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Target
Fatty acid synthase [2202-2509]
Ligand
BDBM24984
Substrate
BDBM24568
Meas. Tech.
Fluorogenic Assay for Detection of FASTE Inhibition
pH
7.5±n/a
Temperature
310.15±n/a K
Ki
380±100 nM
Citation
 Richardson, RD; Smith, JW Novel antagonists of the thioesterase domain of human fatty acid synthase. Mol Cancer Ther 6:2120-6 (2007) [PubMed]  Article 
Target
Name:
Fatty acid synthase [2202-2509]
Synonyms:
FAS | FASN | FAS_HUMAN | Fatty Acid Synthase
Type:
Thioesterase domain
Mol. Mass.:
33927.11
Organism:
Homo sapiens (Human)
Description:
The recombinant thioesterase domain (residues 2202-2509) of FAS was cloned and expressed in Escheria coli. The thioesterase was purified by Ni-affinity chromatography, and analyzed for activity and inhibition by Orlistat.
Residue:
308
Sequence:
CPTPKEDGLAQQQTQLNLRSLLVNPEGPTLMRLNSVQSSERPLFLVHPIEGSTTVFHSLASRLSIPTYGLQCTRAAPLDSIHSLAAYYIDCIRQVQPEGPYRVAGYSYGACVAFEMCSQLQAQQSPAPTHNSLFLFDGSPTYVLAYTQSYRAKLTPGCEAEAETEAICFFVQQFTDMEHNRVLEALLPLKGLEERVAAAVDLIIKSHQGLDRQELSFAARSFYYKLRAAEQYTPKAKYHGNVMLLRAKTGGAYGEDLGADYNLSQVCDGKVSVHVIEGDHRTLLEGSGLESIISIIHSSLAEPRVSVR
  
Inhibitor
Name:
BDBM24984
Synonyms:
(5E)-1-(3,5-dimethylphenyl)-5-[(5-phenylfuran-2-yl)methylidene]-1,3-diazinane-2,4,6-trione | 5-(furan-2-ylmethylene) pyrimidine-2,4,6-trione derivative, 1
Type:
Small organic molecule
Emp. Form.:
C23H18N2O4
Mol. Mass.:
386.4
SMILES:
Cc1cc(C)cc(c1)N1C(=O)NC(=O)C(=Cc2ccc(o2)-c2ccccc2)C1=O |w:15.16|
Structure:
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Substrate
Name:
BDBM24568
Synonyms:
4-methyl-2-oxo-2H-chromen-7-yl heptanoate | 4-methylumbelliferyl heptanoate (4-MUH)
Type:
fluorogenic substrate
Emp. Form.:
C17H20O4
Mol. Mass.:
288.3383
SMILES:
CCCCCCC(=O)Oc1ccc2c(C)cc(=O)oc2c1
Structure:
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