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(1S)-1-cyclohexyl-2-(1,3-dihydro-2H-isoindol-2-yl)-2-oxoethanamine
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IC50: 24 nM
(1S)-1-cyclohexyl-2-(3,4-dihydroisoquinolin-2(1H)-yl)-2-oxoethanamine
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IC50: 3016 nM
(1S)-1-cyclohexyl-2-oxo-2-piperidin-1-ylethanamine
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IC50: 1448 nM
(1S)-1-cyclohexyl-2-oxo-2-pyrrolidin-1-ylethanamine
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IC50: 78 nM
(2S)-1-[(2S)-2-amino-4-(3,4-dihydroisoquinolin-2(1H)-yl)-4-oxobutanoyl]pyrrolidine-2-carbonitrile
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IC50: 19 nM
(2S)-1-[(2S)-2-amino-4-(4-[bis(4-fluorophenyl)methyl]piperazin-1-yl)-4-oxobutanoyl]pyrrolidine-2-carbonitrile
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IC50: 16 nM
(2S)-2-amino-2-cyclohexyl-1-[(2R)-2-(iminomethyl)cyclopentyl]ethanone
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IC50: 27 nM
(2S,3S)-3-methyl-1-oxo-1-(1,3-thiazolidin-3-yl)pentan-2-amine
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IC50: 364 nM
1-(1,3-dihydro-2H-isoindol-2-yl)-4-(3,4-dihydroisoquinolin-2(1H)-yl)-1,4-dioxobutan-2-amine
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IC50: 555 nM
1-(1,3-dihydro-2H-isoindol-2-yl)-4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-1,4-dioxobutan-2-amine
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IC50: 150 nM
4-(4-[bis(4-fluorophenyl)methyl]piperazin-1-yl)-1-(1,3-dihydro-2H-isoindol-2-yl)-1,4-dioxobutan-2-amine
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IC50: 14 nM
6-([2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)ethyl]amino)nicotinonitrile
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IC50: 4574 nM
Carnosinase substrates
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DL-homocysteine
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strong inhibition at 10 and 50 mM, in the presence of 0.1 mM MnCl2
DL-methionine
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strong inhibition at 10 and 50 mM, in the presence of 0.1 mM MnCl2
Gly-Leu
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competitive inhibitor of L-Ala-Gly hydrolysis
L-alanine
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poor competitive inhibitor of Ala-Gly hydrolysis
L-leucine
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strong inhibition of prolinase activity against Pro-Gly regardless wether MnCl2 is present or not
L-methionine
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inhibition at 10 and 50 mM, in the presence of 0.1 mM MnCl2
L-Val
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strong inhibition of prolinase activity against Pro-Gly regardless wether MnCl2 is present or not
N-(2-pyrrolcarbonyl)glycine
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inhibits cleavage of Pro-Gly
N-acetyl-L-methionine
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strong inhibition at 10 and 50 mM, in the presence of 0.1 mM MnCl2
NVP LAF237
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i.e.vildagliptin, IC50: 14219 nM
phenylmethylsulfonyl fluoride
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phloretin
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inhibits at 1 mM
additional information
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inhibition by high substrate concentrations is observed in cases where the Km is low
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1,10-phenanthroline
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1,10-phenanthroline
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1,7-phenanthroline has no effect
2-mercaptoethanol
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-
Co2+
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when substrates are cleaved rapidly by dipeptidase, addition of Co2+ inhibits the reaction. The more slowly a substrate is hydrolyzed in the absence of metals, the greater the activating effect
Co2+
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hydrolysis of the relative poor substrates, Pro-Gly and Gly-Gly is activated, whereas that of Ala-Gly is inhibited
cysteine
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D-Forms of dipeptides
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D-Forms of dipeptides
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D-Leu-Gly
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competitive inhibitor of L-Ala-Gly hydrolysis
D-Leu-Gly
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competitive inhibitor of L-Ala-Gly hydrolysis
DTT
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EDTA
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iodoacetate
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Iodosobenzoate
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-
Mn2+
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when substrates are cleaved rapidly by dipeptidase, addition of Mn2+ inhibits the reaction. The more slowly a substrate is hydrolyzed in the absence of metals, the greater the activating effect
Mn2+
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0.1 mM, inhibits prolinase activity in normal erythrocytes against Pro-Ala, Pro-Val, Pro-Met, Pro-Asp
Mn2+
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hydrolysis of the relative poor substrates, Pro-Gly and Gly-Gly is activated, whereas that of Ala-Gly is inhibited
p-chloromercuribenzoate
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p-chloromercuribenzoate
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p-hydroxymercuribenzoate
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p-hydroxymercuribenzoate
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p-hydroxymercuribenzoate
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p-hydroxymercuribenzoate
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Pb2+
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Zn2+
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inhibits, but activation in phosphate buffer