Target
Histone deacetylase 8
Ligand
BDBM27178
Substrate
Fluor de Lys-HDAC8 Fluorogenic Deacetylase Substrate
Meas. Tech.
HDAC Activity Assay
pH
8±n/a
Temperature
310.15±n/a K
IC50
3740±n/a nM
Citation
 Oyelere, AKChen, PCGuerrant, WMwakwari, SCHood, RZhang, YFan, Y Non-peptide macrocyclic histone deacetylase inhibitors. J Med Chem 52:456-68 (2009) [PubMed]  Article 
Target
Name:
Histone deacetylase 8
Synonyms:
HD8 | HDAC8 | HDAC8_HUMAN | HDACL1 | Histone deacetylase 8 (HDAC-8) | Human HDAC8
Type:
Enzyme
Mol. Mass.:
41749.60
Organism:
Homo sapiens (Human)
Description:
Q9BY41
Residue:
377
Sequence:
MEEPEEPADSGQSLVPVYIYSPEYVSMCDSLAKIPKRASMVHSLIEAYALHKQMRIVKPKVASMEEMATFHTDAYLQHLQKVSQEGDDDHPDSIEYGLGYDCPATEGIFDYAAAIGGATITAAQCLIDGMCKVAINWSGGWHHAKKDEASGFCYLNDAVLGILRLRRKFERILYVDLDLHHGDGVEDAFSFTSKVMTVSLHKFSPGFFPGTGDVSDVGLGKGRYYSVNVPIQDGIQDEKYYQICESVLKEVYQAFNPKAVVLQLGADTIAGDPMCSFNMTPVGIGKCLKYILQWQLATLILGGGGYNLANTARCWTYLTGVILGKTLSSEIPDHEFFTAYGPDYVLEITPSCRPDRNEPHRIQQILNYIKGNLKHVV
  
Inhibitor
Name:
BDBM27178
Synonyms:
6-{4-[4-({[(2S,3R,4S,6R)-2-{[(2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-2-ethyl-3,4,10,13-tetrahydroxy-3,5,6,8,10,12,14-heptamethyl-15-oxo-1-oxa-6-azacyclopentadecan-11-yl]oxy}-3-hydroxy-6-methyloxan-4-yl](methyl)amino}methyl)phenyl]-1H-1,2,3-triazol-1-yl}-N-hydroxyhexanamide | triazole-linked azithromycin-based compound, 16b
Type:
n/a
Emp. Form.:
C44H74N6O11
Mol. Mass.:
863.092
SMILES:
CC[C@H]1OC(=O)[C@H](C)[C@@H](O)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@@H]([C@H]2O)N(C)Cc2ccc(cc2)-c2cn(CCCCCC(=O)NO)nn2)[C@](C)(O)C[C@@H](C)CN(C)[C@H](C)[C@@H](O)[C@]1(C)O
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Fluor de Lys-HDAC8 Fluorogenic Deacetylase Substrate
Synonyms:
n/a
Type:
fluorogenic, diacetylated peptide
Mol. Mass.:
1716.47
Organism:
n/a
Description:
Residues 379-382 of p53.
Residue:
16
Sequence:
ARGHISLYSACLYSAC