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3.4.22.B69: falcipain-2

This is an abbreviated version!
For detailed information about falcipain-2, go to the full flat file.

Word Map on EC 3.4.22.B69

Reaction

The enzyme plays a key role in the hydrolysis of hemoglobin by the parasite Plasmodium falciparum. Preferred cleavage sites display arginine in P1, leucine in P2, and phenylalanine in P1' =

Synonyms

falcipain 2, falcipain-2, FP-2, Fp2, haemoglobinase

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.22 Cysteine endopeptidases
                3.4.22.B69 falcipain-2

Inhibitors

Inhibitors on EC 3.4.22.B69 - falcipain-2

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(1,1-dioxido-3-oxo-1,2-benzothiazol-2(3H)-yl)(1,3,5-triaza-7-phosphatricyclo[3.3.1.13,7]decane-kappaP)gold
-
24% inhibition at 0.02 mM
(4-chloro-2-trifluoromethyl-phenyl)-carbamic acid 5-methyl-2-oxo-1-[(4-oxo-pent-2-enylcarbamoyl)-methyl]-2,3-dihydro-1H-benzo[e][1,4] diazepin-3-methyl ester
-
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(5Z)-3-(2,4-difluorobenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
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(5Z)-3-(3-methoxybenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
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(5Z)-3-(4-fluorobenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
-
(5Z)-3-(4-methylbenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
-
(5Z)-3-benzyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
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(5Z)-3-ethyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
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(5Z)-3-methyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
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(5Z)-3-[4-(trifluoromethyl)benzyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
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(5Z)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
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(S)-2-(1-(4-benzylpiperidin-1-yl)-1-oxo-3-phenylpropan-2-yl)isoindoline-1,3-dione
-
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(S)-2-(1-(4-benzylpiperidin-1-yl)-3-methyl-1-oxobutan-2-yl)isoindoline-1,3-dione
-
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(S)-2-(1-(4-benzylpiperidin-1-yl)-4-methyl-1-oxopentan-2-yl)isoindoline-1,3-dione
-
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2,2'-((2S,2'S)-piperazine-1,4-diylbis(1-oxo-3-phenylpropane-2,1-diyl))bis(isoindoline-1,3-dione)
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2,2'-((2S,2'S)-piperazine-1,4-diylbis(3-methyl-1-oxobutane-2,1-diyl))bis(isoindoline-1,3-dione)
-
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2,2'-((2S,2'S)-piperazine-1,4-diylbis(4-methyl-1-oxopentane-2,1-diyl))bis(isoindoline-1,3-dione)
-
-
2,2'-((2S,2'S,3R,3'R)-piperazine-1,4-diylbis(3-methyl-1-oxopentane-2,1-diyl))bis(isoindoline-1,3-dione)
-
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2-((2S,3S)-1-(4-benzylpiperidin-1-yl)-3-methyl-1-oxopentan-2-yl)isoindoline-1,3-dione
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2-[(2S)-1-(morpholin-4-yl)-1-oxo-3-phenylpropan-2-yl]-1H-isoindole-1,3(2H)-dione
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2-[(2S)-1-oxo-3-phenyl-1-(piperidin-1-yl)propan-2-yl]-1H-isoindole-1,3(2H)-dione
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2-[(2S)-1-oxo-3-phenyl-1-(pyrrolidin-1-yl)propan-2-yl]-1H-isoindole-1,3(2H)-dione
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2-[(2S)-3-methyl-1-(morpholin-4-yl)-1-oxobutan-2-yl]-1H-isoindole-1,3(2H)-dione
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2-[(2S)-3-methyl-1-oxo-1-(piperidin-1-yl)butan-2-yl]-1H-isoindole-1,3(2H)-dione
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2-[(2S)-3-methyl-1-oxo-1-(pyrrolidin-1-yl)butan-2-yl]-1H-isoindole-1,3(2H)-dione
-
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2-[(2S)-4-methyl-1-(morpholin-4-yl)-1-oxopentan-2-yl]-1H-isoindole-1,3(2H)-dione
-
