General Information of the Protein
Protein ID
PT06113
Protein Name
DNA damage-inducible transcript 3 protein
Secondarily
Protein Name
C/EBP zeta
C/EBP-homologous protein
C/EBP-homologous protein 10
CCAAT/enhancer-binding protein homologous protein
Growth arrest and DNA damage-inducible protein GADD153
Gene Name
DDIT3
Secondarily
Gene Name
CHOP
CHOP10
GADD153
Sequence
MAAESLPFSFGTLSSWELEAWYEDLQEVLSSDENGGTYVSPPGNEEEESKIFTTLDPASLAWLTEEEPEPAEVTSTSQSPHSPDSSQSSLAQEEEEEDQGRTRKRKQSGHSPARAGKQRMKEKEQENERKVAQLAEENERLKQEIERLTREVEATRRALIDRMVNLHQA
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Organism
Homo sapiens, Human
Protein Classification
Transcription factor
Function
Multifunctional transcription factor in endoplasmic reticulum (ER) stress response (PubMed:15322075, PubMed:15775988, PubMed:19672300). Plays an essential role in the response to a wide variety of cell stresses and induces cell cycle arrest and apoptosis in response to ER stress (PubMed:15322075, PubMed:15775988). Plays a dual role both as an inhibitor of CCAAT/enhancer-binding protein (C/EBP) function and as an activator of other genes (By similarity). Acts as a dominant-negative regulator of C/EBP-induced transcription: dimerizes with members of the C/EBP family, impairs their association with C/EBP binding sites in the promoter regions, and inhibits the expression of C/EBP regulated genes (By similarity). Positively regulates the transcription of TRIB3, IL6, IL8, IL23, TNFRSF10B/DR5, PPP1R15A/GADD34, BBC3/PUMA, BCL2L11/BIM and ERO1L (PubMed:15775988, PubMed:17709599, PubMed:22761832, PubMed:20876114). Negatively regulates; expression of BCL2 and MYOD1, ATF4-dependent transcriptional activation of asparagine synthetase (ASNS), CEBPA-dependent transcriptional activation of hepcidin (HAMP) and CEBPB-mediated expression of peroxisome proliferator-activated receptor gamma (PPARG) (PubMed:18940792, PubMed:19672300, PubMed:20829347). Together with ATF4, mediates ER-mediated cell death by promoting expression of genes involved in cellular amino acid metabolic processes, mRNA translation and the unfolded protein response (UPR) in response to ER stress (By similarity). Inhibits the canonical Wnt signaling pathway by binding to TCF7L2/TCF4, impairing its DNA-binding properties and repressing its transcriptional activity (PubMed:16434966). Plays a regulatory role in the inflammatory response through the induction of caspase-11 (CASP4/CASP11) which induces the activation of caspase-1 (CASP1) and both these caspases increase the activation of pro-IL1B to mature IL1B which is involved in the inflammatory response (By similarity). Acts as a major regulator of postnatal neovascularization through regulation of endothelial nitric oxide synthase (NOS3)-related signaling (By similarity).
