General Information of the Protein
Protein ID
PT01022
Protein Name
RAC-gamma serine/threonine-protein kinase
Secondarily
Protein Name
Protein kinase Akt-3
Protein kinase B gamma
RAC-PK-gamma
STK-2
Gene Name
AKT3
Secondarily
Gene Name
PKBG
Sequence
MSDVTIVKEGWVQKRGEYIKNWRPRYFLLKTDGSFIGYKEKPQDVDLPYPLNNFSVAKCQLMKTERPKPNTFIIRCLQWTTVIERTFHVDTPEEREEWTEAIQAVADRLQRQEEERMNCSPTSQIDNIGEEEMDASTTHHKRKTMNDFDYLKLLGKGTFGKVILVREKASGKYYAMKILKKEVIIAKDEVAHTLTESRVLKNTRHPFLTSLKYSFQTKDRLCFVMEYVNGGELFFHLSRERVFSEDRTRFYGAEIVSALDYLHSGKIVYRDLKLENLMLDKDGHIKITDFGLCKEGITDAATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHEKLFELILMEDIKFPRTLSSDAKSLLSGLLIKDPNKRLGGGPDDAKEIMRHSFFSGVNWQDVYDKKLVPPFKPQVTSETDTRYFDEEFTAQTITITPPEKYDEDGMDCMDNERRPHFPQFSYSASGRE
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
AGC protein kinase group
>
AGC protein kinase AKT family
Function
AKT3 is one of 3 closely related serine/threonine-protein kinases (AKT1, AKT2 and AKT3) called the AKT kinase, and which regulate many processes including metabolism, proliferation, cell survival, growth and angiogenesis. This is mediated through serine and/or threonine phosphorylation of a range of downstream substrates. Over 100 substrate candidates have been reported so far, but for most of them, no isoform specificity has been reported. AKT3 is the least studied AKT isoform. It plays an important role in brain development and is crucial for the viability of malignant glioma cells. AKT3 isoform may also be the key molecule in up-regulation and down-regulation of MMP13 via IL13. Required for the coordination of mitochondrial biogenesis with growth factor-induced increases in cellular energy demands. Down-regulation by RNA interference reduces the expression of the phosphorylated form of BAD, resulting in the induction of caspase-dependent apoptosis.
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Uniprot ID
Primary ID:
Q9Y243

Secondarily ID:
Q0VAA6
Q5VTI1
Q5VTI2
Q96QV3
Q9UFP5
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Ensembl ID
ENSG00000117020
HGNC ID
HGNC:393
Subcellular Location
Nucleus
Cytoplasm
Membrane
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: CL000157 , NCI-H1975
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0546215
 Compound Info 
N-[3-[2-[4-[4-[12-[[2-(1-adamantyl)acetyl]amino]dodecyl]piperazin-1-yl]-2-methoxyanilino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8-yl]phenyl]cyclopropanecarboxamide
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C53H72N8O4
  1
1
EC50 = 13 nM
 Bioactivity Info 
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CP0551613
 Compound Info 
N-[3-[2-[4-[4-[12-[[2-(1-adamantyl)acetyl]amino]dodecyl]piperazin-1-yl]-2-methoxyanilino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8-yl]phenyl]-2-methylpropanamide
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C53H74N8O4
  1
1
EC50 = 33 nM
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CP0572863
 Compound Info 
N-[3-[2-[4-[4-[12-[[2-(1-adamantyl)acetyl]amino]dodecyl]piperazin-1-yl]-2-methoxyanilino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8-yl]phenyl]propanamide
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C52H72N8O4
  1
1
EC50 = 34 nM
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CP0546212
 Compound Info 
N-[3-[2-[4-[4-[12-[[2-(1-adamantyl)acetyl]amino]dodecyl]piperazin-1-yl]-2-methoxyanilino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8-yl]phenyl]prop-2-enamide
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C52H70N8O4
  1
1
EC50 = 52 nM
 Bioactivity Info 
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CP0573911
 Compound Info 
N-[3-[2-[4-[4-[8-[[2-(1-adamantyl)acetyl]amino]octyl]piperazin-1-yl]-2-methoxyanilino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8-yl]phenyl]prop-2-enamide
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C48H62N8O4
  1
1
EC50 = 52 nM
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CP0544748
 Compound Info 
N-[3-[2-[4-[4-[12-[[2-(1-adamantyl)acetyl]amino]dodecyl]piperazin-1-yl]-2-methoxyanilino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8-yl]phenyl]-2,2-dimethylpropanamide
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C54H76N8O4
  1
1
EC50 = 57 nM
 Bioactivity Info 
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CP0551616
 Compound Info 
N-[12-[4-[4-[[8-(3-acetamidophenyl)-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl]amino]-3-methoxyphenyl]piperazin-1-yl]dodecyl]-2-(1-adamantyl)acetamide
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C51H70N8O4
  1
1
EC50 = 67 nM
