General Information of the Protein
Protein ID
PT05006
Protein Name
Stimulator of interferon genes protein
Secondarily
Protein Name
Endoplasmic reticulum interferon stimulator
Mediator of IRF3 activation
Transmembrane protein 173
Gene Name
STING1
Secondarily
Gene Name
Eris
Mita
Mpys
Sting
Tmem173
Sequence
MPYSNLHPAIPRPRGHRSKYVALIFLVASLMILWVAKDPPNHTLKYLALHLASHELGLLLKNLCCLAEELCHVQSRYQGSYWKAVRACLGCPIHCMAMILLSSYFYFLQNTADIYLSWMFGLLVLYKSLSMLLGLQSLTPAEVSAVCEEKKLNVAHGLAWSYYIGYLRLILPGLQARIRMFNQLHNNMLSGAGSRRLYILFPLDCGVPDNLSVVDPNIRFRDMLPQQNIDRAGIKNRVYSNSVYEILENGQPAGVCILEYATPLQTLFAMSQDAKAGFSREDRLEQAKLFCRTLEEILEDVPESRNNCRLIVYQEPTDGNSFSLSQEVLRHIRQEEKEEVTMNAPMTSVAPPPSVLSQEPRLLISGMDQPLPLRTDLI
    Show/Hide
Organism
Mus musculus, Mouse
Protein Classification
Unclassified protein
Function
Facilitator of innate immune signaling that acts as a sensor of cytosolic DNA from bacteria and viruses and promotes the production of type I interferon (IFN-alpha and IFN-beta) (PubMed:18818105, PubMed:19433799, PubMed:19776740, PubMed:26229117, PubMed:26669264, PubMed:27324217, PubMed:28529930, PubMed:29973723). Innate immune response is triggered in response to non-CpG double-stranded DNA from viruses and bacteria delivered to the cytoplasm (PubMed:18818105, PubMed:19433799, PubMed:19776740, PubMed:26229117, PubMed:26669264). Acts by binding cyclic dinucleotides: recognizes and binds cyclic di-GMP (c-di-GMP), a second messenger produced by bacteria, and cyclic GMP-AMP (cGAMP), a messenger produced by CGAS in response to DNA virus in the cytosol (PubMed:21947006, PubMed:23722158, PubMed:23258412, PubMed:23519410, PubMed:23910378). Upon binding of c-di-GMP or cGAMP, STING1 oligomerizes, translocates from the endoplasmic reticulum and is phosphorylated by TBK1 on the pLxIS motif, leading to recruitment and subsequent activation of the transcription factor IRF3 to induce expression of type I interferon and exert a potent anti-viral state (PubMed:25636800, PubMed:27324217, PubMed:29973723). In addition to promote the production of type I interferons, plays a direct role in autophagy (PubMed:30568238). Following cGAMP-binding, STING1 buds from the endoplasmic reticulum into COPII vesicles, which then form the endoplasmic reticulum-Golgi intermediate compartment (ERGIC) (By similarity). The ERGIC serves as the membrane source for WIPI2 recruitment and LC3 lipidation, leading to formation of autophagosomes that target cytosolic DNA or DNA viruses for degradation by the lysosome (By similarity). The autophagy- and interferon-inducing activities can be uncoupled and autophagy induction is independent of TBK1 phosphorylation (By similarity). Autophagy is also triggered upon infection by bacteria: following c-di-GMP-binding, which is produced by live Gram-positive bacteria, promotes reticulophagy (PubMed:29056340). Exhibits 2',3' phosphodiester linkage-specific ligand recognition: can bind both 2'-3' linked cGAMP (2'-3'-cGAMP) and 3'-3' linked cGAMP but is preferentially activated by 2'-3' linked cGAMP (PubMed:26300263). The preference for 2'-3'-cGAMP, compared to other linkage isomers is probably due to the ligand itself, whichs adopts an organized free-ligand conformation that resembles the STING1-bound conformation and pays low energy costs in changing into the active conformation (By similarity). May be involved in translocon function, the translocon possibly being able to influence the induction of type I interferons (By similarity). May be involved in transduction of apoptotic signals via its association with the major histocompatibility complex class II (MHC-II) (PubMed:18559423).
