Sirtuin

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

Sirtuin Products

All (24) Sirtuin Inhibitors (13) Sirtuin Activators (10) Sirtuin Modulators (1)

Catalog No.	Information	Product Use Citations	Product Validations
S1541	Selisistat (EX 527) Selisistat (EX 527) 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.	Hepatology, 2020, 10.1002/hep.31222 Dev Cell, 2020, 20;53(2):240-252 Aging Cell, 2020, e13164	The eect of Melatonin, luzindole, and EX527 treatment on apoptotic index, infarct size, lactate dehydrogenase (LDH) release, and CK release in IR-injured hearts. Representative photomicrographs of in situ detection of apoptotic myocytes by TUNEL staining. Green ﬂuorescence shows TUNEL-positive nuclei; blue ﬂuorescence shows nuclei of total cardiomyocytes; original magniﬁcation 9x400. Sacle bar: 100 um.
S2804	Sirtinol Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively.	Cell Death Dis, 2020, 21;11(2):141 Bone, 2020, 133:115252 Am J Transl Res, 2019, 11(8):4789-4799	Effects of sirtinol on SIRT1 expression and HIF-1α. hMSCs were treated with sirtinol (100 uM) or equivalent concentration of DMSO (CTR) for 24 h and then exposed to 1% O2 for 6 h. All cells lysates were analyzed for SIRT1, HIF-1α, and tubulin by Western blot.
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.	PLoS Pathog, 2020, 16;16(3):e1008341 Mol Cell, 2019, 73(4):788-802 Mol Cell, 2019, 73(4):788-802	Immunoprecipitation-western blot for analyzing acetylated Snail in Snail-transfected 293T cells (upper) and FaDu-Snail cells (lower) treated with a vehicle control (Ctrl), a HDAC inhibitor TSA 5 nM for 8 hr, a SIRT1 inhibitor NAM(Nicotinamide) 10 mM for 8 hr, or in combination.
S7845	SirReal2 SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.	J Cell Physiol, 2020, 10.1002 Int J Mol Sci, 2019, 20(6) J Steroid Biochem Mol Biol, 2019, 185:27-38
S2176^New	Tenovin-3 Tenovin-3 is an inhibitor of SIRT2. Tenovin-3 is able to increase p53 levels in MCF-7 cells.
S6744^New	Inauhzin Inauhzin is a cell-permeable SIRT1 inhibitor with an IC50 of 0.7-2 μM and reactivates p53 by inhibiting SIRT1 deacetylation activity.
S4900	Tenovin-6 Tenovin-6 is a small molecule activator of p53 transcriptional activity.	Biomed Pharmacother, 2020, 125:109948 J Cell Sci, 2019, 132(6) Nat Biotechnol, 2015, 10.1038/nbt.3130
S7577	AGK2 AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels.	J Med Chem, 2020, 31 Am J Physiol Lung Cell Mol Physiol, 2020, 10.1152/ajplung.00457.2019 Life Sci, 2019, 230:68-75	Masson trichrome staining of tubulointerstitium areas from Sham, UUO, UUO+AGK2 mice (original magnification: × 400).
S8245	Thiomyristoyl Thiomyristoyl is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM. It inhibits SIRT1 with an IC50 value of 98 μM and does not inhibit SIRT3 even at 200 μM.	J Cell Physiol, 2020, 10.1002
S8460	Salermide Salermide is a reverse amide with a strong in vitro inhibitory effect on Sirt1 and Sirt2. Compared with Sirt1, Salermide is even more efficient at inhibiting Sirt2.	Am J Transl Res, 2019, 11(8):4789-4799 J Proteome Res, 2018, 17(4):1436-1451
S8627	OSS_128167 OSS_128167 is a specific SIRT6 inhibitor with IC50 values of 89, 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively.	J Neuroinflammation, 2019, 16(1):47 Arthritis Res Ther, 2019, 21(1):220
S5914	AK 7 AK 7 is a brain-permeable selective SIRT2 inhibitor with an IC50 of 15.5 μM.
S8628	3-TYP 3-TYP is a selective SIRT3 inhibitor which is selective for Sirt3 over Sirt1 and Sirt2. The IC50 values for SITR1, SIRT2, SIRT3 are 88 nM, 92 nM, 16 nM respectively.	Oxid Med Cell Longev, 2020, 2020:6797154 Br J Pharmacol, 2019, 176(22):4388-4401 Br J Haematol, 2019, 187(1):49-64	Effects of HNK or 3‐TYP on surgery/anesthesia‐induced an increased expression of pro‐inflammatory cytokines in hippocampus. (A, E) Representative blots at postoperative 1 and 3 d, respectively. (B, F) MCP‐1 relative expression. (C, G) TNF‐α relative expression. (D, H) IL‐1β relative expression. The data are presented as the mean ±standard error of the mean for each group (n = 6 per group). *P < 0.05 vs the control group; #P < 0.05 vs the surgery+vehicle group; $P < 0.05 vs the honokiol group
