General Information of the Protein
Protein ID
PT00938
Protein Name
Protein kinase C eta type
Secondarily
Protein Name
PKC-L
nPKC-eta
Gene Name
PRKCH
Secondarily
Gene Name
PKCL
PRKCL
Sequence
MSSGTMKFNGYLRVRIGEAVGLQPTRWSLRHSLFKKGHQLLDPYLTVSVDQVRVGQTSTKQKTNKPTYNEEFCANVTDGGHLELAVFHETPLGYDHFVANCTLQFQELLRTTGASDTFEGWVDLEPEGKVFVVITLTGSFTEATLQRDRIFKHFTRKRQRAMRRRVHQINGHKFMATYLRQPTYCSHCREFIWGVFGKQGYQCQVCTCVVHKRCHHLIVTACTCQNNINKVDSKIAEQRFGINIPHKFSIHNYKVPTFCDHCGSLLWGIMRQGLQCKICKMNVHIRCQANVAPNCGVNAVELAKTLAGMGLQPGNISPTSKLVSRSTLRRQGKESSKEGNGIGVNSSNRLGIDNFEFIRVLGKGSFGKVMLARVKETGDLYAVKVLKKDVILQDDDVECTMTEKRILSLARNHPFLTQLFCCFQTPDRLFFVMEFVNGGDLMFHIQKSRRFDEARARFYAAEIISALMFLHDKGIIYRDLKLDNVLLDHEGHCKLADFGMCKEGICNGVTTATFCGTPDYIAPEILQEMLYGPAVDWWAMGVLLYEMLCGHAPFEAENEDDLFEAILNDEVVYPTWLHEDATGILKSFMTKNPTMRLGSLTQGGEHAILRHPFFKEIDWAQLNHRQIEPPFRPRIKSREDVSNFDPDFIKEEPVLTPIDEGHLPMINQDEFRNFSYVSPELQP
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
AGC protein kinase group
>
AGC protein kinase PKC family
>
AGC protein kinase PKC eta subfamily
Function
Calcium-independent, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that is involved in the regulation of cell differentiation in keratinocytes and pre-B cell receptor, mediates regulation of epithelial tight junction integrity and foam cell formation, and is required for glioblastoma proliferation and apoptosis prevention in MCF-7 cells. In keratinocytes, binds and activates the tyrosine kinase FYN, which in turn blocks epidermal growth factor receptor (EGFR) signaling and leads to keratinocyte growth arrest and differentiation. Associates with the cyclin CCNE1-CDK2-CDKN1B complex and inhibits CDK2 kinase activity, leading to RB1 dephosphorylation and thereby G1 arrest in keratinocytes. In association with RALA activates actin depolymerization, which is necessary for keratinocyte differentiation. In the pre-B cell receptor signaling, functions downstream of BLNK by up-regulating IRF4, which in turn activates L chain gene rearrangement. Regulates epithelial tight junctions (TJs) by phosphorylating occludin (OCLN) on threonine residues, which is necessary for the assembly and maintenance of TJs. In association with PLD2 and via TLR4 signaling, is involved in lipopolysaccharide (LPS)-induced RGS2 down-regulation and foam cell formation. Upon PMA stimulation, mediates glioblastoma cell proliferation by activating the mTOR pathway, the PI3K/AKT pathway and the ERK1-dependent phosphorylation of ELK1. Involved in the protection of glioblastoma cells from irradiation-induced apoptosis by preventing caspase-9 activation. In camptothecin-treated MCF-7 cells, regulates NF-kappa-B upstream signaling by activating IKBKB, and confers protection against DNA damage-induced apoptosis. Promotes oncogenic functions of ATF2 in the nucleus while blocking its apoptotic function at mitochondria. Phosphorylates ATF2 which promotes its nuclear retention and transcriptional activity and negatively regulates its mitochondrial localization.
