General Information of the Protein
Protein ID
PT01191
Protein Name
Baculoviral IAP repeat-containing protein 2
Secondarily
Protein Name
Cellular inhibitor of apoptosis 1
IAP homolog B
Inhibitor of apoptosis protein 2
RING finger protein 48
RING-type E3 ubiquitin transferase BIRC2
TNFR2-TRAF-signaling complex protein 2
Gene Name
BIRC2
Secondarily
Gene Name
API1
MIHB
RNF48
Sequence
MHKTASQRLFPGPSYQNIKSIMEDSTILSDWTNSNKQKMKYDFSCELYRMSTYSTFPAGVPVSERSLARAGFYYTGVNDKVKCFCCGLMLDNWKLGDSPIQKHKQLYPSCSFIQNLVSASLGSTSKNTSPMRNSFAHSLSPTLEHSSLFSGSYSSLSPNPLNSRAVEDISSSRTNPYSYAMSTEEARFLTYHMWPLTFLSPSELARAGFYYIGPGDRVACFACGGKLSNWEPKDDAMSEHRRHFPNCPFLENSLETLRFSISNLSMQTHAARMRTFMYWPSSVPVQPEQLASAGFYYVGRNDDVKCFCCDGGLRCWESGDDPWVEHAKWFPRCEFLIRMKGQEFVDEIQGRYPHLLEQLLSTSDTTGEENADPPIIHFGPGESSSEDAVMMNTPVVKSALEMGFNRDLVKQTVQSKILTTGENYKTVNDIVSALLNAEDEKREEEKEKQAEEMASDDLSLIRKNRMALFQQLTCVLPILDNLLKANVINKQEHDIIKQKTQIPLQARELIDTILVKGNAAANIFKNCLKEIDSTLYKNLFVDKNMKYIPTEDVSGLSLEEQLRRLQEERTCKVCMDKEVSVVFIPCGHLVVCQECAPSLRKCPICRGIIKGTVRTFLS
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
Function
Multi-functional protein which regulates not only caspases and apoptosis, but also modulates inflammatory signaling and immunity, mitogenic kinase signaling, and cell proliferation, as well as cell invasion and metastasis. Acts as an E3 ubiquitin-protein ligase regulating NF-kappa-B signaling and regulates both canonical and non-canonical NF-kappa-B signaling by acting in opposite directions: acts as a positive regulator of the canonical pathway and suppresses constitutive activation of non-canonical NF-kappa-B signaling. The target proteins for its E3 ubiquitin-protein ligase activity include: RIPK1, RIPK2, RIPK3, RIPK4, CASP3, CASP7, CASP8, TRAF2, DIABLO/SMAC, MAP3K14/NIK, MAP3K5/ASK1, IKBKG/NEMO, IKBKE and MXD1/MAD1. Can also function as an E3 ubiquitin-protein ligase of the NEDD8 conjugation pathway, targeting effector caspases for neddylation and inactivation. Acts as an important regulator of innate immune signaling via regulation of Toll-like receptors (TLRs), Nodlike receptors (NLRs) and RIG-I like receptors (RLRs), collectively referred to as pattern recognition receptors (PRRs). Protects cells from spontaneous formation of the ripoptosome, a large multi-protein complex that has the capability to kill cancer cells in a caspase-dependent and caspase-independent manner. Suppresses ripoptosome formation by ubiquitinating RIPK1 and CASP8. Can stimulate the transcriptional activity of E2F1. Plays a role in the modulation of the cell cycle.
