phospho-rac-(1-glycerol)
-
paGlpG purified in detergent causes 20% reduction in activity
1-[(3'-methylbiphenyl-4-yl)sulfonyl]-4-phenylazetidin-2-one
1-[(3-bromophenyl)sulfonyl]-4-phenylazetidin-2-one
1-[(3-chlorophenyl)sulfonyl]-4-(2-phenylethyl)azetidin-2-one
1-[(3-chlorophenyl)sulfonyl]-4-(propan-2-yl)azetidin-2-one
1-[(4'-chlorobiphenyl-4-yl)sulfonyl]-4-phenylazetidin-2-one
1-[(4-bromophenyl)sulfonyl]-4-phenylazetidin-2-one
1-[(4-chlorophenyl)sulfonyl]-3-methylazetidin-2-one
1-[(4-methylphenyl)sulfonyl]-4-phenylazetidin-2-one
2-(benzyloxy)-5-chloro-4H-3,1-benzoxazin-4-one
2-(benzyloxy)-5-methyl-4H-3,1-benzoxazin-4-one
2-methylpropyl 2-oxo-4-phenylazetidine-1-carboxylate
beta-lactam inhibitor, forms a single bond to the catalytic serine and the carbonyl oxygen of the inhibitor faces away from the oxyanion hole. The hydrophobic N-substituent of the inhibitor points into a cavity within the enzyme, providing a structural explanation for the specificity of beta-lactams on rhomboid proteases. This same cavity probably represents the S2' substrate binding site
3,3,3-trifluoro-N-[(5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)methyl]-2-(trifluoromethyl)propanamide
3,3,3-trifluoro-N-[2-(propan-2-yloxy)phenyl]-2-(trifluoromethyl)propanamide
3,4-dichloro-1H-2-benzopyran-1-one
-
-
3-butyl-4-(pent-4-yn-1-yl)oxetan-2-one
-
3-methyl-1-[(4-methylphenyl)sulfonyl]-4-phenylazetidin-2-one
-
-
3-[(3-cholamidopropyl)-dimethylammonio]-1-propansulfonate
-
1,2-dimyristoyl-sn-glycero-3-phosphocholine additionally added, paGlpG purified in detergent causes 37% reduction in activity
4-(2-chlorophenyl)-1-[(3-chlorophenyl)sulfonyl]azetidin-2-one
4-(3-bromophenyl)-1-[(3-chlorophenyl)sulfonyl]azetidin-2-one
4-chloro-7-nitro-3-[(5-phenylpentyl)oxy]-1H-2-benzopyran-1-one
inhibitor reacts with virtually all tested rhomboids
4-[(3-methyl-2-oxoazetidin-1-yl)sulfonyl]benzonitrile
7-amino-3-butoxy-4-chloro-1H-isochromen-1-one
-
7-amino-4-chloro-3-(2-phenylethoxy)-1H-isochromen-1-one
-
7-amino-4-chloro-3-methoxyisocoumarin
-
7-amino-4-chloro-3-[(5-phenylpentyl)oxy]-1H-isochromen-1-one
-
acetyl-L-Ile-L-Ala-L-Thr-L-Ala-chloromethylketone
-
inhibitor derived from the natural rhomboid substrate TatA from bacterium Providencia stuartii, binds in a substrate-like manner
acetyl-L-Phe-L-Ala-L-Thr-L-Ala-chloromethylketone
-
inhibitor derived from the natural rhomboid substrate TatA from bacterium Providencia stuartii, binds in a substrate-like manner
benzyl (2S)-1-[(4-methylphenyl)sulfonyl]-4-oxoazetidine-2-carboxylate
cyclopentyl 2-oxo-4-phenylazetidine-1-carboxylate
beta-lactam inhibitor, forms a single bond to the catalytic serine and the carbonyl oxygen of the inhibitor faces away from the oxyanion hole. The hydrophobic N-substituent of the inhibitor points into a cavity within the enzyme, providing a structural explanation for the specificity of beta-lactams on rhomboid proteases. This same cavity probably represents the S2' substrate binding site
diisopropyl fluorophosphonate
irreversible inhibition; mechansim-based inhibitor
dodecyl maltoside
-
paGlpG purified in detergent causes 77% reduction in activity
N-(2,6-dimethylphenyl)-3,3,3-trifluoro-2-(trifluoromethyl)propanamide
n-nonyl-beta-D-glucoside
-
paGlpG purified in detergent causes 45% reduction in activity
