Reaction Details |
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Target | Histone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2 |
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Ligand | BDBM225230 |
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Substrate/Competitor | Nucleosome |
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Meas. Tech. | PRC2 Biochemical Assay |
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pH | 8±n/a |
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IC50 | 53.5±0.0 nM |
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Comments | extracted |
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Citation | Qi, W; Zhao, K; Gu, J; Huang, Y; Wang, Y; Zhang, H; Zhang, M; Zhang, J; Yu, Z; Li, L; Teng, L; Chuai, S; Zhang, C; Zhao, M; Chan, H; Chen, Z; Fang, D; Fei, Q; Feng, L; Feng, L; Gao, Y; Ge, H; Ge, X; Li, G; Lingel, A; Lin, Y; Liu, Y; Luo, F; Shi, M; Wang, L; Wang, Z; Yu, Y; Zeng, J; Zeng, C; Zhang, L; Zhang, Q; Zhou, S; Oyang, C; Atadja, P; Li, E An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED. Nat Chem Biol13:381-388 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Histone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2 |
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Name: | Histone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2 |
Synonyms: | EZH2/PRC2 | Polycomb repressive complex 2 (PRC2) |
Type: | Protein |
Mol. Mass.: | n/a |
Description: | Human five-member PRC2 complex (EZH2/EED/SUZ12/AEBP2/RBAP48) |
Components: | This complex has 5 components. |
Component 1 |
Name: | Histone-lysine N-methyltransferase EZH2 |
Synonyms: | Enhancer of zeste homolog 2 (EZH2) |
Type: | Protein |
Mol. Mass.: | 86024.60 |
Organism: | Homo sapiens (Human) |
Description: | Q15910-2 |
Residue: | 751 |
Sequence: | MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEW
KQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNF
MVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQ
YNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEEL
KEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHRKC
NYSFHATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRR
GRLPNNSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQ
TPIKMKPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESS
IIAPAPAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCP
CVIAQNFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWD
SKNVSCKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRG
KVYDKYMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRA
IQTGEELFFDYRYSQADALKYVGIEREMEIP
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Component 2 |
Name: | Polycomb protein EED |
Synonyms: | EED | EED_HUMAN | WAIT-1 | WD protein associating with integrin cytoplasmic tails 1 | hEED |
Type: | Protein |
Mol. Mass.: | 50201.68 |
Organism: | Homo sapiens (Human) |
Description: | O75530 |
Residue: | 441 |
