General Information of the Protein
Protein ID
PT02288
Protein Name
Signal transducer and activator of transcription 3
Secondarily
Protein Name
Acute-phase response factor
Gene Name
STAT3
Secondarily
Gene Name
Aprf
Sequence
MAQWNQLQQLDTRYLEQLHQLYSDSFPMELRQFLAPWIESQDWAYAASKESHATLVFHNLLGEIDQQYSRFLQESNVLYQHNLRRIKQFLQSRYLEKPMEIARIVARCLWEESRLLQTAATAAQQGGQANHPTAAVVTEKQQMLEQHLQDVRKRVQDLEQKMKVVENLQDDFDFNYKTLKSQGDMQDLNGNNQSVTRQKMQQLEQMLTALDQMRRSIVSELAGLLSAMEYVQKTLTDEELADWKRRQQIACIGGPPNICLDRLENWITSLAESQLQTRQQIKKLEELQQKVSYKGDPIVQHRPMLEERIVELFRNLMKSAFVVERQPCMPMHPDRPLVIKTGVQFTTKVRLLVKFPELNYQLKIKVCIDKDSGDVAALRGSRKFNILGTNTKVMNMEESNNGSLSAEFKHLTLREQRCGNGGRANCDASLIVTEELHLITFETEVYHQGLKIDLETHSLPVVVISNICQMPNAWASILWYNMLTNNPKNVNFFTKPPIGTWDQVAEVLSWQFSSTTKRGLSIEQLTTLAEKLLGPGVNYSGCQITWAKFCKENMAGKGFSFWVWLDNIIDLVKKYILALWNEGYIMGFISKERERAILSTKPPGTFLLRFSESSKEGGVTFTWVEKDISGKTQIQSVEPYTKQQLNNMSFAEIIMGYKIMDATNILVSPLVYLYPDIPKEEAFGKYCRPESQEHPEADPGSAAPYLKTKFICVTPTTCSNTIDLPMSPRTLDSLMQFGNNGEGAEPSAGGQFESLTFDMDLTSECATSPM
    Show/Hide
Organism
Mus musculus, Mouse
Protein Classification
Transcription factor
Function
Signal transducer and transcription activator that mediates cellular responses to interleukins, KITLG/SCF, LEP and other growth factors (By similarity). Once activated, recruits coactivators, such as NCOA1 or MED1, to the promoter region of the target gene (By similarity). May mediate cellular responses to activated FGFR1, FGFR2, FGFR3 and FGFR4 (By similarity). Upon activation of IL6ST/gp130 signaling by interleukin-6 (IL6), binds to the IL6-responsive elements identified in the promoters of various acute-phase protein genes (By similarity). Activated by IL31 through IL31RA (By similarity). Acts as a regulator of inflammatory response by regulating differentiation of naive CD4(+) T-cells into T-helper Th17 or regulatory T-cells (Treg): deacetylation and oxidation of lysine residues by LOXL3, leads to disrupt STAT3 dimerization and inhibit its transcription activity (By similarity). Involved in cell cycle regulation by inducing the expression of key genes for the progression from G1 to S phase, such as CCND1 (By similarity). Mediates the effects of LEP on melanocortin production, body energy homeostasis and lactation (PubMed:12594516). May play an apoptotic role by transctivating BIRC5 expression under LEP activation (PubMed:16825198). Cytoplasmic STAT3 represses macroautophagy by inhibiting EIF2AK2/PKR activity (By similarity). Plays a crucial role in basal beta cell functions, such as regulation of insulin secretion (PubMed:20215569). Plays an important role in host defense in methicillin-resistant S.aureus lung infection by regulating the expression of the antimicrobial lectin REG3G (PubMed:23401489).