N-[2-(cyclopentyloxy)phenyl]-3,3,3-trifluoro-2-(trifluoromethyl)propanamide
N-[2-(cyclopropylmethoxy)phenyl]-3,3,3-trifluoro-2-(trifluoromethyl)propanamide
phenyl 2-oxo-4-phenylazetidine-1-carboxylate
tert-butyl 2-[[3,3,3-trifluoro-2-(trifluoromethyl)propanoyl]amino]benzoate
(3S,4S)-1-[(4-chlorophenyl)sulfonyl]-3-methyl-4-phenylazetidin-2-one
-
-
(3S,4S)-1-[(4-chlorophenyl)sulfonyl]-3-methyl-4-phenylazetidin-2-one
-
-
1-(2,3-dihydro-4H-1,4-benzoxazin-4-yl)-3,3,3-trifluoro-2-(trifluoromethyl)propan-1-one
-
-
1-(2,3-dihydro-4H-1,4-benzoxazin-4-yl)-3,3,3-trifluoro-2-(trifluoromethyl)propan-1-one
-
-
1-(biphenyl-3-ylsulfonyl)-4-phenylazetidin-2-one
-
-
1-(biphenyl-3-ylsulfonyl)-4-phenylazetidin-2-one
-
-
1-(biphenyl-4-ylsulfonyl)-4-phenylazetidin-2-one
-
-
1-(biphenyl-4-ylsulfonyl)-4-phenylazetidin-2-one
-
-
1-[(3'-methylbiphenyl-4-yl)sulfonyl]-4-phenylazetidin-2-one
-
-
1-[(3'-methylbiphenyl-4-yl)sulfonyl]-4-phenylazetidin-2-one
-
-
1-[(3-bromophenyl)sulfonyl]-4-phenylazetidin-2-one
-
-
1-[(3-bromophenyl)sulfonyl]-4-phenylazetidin-2-one
-
-
1-[(3-chlorophenyl)sulfonyl]-4-(2-phenylethyl)azetidin-2-one
-
-
1-[(3-chlorophenyl)sulfonyl]-4-(2-phenylethyl)azetidin-2-one
-
-
1-[(3-chlorophenyl)sulfonyl]-4-(propan-2-yl)azetidin-2-one
-
-
1-[(3-chlorophenyl)sulfonyl]-4-(propan-2-yl)azetidin-2-one
-
-
1-[(4'-chlorobiphenyl-4-yl)sulfonyl]-4-phenylazetidin-2-one
-
-
1-[(4'-chlorobiphenyl-4-yl)sulfonyl]-4-phenylazetidin-2-one
-
-
1-[(4-bromophenyl)sulfonyl]-4-phenylazetidin-2-one
-
-
1-[(4-bromophenyl)sulfonyl]-4-phenylazetidin-2-one
-
-
1-[(4-chlorophenyl)sulfonyl]-3-methylazetidin-2-one
-
-
1-[(4-chlorophenyl)sulfonyl]-3-methylazetidin-2-one
-
-
1-[(4-methylphenyl)sulfonyl]-4-phenylazetidin-2-one
-
-
1-[(4-methylphenyl)sulfonyl]-4-phenylazetidin-2-one
-
-
2-(benzyloxy)-5-chloro-4H-3,1-benzoxazin-4-one
-
covalent, but slow reversible inhibition mechanism
2-(benzyloxy)-5-chloro-4H-3,1-benzoxazin-4-one
-
covalent, but slow reversible inhibition mechanism
2-(benzyloxy)-5-methyl-4H-3,1-benzoxazin-4-one
-
covalent, but slow reversible inhibition mechanism
2-(benzyloxy)-5-methyl-4H-3,1-benzoxazin-4-one
-
covalent, but slow reversible inhibition mechanism
3,3,3-trifluoro-N-[(5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)methyl]-2-(trifluoromethyl)propanamide
-
-
3,3,3-trifluoro-N-[(5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)methyl]-2-(trifluoromethyl)propanamide
-
-
3,3,3-trifluoro-N-[2-(propan-2-yloxy)phenyl]-2-(trifluoromethyl)propanamide
-
-
3,3,3-trifluoro-N-[2-(propan-2-yloxy)phenyl]-2-(trifluoromethyl)propanamide
-
-
3,4-dichloroisocoumarin
-
3,4-dichloroisocoumarin
mechanism-based inhibitor
3,4-dichloroisocoumarin
-
-
4-(2-chlorophenyl)-1-[(3-chlorophenyl)sulfonyl]azetidin-2-one
-
-
4-(2-chlorophenyl)-1-[(3-chlorophenyl)sulfonyl]azetidin-2-one
-
-
4-(3-bromophenyl)-1-[(3-chlorophenyl)sulfonyl]azetidin-2-one
-
-
4-(3-bromophenyl)-1-[(3-chlorophenyl)sulfonyl]azetidin-2-one
-
-
4-[(3-methyl-2-oxoazetidin-1-yl)sulfonyl]benzonitrile
-
-
4-[(3-methyl-2-oxoazetidin-1-yl)sulfonyl]benzonitrile
-
-
benzyl (2S)-1-[(4-methylphenyl)sulfonyl]-4-oxoazetidine-2-carboxylate
-
-
benzyl (2S)-1-[(4-methylphenyl)sulfonyl]-4-oxoazetidine-2-carboxylate
-
-
dichloroisocoumarin
-
below 0.1 mM
dichloroisocoumarin
-
below 0.1 mM
dichloroisocoumarin
-
below 0.1 mM
dichloroisocoumarin
-
below 0.1 mM