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Uniprot ID
Primary ID:
Q13490

Secondarily ID:
B4E026
Q16516
Q4TTG0
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Ensembl ID
ENSG00000110330
HGNC ID
HGNC:590
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: CL000156 , HT-1080
Compound ID Compound Name Compound Formula
CP0436239
methyl (2S)-2-[[(2R)-2-[2-(hydroxyamino)-2-oxoethyl]heptanoyl]amino]propanoate
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C13H24N2O5
 1
1
IC50 = 530 nM
   TI
   LI
   LO
   TS
CP0006370
(S)-methyl 2-((2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoate
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C17H26N2O4
 1
1
IC50 = 690 nM
   TI
   LI
   LO
   TS
CP0436236
methyl (2S)-2-[[(2R)-2-[2-(hydroxyamino)-2-oxoethyl]heptanoyl]amino]-3-phenylpropanoate
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C19H28N2O5
 1
1
IC50 = 840 nM
   TI
   LI
   LO
   TS
CP0399564
methyl (2S)-2-[[(2R)-2-[2-(hydroxyamino)-2-oxoethyl]heptanoyl]amino]-4-methylpentanoate
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C16H30N2O5
 1
1
IC50 = 1060 nM
   TI
   LI
   LO
   TS
CP0436238
methyl (2S)-2-[[(2R)-2-[2-(hydroxyamino)-2-oxoethyl]heptanoyl]amino]-3-methylbutanoate
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C15H28N2O5
 1
1
IC50 = 1250 nM
   TI
   LI
   LO
   TS
CP0484740
methyl 2-[[(2R)-2-[2-(hydroxyamino)-2-oxoethyl]heptanoyl]amino]acetate
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C12H22N2O5
 1
1
IC50 = 1540 nM
   TI
   LI
   LO
   TS
CP0515474
methyl (2S)-2-[[(2R)-2-(butylamino)-4-(hydroxyamino)-4-oxobutanoyl]amino]-4-methylpentanoate
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C15H29N3O5
 1
1
IC50 = 4690 nM
   TI
   LI
   LO
   TS
CP0528494
methyl (2S)-2-[[(2R)-2-(dibutylamino)-4-(hydroxyamino)-4-oxobutanoyl]amino]-4-methylpentanoate
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C19H37N3O5
 1
1
IC50 = 9200 nM
   TI
   LI
   LO
   TS
CP0379017
methyl (2S)-2-[[(2S)-2-[2-(hydroxyamino)-2-oxoethyl]heptanoyl]amino]-4-methylpentanoate
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C16H30N2O5
 1
1
IC50 = 12100 nM
   TI
   LI
   LO
   TS
CP0526917
methyl (2S)-2-[[4-(hydroxyamino)-4-oxobutanoyl]amino]-4-methylpentanoate
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C11H20N2O5
 1
1
IC50 = 19900 nM
   TI
   LI
   LO
   TS
CP0436237
methyl (2S)-2-[[(2R)-2-[2-(hydroxyamino)-2-oxoethyl]heptanoyl]amino]-3,3-dimethylbutanoate
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C16H30N2O5
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0541140
methyl (2S)-2-[[(2R)-2-ethyl-4-(hydroxyamino)-4-oxobutanoyl]amino]-4-methylpentanoate
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C13H24N2O5
 1
1
IC50 = 24100 nM
   TI
   LI
   LO
   TS
CP0537968
methyl (2S)-2-[[(2R)-2-benzyl-4-(hydroxyamino)-4-oxobutanoyl]amino]-4-methylpentanoate
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C18H26N2O5
 1
1
IC50 = 45200 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0230298
(2S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-N-[(1S,2R)-2-[6-[[(1S,2R)-1-[[(2S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]pyrrolidine-2-carbonyl]amino]-2,3-dihydro-1H-inden-2-yl]oxy]hexa-2,4-diynoxy]-2,3-dihydro-1H-inden-1-yl]pyrrolidine-2-carboxamide
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C54H74N8O8
 2
1 EC50 = 0.1 nM
2 IC50 = 15 nM
CP0249134
(2S,5S,8S,11S,17S,20S,23S,26S)-4,19-bis[(2S)-3-methyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-8,23-bis(naphthalen-2-ylmethyl)-6,9,21,24-tetraoxo-1,4,7,10,14,15,16,19,22,25,29,30-dodecazapentacyclo[26.2.1.12,5.113,16.117,20]tetratriaconta-13(33),14,28(31),29-tetraene-11,26-dicarboxylic acid
