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 | H3K27me0 |
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Meas. Tech. | PRC2 Biochemical Assay |
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pH | 8±n/a |
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IC50 | 23.4±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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H3K27me0 |
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Name: | H3K27me0 |
Synonyms: | n/a |
Type: | Protein |
Mol. Mass.: | 2585.54 |
Organism: | Homo sapiens (Human) |
Description: | Human H3 peptide (21-44 aa) |
Residue: | 24 |
Sequence: | |