N-(2,6-dimethylphenyl)-3,3,3-trifluoro-2-(trifluoromethyl)propanamide
-
-
N-(2,6-dimethylphenyl)-3,3,3-trifluoro-2-(trifluoromethyl)propanamide
-
-
N-[2-(cyclopentyloxy)phenyl]-3,3,3-trifluoro-2-(trifluoromethyl)propanamide
-
-
N-[2-(cyclopentyloxy)phenyl]-3,3,3-trifluoro-2-(trifluoromethyl)propanamide
-
-
N-[2-(cyclopropylmethoxy)phenyl]-3,3,3-trifluoro-2-(trifluoromethyl)propanamide
-
-
N-[2-(cyclopropylmethoxy)phenyl]-3,3,3-trifluoro-2-(trifluoromethyl)propanamide
-
-
phenyl 2-oxo-4-phenylazetidine-1-carboxylate
-
-
phenyl 2-oxo-4-phenylazetidine-1-carboxylate
beta-lactam inhibitor, forms a single bond to the catalytic serine and the carbonyl oxygen of the inhibitor faces away from the oxyanion hole. The hydrophobic N-substituent of the inhibitor points into a cavity within the enzyme, providing a structural explanation for the specificity of beta-lactams on rhomboid proteases. This same cavity probably represents the S2' substrate binding site
phenyl 2-oxo-4-phenylazetidine-1-carboxylate
-
-
tert-butyl 2-[[3,3,3-trifluoro-2-(trifluoromethyl)propanoyl]amino]benzoate
-
-
tert-butyl 2-[[3,3,3-trifluoro-2-(trifluoromethyl)propanoyl]amino]benzoate
-
-
additional information
-
no inhibition by EDTA, o-phenanthroline, E64, PMSF, 4-(2-aminoethyl)benzenesulfonyl fluoride and pepstatin A
-
additional information
-
no inhibition by EDTA, o-phenanthroline, E64, PMSF, 4-(2-aminoethyl)benzenesulfonyl fluoride and pepstatin A
-
additional information
-
an alkoxy substituent at the 2-position of enzoxazin-4-one inhibitors is crucial for potency and results in low micromolar inhibitors of rhomboid proteases
-
additional information
-
no inhibition by EDTA, o-phenanthroline, E64, PMSF, 4-(2-aminoethyl)benzenesulfonyl fluoride and pepstatin A
-
additional information
local perturbations around the active site hinder proteolytic activity
-
additional information
identification of beta-lactone inhititors that form covalent and irreversible complexes with the active site serine of GlpG. The presence of alkyne handles on the beta-lactones also allows activity-based labeling
-
additional information
-
identification of beta-lactone inhititors that form covalent and irreversible complexes with the active site serine of GlpG. The presence of alkyne handles on the beta-lactones also allows activity-based labeling
-
additional information
comparison of the inhibitory capacity of 50 small molecules against 13 different rhomboids unsing activity-based protein profiling. Inhibition profile and sequence similarity of rhomboids are not related, which suggests that related rhomboids may be selectively inhibited
-
additional information
-
comparison of the inhibitory capacity of 50 small molecules against 13 different rhomboids unsing activity-based protein profiling. Inhibition profile and sequence similarity of rhomboids are not related, which suggests that related rhomboids may be selectively inhibited
-
additional information
-
an alkoxy substituent at the 2-position of enzoxazin-4-one inhibitors is crucial for potency and results in low micromolar inhibitors of rhomboid proteases
-
additional information
-
inhibitor profiles of rhomboids in micelles and liposomes are similar
-
additional information
-
no inhibition by EDTA, o-phenanthroline, E64, PMSF, 4-(2-aminoethyl)benzenesulfonyl fluoride and pepstatin A
-