Reaction Details Report a problem with these data
Target
Histone deacetylase 4 [653-1084,H976Y]
Ligand
BDBM25150
Substrate
BDBM25143
Meas. Tech.
HDAC Activity Assay
pH
7.5±n/a
Temperature
310.15±n/a K
IC50
24±n/a nM
Citation
Jones, P; Altamura, S; De Francesco, R; Gallinari, P; Lahm, A; Neddermann, P; Rowley, M; Serafini, S; Steinkühler, C Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases. Bioorg Med Chem Lett 18:1814-9 (2008) [PubMed] Article
Target
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:
TTGLVYDTLMLKHQCTCGSSSSHPEHAGRIQSIWSRLQETGLRGKCECIRGRKATLEELQTVHSEAHTLLYGTNPLNRQKLDSKKLLGSLASVFVRLPCGGVGVDSDTIWNEVHSAGAARLAVGCVVELVFKVATGELKNGFAVVRPPGHHAEESTPMGFCYFNSVAVAAKLLQQRLSVSKILIVDWDVHHGNGTQQAFYSDPSVLYMSLHRYDDGNFFPGSGAPDEVGTGPGVGFNVNMAFTGGLDPPMGDAEYLAAFRTVVMPIASEFAPDVVLVSSGFDAVEGHPTPLGGYNLSARCFGYLTKQLMGLAGGRIVLALEGGYDLTAICDASEACVSALLGNELDPLPEKVLQQRPNANAVRSMEKVMEIHSKYWRCLQRTTSTAGRSLIEAQTCENEEAETVTAMASLSVGVKPAEKRPDEEPMEEEPPL
Inhibitor
Name:
BDBM25150
Synonyms:
(2E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide | Belinosta | Belinostat | PXD-101 | PXD101
Type:
Small organic molecule
Emp. Form.:
C15H14N2O4S
Mol. Mass.:
318.348
SMILES:
ONC(=O)\C=C\c1cccc(c1)S(=O)(=O)Nc1ccccc1