Details of the Target

General Information of Target

Target ID LDTP03341
Target Name NF-kappa-B inhibitor alpha (NFKBIA)
Gene Name NFKBIA
Gene ID 4792
Synonyms
IKBA; MAD3; NFKBI; NF-kappa-B inhibitor alpha; I-kappa-B-alpha; IkB-alpha; IkappaBalpha; Major histocompatibility complex enhancer-binding protein MAD3
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MFQAAERPQEWAMEGPRDGLKKERLLDDRHDSGLDSMKDEEYEQMVKELQEIRLEPQEVP
RGSEPWKQQLTEDGDSFLHLAIIHEEKALTMEVIRQVKGDLAFLNFQNNLQQTPLHLAVI
TNQPEIAEALLGAGCDPELRDFRGNTPLHLACEQGCLASVGVLTQSCTTPHLHSILKATN
YNGHTCLHLASIHGYLGIVELLVSLGADVNAQEPCNGRTALHLAVDLQNPDLVSLLLKCG
ADVNRVTYQGYSPYQLTWGRPSTRIQQQLGQLTLENLQMLPESEDEESYDTESEFTEFTE
DELPYDDCVFGGQRLTL
Target Type
Clinical trial
Target Bioclass
Transcription factor
Family
NF-kappa-B inhibitor family
Subcellular location
Cytoplasm
Function
Inhibits the activity of dimeric NF-kappa-B/REL complexes by trapping REL (RELA/p65 and NFKB1/p50) dimers in the cytoplasm by masking their nuclear localization signals. On cellular stimulation by immune and pro-inflammatory responses, becomes phosphorylated promoting ubiquitination and degradation, enabling the dimeric RELA to translocate to the nucleus and activate transcription.
TTD ID
T51672
Uniprot ID
P25963
DrugMap ID
TTSHAEB
Ensemble ID
ENST00000216797.10
HGNC ID
HGNC:7797
ChEMBL ID
CHEMBL2898

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C239(1.68)  LDD0531  [1]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [2]
TFBX
 Probe Info  		N.A.  LDD0148  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HCT 116 C239(1.68)  LDD0531  [1]
 LDCM0230  AC113 HCT 116 C239(1.37)  LDD0547  [1]
 LDCM0231  AC114 HCT 116 C239(0.96)  LDD0548  [1]
 LDCM0232  AC115 HCT 116 C239(1.03)  LDD0549  [1]
 LDCM0233  AC116 HCT 116 C239(0.99)  LDD0550  [1]
 LDCM0234  AC117 HCT 116 C239(0.90)  LDD0551  [1]
 LDCM0235  AC118 HCT 116 C239(0.85)  LDD0552  [1]
 LDCM0236  AC119 HCT 116 C239(0.91)  LDD0553  [1]
 LDCM0238  AC120 HCT 116 C239(0.87)  LDD0555  [1]
 LDCM0239  AC121 HCT 116 C239(0.86)  LDD0556  [1]
 LDCM0240  AC122 HCT 116 C239(0.91)  LDD0557  [1]
 LDCM0241  AC123 HCT 116 C239(1.01)  LDD0558  [1]
 LDCM0242  AC124 HCT 116 C239(0.86)  LDD0559  [1]
 LDCM0243  AC125 HCT 116 C239(0.83)  LDD0560  [1]
 LDCM0244  AC126 HCT 116 C239(1.06)  LDD0561  [1]
 LDCM0245  AC127 HCT 116 C239(0.85)  LDD0562  [1]
 LDCM0259  AC14 HEK-293T C156(1.13)  LDD1512  [4]
 LDCM0279  AC2 HCT 116 C239(1.49)  LDD0596  [1]
 LDCM0282  AC22 HEK-293T C156(1.07)  LDD1521  [4]
 LDCM0285  AC25 HCT 116 C239(1.15)  LDD0602  [1]
