Information on EC 3.6.4.10 - non-chaperonin molecular chaperone ATPase and Organism(s) Homo sapiens

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The expected taxonomic range for this enzyme is: Eukaryota, Bacteria, Archaea


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EC NUMBER
COMMENTARY hide
3.6.4.10
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RECOMMENDED NAME
GeneOntology No.
non-chaperonin molecular chaperone ATPase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + H2O = ADP + phosphate
show the reaction diagram
highly diverse group of enzymes that perform many functions that are similar to those of chaperonins. They comprise a number of heat-shock-cognate proteins. They are also active in clathrin uncoating and in the oligomerization of actin
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of phosphoric ester
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-
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SYSTEMATIC NAME
IUBMB Comments
ATP phosphohydrolase (polypeptide-polymerizing)
This is a highly diverse group of enzymes that perform many functions that are similar to those of chaperonins. They comprise a number of heat-shock-cognate proteins. They are also active in clathrin uncoating and in the oligomerization of actin.
CAS REGISTRY NUMBER
COMMENTARY hide
9000-83-3
-
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
a highly conserved molecular chaperone of the Hsp70 family that is primarily found in the mitochondria
malfunction
in vivo deregulation of mortalin expression and/or function is correlated with agerelated diseases and certain cancers due to its interaction with the p53 protein
metabolism
physiological function
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + H2O
ADP + phosphate
show the reaction diagram
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + H2O
ADP + phosphate
show the reaction diagram
additional information
?
-
-
NEF binding stabilizes the ATPase domain in an open form and thereby facilitates the nucleotide exchange step of the chaperone cycle
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-
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METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Mn2+
-
approx. 15% of activity with Mg2+ at 20 mM
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(1aR,2Z,4E,6Z,14R)-8-chloro-9,11-dihydroxy-14-methyl-6-[[(piperidin-1-ylacetyl)oxy]imino]-1a,6,7,14,15,15a-hexahydro-12H-oxireno[e][2]benzoxacyclotetradecin-12-one
-
-
(1aR,2Z,4E,6Z,14R,15aR)-8-chloro-6-([[(dimethylamino)acetyl]oxy]imino)-9,11-dihydroxy-14-methyl-1a,6,7,14,15,15a-hexahydro-12H-oxireno[e][2]benzoxacyclotetradecin-12-one
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-
(1aR,2Z,4E,6Z,14R,15aR)-8-chloro-9,11-dihydroxy-14-methyl-6-(methylimino)-1a,6,7,14,15,15a-hexahydro-12H-oxireno[e][2]benzoxacyclotetradecin-12-one
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-
(1aR,2Z,4E,6Z,14R,15aR)-8-chloro-9,11-dihydroxy-14-methyl-6-[[(piperidin-1-ylcarbonyl)oxy]imino]-1a,6,7,14,15,15a-hexahydro-12H-oxireno[e][2]benzoxacyclotetradecin-12-one
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-
(1aR,2Z,4E,6Z,14R,15aR)-8-chloro-9,11-dihydroxy-6-(hydroxyimino)-14-methyl-1a,6,7,14,15,15a-hexahydro-12H-oxireno[e][2]benzoxacyclotetradecin-12-one
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KF25706
(1aS,2Z,15R,16aR)-9-chloro-10,12-dihydroxy-15-methyl-1a,15,16,16a-tetrahydro-1H-7,4-(metheno)cyclopropa[h][12,2,3,4]benzoxatriazacyclopentadecin-13(8H)-one
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-
(1R)-2-(5-chloro-2,4-dihydroxybenzoyl)-N-ethyl-2,3-dihydro-1H-isoindole-1-carboxamide
-
-
(3R,5E,9E,11Z)-13-chloro-7,14,16-trihydroxy-3-methyl-11-[[(piperidin-1-ylacetyl)oxy]imino]-3,4,7,8,11,12-hexahydro-1H-2-benzoxacyclotetradecin-1-one
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-
(3S)-14,16-dihydroxy-3-methyl-3,4,5,6,9,10,11,12-octahydro-1H-2-benzoxacyclotetradecine-1,7(8H)-dione
