General Information of the Protein
Protein ID
PT03579
Protein Name
Transcription intermediary factor 1-alpha
Secondarily
Protein Name
E3 ubiquitin-protein ligase TRIM24
RING finger protein 82
RING-type E3 ubiquitin transferase TIF1-alpha
Tripartite motif-containing protein 24
Gene Name
TRIM24
Secondarily
Gene Name
RNF82
TIF1
TIF1A
Sequence
MEVAVEKAVAAAAAASAAASGGPSAAPSGENEAESRQGPDSERGGEAARLNLLDTCAVCHQNIQSRAPKLLPCLHSFCQRCLPAPQRYLMLPAPMLGSAETPPPVPAPGSPVSGSSPFATQVGVIRCPVCSQECAERHIIDNFFVKDTTEVPSSTVEKSNQVCTSCEDNAEANGFCVECVEWLCKTCIRAHQRVKFTKDHTVRQKEEVSPEAVGVTSQRPVFCPFHKKEQLKLYCETCDKLTCRDCQLLEHKEHRYQFIEEAFQNQKVIIDTLITKLMEKTKYIKFTGNQIQNRIIEVNQNQKQVEQDIKVAIFTLMVEINKKGKALLHQLESLAKDHRMKLMQQQQEVAGLSKQLEHVMHFSKWAVSSGSSTALLYSKRLITYRLRHLLRARCDASPVTNNTIQFHCDPSFWAQNIINLGSLVIEDKESQPQMPKQNPVVEQNSQPPSGLSSNQLSKFPTQISLAQLRLQHMQQQVMAQRQQVQRRPAPVGLPNPRMQGPIQQPSISHQQPPPRLINFQNHSPKPNGPVLPPHPQQLRYPPNQNIPRQAIKPNPLQMAFLAQQAIKQWQISSGQGTPSTTNSTSSTPSSPTITSAAGYDGKAFGSPMIDLSSPVGGSYNLPSLPDIDCSSTIMLDNIVRKDTNIDHGQPRPPSNRTVQSPNSSVPSPGLAGPVTMTSVHPPIRSPSASSVGSRGSSGSSSKPAGADSTHKVPVVMLEPIRIKQENSGPPENYDFPVVIVKQESDEESRPQNANYPRSILTSLLLNSSQSSTSEETVLRSDAPDSTGDQPGLHQDNSSNGKSEWLDPSQKSPLHVGETRKEDDPNEDWCAVCQNGGELLCCEKCPKVFHLSCHVPTLTNFPSGEWICTFCRDLSKPEVEYDCDAPSHNSEKKKTEGLVKLTPIDKRKCERLLLFLYCHEMSLAFQDPVPLTVPDYYKIIKNPMDLSTIKKRLQEDYSMYSKPEDFVADFRLIFQNCAEFNEPDSEVANAGIKLENYFEELLKNLYPEKRFPKPEFRNESEDNKFSDDSDDDFVQPRKKRLKSIEERQLLK
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
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Plant homeodomain
Function
Transcriptional coactivator that interacts with numerous nuclear receptors and coactivators and modulates the transcription of target genes. Interacts with chromatin depending on histone H3 modifications, having the highest affinity for histone H3 that is both unmodified at 'Lys-4' (H3K4me0) and acetylated at 'Lys-23' (H3K23ac). Has E3 protein-ubiquitin ligase activity. During the DNA damage response, participates in an autoregulatory feedback loop with TP53. Early in response to DNA damage, ATM kinase phosphorylates TRIM24 leading to its ubiquitination and degradation. After sufficient DNA repair has occurred, TP53 activates TRIM24 transcription, ultimately leading to TRIM24-mediated TP53 ubiquitination and degradation (PubMed:24820418). Plays a role in the regulation of cell proliferation and apoptosis, at least in part via its effects on p53/TP53 levels. Up-regulates ligand-dependent transcription activation by AR, GCR/NR3C1, thyroid hormone receptor (TR) and ESR1. Modulates transcription activation by retinoic acid (RA) receptors, including RARA. Plays a role in regulating retinoic acid-dependent proliferation of hepatocytes (By similarity). Participates also in innate immunity by mediating the specific 'Lys-63'-linked ubiquitination of TRAF3 leading to activation of downstream signal transduction of the type I IFN pathway (PubMed:32324863). Additionally, negatively regulates NLRP3/CASP1/IL-1beta-mediated pyroptosis and cell migration probably by ubiquitinating NLRP3 (PubMed:33724611).