 LDCM0286  AC26 HCT 116 C239(1.15)  LDD0603  [1]
 LDCM0287  AC27 HCT 116 C239(1.07)  LDD0604  [1]
 LDCM0288  AC28 HCT 116 C239(1.21)  LDD0605  [1]
 LDCM0289  AC29 HCT 116 C239(1.05)  LDD0606  [1]
 LDCM0290  AC3 HCT 116 C239(1.77)  LDD0607  [1]
 LDCM0291  AC30 HCT 116 C239(1.07)  LDD0608  [1]
 LDCM0292  AC31 HCT 116 C239(0.95)  LDD0609  [1]
 LDCM0293  AC32 HCT 116 C239(1.05)  LDD0610  [1]
 LDCM0294  AC33 HCT 116 C239(1.27)  LDD0611  [1]
 LDCM0295  AC34 HCT 116 C239(0.77)  LDD0612  [1]
 LDCM0296  AC35 HCT 116 C239(1.02)  LDD0613  [1]
 LDCM0297  AC36 HCT 116 C239(0.70)  LDD0614  [1]
 LDCM0298  AC37 HCT 116 C239(0.87)  LDD0615  [1]
 LDCM0299  AC38 HCT 116 C239(0.67)  LDD0616  [1]
 LDCM0300  AC39 HCT 116 C239(0.71)  LDD0617  [1]
 LDCM0301  AC4 HCT 116 C239(1.54)  LDD0618  [1]
 LDCM0302  AC40 HCT 116 C239(0.65)  LDD0619  [1]
 LDCM0303  AC41 HCT 116 C239(0.66)  LDD0620  [1]
 LDCM0304  AC42 HCT 116 C239(0.74)  LDD0621  [1]
 LDCM0305  AC43 HCT 116 C239(0.63)  LDD0622  [1]
 LDCM0306  AC44 HCT 116 C239(0.77)  LDD0623  [1]
 LDCM0307  AC45 HCT 116 C239(0.75)  LDD0624  [1]
 LDCM0308  AC46 HEK-293T C156(1.03)  LDD1547  [4]
 LDCM0312  AC5 HCT 116 C239(2.09)  LDD0629  [1]
 LDCM0317  AC54 HEK-293T C156(0.94)  LDD1556  [4]
 LDCM0320  AC57 HCT 116 C239(1.01)  LDD0637  [1]
 LDCM0321  AC58 HCT 116 C239(0.87)  LDD0638  [1]
 LDCM0322  AC59 HCT 116 C239(0.99)  LDD0639  [1]
 LDCM0323  AC6 HEK-293T C156(1.06)  LDD1562  [4]
 LDCM0324  AC60 HCT 116 C239(0.80)  LDD0641  [1]
 LDCM0325  AC61 HCT 116 C239(0.77)  LDD0642  [1]
 LDCM0326  AC62 HCT 116 C239(0.87)  LDD0643  [1]
 LDCM0327  AC63 HCT 116 C239(1.15)  LDD0644  [1]
 LDCM0328  AC64 HCT 116 C239(1.06)  LDD0645  [1]
 LDCM0329  AC65 HCT 116 C239(1.41)  LDD0646  [1]
 LDCM0330  AC66 HCT 116 C239(1.15)  LDD0647  [1]
 LDCM0331  AC67 HCT 116 C239(1.03)  LDD0648  [1]
 LDCM0332  AC68 HCT 116 C239(1.20)  LDD0649  [1]
 LDCM0333  AC69 HCT 116 C239(1.26)  LDD0650  [1]
 LDCM0335  AC70 HCT 116 C239(1.17)  LDD0652  [1]
 LDCM0336  AC71 HCT 116 C239(1.27)  LDD0653  [1]
 LDCM0337  AC72 HCT 116 C239(1.74)  LDD0654  [1]
 LDCM0338  AC73 HCT 116 C239(1.41)  LDD0655  [1]
 LDCM0339  AC74 HCT 116 C239(1.24)  LDD0656  [1]
 LDCM0340  AC75 HCT 116 C239(1.36)  LDD0657  [1]
 LDCM0341  AC76 HCT 116 C239(1.62)  LDD0658  [1]
 LDCM0342  AC77 HCT 116 C239(1.23)  LDD0659  [1]
 LDCM0343  AC78 HCT 116 C239(0.99)  LDD0660  [1]
 LDCM0344  AC79 HCT 116 C239(1.05)  LDD0661  [1]
 LDCM0346  AC80 HCT 116 C239(1.03)  LDD0663  [1]
 LDCM0347  AC81 HCT 116 C239(1.05)  LDD0664  [1]