    Show/Hide
Uniprot ID
Primary ID:
Q3TBT3

Secondarily ID:
A7YGY9
Q3TAV5
Q3TYP5
Q3TZY8
Q3UJW3
Q8C227
Q8C5Q3
Q8K393
Q9CZY7
    Show/Hide
Ensembl ID
ENSG00000184584
Subcellular Location
Endoplasmic reticulum membrane
Cytoplasm
Perinuclear region
Endoplasmic reticulum-Golgi intermediate compartment membrane
Golgi apparatus membrane
Cytoplasmic vesicle
Autophagosome membrane
Mitochondrion outer membrane
Cell 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: CL000014 , RAW 264.7
Compound ID Compound Name Compound Formula
CP0444686
9-[(1R,6R,8R,9R,10R,15R,17R,18R)-17-(6-aminopurin-9-yl)-9,18-difluoro-3-hydroxy-12-oxo-12-sulfanyl-3-sulfanylidene-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-8-yl]-1H-purin-6-one
   Show/Hide
C20H21F2N9O9P2S2
 1
1
EC50 = 600 nM
   TI
   LI
   LO
   TS
CP0444685
9-[(1S,6R,8R,9R,10R,15R,17R)-17-(6-aminopurin-9-yl)-9-fluoro-12-hydroxy-3-oxo-3-sulfanyl-12-sulfanylidene-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-8-yl]-1H-purin-6-one
   Show/Hide
C20H22FN9O9P2S2
 1
1
EC50 = 2200 nM
   TI
   LI
   LO
   TS
CP0176927
9-[(1S,6R,8R,9R,10S,15R,17R,18R)-17-(6-aminopurin-9-yl)-9,12,18-trihydroxy-3-oxo-3-sulfanyl-12-sulfanylidene-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-8-yl]-1H-purin-6-one
   Show/Hide
C20H23N9O11P2S2
 1
1
EC50 = 4000 nM
   TI
   LI
   LO
   TS
CP0444689
9-[(1S,6R,8R,9R,10R,15R,17R)-17-(6-aminopurin-9-yl)-9-fluoro-3,12-dihydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-8-yl]-1H-purin-6-one
   Show/Hide
C20H22FN9O11P2
 1
1
EC50 = 5000 nM
   TI
   LI
   LO
   TS
CP0534593
9-[(1R,6R,8R,9R,10R,15R,17R,18R)-17-(6-aminopurin-9-yl)-9,18-difluoro-3,12-dihydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-8-yl]-1H-purin-6-one
   Show/Hide
C20H21F2N9O11P2
 1
1
EC50 = 5100 nM
   TI
   LI
   LO
   TS
CP0220338
9-[(1R,6R,8R,9R,10S,15R,17R,18R)-8-(6-aminopurin-9-yl)-3,9,12,18-tetrahydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.2.1.06,10]octadecan-17-yl]-1H-purin-6-one
   Show/Hide
C20H23N9O13P2
 1
1
EC50 = 6100 nM
   TI
   LI
   LO
   TS
CP0176928
9-[(1S,6R,8R,9R,10S,15R,17R,18R)-17-(6-aminopurin-9-yl)-3,9,12,18-tetrahydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-8-yl]-1H-purin-6-one
   Show/Hide
C20H23N9O13P2
 1
1
EC50 = 8400 nM
   TI
   LI
   LO
   TS
CP0532334
9-[(1R,6R,8R,10S,15R,17R,18R)-17-(6-aminopurin-9-yl)-18-fluoro-3,12-dihydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-8-yl]-1H-purin-6-one
   Show/Hide
C20H22FN9O11P2
 1
1
EC50 = 9100 nM
   TI
   LI
   LO
   TS
CP0444687
9-[(1S,6R,8R,10S,15R,17R)-17-(6-aminopurin-9-yl)-3,12-dihydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-8-yl]-1H-purin-6-one
   Show/Hide
C20H23N9O11P2
 1
1
EC50 = 11600 nM
   TI
   LI
   LO
   TS
CP0537187
9-[(1R,6R,8R,9R,10S,15R,17R,18R)-17-(6-aminopurin-9-yl)-3,9,12,18-tetrahydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.2.1.06,10]octadecan-8-yl]-1H-purin-6-one
   Show/Hide
C20H23N9O13P2
 1
1
EC50 = 15900 nM
   TI
   LI
   LO
   TS
CP0444688
9-[(1R,6R,8R,9R,14R,16R,17R,18R)-16-(6-aminopurin-9-yl)-3,11,17,18-tetrahydroxy-3,11-dioxo-2,4,7,10,12,15-hexaoxa-3lambda5,11lambda5-diphosphatricyclo[12.2.1.16,9]octadecan-8-yl]-1H-purin-6-one
   Show/Hide
C20H23N9O13P2
 1
1
EC50 = 17400 nM
   TI
   LI
   LO
   TS
CP0158277
2-amino-9-[(1R,6R,8R,9R,10S,15R,17R,18R)-8-(6-aminopurin-9-yl)-3,9,12,18-tetrahydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.2.1.06,10]octadecan-17-yl]-1H-purin-6-one
   Show/Hide
C20H24N10O13P2
 1
1
EC50 = 18800 nM
   TI
   LI
   LO