-
-
(4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-amino-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbamate
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IPI-493
(4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-[(4-[[4-(4-chlorophenyl)piperazin-1-yl]methyl]benzoyl)amino]-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbamate
-
-
(4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-[(4-[[benzyl(ethyl)amino]methyl]benzoyl)amino]-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbamate
-
-
(4E,6Z,8S,9S,10E,12S,13R,14S,16R)-20-chloro-13,19-dihydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3-oxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbamate
-
-
(4E,6Z,8S,9S,10E,12S,13R,14S,16R)-9-(carbamoyloxy)-13,20,22-trihydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3-oxo-N-(prop-2-en-1-yl)-2-azabicyclo[16.3.1]docosa-1(22),4,6,10,18,20-hexaen-19-aminium chloride
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IPI-504
(4E,6Z,8S,9S,10E,12S,13R,14S,16S,17R)-22-hydroxy-8,13,14,17-tetramethoxy-4,10,12,16,20-pentamethyl-3-oxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl carbamate
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-
(4E,8S,9S,10E,12S,13R,14S,16R)-13,20-dihydroxy-8,14-dimethoxy-10,12,16-trimethyl-3-oxo-2-azabicyclo[16.3.1]docosa-1(22),4,10,18,20-pentaen-9-yl carbamate
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KOSN1559
(5-[4-amino-6-[(2-methoxyphenyl)sulfanyl]-1,3,5-triazin-2-yl]-2,4-dichlorophenoxy)acetonitrile
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-
(5E)-5-[(1-benzyl-1H-indol-3-yl)methylidene]-1-(2-fluorocyclohexyl)pyrimidine-2,4,6(1H,3H,5H)-trione
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-
(5E,9E,11Z)-13-chloro-14,16-dihydroxy-11-[[(piperidin-1-ylacetyl)oxy]imino]-3,4,7,8,11,12-hexahydro-1H-2-benzoxacyclotetradecin-1-one
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-
(5Z)-7-[4-fluoro-2-(pyridin-3-yl)phenyl]-5-(hydroxyimino)-4-methyl-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-2-amine
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-
(7R)-2-amino-7-[5-(6-methoxypyrazin-2-yl)-1,3-thiazol-4-yl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one
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-
1,3-dihydro-2H-isoindol-2-yl[2,4-dihydroxy-5-(propan-2-yl)phenyl]methanone
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1,3-dihydro-2H-isoindol-2-yl[6-hydroxy-3-(3-methylbenzyl)-1H-indazol-5-yl]methanone
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1-(3H-imidazo[4,5-c]pyridin-2-yl)-2,3-dihydro-5H-pyrrolo[2,1-a]isoindol-5-one
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-
1-(4-aminoquinazolin-6-yl)-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indol-4-one
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1-(5-ethyl-2,4-dihydroxyphenyl)-5-(trifluoromethyl)-1,3-dihydro-2H-benzimidazol-2-one
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1-(6-amino-9H-purin-8-yl)-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one
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-
1-[4-(2-[6-amino-8-[(7-bromo-2,3-dihydro-1,4-benzodioxin-6-yl)sulfanyl]-3H-purin-3-yl]ethyl)piperidin-1-yl]-2-hydroxy-2-methylpropan-1-one
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-
17-(2-dimethylaminoethyl)amino-17-demethoxygeldanamycin
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17-(allylamino)-17-demethoxygeldanamycin
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17-allylamino-17-demethoxygeldanamycin hydroquinone hydrochloride
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17-dimethylaminoethylamino-17-demethoxygeldanamycin hydrochloride
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2'-methoxy-5-[4-(2-methoxyethyl)-4H-1,2,4-triazol-3-yl]-5'-(propan-2-yl)biphenyl-2,4-diol
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-
