Reaction Details Report a problem with these data
Target
Histone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2
Ligand
BDBM225230
Substrate
H3K27me0
Meas. Tech.
PRC2 Biochemical Assay
pH
8±n/a
IC50
23.4±0.0 nM
Comments
extracted
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 Biol 13:381-388 (2017) [PubMed] Article
More Info.:
Target
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:
MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEWKQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNFMVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQYNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEELKEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHRKCNYSFHATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPNNSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKMKPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPAPAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQNFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVSCKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDKYMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGEELFFDYRYSQADALKYVGIEREMEIP
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:
MSEREVSTAPAGTDMPAAKKQKLSSDENSNPDLSGDENDDAVSIESGTNTERPDTPTNTPNAPGRKSWGKGKWKSKKCKYSFKCVNSLKEDHNQPLFGVQFNWHSKEGDPLVFATVGSNRVTLYECHSQGEIRLLQSYVDADADENFYTCAWTYDSNTSHPLLAVAGSRGIIRIINPITMQCIKHYVGHGNAINELKFHPRDPNLLLSVSKDHALRLWNIQTDTLVAIFGGVEGHRDEVLSADYDLLGEKIMSCGMDHSLKLWRINSKRMMNAIKESYDYNPNKTNRPFISQKIHFPDFSTRDIHRNYVDCVRWLGDLILSKSCENAIVCWKPGKMEDDIDKIKPSESNVTILGRFDYSQCDIWYMRFSMDFWQKMLALGNQVGKLYVWDLEVEDPHKAKCTTLTHHKCGAAIRQTSFSRDSSILIAVCDDASIWRWDRLR
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:
MAPQKHGGGGGGGSGPSAGSGGGGFGGSAAVAAATASGGKSGGGSCGGGGSYSASSSSSAAAAAGAAVLPVKKPKMEHVQADHELFLQAFEKPTQIYRFLRTRNLIAPIFLHRTLTYMSHRNSRTNIKRKTFKVDDMLSKVEKMKGEQESHSLSAHLQLTFTGFFHKNDKPSPNSENEQNSVTLEVLLVKVCHKKRKDVSCPIRQVPTGKKQVPLNPDLNQTKPGNFPSLAVSSNEFEPSNSHMVKSYSLLFRVTRPGRREFNGMINGETNENIDVNEELPARRKRNREDGEKTFVAQMTVFDKNRRLQLLDGEYEVAMQEMEECPISKKRATWETILDGKRLPPFETFSQGPTLQFTLRWTGETNDKSTAPIAKPLATRNSESLHQENKPGSVKPTQTIAVKESLTTDLQTRKEKDTPNENRQKLRIFYQFLYNNNTRQQTEARDDLHCPWCTLNCRKLYSLLKHLKLCHSRFIFNYVYHPKGARIDVSINECYDGSYAGNPQDIHRQPGFAFSRNGPVKRTPITHILVCRPKRTKASMSEFLESEDGEVEQQRTYSSGHNRLYFHSDTCLPLRPQEMEVDSEDEKDPEWLREKTITQIEEFSDVNEGEKEVMKLWNLHVMKHGFIADNQMNHACMLFVENYGQKIIKKNLCRNFMLHLVSMHDFNLISIMSIDKAVTKLREMQQKLEKGESASPANEEITEEQNGTANGFSEINSKEKALETDSVSGVSKQSKKQKL
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:
MAAAITDMADLEELSRLSPLPPGSPGSAARGRAEPPEEEEEEEEEEEEAEAEAVAALLLNGGSGGGGGGGGGGVGGGEAETMSEPSPESASQAGEDEDEEEDDEEEEDESSSSGGGEEESSAESLVGSSGGSSSDETRSLSPGAASSSSGDGDGKEGLEEPKGPRGSQGGGGGGSSSSSVVSSGGDEGYGTGGGGSSATSGGRRGSLEMSSDGEPLSRMDSEDSISSTIMDVDSTISSGRSTPAMMNGQGSTTSSSKNIAYNCCWDQCQACFNSSPDLADHIRSIHVDGQRGGVFVCLWKGCKVYNTPSTSQSWLQRHMLTHSGDKPFKCVVGGCNASFASQGGLARHVPTHFSQQNSSKVSSQPKAKEESPSKAGMNKRRKLKNKRRRSLPRPHDFFDAQTLDAIRHRAICFNLSAHIESLGKGHSVVFHSTVIAKRKEDSGKIKLLLHWMPEDILPDVWVNESERHQLKTKVVHLSKLPKDTALLLDPNIYRTMPQKRLKRTLIRKVFNLYLSKQ
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:
MADKEAAFDDAVEERVINEEYKIWKKNTPFLYDLVMTHALEWPSLTAQWLPDVTRPEGKDFSIHRLVLGTHTSDEQNHLVIASVQLPNDDAQFDASHYDSEKGEFGGFGSVSGKIEIEIKINHEGEVNRARYMPQNPCIIATKTPSSDVLVFDYTKHPSKPDPSGECNPDLRLRGHQKEGYGLSWNPNLSGHLLSASDDHTICLWDISAVPKEGKVVDAKTIFTGHTAVVEDVSWHLLHESLFGSVADDQKLMIWDTRSNNTSKPSHSVDAHTAEVNCLSFNPYSEFILATGSADKTVALWDLRNLKLKLHSFESHKDEIFQVQWSPHNETILASSGTDRRLNVWDLSKIGEEQSPEDAEDGPPELLFIHGGHTAKISDFSWNPNEPWVICSVSEDNIMQVWQMAENIYNDEDPEGSVDPEGQGS
Inhibitor
Name:
BDBM225230
Synonyms:
EED226 | US11013745, Compound EED226
Type:
Small organic molecule
Emp. Form.:
C17H15N5O3S
Mol. Mass.:
369.398
SMILES:
CS(=O)(=O)c1ccc(cc1)-c1cnc(NCc2ccco2)n2cnnc12
Substrate
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:
LATKAARKSAPSTGGVKKPHRYRP