 Bioactivity Info 
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CP0562844
 Compound Info 
2-(1-adamantyl)-N-[12-[4-[4-[[8-(3-aminophenyl)-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl]amino]-3-methoxyphenyl]piperazin-1-yl]dodecyl]acetamide
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C49H68N8O3
  1
1
EC50 = 102 nM
 Bioactivity Info 
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CP0546214
 Compound Info 
N-[3-[2-[4-[4-[14-[[2-(1-adamantyl)acetyl]amino]tetradecyl]piperazin-1-yl]-2-methoxyanilino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8-yl]phenyl]prop-2-enamide
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C54H74N8O4
  1
1
EC50 = 120 nM
 Bioactivity Info 
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CP0576645
 Compound Info 
N-[3-[2-[4-[4-[10-[[2-(1-adamantyl)acetyl]amino]decyl]piperazin-1-yl]-2-methoxyanilino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8-yl]phenyl]prop-2-enamide
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C50H66N8O4
  1
1
EC50 = 402 nM
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CP0551614
 Compound Info 
N-[3-[2-[4-[4-[2-[2-[2-[[2-(1-adamantyl)acetyl]amino]ethoxy]ethoxy]ethyl]piperazin-1-yl]-2-methoxyanilino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8-yl]phenyl]prop-2-enamide
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C46H58N8O6
  1
1
EC50 = 564 nM
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CP0546213
 Compound Info 
N-[3-[2-[4-[4-[6-[[2-(1-adamantyl)acetyl]amino]hexyl]piperazin-1-yl]-2-methoxyanilino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8-yl]phenyl]prop-2-enamide
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C46H58N8O4
  1
1
EC50 = 1000 nM
 Bioactivity Info 
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CP0203178
 Compound Info 
N-[3-[2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8-yl]phenyl]prop-2-enamide
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C29H31N7O3
  1
1
EC50 > 1000 nM
 Bioactivity Info 
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CP0551615
 Compound Info 
N-[3-[2-[4-[4-[12-[[2-(1-adamantyl)acetyl]amino]dodecanoyl]piperazin-1-yl]-2-methoxyanilino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8-yl]phenyl]prop-2-enamide
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C52H68N8O5
  1
1
EC50 > 1000 nM
 Bioactivity Info 
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CP0575210
 Compound Info 
N-[4-[2-[4-[4-[12-[[2-(1-adamantyl)acetyl]amino]dodecyl]piperazin-1-yl]-2-methoxyanilino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8-yl]phenyl]prop-2-enamide
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C52H70N8O4
  1
1
EC50 > 1000 nM
 Bioactivity Info 
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CP0576646
 Compound Info 
N-[4-[2-[4-[4-[12-[[2-(1-adamantyl)acetyl]amino]dodecyl]piperazin-1-yl]-2-methoxyanilino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8-yl]phenyl]cyclopropanecarboxamide
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C53H72N8O4
  1
1
EC50 > 1000 nM
 Bioactivity Info 
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Cell Line ID: CL000012 , Sf21
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0088096
 Compound Info 
(2S)-2-(4-chlorophenyl)-1-[4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]piperazin-1-yl]-3-(propan-2-ylamino)propan-1-one
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C24H32ClN5O2
  1
1 IC50 = 26 nM
Clinical Information about the Protein
Target 1 ( RAC-gamma serine/threonine-protein kinase (AKT3) )
Target Type Successful Target
Disease 7 Target-related Diseases  7
1 Breast cancer [ICD-11: 2C60-2C65]
2 Lymphoma [ICD-11: 2A80-2A86]
3 Rectal adenocarcinoma [ICD-11: 2B92]
4 Proteus syndrome [ICD-11: LD2C]
5 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
6 Haematological malignancy [ICD-11: 2B33.Y]
7 Acute myeloid leukaemia [ICD-11: 2A60]
Approved Drug(s) 1 Approved Drug  1
1 Capivasertib
 Drug Info 
Approved
Breast cancer
Clinical Trial Drug(s) 9 Clinical Trial Drugs  9
1 GSK2141795
 Drug Info 
Phase 2
Lymphoma
2 MK-2206
 Drug Info 
Phase 2
Rectal adenocarcinoma
3 ARQ 092
 Drug Info 
Phase 2
Proteus syndrome
4 BAY1125976
 Drug Info 
Phase 1
Solid tumour/cancer
5 GSK690693
 Drug Info 
Phase 1
Haematological malignancy
6 M2698
 Drug Info 
Phase 1
Solid tumour/cancer
7 SR13668
 Drug Info 
Phase 1
Solid tumour/cancer
8 TCN-P
 Drug Info 
Phase 1
Acute myeloid leukaemia
9 XL418
 Drug Info 
Phase 1
Solid tumour/cancer
Target 2 ( AKT3 messenger RNA (AKT3 mRNA) )
Target Type Literature-reported Target