2,4-dihydroxy-5-[5-hydroxy-4-(2-methylphenyl)-4H-1,2,4-triazol-3-yl]-N-methyl-N-pentylbenzamide
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2,4-dihydroxy-5-[5-hydroxy-4-(2-methylphenyl)-4H-1,2,4-triazol-3-yl]-N-methyl-N-[2-(3-methylphenyl)ethyl]benzamide
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2,4-dihydroxy-N-methyl-N-(3-methylbenzyl)-5-[1-(2-methylphenyl)-1H-pyrazol-5-yl]benzamide
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2,5-dichloro-N-[4-hydroxy-3-(2-hydroxynaphthalen-1-yl)phenyl]benzenesulfonamide
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2-(5-[3-[2,4-dihydroxy-5-(propan-2-yl)phenyl]-5-hydroxy-4H-1,2,4-triazol-4-yl]-1H-indol-1-yl)ethyl dihydrogen phosphate
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-
2-([3-[2-(dimethylamino)ethoxy]-4-methoxyphenyl]amino)-4-(3,6,6-trimethyl-4-oxo-4,5,6,7-tetrahydro-1H-indazol-1-yl)benzamide
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-
2-amino-4-chloro-8-[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]-5-propyl-7,8-dihydropteridin-6(5H)-one
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2-amino-4-methyl-7-[2-(phenylamino)phenyl]-7,8-dihydroquinazolin-5(6H)-one
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2-amino-4-[2,4-dichloro-5-[3-(pyrrolidin-1-yl)propoxy]phenyl]-N-ethylthieno[2,3-d]pyrimidine-6-carboxamide
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NVP-BEP800/VER-82576
2-amino-6-benzyl-4-(2,4-dichlorophenyl)-5,6-dihydro-7H-pyrrolo[3,4-d]pyrimidin-7-one
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-
2-amino-6-chloro-9-[(4-iodo-3,5-dimethylpyridin-2-yl)methyl]-7-[2-(1H-pyrrol-1-yl)ethyl]-7,9-dihydro-8H-purin-8-one
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-
2-amino-N-ethyl-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
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SNX-7081, weak inhibitor
2-bromo-4-(5-oxo-5,6,7,8-tetrahydronaphthalen-1-yl)benzonitrile
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-
2-chloro-6-(2,4-dichlorophenyl)-9H-purine
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2-chloro-N-[3-(5-ethyl-2,4-dihydroxyphenyl)-1H-pyrazol-4-yl]benzamide
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2-fluoro-6-(tetrahydro-2H-pyran-4-ylamino)-4-(2,3,6,6-tetramethyl-4-oxo-4,5,6,7-tetrahydro-1H-indol-1-yl)benzamide
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-
2-fluoro-8-[(6-iodo-1,3-benzodioxol-5-yl)methyl]-9-[3-(propan-2-ylamino)propyl]-9H-purin-6-amine
2-[(2-methoxyethyl)amino]-4-(4-oxo-1,2,3,4-tetrahydro-9H-carbazol-9-yl)benzamide
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-
2-[(6-bromo-1,3-benzodioxol-5-yl)methyl]-1-methyl-5-(propanoylamino)-1H-imidazole-4-carboxamide
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-
2-[(E)-2-(2-hydroxy-3-methoxyphenyl)ethenyl]-3-(4-methoxycyclohexyl)quinazolin-4(3H)-one
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-
2-[(E)-2-(2-hydroxy-3-methoxyphenyl)ethenyl]-3-(4-methoxyphenyl)quinazolin-4(3H)-one
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micromolar inhibitor
2-[2-[(4-methoxy-3,5-dimethyl-3,4-dihydropyridin-2-yl)methyl]-7,8-dihydro-2H-6-thia-1,2,3,5-tetraazaacenaphthylen-7-yl]-N-(5-methyl-1,3-thiazol-2-yl)acetamide
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2-[4-(1-methyl-1H-indol-5-yl)-5-sulfanyl-4H-1,2,4-triazol-3-yl]-6-(propan-2-yl)pyridine-3,5-diol
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2-[6-amino-2-fluoro-8-[(6-iodo-1,3-benzodioxol-5-yl)methyl]-9H-purin-9-yl]ethyl sulfamate
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2-[6-amino-8-[(6-bromo-1,3-benzodioxol-5-yl)sulfanyl]-9H-purin-9-yl]-N-hydroxyacetamide
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2-[[4-(2-chloro-5-hydroxy-4-methoxyphenyl)-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-2-yl]sulfanyl]-N,N-dimethylacetamide
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2-[[5-(1,3-benzodioxol-5-yl)-4-phenyl-4H-1,2,4-triazol-3-yl]sulfanyl]-1-phenylethanone