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Uniprot ID
Primary ID:
P35638

Secondarily ID:
F8VS99
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Ensembl ID
ENSG00000175197
HGNC ID
HGNC:2726
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: CL000026 , CHO-K1
Compound ID Compound Name Compound Formula
CP0910317
N-(4-(4,4-dimethylpiperidin-1-ylsulfonyl)phenyl)-5-nitrofuran-2-carboxamide
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C18H21N3O6S
 1
1
AC50 = 600 nM
   TI
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CP0956148
N-(4-(4-fluoropiperidin-1-ylsulfonyl)phenyl)-5-nitrofuran-2-carboxamide
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C16H16FN3O6S
 1
1
AC50 = 600 nM
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CP0845997
N-(4-(cyclohexylsulfonyl)phenyl)-5-nitrofuran-2-carboxamide
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C17H18N2O6S
 1
1
AC50 = 700 nM
   TI
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CP0864061
N-(4-(4-tert-butylpiperidin-1-ylsulfonyl)phenyl)-5-nitrofuran-2-carboxamide
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C20H25N3O6S
 1
1
AC50 = 700 nM
   TI
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CP0904259
N-(4-(4-methylpiperidin-1-ylsulfonyl)phenyl)-5-nitrofuran-2-carboxamide
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C17H19N3O6S
 1
1
AC50 = 700 nM
   TI
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CP0910318
N-(4-(3-azaspiro[5.5]undecan-3-ylsulfonyl)phenyl)-5-nitrofuran-2-carboxamide
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C21H25N3O6S
 1
1
AC50 = 700 nM
   TI
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CP0849118
N-(4-(4-chloropiperidin-1-ylsulfonyl)phenyl)-5-nitrofuran-2-carboxamide
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C16H16ClN3O6S
 1
1
AC50 = 800 nM
   TI
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CP0873506
SID85198654
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C15H15N3O6S
 1
1
AC50 = 800 nM
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CP0849119
5-nitro-N-(4-(phenylsulfonyl)phenyl)furan-2-carboxamide
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C17H12N2O6S
 1
1
AC50 = 1100 nM
   TI
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CP0904260
5-nitro-N-(4-(tetrahydro-2H-pyran-4-ylsulfonyl)phenyl)furan-2-carboxamide
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C16H16N2O7S
 1
1
AC50 = 1200 nM
   TI
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CP0910316
5-nitro-N-(4-(piperidin-1-ylsulfonyl)phenyl)furan-2-carboxamide
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C16H17N3O6S
 1
1
AC50 = 1200 nM
   TI
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CP0910315
N-(4-(2,6-dimethylmorpholinosulfonyl)phenyl)-5-nitrofuran-2-carboxamide
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C17H19N3O7S
 1
1
AC50 = 1400 nM
   TI
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CP0176366
MLS000775269
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C15H15N3O7S
 1
1
AC50 = 1900 nM
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CP0846005
N-(4-(4-hydroxypiperidin-1-ylsulfonyl)phenyl)-5-nitrofuran-2-carboxamide
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C16H17N3O7S
 1
1
AC50 = 2000 nM
   TI
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CP0846007
SID56323601
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C15H15N3O6S2
 1
1
AC50 = 13500 nM
   TI
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CP0864877
5-nitro-N-(4-(piperazin-1-ylsulfonyl)phenyl)furan-2-carboxamide
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C15H16N4O6S
 1
1
AC50 = 26400 nM
   TI
   LI
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CP0375241
MLS000062685
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C15H16N2O5S
 1
1
AC50 > 80000 nM
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CP0845998
5-bromo-N-(4-(morpholinosulfonyl)phenyl)furan-2-carboxamide
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C15H15BrN2O5S
 1
1
AC50 > 80000 nM
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CP0846008
SID49671513
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C17H18N2O4S
 1
1
AC50 > 80000 nM
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CP0849121
N-(4-(morpholinosulfonyl)phenyl)thiophene-2-carboxamide
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C15H16N2O4S2
 1
1
AC50 > 80000 nM
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CP0849122
N-(4-(4,4-dimethylpiperidin-1-ylsulfonyl)phenyl)-1-methyl-5-nitro-1H-imidazole-2-carboxamide
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C18H23N5O5S
 1
1
AC50 > 80000 nM
   TI
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CP0891808
N-(4-(4,4-dimethylpiperidin-1-ylsulfonyl)phenyl)-5-(trifluoromethyl)furan-2-carboxamide
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C19H21F3N2O4S
 1
1
AC50 > 80000 nM
   TI
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CP0943812
N-(4-(morpholinosulfonyl)phenyl)-4-nitrobenzamide
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C17H17N3O6S
 1
1
AC50 > 80000 nM
   TI
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CP0950654
5-methyl-N-(4-(morpholinosulfonyl)phenyl)furan-2-carboxamide
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C16H18N2O5S
 1
1
AC50 > 80000 nM
   TI
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CP0957233
N-(4-(4,4-dimethylpiperidin-1-ylsulfonyl)phenyl)-3-nitrobenzamide
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C20H23N3O5S
 1
1
AC50 > 80000 nM
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