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2-[(2S)-4-methyl-1-oxo-1-(piperidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
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2-[(2S)-4-methyl-1-oxo-1-(pyrrolidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
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2-[(2S,3R)-3-methyl-1-(morpholin-4-yl)-1-oxopentan-2-yl]-1H-isoindole-1,3(2H)-dione
-
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2-[(2S,3R)-3-methyl-1-oxo-1-(piperidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
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2-[(2S,3R)-3-methyl-1-oxo-1-(pyrrolidin-1-yl)pentan-2-yl]-1H-isoindole-1,3(2H)-dione
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2-[3-(isobutylamino-methyl)-2-oxo-5-phenyl-2,3-dihydrobenzo[e][1,4]diazepin-1-yl]-N-(4-oxo-pent-2-enyl)-acetamide
-
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3,3'-(3,7,12,17-tetramethylporphyrin-2,18-diyl)dipropanoic acid
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3-((2-chloro-6-methoxyquinolin-3-yl)methylene)-5-(2,4-dimethylphenyl)furan-2(3H)-one
IC50 value on parasite 0.50 microg/ml
3-((2-chloro-6-methoxyquinolin-3-yl)methylene)-5-(4-chlorophenyl)furan-2(3H)-one
IC50 value on parasite 0.61 micro/ml
3-(1-benzoyl-5-(4-flurophenyl)-4,5-dihydro-1H-pyrazol-3yl)-7-(diethyamino)-2H-chromen-2-one
3-adamantyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-(2-chlorophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-(4-chlorophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-(4-cyanophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
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3-[2-oxo-2-(4-(4-methoxyphenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-cyclohexylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-methylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenoxypiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,4-dichlorobenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,4-dimethoxybenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,5-ditrifluoromethylbenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2-bromobenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2-chlorobenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2-trifluoromethoxybenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3,4-difluorobenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-carboxybenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-fluorobenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-isopropylbenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-methoxybenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-methylbenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-trifluoromethoxybenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-chlorobenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-fluorobenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-methoxybenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-methylbenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-trifluoromethoxybenzylidene)1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-trifluoromethylbenzylidene)
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3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-benzylidene-1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(4-pyridylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
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3-[2-oxo-2-(piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
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3-[4-(benzylsulfamoyl)phenyl]-N-(2,3-dihydro-1,4-benzodioxin-6-yl)propanamide
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less than 5% inhibition at 0.01 mM
3-[4-[(2-phenylethyl)sulfamoyl]phenyl]-N-(5-phenyl-1,3,4-thiadiazol-2-yl)propanamide
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94.5% inhibition at 0.01 mM
3-[4-[(2-phenylethyl)sulfamoyl]phenyl]-N-(pyridin-2-ylmethyl)propanamide
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10.7% inhibition at 0.01 mM
3-[4-[(2-phenylethyl)sulfamoyl]phenyl]-N-(thiophen-2-ylmethyl)propanamide
