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TargetHistone deacetylase
LigandBDBM29603
Substrate/CompetitorpfHDAC-1 Substrate
Meas. Tech.pfHDAC-1 Enzyme Assay
pH7.5±n/a
Temperature296.15±n/a K
IC50 36±6 nM
Km30000±2000 nM
kcat0.19±0.01 1/sec
Citation Patel, VMazitschek, RColeman, BNguyen, CUrgaonkar, SCortese, JBarker, RHGreenberg, ETang, WBradner, JESchreiber, SLDuraisingh, MTWirth, DFClardy, J Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum. J Med Chem52:2185-7 (2009) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
Histone deacetylase
Name:Histone deacetylase
Synonyms:Histone Deacetylase (pfHDAC-1)
Type:Enzyme
Mol. Mass.:51371.91
Organism:Plasmodium falciparum (isolate 3D7)
Description:Assays were performed using recombinant pfHDAC-1 expressed and purified from S2 insect cells.
Residue:449
Sequence:
MSNRKKVAYFHDPDIGSYYYGAGHPMKPQRIRMTHSLIVSYNLYKYMEVYRPHKSDVNEL
TLFHDYEYIDFLSSISLENYREFTYQLKRFNVGEATDCPVFDGLFQFQQSCAGASIDGAS
KLNHHCADICVNWSGGLHHAKMSEASGFCYINDIVLGILELLKYHARVMYIDIDVHHGDG
VEEAFYVTHRVMTVSFHKFGDYFPGTGDITDVGVNHGKYYSVNVPLNDGMTDDAFVDLFK
VVIDKCVQTYRPGAIIIQCGADSLTGDRLGRFNLTIKGHARCVEHVRSYNIPLLVLGGGG
YTIRNVSRCWAYETGVVLNKHHEMPDQISLNDYYDYYAPDFQLHLQPSNIPNYNSPEHLS
RIKMKIAENLRHIEHAPGVQFSYVPPDFFNSDIDDESDKNQYELKDDSGGGRAPGTRAKE
HSTTHHLRRKNYDDDFFDLSDRDQSIVPY
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM29603
pfHDAC-1 Substrate
Name:pfHDAC-1 Substrate
Synonyms:n/a
Type:fluorogenic, acetylated peptide
Mol. Mass.:1609.93
Organism:n/a
Description:n/a
Residue:15
Sequence:
Ac-Leu-Gly-Lys (Ac)-AMC