Sequence: | MSEREVSTAPAGTDMPAAKKQKLSSDENSNPDLSGDENDDAVSIESGTNTERPDTPTNTP
NAPGRKSWGKGKWKSKKCKYSFKCVNSLKEDHNQPLFGVQFNWHSKEGDPLVFATVGSNR
VTLYECHSQGEIRLLQSYVDADADENFYTCAWTYDSNTSHPLLAVAGSRGIIRIINPITM
QCIKHYVGHGNAINELKFHPRDPNLLLSVSKDHALRLWNIQTDTLVAIFGGVEGHRDEVL
SADYDLLGEKIMSCGMDHSLKLWRINSKRMMNAIKESYDYNPNKTNRPFISQKIHFPDFS
TRDIHRNYVDCVRWLGDLILSKSCENAIVCWKPGKMEDDIDKIKPSESNVTILGRFDYSQ
CDIWYMRFSMDFWQKMLALGNQVGKLYVWDLEVEDPHKAKCTTLTHHKCGAAIRQTSFSR
DSSILIAVCDDASIWRWDRLR
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Component 3 |
Name: | Polycomb protein SUZ12 |
Synonyms: | CHET9 | ChET 9 protein | Chromatin precipitated E2F target 9 protein | JJAZ1 | Joined to JAZF1 protein | KIAA0160 | Polycomb protein SUZ12 | Polycomb protein SUZ12 (SUZ12) | SUZ12 | SUZ12_HUMAN | Suppressor of zeste 12 protein homolog |
Type: | Protein |
Mol. Mass.: | 83080.09 |
Organism: | Homo sapiens (Human) |
Description: | Q15022 |
Residue: | 739 |
Sequence: | MAPQKHGGGGGGGSGPSAGSGGGGFGGSAAVAAATASGGKSGGGSCGGGGSYSASSSSSA
AAAAGAAVLPVKKPKMEHVQADHELFLQAFEKPTQIYRFLRTRNLIAPIFLHRTLTYMSH
RNSRTNIKRKTFKVDDMLSKVEKMKGEQESHSLSAHLQLTFTGFFHKNDKPSPNSENEQN
SVTLEVLLVKVCHKKRKDVSCPIRQVPTGKKQVPLNPDLNQTKPGNFPSLAVSSNEFEPS
NSHMVKSYSLLFRVTRPGRREFNGMINGETNENIDVNEELPARRKRNREDGEKTFVAQMT
VFDKNRRLQLLDGEYEVAMQEMEECPISKKRATWETILDGKRLPPFETFSQGPTLQFTLR
WTGETNDKSTAPIAKPLATRNSESLHQENKPGSVKPTQTIAVKESLTTDLQTRKEKDTPN
ENRQKLRIFYQFLYNNNTRQQTEARDDLHCPWCTLNCRKLYSLLKHLKLCHSRFIFNYVY
HPKGARIDVSINECYDGSYAGNPQDIHRQPGFAFSRNGPVKRTPITHILVCRPKRTKASM
SEFLESEDGEVEQQRTYSSGHNRLYFHSDTCLPLRPQEMEVDSEDEKDPEWLREKTITQI
EEFSDVNEGEKEVMKLWNLHVMKHGFIADNQMNHACMLFVENYGQKIIKKNLCRNFMLHL
VSMHDFNLISIMSIDKAVTKLREMQQKLEKGESASPANEEITEEQNGTANGFSEINSKEK
ALETDSVSGVSKQSKKQKL
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Component 4 |
Name: | Zinc finger protein AEBP2 |
Synonyms: | AEBP2 | AEBP2_HUMAN | Adipocyte enhancer-binding protein 2 (AEBP2) | Zinc finger protein AEBP2 |
Type: | Protein |
Mol. Mass.: | 54448.84 |
Organism: | Homo sapiens (Human) |
Description: | Q6ZN18 |
Residue: | 517 |
Sequence: | MAAAITDMADLEELSRLSPLPPGSPGSAARGRAEPPEEEEEEEEEEEEAEAEAVAALLLN
GGSGGGGGGGGGGVGGGEAETMSEPSPESASQAGEDEDEEEDDEEEEDESSSSGGGEEES
SAESLVGSSGGSSSDETRSLSPGAASSSSGDGDGKEGLEEPKGPRGSQGGGGGGSSSSSV
VSSGGDEGYGTGGGGSSATSGGRRGSLEMSSDGEPLSRMDSEDSISSTIMDVDSTISSGR
STPAMMNGQGSTTSSSKNIAYNCCWDQCQACFNSSPDLADHIRSIHVDGQRGGVFVCLWK
GCKVYNTPSTSQSWLQRHMLTHSGDKPFKCVVGGCNASFASQGGLARHVPTHFSQQNSSK
VSSQPKAKEESPSKAGMNKRRKLKNKRRRSLPRPHDFFDAQTLDAIRHRAICFNLSAHIE
SLGKGHSVVFHSTVIAKRKEDSGKIKLLLHWMPEDILPDVWVNESERHQLKTKVVHLSKL
PKDTALLLDPNIYRTMPQKRLKRTLIRKVFNLYLSKQ
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Component 5 |
Name: | Histone-binding protein RBBP4 |
Synonyms: | RBAP48 | RBBP4 | RBBP4_HUMAN | Retinoblastoma-binding protein p48 (RBAP48) |
Type: | Protein |
Mol. Mass.: | 47627.91 |
Organism: | Homo sapiens (Human) |
Description: | Q09028 |
Residue: | 425 |
Sequence: | MADKEAAFDDAVEERVINEEYKIWKKNTPFLYDLVMTHALEWPSLTAQWLPDVTRPEGKD