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2-[[6-(dimethylamino)-1,3-benzodioxol-5-yl]sulfanyl]-1-[2-[(2,2-dimethylpropyl)amino]ethyl]-1H-imidazo[4,5-c]pyridin-4-amine
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CUDC-305
3,6-diamino-5-cyano-4-(4-methoxy-3-[[3-(trifluoromethyl)benzoyl]amino]phenyl)thieno[2,3-b]pyridine-2-carboxamide
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3-(5-chloro-2,4-dihydroxyphenyl)-N-(4-fluorophenyl)-4H-pyrazole-4-carboxamide
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3-(5-chloro-2,4-dihydroxyphenyl)-N-(4-methoxyphenyl)-4H-pyrazole-4-carboxamide
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3-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)-1H-pyrazole-5-carboxamide
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VER-49009
3-(5-chloro-2,4-dihydroxyphenyl)-N-[3-(trifluoromethyl)phenyl]-4H-pyrazole-4-carboxamide
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3-(cyclopentylmethyl)-6-hydroxy-N-methyl-N-[4-(morpholin-4-yl)phenyl]-1H-indazole-5-carboxamide
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3-benzyl-4-fluoro-1H-indazol-6-ol
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3-[(4-hydroxycyclohexyl)amino]-2',3'-dimethoxybiphenyl-4-carbonitrile
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3-[(E)-[2-[(2-amino-6-methylpyrimidin-4-yl)ethynyl]benzylidene]amino]-1,3-oxazolidin-2-one
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4-(1,3-benzodioxol-5-yl)-3-(5-ethyl-2,4-dihydroxyphenyl)-1H-pyrazole-5-carboxylic acid
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G3129
4-(1-phenyl-1H-1,2,3-triazol-4-yl)-6-(propan-2-yl)benzene-1,3-diol
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4-(2,4-dichloro-5-methoxyphenyl)-2,6-dimethyl-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
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4-(2,4-dichloro-5-methoxyphenyl)-2-[2-(diethylamino)ethoxy]-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
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4-(2,4-dichlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile
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4-(4-[4-methoxy-3-[methyl(2-methylpropyl)amino]phenyl]-5-sulfanyl-4H-1,2,4-triazol-3-yl)-6-(propan-2-yl)benzene-1,3-diol
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4-(but-2-yn-1-yl)-6-[4-(4-methoxyphenyl)-5-methyl-1,2-oxazol-3-yl]benzene-1,3-diol
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4-([2-carbamoyl-5-[6,6-dimethyl-4-oxo-3-(trifluoromethyl)-3a,4,5,6,7,7a-hexahydro-1H-indazol-1-yl]phenyl]amino)cyclohexyl glycinate
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SNX-5422
4-([2-[3,5-bis(trifluoromethyl)phenyl]-4,5-bis(4-methoxyphenyl)-1H-imidazol-1-yl]methyl)benzoic acid
-
inhibits the ATPase activity of Hsc70 by binding to its ATPase domain
4-amino-11,18,20-trimethyl-7-thia-3,5,11,15-tetraazatricyclo[15.3.1.12,6]docosa-1(21),2(22),3,5,17,19-hexaene-10,16-dione
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-
4-chloro-6-(2,4-dichlorophenyl)pyrimidin-2-amine
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-
4-chloro-6-(4-[4-[4-(methylsulfonyl)benzyl]piperazin-1-yl]-1H-pyrazol-3-yl)benzene-1,3-diol
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-
4-chloro-6-(5-[[2-(morpholin-4-yl)ethyl]amino]-1,2-benzoxazol-3-yl)benzene-1,3-diol
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-
4-chloro-6-phenylpyrimidin-2-amine
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-
4-chloro-6-[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-methyl-1H-pyrazol-3-yl]benzene-1,3-diol
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CCT072440
4-chloro-6-[5-(4-ethoxyphenyl)-1,2,3-thiadiazol-4-yl]benzene-1,3-diol
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-
4-ethyl-6-[4-(1H-imidazol-4-yl)-1H-pyrazol-3-yl]benzene-1,3-diol
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G3130
