General Information of the Protein
Protein ID
PT01503
Protein Name
Signal transducer and activator of transcription 3
Secondarily
Protein Name
Acute-phase response factor
Gene Name
STAT3
Secondarily
Gene Name
APRF
Sequence
MAQWNQLQQLDTRYLEQLHQLYSDSFPMELRQFLAPWIESQDWAYAASKESHATLVFHNLLGEIDQQYSRFLQESNVLYQHNLRRIKQFLQSRYLEKPMEIARIVARCLWEESRLLQTAATAAQQGGQANHPTAAVVTEKQQMLEQHLQDVRKRVQDLEQKMKVVENLQDDFDFNYKTLKSQGDMQDLNGNNQSVTRQKMQQLEQMLTALDQMRRSIVSELAGLLSAMEYVQKTLTDEELADWKRRQQIACIGGPPNICLDRLENWITSLAESQLQTRQQIKKLEELQQKVSYKGDPIVQHRPMLEERIVELFRNLMKSAFVVERQPCMPMHPDRPLVIKTGVQFTTKVRLLVKFPELNYQLKIKVCIDKDSGDVAALRGSRKFNILGTNTKVMNMEESNNGSLSAEFKHLTLREQRCGNGGRANCDASLIVTEELHLITFETEVYHQGLKIDLETHSLPVVVISNICQMPNAWASILWYNMLTNNPKNVNFFTKPPIGTWDQVAEVLSWQFSSTTKRGLSIEQLTTLAEKLLGPGVNYSGCQITWAKFCKENMAGKGFSFWVWLDNIIDLVKKYILALWNEGYIMGFISKERERAILSTKPPGTFLLRFSESSKEGGVTFTWVEKDISGKTQIQSVEPYTKQQLNNMSFAEIIMGYKIMDATNILVSPLVYLYPDIPKEEAFGKYCRPESQEHPEADPGSAAPYLKTKFICVTPTTCSNTIDLPMSPRTLDSLMQFGNNGEGAEPSAGGQFESLTFDMELTSECATSPM
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Organism
Homo sapiens, Human
Protein Classification
Transcription factor
Function
Signal transducer and transcription activator that mediates cellular responses to interleukins, KITLG/SCF, LEP and other growth factors (PubMed:10688651, PubMed:12359225, PubMed:12873986, PubMed:15194700, PubMed:17344214, PubMed:18242580, PubMed:22306293, PubMed:23084476, PubMed:32929201). Once activated, recruits coactivators, such as NCOA1 or MED1, to the promoter region of the target gene (PubMed:17344214, PubMed:32929201). May mediate cellular responses to activated FGFR1, FGFR2, FGFR3 and FGFR4 (PubMed:12873986). 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 (PubMed:12359225). Activated by IL31 through IL31RA (PubMed:15194700). 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 (PubMed:28065600). Involved in cell cycle regulation by inducing the expression of key genes for the progression from G1 to S phase, such as CCND1 (PubMed:17344214). Mediates the effects of LEP on melanocortin production, body energy homeostasis and lactation (By similarity). May play an apoptotic role by transctivating BIRC5 expression under LEP activation (PubMed:18242580). Cytoplasmic STAT3 represses macroautophagy by inhibiting EIF2AK2/PKR activity (PubMed:23084476). Plays a crucial role in basal beta cell functions, such as regulation of insulin secretion (By similarity).
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Uniprot ID
Primary ID:
P40763

Secondarily ID:
A8K7B8
K7ENL3
O14916
Q9BW54
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Ensembl ID
ENSG00000168610
HGNC ID
HGNC:11364
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: CL000068 , A-549
Compound ID Compound Name Compound Formula
CP0382251
N-[2-(4-cyano-3-fluorophenyl)phenyl]-4-methoxybenzenesulfonamide
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C20H15FN2O3S
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0494804
N-[2-(4-cyanophenyl)phenyl]-N-(4-methoxyphenyl)sulfonylacetamide
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C22H18N2O4S
 1
1
IC50 = 320 nM
   TI
   LI
   LO
   TS
CP0557022
N-[2-(4-cyanophenyl)phenyl]-4-methoxybenzenesulfonamide
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C20H16N2O3S
 1
1
IC50 = 440 nM
   TI
   LI
   LO
   TS
CP0428553
N-[2-(3,4-difluorophenyl)phenyl]-4-methoxybenzenesulfonamide
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C19H15F2NO3S
 1
1
IC50 = 2750 nM
   TI
   LI
   LO
   TS
CP0534582
N-[2-(4-fluorophenyl)phenyl]-4-methoxybenzenesulfonamide
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C19H16FNO3S
 1
1
IC50 = 4020 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0176150
6-nitro-1-benzothiophene 1,1-dioxide
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C8H5NO4S
 2
1 IC50 = 5100 nM
2 Kd = 1528 nM
CP0091827
4-[[3-(carboxymethylsulfanyl)-4-hydroxynaphthalen-1-yl]sulfamoyl]benzoic acid
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C19H15NO7S2
 1
1 IC50 = 20000 nM
CP0265749
4-[5-[(Z)-(3-ethyl-4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene)methyl]furan-2-yl]benzoic acid
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C17H13NO4S2
 1
1 IC50 = 30000 nM
CP0176149
2-methoxy-N-[2-[2-[[(1S)-1-(4-methoxyphenyl)ethyl]amino]-2-oxoethyl]sulfanyl-1,3-benzothiazol-6-yl]-3-methyl-4-pentan-2-yloxybenzamide
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C32H37N3O5S2
 1
1 Kd = 53.04 nM
CP0129941
2-methoxy-3-methyl-N-[2-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]sulfanyl-1,3-benzothiazol-6-yl]-4-pentan-2-yloxybenzamide
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C31H35N3O4S2
 1
1 Kd = 62.61 nM
CP0273749
[4-[[4-(2,2,2-trifluoroethoxy)phenyl]methyl]piperazin-1-yl]-[4-[5-[4-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-3-yl]phenyl]methanone
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C29H24F6N4O3
 2
1 Kd = 76.4 nM
2 Kd = 114 nM
Clinical Information about the Protein
Target 1 ( Signal transducer and activator of transcription 3 (STAT3) )
Target Type Successful Target
Disease 4 Target-related Diseases  4
1 Psoriasis vulgaris [ICD-11: EA90]
2 Pancreatic cancer [ICD-11: 2C10]
3 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
4 Recurrent glioblastoma [ICD-11: 2A00.00]
Approved Drug(s) 1 Approved Drug  1
1 Acitretin Approved
Psoriasis vulgaris
Clinical Trial Drug(s) 3 Clinical Trial Drugs  3
1 Napabucasin Phase 3
Pancreatic cancer
2 NT219 Phase 1/2
Solid tumour/cancer
3 WP-1066 Phase 1/2
Recurrent glioblastoma
Target 2 ( STAT3 messenger RNA (STAT3 mRNA) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 C188-9 Phase 1
Solid tumour/cancer
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT02288 Signal transducer and activator of transcription 3 Mus musculus, Mouse