Reaction Details |
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Target | Histone deacetylase 4 [653-1084,H976Y] |
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Ligand | BDBM21709 |
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Substrate/Competitor | BDBM25143 |
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Meas. Tech. | HDAC Activity Assay |
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Temperature | 298.15±n/a K |
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IC50 | 4200±n/a nM |
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Comments | extracted |
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Citation | Jones, P; Altamura, S; De Francesco, R; Paz, OG; Kinzel, O; Mesiti, G; Monteagudo, E; Pescatore, G; Rowley, M; Verdirame, M; Steinkühler, C A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo. J Med Chem51:2350-3 (2008) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Histone deacetylase 4 [653-1084,H976Y] |
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Name: | Histone deacetylase 4 [653-1084,H976Y] |
Synonyms: | HDAC4 | HDAC4_HUMAN | Histone Deacetylase 4 (HDAC4) Mutant (H976Y) | Histone deacetylase 4 gain of function (GOF) mutant | KIAA0288 |
Type: | Catalytic domain |
Mol. Mass.: | 46476.72 |
Organism: | Homo sapiens (Human) |
Description: | His-tagged HDAC4 GOF(gain of function, H976Y) catalytic domains (T653-L1084) was expressed in E.coli and purified by Nickel-Chelation affinity chromatography and anion exchange (MonoQ) chromatography. |
Residue: | 432 |
Sequence: | TTGLVYDTLMLKHQCTCGSSSSHPEHAGRIQSIWSRLQETGLRGKCECIRGRKATLEELQ
TVHSEAHTLLYGTNPLNRQKLDSKKLLGSLASVFVRLPCGGVGVDSDTIWNEVHSAGAAR
LAVGCVVELVFKVATGELKNGFAVVRPPGHHAEESTPMGFCYFNSVAVAAKLLQQRLSVS
KILIVDWDVHHGNGTQQAFYSDPSVLYMSLHRYDDGNFFPGSGAPDEVGTGPGVGFNVNM
AFTGGLDPPMGDAEYLAAFRTVVMPIASEFAPDVVLVSSGFDAVEGHPTPLGGYNLSARC
FGYLTKQLMGLAGGRIVLALEGGYDLTAICDASEACVSALLGNELDPLPEKVLQQRPNAN
AVRSMEKVMEIHSKYWRCLQRTTSTAGRSLIEAQTCENEEAETVTAMASLSVGVKPAEKR
PDEEPMEEEPPL
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BDBM21709 |
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BDBM25143 |
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Name | BDBM21709 |
Synonyms: | 2-ethyl-1-[(3R)-1-[(5-methoxy-1H-1,3-benzodiazol-2-yl)carbonyl]pyrrolidin-3-yl]-1H-1,3-benzodiazole | benzimidazole, 18 |
Type | Small organic molecule |
Emp. Form. | C22H23N5O2 |
Mol. Mass. | 389.4503 |
SMILES | CCc1nc2ccccc2n1[C@@H]1CCN(C1)C(=O)c1nc2ccc(OC)cc2[nH]1 |r| |
Structure |
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