4-ethyl-6-[4-(4-methoxynaphthalen-1-yl)-5-sulfanyl-4H-1,2,4-triazol-3-yl]benzene-1,3-diol
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-
4-ethyl-6-[5-hydroxy-4-(naphthalen-1-yl)-1H-pyrazol-3-yl]benzene-1,3-diol
-
-
4-[2-amino-4-chloro-7-[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]but-3-yn-1-ol
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-
4-[4-(1,3-benzodioxol-5-yl)-5-methyl-1H-pyrazol-3-yl]-6-ethylbenzene-1,3-diol
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-
4-[4-(1-methyl-1H-indol-5-yl)-5-[(pyridin-3-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]-6-(propan-2-yl)benzene-1,3-diol
-
-
4-[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-methyl-1H-pyrazol-3-yl]-6-ethylbenzene-1,3-diol
-
CCT08159/RBT0028535
4-[4-(2-fluorophenyl)-5-hydroxy-4H-1,2,4-triazol-3-yl]-6-(2-phenylethyl)benzene-1,3-diol
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-
4-[4-(2-methyl-1,3-thiazol-4-yl)-5-(trifluoromethyl)-1,2-oxazol-3-yl]benzene-1,3-diol
-
micromolar inhibitor
4-[4-(4-benzylpiperazin-1-yl)-1H-pyrazol-3-yl]-6-chlorobenzene-1,3-diol
-
-
4-[4-(6-fluoro-1H-benzimidazol-2-yl)-9H-carbazol-9-yl]-2-[(trans-4-hydroxycyclohexyl)amino]benzamide
-
-
4-[4-(diethylamino)phenyl]-5-[2,4-dihydroxy-5-(propan-2-yl)phenyl]-N-ethyl-1,2-oxazole-3-carboxamide
-
-
4-[5-hydroxy-4-(1-methyl-1H-indol-5-yl)-4H-1,2,4-triazol-3-yl]-6-(propan-2-yl)benzene-1,3-diol
-
-
4-[5-hydroxy-4-[4-(morpholin-4-yl)phenyl]-4H-1,2,4-triazol-3-yl]-6-(propan-2-yl)benzene-1,3-diol
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-
4-[6,6-dimethyl-4-oxo-3-(trifluoromethyl)-3a,4,5,6,7,7a-hexahydro-1H-indazol-1-yl]-2-[(4-hydroxycyclohexyl)amino]benzamide
-
SNX-2112
5-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)-1,2-oxazole-3-carboxamide
5-(5-ethyl-2,4-dihydroxyphenyl)-1-(naphthalen-1-yl)-1,3-dihydro-2H-imidazol-2-one
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-
5-amino-1-(5-aminopentyl)-2-[(6-iodo-1,3-benzodioxol-5-yl)sulfanyl]-1H-imidazole-4-carboxamide
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-
5-amino-1-[(2S,3S,4R,5S)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-1H-imidazole-4-carboxamide
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-
5-hydroxy-4-[5-hydroxy-4-[6-(morpholin-4-yl)pyridin-3-yl]-4H-1,2,4-triazol-3-yl]-2-(propan-2-yl)phenyl dihydrogen phosphate
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-
5-[2,4-dihydroxy-5-(propan-2-yl)phenyl]-N-ethyl-4-[4-(morpholin-4-yl)phenyl]-1,2-oxazole-3-carboxamide
6-(4-benzylpiperazin-1-yl)-2-chloro-9H-purine
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-
6-bromo-N-[4-(quinolin-3-yl)-9H-fluoren-9-yl]-1,8a-dihydropyrido[2,3-d]pyrimidine-5-carboxamide
-
-
6-chloro-9-[(3,5-dimethylpyridin-2-yl)methyl]-9H-purin-2-amine
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-
6-chloro-9-[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]-9H-purin-2-amine
6-chloro-9-[(5-methoxy-4,6-dimethylpyridin-3-yl)methyl]-9H-purin-2-amine
-
-
6-[(2R)-2-[(5-fluoro-2-methoxyphenoxy)methyl]pyrrolidin-1-yl]-9H-purine
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-
7-[2,4-dichloro-6-[2-(1H-pyrazol-1-yl)ethoxy]phenyl][1,3]thiazolo[5,4-d]pyrimidin-5-amine
-
-
8-(2-chloro-3,4,5-trimethoxybenzyl)-2-fluoro-9-(pent-4-yn-1-yl)-9H-purin-6-amine
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PU24FCl
8-[(2-iodo-5-methoxyphenyl)sulfanyl]-9-(pent-4-yn-1-yl)-9H-purin-6-amine
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-
8-[(6-bromo-1,3-benzodioxol-5-yl)sulfanyl]-9-(pent-4-yn-1-yl)-9H-purin-6-amine
-
potent Hsp90 binder
8-[(6-iodo-1,3-benzodioxol-5-yl)sulfanyl]-9-[3-(propan-2-ylamino)propyl]-9H-purin-6-amine
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PU-H71
8-[(7-chloro-1,3-benzothiazol-2-yl)sulfanyl]-9-[2-(cyclopropylamino)ethyl]-9H-purin-6-amine
-
-
8-[(7-chloro-1,3-benzothiazol-2-yl)sulfanyl]-9-[2-[(2,2-dimethylpropyl)amino]ethyl]-9H-purin-6-amine
-
-