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15.2% inhibition at 0.01 mM
3-[4-[(3-chloro-4-fluorophenyl)sulfamoyl]phenyl]-N-(2,3-dihydro-1,4-benzodioxin-6-yl)propanamide
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32.7% inhibition at 0.01 mM
3-[4-[(3-chloro-4-fluorophenyl)sulfamoyl]phenyl]-N-(5-ethyl-1,3,4-thiadiazol-2-yl)propanamide
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45.1% inhibition at 0.01 mM
amino[(2E)-2-[1-(4-methoxyphenyl)ethylidene]hydrazinyl]methanethiol
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artemisinin
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artesunate
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auranofin
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30% inhibition at 0.02 mM
benzyl (1-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]cyclohexyl)carbamate
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benzyl [1-[(2-oxoethyl)carbamoyl]cyclohexyl]carbamate
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benzyl [1-[(cyanomethyl)amino]-2-methyl-1-oxopropan-2-yl]carbamate
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benzyl [1-[(cyanomethyl)carbamoyl]cyclohexyl]carbamate
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chicken egg white cystatin
-
-
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Chloroquine
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Chloroquine diphosphate
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chloro[N-[1-(hydroxy-kappaO)-3-methylbutan-2-yl]pyridine-2-carboxamidato(2-)-kappa2N1,N2]aurate(2-)
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43% inhibition at 0.02 mM
cisplatin
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43% inhibition at 0.02 mM
coproporphyrin
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deuteroporphyrin IX 2,4 (4,2) hydroxyvinyl
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deuteroporphyrin IX 2-vinyl, 4-hydroxymethyl
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dichloro[3-(propan-2-yl)-2-(pyridin-2-yl-kappaN)-4,5-dihydro-1,3-oxazol-3-ium-kappaN]aurate(1-) hexafluorophosphate
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59% inhibition at 0.02 mM
heme
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heme inhibits falcipain-2 activity against both human hemoglobin and chromogenic peptide substrates through a noncompetitive-like mechanism
isohematoporphyrin IX
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leupeptide
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-
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mesoporphyrin IX dimethyl ester
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methyl (2E)-4-[({(3R)-3-[({[4-chloro-2-(trifluoromethyl)phenyl]carbamoyl}oxy)methyl]-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-1-yl}acetyl)amino]but-2-enoate
-
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N-((S)-1-(((S)-1-(((S)-1-(2-((4-fluorophenoxy)methyl)-4,5-dihydro-1H-imidazol-1-yl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)piperidine-1-carboxamide
compound inhibits the growth of the drug resistant parasite Dd2. IC50 value for strain 3D/ 0.0055 mM
N-((S)-1-(((S)-1-(((S)-2-((S)-2-((4-fluorophenoxy)methyl)pyrrolidin-1-yl)-2-oxo-1-phenylethyl)amino)-4-methyl-1-oxopentan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)morpholine-4-carboxamide
compound exhibits potent anti-parasitic activity and a 7- to 12fold higher potency against drug resistant Dd2 and MCamp isolates, than the laboratory strain 3D7. IC50 value for strain 3D7 0.0009 mM
N-(1,3-benzothiazol-2-yl)-3-[4-[(2-phenylethyl)sulfamoyl]phenyl]propanamide
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41.5% inhibition at 0.01 mM
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-[4-[(2-phenylethyl)sulfamoyl]phenyl]acetamide
-
less than 5% inhibition at 0.01 mM
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-[4-[(2-phenylethyl)sulfamoyl]phenyl]propanamide
-
23% inhibition at 0.01 mM
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-[4-[(3,4-dimethoxyphenyl)sulfamoyl]phenyl]propanamide