   TS
CP0197694
AS-1404
   Show/Hide
C17H14O4
 1
1
EC50 = 35200 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0248635
1-[(E)-4-[5-carbamoyl-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-(3-morpholin-4-ylpropoxy)benzimidazol-1-yl]but-2-enyl]-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-methoxybenzimidazole-5-carboxamide
   Show/Hide
C42H51N13O7
 3
1 EC50 = 54 nM
2 EC50 = 186 nM
3 IC50 = 2.6 nM
CP0176928
9-[(1S,6R,8R,9R,10S,15R,17R,18R)-17-(6-aminopurin-9-yl)-3,9,12,18-tetrahydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.3.0.06,10]octadecan-8-yl]-1H-purin-6-one
   Show/Hide
C20H23N9O13P2
 2
1 EC50 = 180 nM
2 IC50 = 7.7 nM
CP0353766
N-[(5-chloro-7,9-dioxofuro[2,3-f][1,3]benzoxazin-2-yl)methyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
   Show/Hide
C18H10ClN5O5
 2
1 EC50 = 940 nM
2 IC50 = 50 nM
CP0353763
5-chloro-6-hydroxy-2-[(pyrazolo[1,5-a]pyrimidine-3-carbonylamino)methyl]-1-benzofuran-7-carboxylic acid
   Show/Hide
C17H11ClN4O5
 2
1 EC50 = 3300 nM
2 IC50 = 230 nM
CP0357335
N-[[5-chloro-7-(2H-tetrazol-5-yl)-1-benzofuran-2-yl]methyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
   Show/Hide
C17H11ClN8O2
 2
1 EC50 = 9100 nM
2 IC50 = 370 nM
CP0260705
5-chloro-2-[(1,6-naphthyridine-8-carbonylamino)methyl]-1-benzofuran-7-carboxylic acid
   Show/Hide
C19H12ClN3O4
 2
1 EC50 = 14000 nM
2 IC50 = 2300 nM
CP0262000
2-[(pyrazolo[1,5-a]pyrimidine-3-carbonylamino)methyl]-1-benzofuran-7-carboxylic acid
   Show/Hide
C17H12N4O4
 2
1 EC50 = 14000 nM
2 IC50 = 1100 nM
CP0197694
AS-1404
   Show/Hide
C17H14O4
 4
1 EC50 = 15000 nM
2 IC50 = 1200 nM
3 Kd = 130 nM
4 Kd = 710 nM
CP0273542
5-chloro-2-[(pyrazolo[1,5-a]pyrimidine-3-carbonylamino)methyl]-1-benzofuran-7-carboxylic acid
   Show/Hide
C17H11ClN4O4
 2
1 EC50 = 16000 nM
2 IC50 = 1000 nM
CP0345476
3-chloro-5-methyl-2-[(pyrazolo[1,5-a]pyrimidine-3-carbonylamino)methyl]-1-benzofuran-7-carboxylic acid
   Show/Hide
C18H13ClN4O4
 2
1 EC50 = 37000 nM
2 IC50 = 11000 nM
CP0228629
2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-1-[(E)-4-[2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-methoxy-5-(1H-1,2,4-triazol-5-yl)benzimidazol-1-yl]but-2-enyl]-7-(3-morpholin-4-ylpropoxy)benzimidazole-5-carboxamide
   Show/Hide
C43H51N15O6
 1
1 EC50 = 39500 nM
CP0344146
4-(4-fluoro-5,6-dimethoxybenzo[b]thiophen- 2-yl)-4-oxobutanoic acid
   Show/Hide
C14H13FO5S
 2
1 EC50 = 42000 nM
2 IC50 = 7400 nM
CP0260706
2,2,2-trifluoroethyl 5-fluoro-2-[(pyrazolo[1,5-a]pyrimidine-3-carbonylamino)methyl]-1-benzofuran-7-carboxylate
   Show/Hide
C19H12F4N4O4
 2
1 EC50 > 100000 nM
2 IC50 > 100000 nM
CP0261999
methyl 2-[(pyrazolo[1,5-a]pyrimidine-3-carbonylamino)methyl]-1-benzofuran-7-carboxylate
   Show/Hide
C18H14N4O4
 2
1 EC50 > 100000 nM
2 IC50 > 100000 nM
CP0344145
[(2R)-1,1,1-trifluoropropan-2-yl] 5-chloro-2-[(pyrazolo[1,5-a]pyrimidine-3-carbonylamino)methyl]-1-benzofuran-7-carboxylate
   Show/Hide
C20H14ClF3N4O4
 2
1 EC50 > 100000 nM
2 IC50 > 100000 nM
CP0355729
dimethyl 5-(pyrazolo[1,5-a]pyrimidine-3-carbonylamino)benzene-1,3-dicarboxylate
   Show/Hide
C17H14N4O5
 2
1 EC50 > 100000 nM
2 IC50 > 100000 nM
CP0357336
methyl 2-[(3-oxo-1H-pyrrolo[3,4-c]pyridin-2-yl)methyl]-1-benzofuran-7-carboxylate
   Show/Hide
C18H14N2O4
 2
1 EC50 > 100000 nM
2 IC50 > 100000 nM
CP0158277
2-amino-9-[(1R,6R,8R,9R,10S,15R,17R,18R)-8-(6-aminopurin-9-yl)-3,9,12,18-tetrahydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.2.1.06,10]octadecan-17-yl]-1H-purin-6-one
   Show/Hide
C20H24N10O13P2
 1
1 Kd < 0.01 nM