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Uniprot ID
Primary ID:
P24723

Secondarily ID:
B4DJN5
Q16246
Q8NE03
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Ensembl ID
ENSG00000027075
HGNC ID
HGNC:9403
Subcellular Location
Cytoplasm
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000013 , Sf9
Compound ID Compound Name Compound Formula
CP0040070
2-{[2,6-dihydroxy-4-({[(1R,2R)-2-[(4-hydroxybenzene)amido]cyclopentyl]oxy}carbonyl)phenyl]carbonyl}-3-hydroxybenzoic acid
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C27H23NO10
 1
1
IC50 = 0.6 nM
   TI
   LI
   LO
   TS
CP0040333
2-{[2,6-dihydroxy-4-({[(3R,4R)-4-[(4-hydroxybenzene)amido]pyrrolidin-3-yl]oxy}carbonyl)phenyl]carbonyl}-3-hydroxybenzoic acid
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C26H22N2O10
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0398629
(3R,4R)-4-[(4-hydroxybenzene)amido]pyrrolidin-3-yl 4-{[2-({[(2,2-dimethylpropanoyl)oxy]methoxy}carbonyl)-6-hydroxyphenyl]carbonyl}-3,5-dihydroxybenzoate
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C32H32N2O12
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0372635
(3R,4R)-4-[(4-hydroxybenzene)amido]pyrrolidin-3-yl 4-[(2-{[(acetyloxy)methoxy]carbonyl}-6-hydroxyphenyl)carbonyl]-3,5-dihydroxybenzoate
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C29H26N2O12
 1
1
IC50 = 14 nM
   TI
   LI
   LO
   TS
CP0495469
(3R,4R)-4-[(4-hydroxybenzene)amido]pyrrolidin-3-yl 3,5-dihydroxy-4-{[2-hydroxy-6-(methoxycarbonyl)phenyl]carbonyl}benzoate
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C27H24N2O10
 1
1
IC50 = 16 nM
   TI
   LI
   LO
   TS
CP0405218
(3R,4R)-4-[(4-hydroxybenzene)amido]pyrrolidin-3-yl 4-{[2-(ethoxycarbonyl)-6-hydroxyphenyl]carbonyl}-3,5-dihydroxybenzoate
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C28H26N2O10
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0038373
2-{[2,6-dihydroxy-4-({[(3R,4R)-3-[(4-hydroxybenzene)amido]azepan-4-yl]oxy}carbonyl)phenyl]carbonyl}-3-hydroxybenzoic acid
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C28H26N2O10
 1
1
IC50 = 22 nM
   TI
   LI
   LO
   TS
CP0405508
(3R,4R)-4-[(4-hydroxybenzene)amido]pyrrolidin-3-yl 4-{[2-(butoxycarbonyl)-6-hydroxyphenyl]carbonyl}-3,5-dihydroxybenzoate
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C30H30N2O10
 1
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
CP0405497
(3R,4R)-4-[(4-hydroxybenzene)amido]pyrrolidin-3-yl 4-({2-[(cyclohexylmethoxy)carbonyl]-6-hydroxyphenyl}carbonyl)-3,5-dihydroxybenzoate
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C33H34N2O10
 1
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
CP0419325
(3R,4R)-4-[(4-hydroxybenzene)amido]pyrrolidin-3-yl 3,5-dihydroxy-4-({2-hydroxy-6-[(2-methylpropoxy)carbonyl]phenyl}carbonyl)benzoate
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C30H30N2O10
 1
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
CP0391277
(1R,2R)-2-[(4-hydroxybenzene)amido]cyclopentyl 4-{[2-(ethoxycarbonyl)-6-hydroxyphenyl]carbonyl}-3,5-dihydroxybenzoate
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C29H27NO10
 1
1
IC50 = 52 nM
   TI
   LI
   LO
   TS
CP0487436
(1R,2R)-2-[(4-hydroxybenzene)amido]cyclopentyl 3,5-dihydroxy-4-({2-hydroxy-6-[(propan-2-yloxy)carbonyl]phenyl}carbonyl)benzoate
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C30H29NO10
 1
1
IC50 = 260 nM
   TI
   LI
   LO
   TS
CP0382649
3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]-methylamino]ethoxy]ethoxy]ethoxy]ethyl]propanamide
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C50H56BF2N7O7
 1
1
Kd = 37 nM
   TI
   LI
   LO
   TS
CP0382724
3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]amino]ethoxy]ethoxy]ethoxy]ethyl]propanamide
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C49H54BF2N7O7
 1
1
Kd = 61 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0040070
2-{[2,6-dihydroxy-4-({[(1R,2R)-2-[(4-hydroxybenzene)amido]cyclopentyl]oxy}carbonyl)phenyl]carbonyl}-3-hydroxybenzoic acid
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C27H23NO10
 2
1 IC50 = 0.6 nM
2 IC50 = 1 nM
CP0038373
2-{[2,6-dihydroxy-4-({[(3R,4R)-3-[(4-hydroxybenzene)amido]azepan-4-yl]oxy}carbonyl)phenyl]carbonyl}-3-hydroxybenzoic acid
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C28H26N2O10
 4
1 IC50 = 3 nM
2 IC50 = 4 nM
3 IC50 = 20 nM
4 IC50 = 22 nM
CP0040333
2-{[2,6-dihydroxy-4-({[(3R,4R)-4-[(4-hydroxybenzene)amido]pyrrolidin-3-yl]oxy}carbonyl)phenyl]carbonyl}-3-hydroxybenzoic acid
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C26H22N2O10
 1
1 IC50 = 4 nM
Clinical Information about the Protein
Target 1 ( PKC-eta messenger RNA (PRKCH mRNA) )
Target Type Literature-reported Target
Disease 1 Target-related Disease  1
1 Human immunodeficiency virus infection [ICD-11: 1C62]
Investigative Drug(s) 1 Investigative Drug  1
1 PROSTRATIN Investigative
Human immunodeficiency virus infection