 LDCM0348  AC82 HCT 116 C239(1.38)  LDD0665  [1]
 LDCM0368  CL10 HEK-293T C156(1.80)  LDD1572  [4]
 LDCM0369  CL100 HCT 116 C239(1.49)  LDD0686  [1]
 LDCM0382  CL112 HCT 116 C239(1.18)  LDD0699  [1]
 LDCM0383  CL113 HCT 116 C239(0.72)  LDD0700  [1]
 LDCM0384  CL114 HCT 116 C239(0.89)  LDD0701  [1]
 LDCM0385  CL115 HCT 116 C239(1.00)  LDD0702  [1]
 LDCM0386  CL116 HCT 116 C239(1.15)  LDD0703  [1]
 LDCM0387  CL117 HCT 116 C239(0.64)  LDD0704  [1]
 LDCM0388  CL118 HCT 116 C239(0.82)  LDD0705  [1]
 LDCM0389  CL119 HCT 116 C239(0.90)  LDD0706  [1]
 LDCM0391  CL120 HCT 116 C239(0.68)  LDD0708  [1]
 LDCM0396  CL125 HCT 116 C239(1.11)  LDD0713  [1]
 LDCM0397  CL126 HCT 116 C239(0.86)  LDD0714  [1]
 LDCM0398  CL127 HCT 116 C239(0.69)  LDD0715  [1]
 LDCM0399  CL128 HCT 116 C239(0.97)  LDD0716  [1]
 LDCM0403  CL16 HCT 116 C239(0.79)  LDD0720  [1]
 LDCM0404  CL17 HCT 116 C239(1.01)  LDD0721  [1]
 LDCM0405  CL18 HCT 116 C239(0.73)  LDD0722  [1]
 LDCM0406  CL19 HCT 116 C239(0.78)  LDD0723  [1]
 LDCM0408  CL20 HCT 116 C239(0.98)  LDD0725  [1]
 LDCM0409  CL21 HCT 116 C239(1.14)  LDD0726  [1]
 LDCM0410  CL22 HCT 116 C239(1.44)  LDD0727  [1]
 LDCM0411  CL23 HCT 116 C239(0.90)  LDD0728  [1]
 LDCM0412  CL24 HCT 116 C239(0.78)  LDD0729  [1]
 LDCM0413  CL25 HCT 116 C239(1.10)  LDD0730  [1]
 LDCM0414  CL26 HCT 116 C239(0.87)  LDD0731  [1]
 LDCM0415  CL27 HCT 116 C239(1.02)  LDD0732  [1]
 LDCM0416  CL28 HCT 116 C239(0.86)  LDD0733  [1]
 LDCM0417  CL29 HCT 116 C239(0.93)  LDD0734  [1]
 LDCM0419  CL30 HCT 116 C239(0.89)  LDD0736  [1]
 LDCM0423  CL34 HEK-293T C156(1.13)  LDD1627  [4]
 LDCM0436  CL46 HEK-293T C156(1.05)  LDD1640  [4]
 LDCM0449  CL58 HEK-293T C156(1.12)  LDD1652  [4]
 LDCM0463  CL70 HEK-293T C156(1.18)  LDD1666  [4]
 LDCM0469  CL76 HCT 116 C239(0.82)  LDD0786  [1]
 LDCM0470  CL77 HCT 116 C239(1.14)  LDD0787  [1]
 LDCM0471  CL78 HCT 116 C239(1.07)  LDD0788  [1]
 LDCM0472  CL79 HCT 116 C239(0.99)  LDD0789  [1]
 LDCM0474  CL80 HCT 116 C239(0.74)  LDD0791  [1]
 LDCM0475  CL81 HCT 116 C239(0.96)  LDD0792  [1]
 LDCM0476  CL82 HCT 116 C239(0.85)  LDD0793  [1]
 LDCM0477  CL83 HCT 116 C239(0.86)  LDD0794  [1]
 LDCM0478  CL84 HCT 116 C239(1.20)  LDD0795  [1]
 LDCM0479  CL85 HCT 116 C239(0.82)  LDD0796  [1]
 LDCM0480  CL86 HCT 116 C239(0.82)  LDD0797  [1]
 LDCM0481  CL87 HCT 116 C239(1.33)  LDD0798  [1]
 LDCM0482  CL88 HCT 116 C239(1.10)  LDD0799  [1]
 LDCM0483  CL89 HCT 116 C239(0.97)  LDD0800  [1]
 LDCM0485  CL90 HCT 116 C239(0.64)  LDD0802  [1]
 LDCM0486  CL91 HCT 116 C239(1.14)  LDD0803  [1]