8-[[5-(diethylamino)pentyl]amino]quinolin-6-ol
-
-
9-butyl-8-(3,4,5-trimethoxybenzyl)-9H-purin-6-amine
-
PU3
9-butyl-8-[(7-chloro-1,3-benzothiazol-2-yl)sulfanyl]-9H-purin-6-amine
-
-
9-[2-(tert-butylamino)ethyl]-8-[(2-iodo-5-methoxyphenyl)sulfanyl]-9H-purin-6-amine
-
-
9-[2-[(2,2-dimethylpropyl)amino]ethyl]-8-[(2-iodo-5-methoxyphenyl)sulfanyl]-9H-purin-6-amine
-
-
9-[3-(tert-butylamino)propyl]-8-[(2-iodo-5-methoxyphenyl)sulfanyl]-9H-purin-6-amine
-
-
alvespimycin
-
-
apoptozole
-
inhibits Hsc70 activity by binding to its ATPase domain
cisplatin
-
-
CNF1010
-
-
-
cyclohexyl 5-[6-amino-8-[(6-iodo-1,3-benzodioxol-5-yl)sulfanyl]-9H-purin-9-yl]-L-norvalinate
-
-
cycloproparadicicol
-
-
deguelin
-
inhibits HSP90 by interacting with its ATP-binding pocket
desmethoxy-geldanamycin
-
-
diethyl (2-[6-amino-8-[(7-bromo[1,3]thiazolo[4,5-c]pyridin-2-yl)sulfanyl]-9H-purin-9-yl]ethyl)phosphonate
-
-
diethyl (2-[6-amino-8-[(7-chloro-1,3-benzothiazol-2-yl)sulfanyl]-9H-purin-9-yl]ethyl)phosphonate
-
-
diethyl (2-[6-amino-8-[(7-chloro[1,3]thiazolo[4,5-c]pyridin-2-yl)sulfanyl]-9H-purin-9-yl]ethyl)phosphonate
-
-
ethyl (4-[3-[2,4-dihydroxy-5-(propan-2-yl)phenyl]-5-sulfanyl-4H-1,2,4-triazol-4-yl]benzyl)carbamate
-
-
ethyl 2-amino-4-(4-bromo-2-chloro-5-methoxyphenyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxylate
-
-
ethyl 4-[2,4-dihydroxy-5-(propan-2-yl)phenyl]-6-methyl-2-oxo-1,2-dihydropyrimidine-5-carboxylate
-
-
geldanamycin
KW-2478
-
-
methyl (2E)-3-[2-amino-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)quinazolin-6-yl]prop-2-enoate
-
-
Mg2+
-
above 20 mM, approx. 50% inhibition at 100 mM
MPC-3100
-
-
mycograb
-
-
-
N-(4-acetylphenyl)-3-(5-chloro-2,4-dihydroxyphenyl)-1H-pyrazole-4-carboxamide
-
-
N-(4-acetylphenyl)-3-(5-chloro-2,4-dihydroxyphenyl)-4H-pyrazole-4-carboxamide
-
-
N-benzyl-6-(3-[[(2,6-dichloro-9H-purin-9-yl)acetyl]amino]-8-azabicyclo[3.2.1]oct-8-yl)pyridine-3-carboxamide
-
-
N-butyl-2,4-dihydroxy-5-[(5-hydroxy-1,3-dihydro-2H-isoindol-2-yl)carbonyl]benzamide
-
-
N-ethylmaleimide
-
5 mM, approx. 85% inhibition
N-[2-(dimethylamino)ethyl]-6-[3-[(4-methoxy-2-methylbenzoyl)amino]-8-azabicyclo[3.2.1]oct-8-yl]pyridine-3-carboxamide
-
-
N-[4-(3H-imidazo[4,5-c]pyridin-2-yl)-9H-fluoren-9-yl]quinoline-5-carboxamide
-
-
N-[4-(aminosulfonothioyl)benzyl]-3-(5-chloro-2,4-dihydroxyphenyl)-1H-pyrazole-4-carboxamide
-
-
N-[4-hydroxy-3-(2-hydroxynaphthalen-1-yl)phenyl]thiophene-2-sulfonamide
-
-
NaCl
-
approx. 50% inhibition at 100 mM, approx. 90% inhibition at 600 mM
novobiocin
-
analogs
NVPHSP990
-
-
p23 protein
-
cochaperone, interacts with Hsp90 in both the absence and presence of nucleotide, with a higher affinity in presence of the ATP analogue 5'-adenylyl-beta,gamma-imidodiphosphate. Mixed inhibition, one p23 binds to each subunit of the Hsp90 dimer. Complex formation between Hsp90 and p23 increases the apparent affinity of Hsp90 for 5'-adenylyl-beta,gamma-imidodiphosphate and completely inhibits the ATPase activity
-
pochonin A
-
good inhibitor of Hsp90
pochonin D
radamide
-
-
radester
-
-
radicicol
retaspimycin
-
IP-504
STA-1474
-
-
STA-9090
-
-
tanespimycin
-
-
XL888
-
-
[(2R)-1-(5-chloro-2,4-dihydroxybenzoyl)pyrrolidin-2-yl](1,3-dihydro-2H-isoindol-2-yl)methanone
-
-
[1-(3-bromo-4-cyanophenyl)-2-oxo-2,4,5,6,7,7a-hexahydro-1H-indol-3-yl]acetic acid
-
-
[2,4-dihydroxy-5-(propan-2-yl)phenyl](5-[[methyl(piperidin-1-yl)amino]methyl]-1,3-dihydro-2H-isoindol-2-yl)methanone
-
AT-13387
[4-[(2S)-1-(5-chloro-2,4-dihydroxybenzoyl)pyrrolidin-2-yl]phenyl](3,3-difluoropyrrolidin-1-yl)methanone
-
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
Hsc20
-
the ATPase activity of mtHSP70 is accelerated by co-chaperone HSC20 and further accelerated by HSC20 plus scaffold protein ISCU. mtHSP70 binds preferentially to the D-state of ISCU and that HSC20 binds preferentially to the S-state of ISCU
-
ISCU
-