FSIHRLVLGTHTSDEQNHLVIASVQLPNDDAQFDASHYDSEKGEFGGFGSVSGKIEIEIK
INHEGEVNRARYMPQNPCIIATKTPSSDVLVFDYTKHPSKPDPSGECNPDLRLRGHQKEG
YGLSWNPNLSGHLLSASDDHTICLWDISAVPKEGKVVDAKTIFTGHTAVVEDVSWHLLHE
SLFGSVADDQKLMIWDTRSNNTSKPSHSVDAHTAEVNCLSFNPYSEFILATGSADKTVAL
WDLRNLKLKLHSFESHKDEIFQVQWSPHNETILASSGTDRRLNVWDLSKIGEEQSPEDAE
DGPPELLFIHGGHTAKISDFSWNPNEPWVICSVSEDNIMQVWQMAENIYNDEDPEGSVDP
EGQGS
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BDBM225230 |
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Name | BDBM50003644 |
Synonyms: | CHEMBL485503 |
Type | Small organic molecule |
Emp. Form. | C20H19BrN2O5 |
Mol. Mass. | 447.279 |
SMILES | COCCOc1ccc(CN\C=C2/C(=O)NC(=O)c3ccc(Br)cc23)cc1O |
Structure |
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Nucleosome |
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Name: | Nucleosome |
Synonyms: | n/a |
Type: | Protein |
Mol. Mass.: | n/a |
Description: | Histone octamer consists of 2 copies of H2A, H2B, H3, and H4 wrapped with 147 bp DNA |
Components: | This complex has 8 components. |
Component 1 |
Name: | Histone H2A |
Synonyms: | H2AFY | H2AY_HUMAN | MACROH2A1 |
Type: | Protein |
Mol. Mass.: | 39644.79 |
Organism: | Homo sapiens (Human) |
Description: | O75367 |
Residue: | 372 |
Sequence: | MSSRGGKKKSTKTSRSAKAGVIFPVGRMLRYIKKGHPKYRIGVGAPVYMAAVLEYLTAEI
LELAGNAARDNKKGRVTPRHILLAVANDEELNQLLKGVTIASGGVLPNIHPELLAKKRGS
KGKLEAIITPPPAKKAKSPSQKKPVSKKAGGKKGARKSKKKQGEVSKAASADSTTEGTPA
DGFTVLSTKSLFLGQKLNLIHSEISNLAGFEVEAIINPTNADIDLKDDLGNTLEKKGGKE
FVEAVLELRKKNGPLEVAGAAVSAGHGLPAKFVIHCNSPVWGADKCEELLEKTVKNCLAL
ADDKKLKSIAFPSIGSGRNGFPKQTAAQLILKAISSYFVSTMSSSIKTVYFVLFDSESIG
IYVQEMAKLDAN
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Component 2 |
Name: | Histone H2B |
Synonyms: | H2B1C_HUMAN | H2BC4 | H2BFA | H2BFG | H2BFH | H2BFK | H2BFL | HIST1H2BC | HIST1H2BE | HIST1H2BF | HIST1H2BG | HIST1H2BI |
Type: | Protein |
Mol. Mass.: | 13925.62 |
Organism: | Homo sapiens (Human) |
Description: | P62807 |
Residue: | 126 |
Sequence: | MPEPAKSAPAPKKGSKKAVTKAQKKDGKKRKRSRKESYSVYVYKVLKQVHPDTGISSKAM
GIMNSFVNDIFERIAGEASRLAHYNKRSTITSREIQTAVRLLLPGELAKHAVSEGTKAVT
KYTSSK
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Component 3 |
Name: | Histone H3 |
Synonyms: | H3-3A | H3.3A | H3.3B | H33_HUMAN | H3F3 | H3F3A | H3F3B |
Type: | Protein |
Mol. Mass.: | 15348.89 |
Organism: | Homo sapiens (Human) |
Description: | P84243 |
Residue: | 136 |
Sequence: | MARTKQTARKSTGGKAPRKQLATKAARKSAPSTGGVKKPHRYRPGTVALREIRRYQKSTE
LLIRKLPFQRLVREIAQDFKTDLRFQSAAIGALQEASEAYLVGLFEDTNLCAIHAKRVTI
MPKDIQLARRIRGERA
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Component 4 |
Name: | Histone H4 |
Synonyms: | H4-16 | H4/A | H4/B | H4/C | H4/D | H4/E | H4/G | H4/H | H4/I | H4/J | H4/K | H4/M | H4/N | H4/O | H4C1 | H4F2 | H4FA | H4FB | H4FC | H4FD | H4FE | H4FG | H4FH | H4FI | H4FJ | H4FK | H4FM | H4FN | H4FO | H4_HUMAN | HIST1H4A | HIST1H4B | HIST1H4C | HIST1H4D | HIST1H4E | HIST1H4F | HIST1H4H | HIST1H4I | HIST1H4J | HIST1H4K | HIST1H4L | HIST2H4 | HIST2H4A | HIST2H4B | HIST4H4 | and | andH4/B | andH4/C | andH4/D | andH4/E | andH4/G | andH4/H | andH4/I | andH4/J | andH4/K | andH4/M | andH4/N | andH4/O |