    Show/Hide
Uniprot ID
Primary ID:
P42227

Secondarily ID:
A2A5D1
B7ZC17
    Show/Hide
Ensembl ID
ENSG00000168610
Subcellular Location
Cytoplasm
Nucleus
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: CL000035 , NIH 3T3
Compound ID Compound Name Compound Formula
CP0310497
(S)-3-(((S)-1-((5-(Benzylcarbamoyl)-4'-carbamoyl-[1,1'-biphenyl]-3-yl)amino)-4-methyl-1-oxopentan-2-yl)amino)-2-(4-cyanobenzamido)-3-oxopropyl)phenyl dihydrogen phosphate
   Show/Hide
C44H43N6O9P
 1
1
IC50 = 5000 nM
   TI
   LI
   LO
   TS
CP0511445
4-((S)-3-(((S)-1-((6-(Benzylcarbamoyl)-4'-cyano-[1,1'-biphenyl]-3-yl)amino)-4-methyl-1-oxopentan-2-yl)amino)-2-(4-cyanobenzamido)-3-oxopropyl)phenyl dihydrogen phosphate
   Show/Hide
C44H41N6O8P
 1
1
IC50 = 33000 nM
   TI
   LI
   LO
   TS
CP0437125
methyl 3-[2-(benzylcarbamoyl)-5-[[(2S)-2-[[(2S)-2-[(4-cyanobenzoyl)amino]-3-(4-phosphonooxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]phenyl]benzoate
   Show/Hide
C45H44N5O10P
 1
1
IC50 = 40000 nM
   TI
   LI
   LO
   TS
CP0425628
4-((S)-3-(((S)-1-((5-(Benzylcarbamoyl)-4'-cyano-[1,1'-biphenyl]-3-yl)amino)-4-methyl-1-oxopentan-2-yl)amino)-2-(4-cyanobenzamido)-3-oxopropyl)phenyl dihydrogen phosphate
   Show/Hide
C44H41N6O8P
 1
1
IC50 = 60000 nM
   TI
   LI
   LO
   TS
CP0487305
4-((S)-3-(((S)-1-((6-(Benzylcarbamoyl)-3'-carbamoyl-[1,1'-biphenyl]-3-yl)amino)-4-methyl-1-oxopentan-2-yl)-amino)-2-(4-cyanobenzamido)-3-oxopropyl)phenyl dihydrogen phosphate
   Show/Hide
C44H43N6O9P
 1
1
IC50 = 62000 nM
   TI
   LI
   LO
   TS
CP0516585
4-((S)-3-(((S)-1-((6-(Benzylcarbamoyl)-3'-cyano-[1,1'-biphenyl]-3-yl)amino)-4-methyl-1-oxopentan-2-yl)amino)-2-(4-cyanobenzamido)-3-oxopropyl)phenyl dihydrogen phosphate
   Show/Hide
C44H41N6O8P
 1
1
IC50 = 64000 nM
   TI
   LI
   LO
   TS
CP0511444
methyl 3-[3-(benzylcarbamoyl)-5-[[(2S)-2-[[(2S)-2-[(4-cyanobenzoyl)amino]-3-(4-phosphonooxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]phenyl]benzoate
   Show/Hide
C45H44N5O10P
 1
1
IC50 = 66000 nM
   TI
   LI
   LO
   TS
CP0225105
4-((S)-3-((S)-1-(6-(Benzylcarbamoyl)-4'-carbamoylbiphenyl-3-ylamino)-4-methyl-1-oxopentan-2-ylamino)-2-(4-cyanobenzamido)-3-oxopropyl)phenyl dihydrogen phosphate
   Show/Hide
C44H43N6O9P
 1
1
IC50 = 73100 nM
   TI
   LI
   LO
   TS
CP0426562
4-((S)-3-(((S)-1-((5-(Benzylcarbamoyl)-3'-cyano-[1,1'-biphenyl]-3-yl)amino)-4-methyl-1-oxopentan-2-yl)amino)-2-(4-cyanobenzamido)-3-oxopropyl)phenyl dihydrogen phosphate
   Show/Hide
C44H41N6O8P
 1
1
IC50 = 92000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0143063
4-[(4-cyclohexylphenyl)methyl-[2-[methyl-(4-methylphenyl)sulfonylamino]acetyl]amino]-2-hydroxybenzoic acid
   Show/Hide
C30H34N2O6S
 2
1 IC50 = 35000 nM
2 Ki = 15000 nM
CP0310497
(S)-3-(((S)-1-((5-(Benzylcarbamoyl)-4'-carbamoyl-[1,1'-biphenyl]-3-yl)amino)-4-methyl-1-oxopentan-2-yl)amino)-2-(4-cyanobenzamido)-3-oxopropyl)phenyl dihydrogen phosphate
   Show/Hide
C44H43N6O9P
 1
1 Kd = 205 nM
CP0225105
4-((S)-3-((S)-1-(6-(Benzylcarbamoyl)-4'-carbamoylbiphenyl-3-ylamino)-4-methyl-1-oxopentan-2-ylamino)-2-(4-cyanobenzamido)-3-oxopropyl)phenyl dihydrogen phosphate
   Show/Hide
C44H43N6O9P
 1
1 Kd = 900 nM
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT01503 Signal transducer and activator of transcription 3 Homo sapiens, Human