 LDCM0487  CL92 HCT 116 C239(1.10)  LDD0804  [1]
 LDCM0488  CL93 HCT 116 C239(1.35)  LDD0805  [1]
 LDCM0489  CL94 HCT 116 C239(1.48)  LDD0806  [1]
 LDCM0490  CL95 HCT 116 C239(1.32)  LDD0807  [1]
 LDCM0491  CL96 HCT 116 C239(1.23)  LDD0808  [1]
 LDCM0492  CL97 HCT 116 C239(1.23)  LDD0809  [1]
 LDCM0493  CL98 HCT 116 C239(1.45)  LDD0810  [1]
 LDCM0494  CL99 HCT 116 C239(1.88)  LDD0811  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
26S proteasome non-ATPase regulatory subunit 3 (PSMD3) Proteasome subunit S3 family O43242
Beta-adrenergic receptor kinase 1 (GRK2) AGC Ser/Thr protein kinase family P25098
G protein-coupled receptor kinase 5 (GRK5) AGC Ser/Thr protein kinase family P34947
Inhibitor of nuclear factor kappa-B kinase subunit alpha (CHUK) Ser/Thr protein kinase family O15111
Inhibitor of nuclear factor kappa-B kinase subunit beta (IKBKB) Ser/Thr protein kinase family O14920
Small ribosomal subunit protein uS3 (RPS3) Universal ribosomal protein uS3 family P23396
Hypoxia-inducible factor 1-alpha inhibitor (HIF1AN) . Q9NWT6
Transcription factor
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
NF-kappa-B inhibitor alpha (NFKBIA) NF-kappa-B inhibitor family P25963
Nuclear factor NF-kappa-B p100 subunit (NFKB2) . Q00653
Nuclear factor NF-kappa-B p105 subunit (NFKB1) . P19838
Proto-oncogene c-Rel (REL) . Q04864
Transcription factor p65 (RELA) . Q04206
Other
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Enhancer of filamentation 1 (NEDD9) CAS family Q14511
T-cell leukemia/lymphoma protein 1A (TCL1A) TCL1 family P56279
Polyubiquitin-C (UBC) Ubiquitin family P0CG48
Catenin alpha-1 (CTNNA1) Vinculin/alpha-catenin family P35221
COMM domain-containing protein 1 (COMMD1) . Q8N668
Enkurin domain-containing protein 1 (ENKD1) . Q9H0I2
F-box/WD repeat-containing protein 11 (FBXW11) . Q9UKB1
NF-kappa-B essential modulator (IKBKG) . Q9Y6K9

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Acetylsalicylic Acid Small molecular drug DB00945
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
I3c Small molecular drug DN62DG
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fucoxanthin Small molecular drug DEZ3D7
Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bardoxolone Methyl Small molecular drug DB05983
Astaxanthin . DB06543

References

1 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
2 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
3 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
4 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402