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Target
NAD-dependent protein deacetylase sirtuin-1
Ligand
BDBM29041
Substrate
Fluor de Lys-SIRT1
Meas. Tech.
Enzyme Inhibition Assay
pH
8±n/a
Temperature
310.15±n/a K
Comments
15.5 +/- 2 % inhibition @ 60 uM.
Citation
 Medda, F; Russell, RJ; Higgins, M; McCarthy, AR; Campbell, J; Slawin, AM; Lane, DP; Lain, S; Westwood, NJ Novel cambinol analogs as sirtuin inhibitors: synthesis, biological evaluation, and rationalization of activity. J Med Chem 52:2673-82 (2009) [PubMed]  Article 
Target
Name:
NAD-dependent protein deacetylase sirtuin-1
Synonyms:
NAD-Dependent Deacetylase Sirtuin-1 | NAD-dependent deacetylase sirtuin 1 | NAD-dependent protein deacetylase sirtuin-1 (SIRT1) | SIR1_HUMAN | SIR2-like protein 1 | SIR2L1 | SIRT1 | Sirtuin 1 (SIRT1) | Sirtuin-1 (SIRT1) | hSIR2
Type:
Developmental protein; hydrolase
Mol. Mass.:
81626.66
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
747
Sequence:
MADEAALALQPGGSPSAAGADREAASSPAGEPLRKRPRRDGPGLERSPGEPGGAAPEREVPAAARGCPGAAAAALWREAEAEAAAAGGEQEAQATAAAGEGDNGPGLQGPSREPPLADNLYDEDDDDEGEEEEEAAAAAIGYRDNLLFGDEIITNGFHSCESDEEDRASHASSSDWTPRPRIGPYTFVQQHLMIGTDPRTILKDLLPETIPPPELDDMTLWQIVINILSEPPKRKKRKDINTIEDAVKLLQECKKIIVLTGAGVSVSCGIPDFRSRDGIYARLAVDFPDLPDPQAMFDIEYFRKDPRPFFKFAKEIYPGQFQPSLCHKFIALSDKEGKLLRNYTQNIDTLEQVAGIQRIIQCHGSFATASCLICKYKVDCEAVRGDIFNQVVPRCPRCPADEPLAIMKPEIVFFGENLPEQFHRAMKYDKDEVDLLIVIGSSLKVRPVALIPSSIPHEVPQILINREPLPHLHFDVELLGDCDVIINELCHRLGGEYAKLCCNPVKLSEITEKPPRTQKELAYLSELPPTPLHVSEDSSSPERTSPPDSSVIVTLLDQAAKSNDDLDVSESKGCMEEKPQEVQTSRNVESIAEQMENPDLKNVGSSTGEKNERTSVAGTVRKCWPNRVAKEQISRRLDGNQYLFLPPNRYIFHGAEVYSDSEDDVLSSSSCGSNSDSGTCQSPSLEEPMEDESEIEEFYNGLEDEPDVPERAGGAGFGTDGDDQEAINEAISVKQEVTDMNYPSNKS
  
Inhibitor
Name:
BDBM29041
Synonyms:
cambinol analog, 6a
Type:
Small organic molecule
Emp. Form.:
C21H16N2O3
Mol. Mass.:
344.3633
SMILES:
Oc1ccc2ccccc2c1Cc1c([nH]c(=O)[nH]c1=O)-c1ccccc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Fluor de Lys-SIRT1
Synonyms:
n/a
Type:
fluorogenic, acetylated peptide
Mol. Mass.:
1542.25
Organism:
n/a
Description:
Based on residues 379-382 of p53.
Residue:
14
Sequence:
ARGHISLYSLYSAC