S1129	SRT1720 HCl SRT1720 HCl 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. SRT1720 induces autophagy.	Redox Biol, 2020, 28:101356 Antioxid Redox Signal, 2020, 7 J Med Chem, 2020, 31	PAI-1 expression in HUVECs treated with drugs as indicated.(D) senescent HUVECs were treated with SRT1720, culturing for 24, 48 hours. PAI-1 mRNA and protein (E) levels were analyzed using real-time RT–PCR and Western blotting, respectively. The RNA and protein levels were normalized to the internal control β-actin. Data are presented as the mean±SEM of three independent experiments. P < 0.05 vs. corresponding control. P < 0.01 vs. corresponding control **P < 0.001 vs. corresponding control.
S8909^New	UBCS039 UBCS039 is the first synthetic SIRT6 activator with EC50 of 38 μM,induces a time-dependent activation of autophagy in several human tumor cell lines.
S2935^New	Nicotinamide Riboside Chloride (NIAGEN) Nicotinamide Riboside Chloride (NIAGEN) is the chloride salt form of nicotinamide riboside(NR).NR is a new form pyridine-nucleoside of vitamin B3 that functions as a precursor to nicotinamide adenine dinucleotide(NAD) or NAD⁺ .NIAGEN is generally recognized as safe (GRAS) in the United States for use in food products. Nicotinamide riboside chloride is a crystal form of Nicotinamide riboside (NR) chloride. Nicotinamide riboside chloride increases NAD[+] levels and activates SIRT1 and SIRT3, culminating in enhanced oxidative metabolism and protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside chloride is used in dietary supplements.
S4735	Salvianolic acid B Salvianolic acid B (Sal B), an antioxidant and free radical scavenging compound, is the most abundant bioactive compound extracted from the root of Salvia miltiorrhiza Bunge.	J Cell Mol Med, 2020, 29
S8270	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.	Hepatology, 2020, 10.1002/hep.31222 Cancer Res, 2020, 4 pii: canres Aging Cell, 2020, 19(6):e13163
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.	Cell Res, 2020, 27;1-16 Stem Cell Res Ther, 2020, 11(1):270 Front Oncol, 2020, 10;10:331	After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of Quercetin for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
S2298	Fisetin Fisetin (Fustel) is a potent sirtuin activating compound (STAC) and an agent that modulates sirtuins.	Cell Res, 2020, 27;1-16 BMC Cancer, 2020, 20(1):4 Drug Des Devel Ther, 2020, 14:773-782	Liver pathology and serum markers of liver injury in mice fed control (Ctrl), or ethanol (EtOH), or ethanol combined with fisetin (E/Fisetin) diet for 4 weeks. (A) Light microscopy with hematoxylin and eosin staining shows lipid accumulation (arrows) in the liver of mice after alcohol exposure, which was alleviated by fisetin administration. (B) Plasma alanine aminotransferase (ALT) and (C) aspartate aminotransferase (AST) activities. Infinity ALT and AST reagents were used formeasuring ALT and AST activities. Scale bar: 50 lm. Results are mean±SD (n = 3 to 6). Results for bars that do not share a letter differed significantly among groups (p < 0.05). Significant differences among groups are determined by analysis of variance followed by Tukey’s test.
S5918	CAY10602 CAY10602 is a potent SIRT1 activator.	J Med Chem, 2020, 31
S8481	SRT3025 HCl SRT3025 is an orally available small molecule activator of the SIRT1 enzyme.	Aging Cell, 2020, e13164 Acta Haematol, 2019, 142(3):142-148
S2347	Quercetin Dihydrate Quercetin, a polyphenolic flavonoid found in a wide variety of plant-based foods, such as apples, onions, berries, and red wine, is utilized in many different cultures for their nervous system and anticancer effects. Quercetin (dihydrate), a natural flavonoid, is a stimulator of recombinant SIRT1 and a PI3K inhibitor with IC50s of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.	Biomed Pharmacother, 2020, 127:110205	After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of Quercetin for 3h,followed by 20-minute stimolation of 100ng/ml EGF.