the iron-sulfur cluster scaffold protein, the ATPase activity of mtHSP70 is accelerated by co-chaperone HSC20 and further accelerated by HSC20 plus scaffold protein ISCU. mtHSP70 binds preferentially to the D-state of ISCU and that HSC20 binds preferentially to the S-state of ISCU, detailed interaction analysis
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.19 - 0.33
ATP
additional information
additional information
Michaelis-Menten kinetics
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0025
ATP
recombinant enzyme, pH 7.5, 37C
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00009
2-fluoro-8-[(6-iodo-1,3-benzodioxol-5-yl)methyl]-9-[3-(propan-2-ylamino)propyl]-9H-purin-6-amine
Homo sapiens;
-
pH and temperature not specified in the publication
0.0003
6-chloro-9-[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]-9H-purin-2-amine
Homo sapiens;
-
pH and temperature not specified in the publication
0.0002
6-chloro-9-[(5-methoxy-4,6-dimethylpyridin-3-yl)methyl]-9H-purin-2-amine
Homo sapiens;
-
pH and temperature not specified in the publication
0.0046
8-(2-chloro-3,4,5-trimethoxybenzyl)-2-fluoro-9-(pent-4-yn-1-yl)-9H-purin-6-amine
Homo sapiens;
-
pH and temperature not specified in the publication
0.00028
8-[(2-iodo-5-methoxyphenyl)sulfanyl]-9-(pent-4-yn-1-yl)-9H-purin-6-amine
Homo sapiens;
-
pH and temperature not specified in the publication
0.0003
8-[(6-bromo-1,3-benzodioxol-5-yl)sulfanyl]-9-(pent-4-yn-1-yl)-9H-purin-6-amine
Homo sapiens;
-
pH and temperature not specified in the publication
0.00005
8-[(6-iodo-1,3-benzodioxol-5-yl)sulfanyl]-9-[3-(propan-2-ylamino)propyl]-9H-purin-6-amine
Homo sapiens;
-
pH and temperature not specified in the publication
0.00011
8-[(7-chloro-1,3-benzothiazol-2-yl)sulfanyl]-9-[2-(cyclopropylamino)ethyl]-9H-purin-6-amine
Homo sapiens;
-
pH and temperature not specified in the publication
0.000035
8-[(7-chloro-1,3-benzothiazol-2-yl)sulfanyl]-9-[2-[(2,2-dimethylpropyl)amino]ethyl]-9H-purin-6-amine
Homo sapiens;
-
pH and temperature not specified in the publication
0.001 - 0.002
9-butyl-8-(3,4,5-trimethoxybenzyl)-9H-purin-6-amine
Homo sapiens;
-
pH and temperature not specified in the publication
0.00018
9-butyl-8-[(7-chloro-1,3-benzothiazol-2-yl)sulfanyl]-9H-purin-6-amine
Homo sapiens;
-
pH and temperature not specified in the publication
0.00014
9-[3-(tert-butylamino)propyl]-8-[(2-iodo-5-methoxyphenyl)sulfanyl]-9H-purin-6-amine
Homo sapiens;
-
pH and temperature not specified in the publication
0.000028
diethyl (2-[6-amino-8-[(7-bromo[1,3]thiazolo[4,5-c]pyridin-2-yl)sulfanyl]-9H-purin-9-yl]ethyl)phosphonate
Homo sapiens;
-
pH and temperature not specified in the publication
0.00003
diethyl (2-[6-amino-8-[(7-chloro-1,3-benzothiazol-2-yl)sulfanyl]-9H-purin-9-yl]ethyl)phosphonate
Homo sapiens;
-
pH and temperature not specified in the publication
0.00003
diethyl (2-[6-amino-8-[(7-chloro[1,3]thiazolo[4,5-c]pyridin-2-yl)sulfanyl]-9H-purin-9-yl]ethyl)phosphonate
Homo sapiens;
-
pH and temperature not specified in the publication
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.00086
purified recombinant enzyme, pH 7.5, 37C
0.00167
-
purified recombinant enzyme, pH 7.5, 25C, in absence of activators
0.00283
-
purified recombinant enzyme, pH 7.5, 25C, in presence of 0.006 mM HSC20
0.0075
-
purified recombinant enzyme, pH 7.5, 25C, in presence of 0.015 mM ISCU
0.025
-
purified recombinant enzyme, pH 7.5, 25C, in presence of 0.004 mM HSC20 and 0.015 mM ISCU
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7
-
assay at
7.4
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
25
-
assay at
50 - 55
-
-
TEMPERATURE RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
25 - 70
-
approx. 64% of maximal activity at 40C, approx. 50% of maximal activity at 65C
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
overexpression of mortalin/mtHsp70 extends the in vitro lifespan of normal human fibroblasts
Manually annotated by BRENDA team
-
