| Reaction Details |
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 | Report a problem with these data |
| Target | Histone-lysine N-methyltransferase EZH2/Polycomb protein EED [40-441]/Polycomb protein SUZ12 [559-739] |
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| Ligand | BDBM225230 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | Isothermal Titration Calorimetry (ITC) |
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| pH | 8±0 |
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| Temperature | 1663.9±0 K |
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| Kd | 114±0.0 nM |
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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-lysine N-methyltransferase EZH2/Polycomb protein EED [40-441]/Polycomb protein SUZ12 [559-739] |
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| Name: | Histone-lysine N-methyltransferase EZH2/Polycomb protein EED [40-441]/Polycomb protein SUZ12 [559-739] |
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| Synonyms: | Polycomb repressive complex 2 (PRC2) |
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| Type: | Protein |
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| Mol. Mass.: | n/a |
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| Description: | Human three-member PRC2 complex (EZH2(1-751 aa)/EED(40-441 aa)/SUZ12(559-739 aa)) |
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| Components: | This complex has 3 components. |
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| Component 1 |
| Name: | Histone-lysine N-methyltransferase EZH2 |
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| Synonyms: | Enhancer of zeste homolog 2 (EZH2) |
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| Type: | Protein |
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| Mol. Mass.: | 86024.60 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q15910-2 |
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| Residue: | 751 |
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| Sequence: | MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEW
KQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNF
MVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQ
YNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEEL
KEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHRKC
NYSFHATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRR
GRLPNNSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQ
TPIKMKPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESS
IIAPAPAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCP
CVIAQNFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWD
SKNVSCKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRG
KVYDKYMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRA
IQTGEELFFDYRYSQADALKYVGIEREMEIP
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| Component 2 |
| Name: | Polycomb protein EED [40-441] |
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| Synonyms: | EED | EED_HUMAN | Polycomb protein EED (EED) |
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| Type: | Protein |
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| Mol. Mass.: | 46101.42 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Human polycomb protein EED (40-441 aa) |
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| Residue: | 402 |
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| Sequence: | DAVSIESGTNTERPDTPTNTPNAPGRKSWGKGKWKSKKCKYSFKCVNSLKEDHNQPLFGV
QFNWHSKEGDPLVFATVGSNRVTLYECHSQGEIRLLQSYVDADADENFYTCAWTYDSNTS
HPLLAVAGSRGIIRIINPITMQCIKHYVGHGNAINELKFHPRDPNLLLSVSKDHALRLWN
IQTDTLVAIFGGVEGHRDEVLSADYDLLGEKIMSCGMDHSLKLWRINSKRMMNAIKESYD
YNPNKTNRPFISQKIHFPDFSTRDIHRNYVDCVRWLGDLILSKSCENAIVCWKPGKMEDD
IDKIKPSESNVTILGRFDYSQCDIWYMRFSMDFWQKMLALGNQVGKLYVWDLEVEDPHKA
KCTTLTHHKCGAAIRQTSFSRDSSILIAVCDDASIWRWDRLR
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| Component 3 |
| Name: | Polycomb protein SUZ12 [559-739] |
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| Synonyms: | CHET9 | JJAZ1 | KIAA0160 | Polycomb protein SUZ12 (SUZ12) | SUZ12 | SUZ12_HUMAN |
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| Type: | Protein |
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| Mol. Mass.: | 20870.88 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Human polycomb protein SUZ12 (559-739 aa) |
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| Residue: | 181 |
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| Sequence: | SGHNRLYFHSDTCLPLRPQEMEVDSEDEKDPEWLREKTITQIEEFSDVNEGEKEVMKLWN
LHVMKHGFIADNQMNHACMLFVENYGQKIIKKNLCRNFMLHLVSMHDFNLISIMSIDKAV
TKLREMQQKLEKGESASPANEEITEEQNGTANGFSEINSKEKALETDSVSGVSKQSKKQK
L
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| BDBM225230 |
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| n/a |
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| Name | BDBM225230 |
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| Synonyms: | EED226 | US11013745, Compound EED226 |
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| Type | Small organic molecule |
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| Emp. Form. | C17H15N5O3S |
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| Mol. Mass. | 369.398 |
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| SMILES | CS(=O)(=O)c1ccc(cc1)-c1cnc(NCc2ccco2)n2cnnc12 |
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| Structure | 
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