-
6.3% inhibition at 0.01 mM
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-[4-[(3-methoxyphenyl)sulfamoyl]phenyl]propanamide
-
17.9% inhibition at 0.01 mM
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-[(2-phenylethyl)sulfamoyl]benzamide
-
less than 5% inhibition at 0.01 mM
N-(3,4-dimethoxyphenyl)-3-[4-[(2-phenylethyl)sulfamoyl]phenyl]propanamide
-
15% inhibition at 0.01 mM
N-(3-hydroxy-4-methoxyphenyl)-3-[4-[(2-phenylethyl)sulfamoyl]phenyl]propanamide
-
13.6% inhibition at 0.01 mM
N-(4-oxo-pent-2-enyl)-2-(2-oxo-5-phenyl-3-morpholin-1-ylmethyl-2,3-dihydro-benzo[e][1,4]diazepin-1-yl)-acetamide
-
-
N-(4-oxo-pent-2-enyl)-2-(2-oxo-5-phenyl-3-piperidin-1-ylmethyl-2,3-dihydro-benzo[e][1,4] diazepin-1-yl)-acetamide
-
80% inhibition at 0.1 mM, no inhibition at 0.03 mM
N-(5-ethyl-1,3,4-thiadiazol-2-yl)-3-[4-[(2-phenylethyl)sulfamoyl]phenyl]propanamide
-
46.5% inhibition at 0.01 mM
N-(5-ethyl-1,3,4-thiadiazol-2-yl)-3-[4-[(4-fluorophenyl)sulfamoyl]phenyl]propanamide
-
72.9% inhibition at 0.01 mM
N-(cyanomethyl)-1-([[(1S,2S)-2-phenylcyclopropyl]carbonyl]amino)cyclohexanecarboxamide
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N-(cyanomethyl)-1-[(3-cyclopentylpropanoyl)amino]cyclohexanecarboxamide
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N-(cyanomethyl)-1-[(cyclopentylacetyl)amino]cyclohexanecarboxamide
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N-(cyanomethyl)-1-[[3-(2,3-dimethoxyphenyl)propanoyl]amino]cyclohexanecarboxamide
-
N-(cyanomethyl)-1-[[3-(2-methoxyphenyl)propanoyl]amino]cyclohexanecarboxamide
-
N-(cyanomethyl)-1-[[3-(4-methoxyphenyl)propanoyl]amino]cyclohexanecarboxamide
-
N-(cyanomethyl)-1-[[3-(furan-2-yl)propanoyl]amino]cyclohexanecarboxamide
-
N-(cyanomethyl)-1-[[3-(pyridin-3-yl)propanoyl]amino]cyclohexanecarboxamide
-
N-(cyanomethyl)-1-[[3-(thiophen-2-yl)propanoyl]amino]cyclohexanecarboxamide
-
N-methyl mesoporphyrin
-
-
N-methyl protoporphyrin IX
-
-
N-[(2S)-1-[(1-cyanocyclopropyl)amino]-1-oxo-3-(pyridin-3-yl)propan-2-yl]-3-(1H-imidazol-2-yl)benzamide
P2-modified aminonitrile based inhibitor, not cytotoxic to either cancer (HeLa) or normal (Huvec) human cell lines
N-[(2S)-1-[(1-cyanocyclopropyl)amino]-1-oxo-3-(pyridin-3-yl)propan-2-yl]-3-(1H-tetrazol-1-yl)benzamide
compound shows more than 500fold selectivity for falcipain-2 over cathepsin B, K and L and about 30fold selectivity over cathepsin S. Not cytotoxic to either cancer (HeLa) or normal (Huvec) human cell lines
potassium bis(1,1-dioxido-3-oxo-1,2-benzothiazol-2(3H)-yl)aurate(1-)
-
66% inhibition at 0.02 mM
protoporphyrin IX
-
-
RLLGAP-(cis-4-aminocyclohexane carboxylic acid)-QLVSGI
-
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RLLGAP-(cis-4-aminocyclohexane carboxylic acid)-QLVSGI-betaAla-betaAla-PW
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RLLGAP-gamma-aminobutyric acid-QLVSGI
-
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RLLGAP-gamma-aminobutyric acid-QLVSGI-betaAla-betaAla-PW
-
-
RLLGAPV-(cis-4-aminocyclohexane carboxylic acid)-RQLVSGI
-
63% inhibition at 0.005 mM
RLLGAPV-(cis-4-aminocyclohexane carboxylic acid)-RQLVSGI-betaAla-betaAla-PW
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RLLGAPV-gamma-aminobutyric acid-RQLVSGI
-
57% inhibition at 0.005 mM
RLLGAPV-gamma-aminobutyric acid-RQLVSGI-betaAla-betaAla-PW
-
-
SERPINB3
potent cross-class inhibitor of cysteine cathepsins L, K, S and papain, inhibits proteolytic activities as well as specific hemoglobinolytic activity of FP2 via noncovalent interaction. Disease state mutant serpin-Gly351Ala displays better anti-protease activity against FP2
-
[(3R)-2-oxo-1-(2-oxo-2-[[(2E)-4-oxopent-2-en-1-yl]amino]ethyl)-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl]methyl [4-chloro-2-(trifluoromethyl)phenyl]carbamate
-
-
[(5Z)-2,4-dioxo-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidin-3-yl]acetic acid
-
-
[3-benzyl-2-(pyridin-2-yl-kappaN)-4,5-dihydro-1,3-oxazol-3-ium-kappaN](dichloro)aurate(1-) hexafluorophosphate
-
54% inhibition at 0.02 mM
additional information
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