An EC 3.5.1.98 (histone deacetylase) inhibitor that interferes with the action of Sir2.
ChEBI ID: 71181
| Member | Definition | Class |
|---|---|---|
| fenofibrate | A benzochromenone that is 2,3-dihydro-1H-benzo[f]chromene substituted by an oxo group at position 3. It has been found to exhibit potential inhibitory activity against Sir2 proteins. | splitomicin |
| niacinamide | A pyridinecarboxamide that is pyridine in which the hydrogen at position 3 is replaced by a carboxamide group. | nicotinamide |
| sirtinol | A benzamide obtained by formal condensation of the carboxy group of 2-{[(2-hydroxy-1-naphthyl)methylene]amino}benzoic acid with the amino group of 1-phenylethylamine. | sirtinol |
| tenovin-6 | A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-(dimethylamino)pentanoic acid with the aromatic amino group of N-[(4-aminophenyl)carbamothioyl]-4-tert-butylbenzamide. | tenovin-6 |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 3,402 (26.68) | 18.7374 |
| 1990's | 1,160 (9.10) | 18.2507 |
| 2000's | 1,708 (13.40) | 29.6817 |
| 2010's | 5,476 (42.95) | 24.3611 |
| 2020's | 1,003 (7.87) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 1,097 (8.05%) | 5.53% |
| Reviews | 1,247 (9.15%) | 6.00% |
| Case Studies | 728 (5.34%) | 4.05% |
| Observational | 35 (0.26%) | 0.25% |
| Other | 10,516 (77.19%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 26.0258 | 1 | 1 |
| alpha-galactosidase | Homo sapiens (human) | Potency | 41.6060 | 2 | 3 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 28.9525 | 1 | 1 |
| Ataxin-2 | Homo sapiens (human) | Potency | 16.8966 | 1 | 1 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 16.8966 | 1 | 1 |
| caspase-3 | Cricetulus griseus (Chinese hamster) | Potency | 81.5991 | 1 | 1 |
| Caspase-7 | Cricetulus griseus (Chinese hamster) | Potency | 81.5991 | 1 | 1 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 32.4648 | 2 | 2 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 0.0025 | 1 | 2 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 32.4648 | 2 | 2 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 0.0794 | 1 | 1 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 7.9433 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 12.1080 | 1 | 2 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 53.4317 | 1 | 1 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 26.6011 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 6.5131 | 1 | 1 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 25.8390 | 2 | 3 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 29.8816 | 1 | 2 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 2.6832 | 1 | 2 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 7.9433 | 1 | 3 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 6.7016 | 1 | 1 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 53.4317 | 1 | 1 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 31.9999 | 1 | 2 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 56.2341 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Chain A, NAD-dependent deacetylase | Thermotoga maritima | IC50 | 1,000.0000 | 1 | 1 |
| Coagulation factor VII | Homo sapiens (human) | Ki | 8,000.0000 | 1 | 1 |
| Cytochrome P450 3A5 | Homo sapiens (human) | IC50 | 117.0000 | 1 | 2 |
| Fatty-acid amide hydrolase 1 | Rattus norvegicus (Norway rat) | IC50 | 3.3000 | 1 | 1 |
| Histone deacetylase | Plasmodium falciparum (malaria parasite P. falciparum) | IC50 | 10.0000 | 1 | 1 |
| Histone deacetylase 1 | Homo sapiens (human) | IC50 | 75.0000 | 1 | 1 |
| Histone deacetylase 11 | Homo sapiens (human) | IC50 | 75.0000 | 1 | 1 |
| Histone deacetylase 2 | Homo sapiens (human) | IC50 | 75.0000 | 1 | 1 |
| Histone deacetylase 3 | Homo sapiens (human) | IC50 | 75.0000 | 2 | 2 |
| Histone deacetylase 3 | Homo sapiens (human) | Ki | 75.0000 | 1 | 1 |
| Histone deacetylase 4 | Homo sapiens (human) | IC50 | 75.0000 | 1 | 1 |
| Histone deacetylase 5 | Homo sapiens (human) | IC50 | 75.0000 | 1 | 1 |
| Histone deacetylase 6 | Homo sapiens (human) | IC50 | 75.0000 | 2 | 2 |
| Histone deacetylase 6 | Homo sapiens (human) | Ki | 75.0000 | 1 | 1 |
| Histone deacetylase 7 | Homo sapiens (human) | IC50 | 75.0000 | 1 | 1 |
| Histone deacetylase 8 | Homo sapiens (human) | IC50 | 75.0000 | 1 | 1 |
| Histone deacetylase 9 | Homo sapiens (human) | IC50 | 75.0000 | 1 | 1 |
| NAD-dependent histone deacetylase SIR2 | Saccharomyces cerevisiae S288C | IC50 | 60.0000 | 5 | 5 |
| NAD-dependent protein deacetylase | Schistosoma mansoni | IC50 | 221.5500 | 2 | 2 |
| NAD-dependent protein deacetylase HST2 | Saccharomyces cerevisiae S288C | IC50 | 209.7500 | 1 | 4 |
| NAD-dependent protein deacetylase sirtuin-1 | Homo sapiens (human) | IC50 | 111.4333 | 27 | 33 |
| NAD-dependent protein deacetylase sirtuin-2 | Homo sapiens (human) | IC50 | 39.9789 | 32 | 37 |
| NAD-dependent protein deacetylase sirtuin-3, mitochondrial | Homo sapiens (human) | IC50 | 72.4550 | 10 | 10 |
| NAD-dependent protein deacetylase sirtuin-6 | Homo sapiens (human) | IC50 | 173.3500 | 4 | 4 |
| NAD-dependent protein deacylase sirtuin-5, mitochondrial | Homo sapiens (human) | IC50 | 74.7857 | 4 | 7 |
| NAD(+) hydrolase SARM1 | Homo sapiens (human) | IC50 | 43.8000 | 1 | 1 |
| Nuclear receptor corepressor 2 | Homo sapiens (human) | IC50 | 75.0000 | 1 | 1 |
| Nuclear receptor corepressor 2 | Homo sapiens (human) | Ki | 75.0000 | 1 | 1 |
| Poly [ADP-ribose] polymerase 1 | Homo sapiens (human) | IC50 | 187.0070 | 6 | 7 |
| Poly [ADP-ribose] polymerase 2 | Mus musculus (house mouse) | IC50 | 129.5245 | 1 | 2 |
| Polyamine deacetylase HDAC10 | Homo sapiens (human) | IC50 | 75.0000 | 1 | 1 |
| Protein mono-ADP-ribosyltransferase PARP15 | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| Tissue factor | Homo sapiens (human) | Ki | 8,000.0000 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| NAD-dependent histone deacetylase SIR2 | Saccharomyces cerevisiae S288C | Inhibition | 0.6600 | 1 | 1 |
| NAD-dependent histone deacetylase SIR2 | Saccharomyces cerevisiae S288C | MGC | 0.4900 | 1 | 1 |