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Uniprot ID
Primary ID:
O15164

Secondarily ID:
A4D1R7
A4D1R8
O95854
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Ensembl ID
ENSG00000122779
HGNC ID
HGNC:11812
Subcellular Location
Nucleus
Cytoplasm
Mitochondrion
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: CL000017 , HeLa
Compound ID Compound Name Compound Formula
CP0250495
N-[6-[3-[4-(dimethylamino)butoxy]-5-propoxyphenoxy]-1,3-dimethyl-2-oxobenzimidazol-5-yl]-3,4-dimethoxybenzenesulfonamide
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C32H42N4O8S
 1
1
EC50 = 50 nM
   TI
   LI
   LO
   TS
CP0409012
N-[6-[3-(4-aminobutoxy)-5-propoxyphenoxy]-1,3-dimethyl-2-oxobenzimidazol-5-yl]-3,4-dimethoxybenzenesulfonamide
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C30H38N4O8S
 1
1
EC50 = 59 nM
   TI
   LI
   LO
   TS
CP0407635
N-[6-[3-(5-aminopentoxy)-5-propoxyphenoxy]-1,3-dimethyl-2-oxobenzimidazol-5-yl]-1-methylimidazole-4-sulfonamide
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C27H36N6O6S
 1
1
EC50 = 110 nM
   TI
   LI
   LO
   TS
CP0383067
N-[6-[3-(4-aminobutoxy)-5-propoxyphenoxy]-1,3-dimethyl-2-oxobenzimidazol-5-yl]-1-methylimidazole-4-sulfonamide
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C26H34N6O6S
 1
1
EC50 = 120 nM
   TI
   LI
   LO
   TS
CP0403064
N-[6-[3-(3-aminopropoxy)-5-propoxyphenoxy]-1,3-dimethyl-2-oxobenzimidazol-5-yl]-3,4-dimethoxybenzenesulfonamide
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C29H36N4O8S
 1
1
EC50 = 120 nM
   TI
   LI
   LO
   TS
CP0383068
N-[6-[3-(6-aminohexoxy)-5-propoxyphenoxy]-1,3-dimethyl-2-oxobenzimidazol-5-yl]-1-methylimidazole-4-sulfonamide
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C28H38N6O6S
 1
1
EC50 = 170 nM
   TI
   LI
   LO
   TS
CP0474186
N-[6-[3-(6-aminohexoxy)-5-propoxyphenoxy]-1,3-dimethyl-2-oxobenzimidazol-5-yl]-3,4-dimethoxybenzenesulfonamide
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C32H42N4O8S
 1
1
EC50 = 170 nM
   TI
   LI
   LO
   TS
CP0398747
N-[1,3-dimethyl-2-oxo-6-(3-propoxyphenoxy)benzimidazol-5-yl]-3,4-dimethoxybenzenesulfonamide
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C26H29N3O7S
 1
1
EC50 = 830 nM
   TI
   LI
   LO
   TS
CP0404481
N-[1,3-dimethyl-2-oxo-6-(3-propoxyphenoxy)benzimidazol-5-yl]-1,2-dimethylimidazole-4-sulfonamide
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C23H27N5O5S
 1
1
EC50 = 950 nM
   TI
   LI
   LO
   TS
CP0398745
N-[1,3-dimethyl-6-[3-(2-methylpropoxy)phenoxy]-2-oxobenzimidazol-5-yl]-1,2-dimethylimidazole-4-sulfonamide
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C24H29N5O5S
 1
1
EC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0403062
N-[6-[3-(6-hydroxyhexoxy)-5-propoxyphenoxy]-1,3-dimethyl-2-oxobenzimidazol-5-yl]-1-methylimidazole-4-sulfonamide
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C28H37N5O7S
 1
1
EC50 = 1800 nM
   TI
   LI
   LO
   TS
CP0459852
N-[1,3-dimethyl-2-oxo-6-[3-(oxolan-3-ylmethoxy)phenoxy]benzimidazol-5-yl]-1-methylimidazole-4-sulfonamide
