Sirtuin

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S1541

EX 527 (Selisistat)

EX 527 (Selisistat) is a potent and selective SIRT1 inhibitor with IC50 of 38 nM in a cell-free assay, exhibits >200-fold selectivity against SIRT2 and SIRT3. Phase 2.

S2804

Sirtinol

Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively.

S1899

Nicotinamide (Vitamin B3)

Nicotinamide (Vitamin B3), a water-soluble vitamin, is an active component of coenzymes NAD and NADP, and also act as an inhibitor of sirtuins.

S7845

SirReal2

SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.

S4900

Tenovin-6

Tenovin-6 is a small molecule activator of p53 transcriptional activity.

S7577

AGK2

AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM.

S7593

Splitomicin

Splitomicin is a selective NAD(+)-dependent histone deacetylase Sir2p inhibitor with IC50 of 60 μM, showing a higher activity in a cell-based assay.

S1129

SRT1720

SRT1720 is a selective SIRT1 activator with EC50 of 0.16 μM in a cell-free assay, but is >230-fold less potent for SIRT2 and SIRT3.

S1396

Resveratrol

Resveratrol is a phytoalexin produced naturally by several plants with anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects.

S8270New

SRT2183

SRT2183 is a small-molecule activator of the sirtuin subtype SIRT1, currently being developed by Sirtris Pharmaceuticals.

S7792

SRT2104 (GSK2245840)

SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.

S2391

Quercetin

Quercetin, a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Phase 4.

S2298

Fisetin

Fisetin (Fustel) is a potent sirtuin activating compound (STAC) and an agent that modulates sirtuins.

Catalog No. Information Product Use Citations Product Validations
S1541

EX 527 (Selisistat)

EX 527 (Selisistat) is a potent and selective SIRT1 inhibitor with IC50 of 38 nM in a cell-free assay, exhibits >200-fold selectivity against SIRT2 and SIRT3. Phase 2.

S2804

Sirtinol

Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively.

S1899

Nicotinamide (Vitamin B3)

Nicotinamide (Vitamin B3), a water-soluble vitamin, is an active component of coenzymes NAD and NADP, and also act as an inhibitor of sirtuins.

S7845

SirReal2

SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.

S4900

Tenovin-6

Tenovin-6 is a small molecule activator of p53 transcriptional activity.

S7577

AGK2

AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM.

S7593

Splitomicin

Splitomicin is a selective NAD(+)-dependent histone deacetylase Sir2p inhibitor with IC50 of 60 μM, showing a higher activity in a cell-based assay.

Catalog No. Information Product Use Citations Product Validations
S1129

SRT1720

SRT1720 is a selective SIRT1 activator with EC50 of 0.16 μM in a cell-free assay, but is >230-fold less potent for SIRT2 and SIRT3.

2015, 10.1038/nm.3821

2013, 32(6):791-804

2013, 74(1):298-308

S1396

Resveratrol

Resveratrol is a phytoalexin produced naturally by several plants with anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects.

2016,

2016, 1859(2):294-305

2015, 35(6):2255-2271

S8270New

SRT2183

SRT2183 is a small-molecule activator of the sirtuin subtype SIRT1, currently being developed by Sirtris Pharmaceuticals.

S7792

SRT2104 (GSK2245840)

SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.

S2391

Quercetin

Quercetin, a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Phase 4.

S2298

Fisetin

Fisetin (Fustel) is a potent sirtuin activating compound (STAC) and an agent that modulates sirtuins.

2016, 40(10):2076-2084

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