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Literature summary for 3.1.1.98 extracted from

  • Suciu, R.M.; Cognetta, A.B.; Potter, Z.E.; Cravatt, B.F.
    Selective irreversible inhibitors of the Wnt-deacylating enzyme NOTUM developed by activity-based protein profiling (2018), ACS Med. Chem. Lett., 9, 563-568 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.1.1.98

Application

Application Comment Organism
drug development NOTUM inhibitors have potential for treating degenerative diseases Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-[(2,3-dihydro-4H-1,4-benzoxazine-4-carbonyl)oxy]-7-[(6-phenoxypyridin-3-yl)methyl]tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione
-
 Homo sapiens
7-(4-chlorobenzoyl)-2-[(2,3-dihydro-4H-1,4-benzoxazine-4-carbonyl)oxy]tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione
-
 Homo sapiens
7-(4-chlorobenzyl)-1,3-dioxohexahydroimidazo[1,5-a]pyrazin-2(3H)-yl 2,3-dihydro-4Hbenzo[b][1,4]oxazine-4-carboxylate i.e. ABC99, selective irreversible inhibitor. The optimized -hydroxyhydantoin carbamate inhibitor preserves Wnt-mediated cell signaling in the presence of NOTUM and is also converted into an ABPP probe for visualizing NOTUM in native biological systems Homo sapiens
7-[(2-chlorophenyl)methyl]-2-([4-(4-methoxyphenyl)piperazine-1-carbonyl]oxy)tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione
-
 Homo sapiens
7-[(3-chlorophenyl)methyl]-2-([4-(4-methoxyphenyl)piperazine-1-carbonyl]oxy)tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione
-
 Homo sapiens
7-[(4-bromophenyl)methyl]-2-[[4-(4-methoxyphenyl)piperazine-1-carbonyl]oxy]tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione
-
 Homo sapiens
7-[(4-chlorophenyl)methyl]-2-([4-(4-methoxyphenyl)piperazine-1-carbonyl]oxy)tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione
-
 Homo sapiens
7-[(4-chlorophenyl)methyl]-2-[(2,3-dihydro-4H-1,4-benzoxazine-4-carbonyl)oxy]tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione the optimized N-hydroxyhydantoin carbamate inhibitor preserves Wnt-mediated cell signaling in the presence of NOTUM and is also converted into an activity-based protein profiling (ABPP) probe for visualizing NOTUM in native biological systems. NOTUM inhibitors have potential for treating degenerative diseases Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
54000
-
 calculated from sequence Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
[Wnt]-O-(9Z)-hexadec-9-enoyl-L-serine + H2O Homo sapiens the enzyme removes the palmitoleate modification that is introduced to specific L-serine residues in Wnt proteins by [Wnt protein]-O-palmitoleoyl transferase [Wnt]-L-serine + (9Z)-hexadec-9-enoate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Homo sapiens Q6P988
-
-

Source Tissue

Source Tissue Comment Organism Textmining
SW-620 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
[Wnt]-O-(9Z)-hexadec-9-enoyl-L-serine + H2O
-
 Homo sapiens [Wnt]-L-serine + (9Z)-hexadec-9-enoate
-
 ?
[Wnt]-O-(9Z)-hexadec-9-enoyl-L-serine + H2O the enzyme removes the palmitoleate modification that is introduced to specific L-serine residues in Wnt proteins by [Wnt protein]-O-palmitoleoyl transferase Homo sapiens [Wnt]-L-serine + (9Z)-hexadec-9-enoate
-
 ?

Synonyms

Synonyms Comment Organism
Notum
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000013
-
 pH and temperature not specified in the publication Homo sapiens 7-(4-chlorobenzyl)-1,3-dioxohexahydroimidazo[1,5-a]pyrazin-2(3H)-yl 2,3-dihydro-4Hbenzo[b][1,4]oxazine-4-carboxylate
0.000013
-
 IC50 value is determined by competitive gel-based activity-based protein profiling, pH and temperature not specified in the publication Homo sapiens 7-[(4-chlorophenyl)methyl]-2-[(2,3-dihydro-4H-1,4-benzoxazine-4-carbonyl)oxy]tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione
0.0002
-
 IC50 value is determined by competitive gel-based activity-based protein profiling, pH and temperature not specified in the publication Homo sapiens 7-[(2-chlorophenyl)methyl]-2-([4-(4-methoxyphenyl)piperazine-1-carbonyl]oxy)tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione
0.00029
-
 IC50 value is determined by competitive gel-based activity-based protein profiling, pH and temperature not specified in the publication Homo sapiens 7-[(4-chlorophenyl)methyl]-2-([4-(4-methoxyphenyl)piperazine-1-carbonyl]oxy)tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione
0.000677
-
 IC50 value is determined by competitive gel-based activity-based protein profiling, pH and temperature not specified in the publication Homo sapiens 7-[(4-bromophenyl)methyl]-2-[[4-(4-methoxyphenyl)piperazine-1-carbonyl]oxy]tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione
0.001506
-
 IC50 value is determined by competitive gel-based activity-based protein profiling, pH and temperature not specified in the publication Homo sapiens 2-[(2,3-dihydro-4H-1,4-benzoxazine-4-carbonyl)oxy]-7-[(6-phenoxypyridin-3-yl)methyl]tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione
0.01
-
 above 0.01 mM, IC50 value is determined by competitive gel-based activity-based protein profiling, pH and temperature not specified in the publication Homo sapiens 7-[(3-chlorophenyl)methyl]-2-([4-(4-methoxyphenyl)piperazine-1-carbonyl]oxy)tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione
0.01
-
 above 0.01 mM, IC50 value is determined by competitive gel-based activity-based protein profiling, pH and temperature not specified in the publication Homo sapiens 7-(4-chlorobenzoyl)-2-[(2,3-dihydro-4H-1,4-benzoxazine-4-carbonyl)oxy]tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione

General Information

General Information Comment Organism
metabolism the enzyme removes the palmitoleate modification that is introduced to specific L-serine residues in Wnt proteins by [Wnt protein]-O-palmitoleoyl transferase Homo sapiens