Type: | Protein |
Mol. Mass.: | 11386.36 |
Organism: | Homo sapiens (Human) |
Description: | P62805 |
Residue: | 103 |
Sequence: | MSGRGKGGKGLGKGGAKRHRKVLRDNIQGITKPAIRRLARRGGVKRISGLIYEETRGVLK
VFLENVIRDAVTYTEHAKRKTVTAMDVVYALKRQGRTLYGFGG
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Component 5 |
Name: | Histone H2A |
Synonyms: | H2AFY | H2AY_HUMAN | MACROH2A1 |
Type: | Protein |
Mol. Mass.: | 39644.79 |
Organism: | Homo sapiens (Human) |
Description: | O75367 |
Residue: | 372 |
Sequence: | MSSRGGKKKSTKTSRSAKAGVIFPVGRMLRYIKKGHPKYRIGVGAPVYMAAVLEYLTAEI
LELAGNAARDNKKGRVTPRHILLAVANDEELNQLLKGVTIASGGVLPNIHPELLAKKRGS
KGKLEAIITPPPAKKAKSPSQKKPVSKKAGGKKGARKSKKKQGEVSKAASADSTTEGTPA
DGFTVLSTKSLFLGQKLNLIHSEISNLAGFEVEAIINPTNADIDLKDDLGNTLEKKGGKE
FVEAVLELRKKNGPLEVAGAAVSAGHGLPAKFVIHCNSPVWGADKCEELLEKTVKNCLAL
ADDKKLKSIAFPSIGSGRNGFPKQTAAQLILKAISSYFVSTMSSSIKTVYFVLFDSESIG
IYVQEMAKLDAN
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Component 6 |
Name: | Histone H2B |
Synonyms: | H2B1C_HUMAN | H2BC4 | H2BFA | H2BFG | H2BFH | H2BFK | H2BFL | HIST1H2BC | HIST1H2BE | HIST1H2BF | HIST1H2BG | HIST1H2BI |
Type: | Protein |
Mol. Mass.: | 13925.62 |
Organism: | Homo sapiens (Human) |
Description: | P62807 |
Residue: | 126 |
Sequence: | MPEPAKSAPAPKKGSKKAVTKAQKKDGKKRKRSRKESYSVYVYKVLKQVHPDTGISSKAM
GIMNSFVNDIFERIAGEASRLAHYNKRSTITSREIQTAVRLLLPGELAKHAVSEGTKAVT
KYTSSK
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Component 7 |
Name: | Histone H3 |
Synonyms: | H3-3A | H3.3A | H3.3B | H33_HUMAN | H3F3 | H3F3A | H3F3B |
Type: | Protein |
Mol. Mass.: | 15348.89 |
Organism: | Homo sapiens (Human) |
Description: | P84243 |
Residue: | 136 |
Sequence: | MARTKQTARKSTGGKAPRKQLATKAARKSAPSTGGVKKPHRYRPGTVALREIRRYQKSTE
LLIRKLPFQRLVREIAQDFKTDLRFQSAAIGALQEASEAYLVGLFEDTNLCAIHAKRVTI
MPKDIQLARRIRGERA
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Component 8 |
Name: | Histone H4 |
Synonyms: | H4-16 | H4/A | H4/B | H4/C | H4/D | H4/E | H4/G | H4/H | H4/I | H4/J | H4/K | H4/M | H4/N | H4/O | H4C1 | H4F2 | H4FA | H4FB | H4FC | H4FD | H4FE | H4FG | H4FH | H4FI | H4FJ | H4FK | H4FM | H4FN | H4FO | H4_HUMAN | HIST1H4A | HIST1H4B | HIST1H4C | HIST1H4D | HIST1H4E | HIST1H4F | HIST1H4H | HIST1H4I | HIST1H4J | HIST1H4K | HIST1H4L | HIST2H4 | HIST2H4A | HIST2H4B | HIST4H4 | and | andH4/B | andH4/C | andH4/D | andH4/E | andH4/G | andH4/H | andH4/I | andH4/J | andH4/K | andH4/M | andH4/N | andH4/O |
Type: | Protein |
Mol. Mass.: | 11386.36 |
Organism: | Homo sapiens (Human) |
Description: | P62805 |
Residue: | 103 |
Sequence: | MSGRGKGGKGLGKGGAKRHRKVLRDNIQGITKPAIRRLARRGGVKRISGLIYEETRGVLK
VFLENVIRDAVTYTEHAKRKTVTAMDVVYALKRQGRTLYGFGG
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