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Target
Histone deacetylase 8
Ligand
BDBM19410
Substrate
Fluor de Lys-HDAC8 Fluorogenic Deacetylase Substrate
Meas. Tech.
HDAC Activity Assay
pH
8±n/a
Temperature
310.15±n/a K
IC50
>10000±n/a nM
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 Chem 51:2350-3 (2008) [PubMed] Article
More Info.:
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:
BDBM19410
Synonyms:
CHEMBL27759 | MS-275 | US11377423, MS-275 | US11672788, Compound Entinostat | US9265734, MS-275 | US9796664, Compound MS-275 | benzamide-type inhibitor, 3 | pyridin-3-ylmethyl N-({4-[(2-aminophenyl)carbamoyl]phenyl}methyl)carbamate
Type:
Small organic molecule
Emp. Form.:
C21H20N4O3
Mol. Mass.:
376.4085
SMILES:
Nc1ccccc1NC(=O)c1ccc(CNC(=O)OCc2cccnc2)cc1
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