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TargetLysine-specific demethylase 4A (KDM4A)
LigandBDBM191599
Substrate/Competitorn/a
Meas. Tech.AlphaScreen Assay
IC50 1e+4±3.0e+3 nM
Citation Tumber ANuzzi AHookway ESHatch SBVelupillai SJohansson CKawamura ASavitsky PYapp CSzykowska AWu NBountra CStrain-Damerell CBurgess-Brown NARuda GFFedorov OMunro SEngland KSNowak RPSchofield CJLa Thangue NBPawlyn CDavies FMorgan GAthanasou NMüller SOppermann UBrennan PE Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells. Cell Chem Biol 24:371-380 (2017) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Lysine-specific demethylase 4A (KDM4A)
Name:Lysine-specific demethylase 4A
Synonyms:JmjC domain-containing histone demethylation protein 3A | Jumonji domain-containing protein 2A | Lysine-specific demethylase 4A
Type:Enzyme
Mol. Mass.:120647.83
Organism:Homo sapiens (Human)
Description:O75164
Residue:1064
Sequence:
MASESETLNPSARIMTFYPTMEEFRNFSRYIAYIESQGAHRAGLAKVVPPKEWKPRASYD
DIDDLVIPAPIQQLVTGQSGLFTQYNIQKKAMTVREFRKIANSDKYCTPRYSEFEELERK
YWKNLTFNPPIYGADVNGTLYEKHVDEWNIGRLRTILDLVEKESGITIEGVNTPYLYFGM
WKTSFAWHTEDMDLYSINYLHFGEPKSWYSVPPEHGKRLERLAKGFFPGSAQSCEAFLRH
KMTLISPLMLKKYGIPFDKVTQEAGEFMITFPYGYHAGFNHGFNCAESTNFATRRWIEYG
KQAVLCSCRKDMVKISMDVFVRKFQPERYKLWKAGKDNTVIDHTLPTPEAAEFLKESELP
PRAGNEEECPEEDMEGVEDGEEGDLKTSLAKHRIGTKRHRVCLEIPQEVSQSELFPKEDL
SSEQYEMTECPAALAPVRPTHSSVRQVEDGLTFPDYSDSTEVKFEELKNVKLEEEDEEEE
QAAAALDLSVNPASVGGRLVFSGSKKKSSSSLGSGSSRDSISSDSETSEPLSCRAQGQTG
VLTVHSYAKGDGRVTVGEPCTRKKGSAARSFSERELAEVADEYMFSLEENKKSKGRRQPL
SKLPRHHPLVLQECVSDDETSEQLTPEEEAEETEAWAKPLSQLWQNRPPNFEAEKEFNET
MAQQAPHCAVCMIFQTYHQVEFGGFNQNCGNASDLAPQKQRTKPLIPEMCFTSTGCSTDI
NLSTPYLEEDGTSILVSCKKCSVRVHASCYGVPPAKASEDWMCSRCSANALEEDCCLCSL
RGGALQRANDDRWVHVSCAVAILEARFVNIAERSPVDVSKIPLPRFKLKCIFCKKRRKRT
AGCCVQCSHGRCPTAFHVSCAQAAGVMMQPDDWPFVVFITCFRHKIPNLERAKGALQSIT
AGQKVISKHKNGRFYQCEVVRLTTETFYEVNFDDGSFSDNLYPEDIVSQDCLQFGPPAEG
EVVQVRWTDGQVYGAKFVASHPIQMYQVEFEDGSQLVVKRDDVYTLDEELPKRVKSRLSV
ASDMRFNEIFTEKEVKQEKKRQRVINSRYREDYIEPALYRAIME
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  Blast E-value cutoff:
BDBM191599
n/a
NameBDBM191599
Synonyms:KDOAM-21 | ethyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate (KDM5-C70)
TypeSmall organic molecule
Emp. Form.C17H28N4O3
Mol. Mass.336.4292
SMILESCCOC(=O)c1ccnc(CNCC(=O)N(CC)CCN(C)C)c1
Structure
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