Helicobacter pylori (cagA+, vacA+) and Hp (cagA-, vacA-) inhibit expression of HSP70 in gastric carcinoma MKN7 cells independently of the presence or absence of cagA genes
Manually annotated by BRENDA team
-
knock-down of mortalin/mtHsp70 causes their growth arrest
Manually annotated by BRENDA team
additional information
-
Hsp90s are overexpressed in cancer cells
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
accumulation during heat shock
Manually annotated by BRENDA team
PDB
SCOP
CATH
UNIPROT
ORGANISM
Homo sapiens;
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
homodimer
-
-
monomer
1 * 36000-66000, recombinant enzyme, monomeric and monodisperse mortalin, analytical ultracentrifugation and crystal structure analysis, mortalin has an elongated shape in solution, modeling, overview
additional information
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
41.9-kDa human Hsp70 ATPase domain
-
atomic resolution analysis of the Hsp90 N-terminal domain binding energy landscape by simulating protein dynamics with binding partners such as ATP, ADP, shepherdin. The activity of the molecular chaperone may be linked to local folding-unfolding transitions and conformational switching of the active site lid upon binding and differences in the underlying protein dynamics as a function of the binding partner
-
Bag2-BNB-Hsc70-nucleotide-binding domain complex
-
cDNa sequence encoding alphabeta crystallin inserted into pET16b, expressed in Escherichia coli Bl21
-
crystal structures of four human Hsp70 isoforms are presented: nucleotide binding domains NBDs of HSPA1L, HSPA2, HSPA5 and HSPA6. All four proteins crystallize in a closed cleft conformation, although a slight cleft opening through rotation of subdomain IIB is observed for the HSPA5-ADP complex. The structures presented support the view that the nucleotide binding domains of human Hsp70 function by conserved mechanisms and contribute little to isoform specificity, which instead is brought about by the substrate binding domains and by accessory proteins
-
molecular docking studies with Hsc70 and apoptozole. The 3,5-bis(trifluoromethyl)phenyl group of apoptozole interacts with the binding site of a triphosphate moiety of ATP through polar interactions, and the two 4-methoxy phenyl moieties of apoptozole are located at the adenosine binding site of Hsc70. The CONH2 group of apoptozole can interact with the Glu376 side chain of Hsc70 via a hydrogen-bonding interaction
-
purified recombinant enzyme, X-ray diffraction structure determination and analysis, small angle X-ray scattering, modeling
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
recombinant His-tagged enzyme by nickel affinity chromatography and gel filtration
recombinant His-tagged SUMO fusion enzyme mtHSP70 from Escherichia coli by nickel affinity chromatography, His-tag and SUMO cleavage and again nickel affinity exchange chromatography for tag removal, followed by gel filtration
-
recombinant p97-VCP
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
expressed in Escherichia coli
-
expression of GFP-Hsp70 fusion protein in HeLa cells
-
Hsc 70, Hsc70 nucleotide binding domain (residue 1-381)
-
Hsp90beta, Hsp90beta-delta, Hsp90 C-terminal domain (residue 546-724), Hsp90beta-MC (residue 546-724)
-
recombinant expression of His-tagged enzyme in Escherichia coli strain BL21(DE3), production of folded and soluble recombinant mortalin when co-expressed with the human Hsp70-escort protein 1, but Hsp70 is still likely prone to self-association
recombinant expression of His-tagged enzyme mtHSP70 as N-terminal SUMO fusion protein, lacking the gene sequence coding for N-terminal mitochondrial targeting peptide, in Escherichia coli
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
A116N
-
reduced affinity to co-chaperone Hop in the presence of ATP analogue AMPPNP
K71E
-
no ATPase activity
T110I
-
wild-type affinity to co-chaperone Hop
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
drug development
medicine