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C24H27N5O6S
 1
1
EC50 = 1900 nM
   TI
   LI
   LO
   TS
CP0566905
N-[6-(3-ethoxyphenoxy)-1,3-dimethyl-2-oxobenzimidazol-5-yl]-1,2-dimethylimidazole-4-sulfonamide
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C22H25N5O5S
 1
1
EC50 = 2300 nM
   TI
   LI
   LO
   TS
CP0404480
N-[6-[3-(3-methoxypropoxy)phenoxy]-1,3-dimethyl-2-oxobenzimidazol-5-yl]-1,2-dimethylimidazole-4-sulfonamide
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C24H29N5O6S
 1
1
EC50 = 2700 nM
   TI
   LI
   LO
   TS
CP0455573
N-[6-(3-butoxyphenoxy)-1,3-dimethyl-2-oxobenzimidazol-5-yl]-1,2-dimethylimidazole-4-sulfonamide
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C24H29N5O5S
 1
1
EC50 = 3000 nM
   TI
   LI
   LO
   TS
CP0383069
N-[6-[3-[4-(dimethylamino)butoxy]phenoxy]-1,3-dimethyl-2-oxobenzimidazol-5-yl]-3,4-dimethoxybenzenesulfonamide
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C29H36N4O7S
 1
1
EC50 = 3200 nM
   TI
   LI
   LO
   TS
CP0403063
N-[1,3-dimethyl-2-oxo-6-(3-phenylmethoxyphenoxy)benzimidazol-5-yl]-3,4-dimethoxybenzenesulfonamide
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C30H29N3O7S
 1
1
EC50 = 3900 nM
   TI
   LI
   LO
   TS
CP0545273
N-[1,3-dimethyl-2-oxo-6-(3-phenylmethoxyphenoxy)benzimidazol-5-yl]-1,2-dimethylimidazole-4-sulfonamide
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C27H27N5O5S
 1
1
EC50 = 4900 nM
   TI
   LI
   LO
   TS
CP0383070
N-[1,3-dimethyl-6-[3-(2-methylpropoxy)phenoxy]-2-oxobenzimidazol-5-yl]cyclopropanesulfonamide
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C22H27N3O5S
 1
1
EC50 = 5000 nM
   TI
   LI
   LO
   TS
CP0391605
tert-butyl N-[6-[3-[1,3-dimethyl-6-[(1-methylimidazol-4-yl)sulfonylamino]-2-oxobenzimidazol-5-yl]oxy-5-propoxyphenoxy]hexyl]carbamate
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C33H46N6O8S
 1
1
EC50 = 5500 nM
   TI
   LI
   LO
   TS
CP0407639
N-[1,3-dimethyl-2-oxo-6-(3-phenylmethoxyphenoxy)benzimidazol-5-yl]-1-methylimidazole-4-sulfonamide
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C26H25N5O5S
 1
1
EC50 = 6200 nM
   TI
   LI
   LO
   TS
CP0551607
N-[1,3-dimethyl-2-oxo-6-(4-phenylmethoxyphenoxy)benzimidazol-5-yl]-1-methylimidazole-4-sulfonamide
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C26H25N5O5S
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0474187
1,3-dimethyl-5-[3-(2-methylpropoxy)phenoxy]benzimidazol-2-one
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C19H22N2O3
 1
1
EC50 > 36000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0250495
N-[6-[3-[4-(dimethylamino)butoxy]-5-propoxyphenoxy]-1,3-dimethyl-2-oxobenzimidazol-5-yl]-3,4-dimethoxybenzenesulfonamide
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C32H42N4O8S
 2
1 IC50 = 11.07 nM
2 IC50 = 150 nM
Clinical Information about the Protein
Target 1 ( Tripartite motif-containing 24 (TRIM24) )
Target Type Literature-reported Target