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C64H80N16O12
 2
1 IC50 = 3 nM
2 IC50 = 9 nM
CP0051683
(8S,11S,14S,17S,29S,32S,35S,38S)-10,31-bis[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-14,35-bis(naphthalen-2-ylmethyl)-12,15,33,36-tetraoxo-2,23-dioxa-5,6,7,10,13,16,26,27,28,31,34,37-dodecazaheptacyclo[38.2.2.219,22.14,7.18,11.125,28.129,32]pentaconta-1(43),4(50),5,19,21,25(46),26,40(44),41,47-decaene-17,38-dicarboxylic acid
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C80H96N16O14
 2
1 IC50 = 5 nM
2 IC50 = 22 nM
CP0089066
(8S,11S,14S,17S,29S,32S,35S,38S)-10,31-bis[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-14,35-bis(naphthalen-2-ylmethyl)-12,15,33,36-tetraoxo-2,23-dioxa-5,6,7,10,13,16,26,27,28,31,34,37-dodecazaheptacyclo[38.2.2.219,22.14,7.18,11.125,28.129,32]pentaconta-1(43),4(50),5,19,21,25(46),26,40(44),41,47-decaene-17,38-dicarboxylic acid
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C84H100N16O14
 2
1 IC50 = 7 nM
2 IC50 = 24 nM
CP0435112
(2S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-N-[(1S,2R)-2-prop-2-ynoxy-1,2,3,4-tetrahydronaphthalen-1-yl]pyrrolidine-2-carboxamide
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C28H40N4O4
 1
1 IC50 = 10 nM
CP0356374
1-[6-[(4-fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-2H-pyrrolo[3,2-b]pyridin-1-yl]-2-[(2R,5R)-5-methyl-2-[[(3R)-3-methylmorpholin-4-yl]methyl]piperazin-1-yl]ethanone
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C30H42FN5O3
 1
1 IC50 = 12 nM
CP0069638
(2S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-N-[(1S,2S)-2-prop-2-ynoxy-1,2,3,4-tetrahydronaphthalen-1-yl]pyrrolidine-2-carboxamide
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C28H40N4O4
 1
1 IC50 = 14 nM
CP0218662
(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-[(1S,2R)-2-[6-[[(1S,2R)-1-[[(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-2,3-dihydro-1H-inden-2-yl]oxy]hexa-2,4-diynoxy]-2,3-dihydro-1H-inden-1-yl]pyrrolidine-2-carboxamide
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C58H78N8O8
 1
1 IC50 = 15 nM
CP0106277
US9018214, 190
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C24H35F2N5O2
 1
1 IC50 = 29 nM
CP0258426
(2S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-N-[(1R,2S)-2-prop-2-ynoxy-1,2,3,4-tetrahydronaphthalen-1-yl]pyrrolidine-2-carboxamide
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C28H40N4O4
 1
1 IC50 = 40 nM
CP0223574
US9018214, 188
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C23H33F2N5O2
 1
1 IC50 = 40 nM
CP0077521
(2S)-N-[(1S)-1-cyclohexyl-2-[(2S)-2-[4-(4-fluorobenzoyl)-1,3-thiazol-2-yl]pyrrolidin-1-yl]-2-oxoethyl]-2-(methylamino)propanamide
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C26H33FN4O3S
 5
1 IC50 = 58 nM
2 IC50 = 61 nM
3 IC50 = 2140 nM
4 IC50 = 2720 nM
5 Kd = 10.4 nM
CP0180985
(2S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-N-[(1R,2R)-2-prop-2-ynoxy-1,2,3,4-tetrahydronaphthalen-1-yl]pyrrolidine-2-carboxamide
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C28H40N4O4
 1
1 IC50 = 290 nM
Clinical Information about the Protein
Target 1 ( Cellular inhibitor of apoptosis 1 (BIRC2) )
Target Type Clinical trial Target
Disease 2 Target-related Diseases  2
1 Lymphoma [ICD-11: 2A80-2A86]
2 Squamous head and neck cell carcinom [ICD-11: 2D60.0]
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 Birinapant Phase 2
Lymphoma
2 AT-406 Phase 3
Squamous head and neck cell carcinom