Catalog No.	Information	Product Use Citations	Product Validations
S1541	Selisistat (EX 527) Selisistat (EX 527) 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.	Hepatology, 2020, 10.1002/hep.31222 Dev Cell, 2020, 20;53(2):240-252 Aging Cell, 2020, e13164	The eect of Melatonin, luzindole, and EX527 treatment on apoptotic index, infarct size, lactate dehydrogenase (LDH) release, and CK release in IR-injured hearts. Representative photomicrographs of in situ detection of apoptotic myocytes by TUNEL staining. Green ﬂuorescence shows TUNEL-positive nuclei; blue ﬂuorescence shows nuclei of total cardiomyocytes; original magniﬁcation 9x400. Sacle bar: 100 um.
S2804	Sirtinol Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively.	Cell Death Dis, 2020, 21;11(2):141 Bone, 2020, 133:115252 Am J Transl Res, 2019, 11(8):4789-4799	Effects of sirtinol on SIRT1 expression and HIF-1α. hMSCs were treated with sirtinol (100 uM) or equivalent concentration of DMSO (CTR) for 24 h and then exposed to 1% O2 for 6 h. All cells lysates were analyzed for SIRT1, HIF-1α, and tubulin by Western blot.
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.	PLoS Pathog, 2020, 16;16(3):e1008341 Mol Cell, 2019, 73(4):788-802 Mol Cell, 2019, 73(4):788-802	Immunoprecipitation-western blot for analyzing acetylated Snail in Snail-transfected 293T cells (upper) and FaDu-Snail cells (lower) treated with a vehicle control (Ctrl), a HDAC inhibitor TSA 5 nM for 8 hr, a SIRT1 inhibitor NAM(Nicotinamide) 10 mM for 8 hr, or in combination.
S7845	SirReal2 SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.	J Cell Physiol, 2020, 10.1002 Int J Mol Sci, 2019, 20(6) J Steroid Biochem Mol Biol, 2019, 185:27-38
S2176^New	Tenovin-3 Tenovin-3 is an inhibitor of SIRT2. Tenovin-3 is able to increase p53 levels in MCF-7 cells.
S6744^New	Inauhzin Inauhzin is a cell-permeable SIRT1 inhibitor with an IC50 of 0.7-2 μM and reactivates p53 by inhibiting SIRT1 deacetylation activity.
S4900	Tenovin-6 Tenovin-6 is a small molecule activator of p53 transcriptional activity.	Biomed Pharmacother, 2020, 125:109948 J Cell Sci, 2019, 132(6) Nat Biotechnol, 2015, 10.1038/nbt.3130
S7577	AGK2 AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels.	J Med Chem, 2020, 31 Am J Physiol Lung Cell Mol Physiol, 2020, 10.1152/ajplung.00457.2019 Life Sci, 2019, 230:68-75	Masson trichrome staining of tubulointerstitium areas from Sham, UUO, UUO+AGK2 mice (original magnification: × 400).
S8245	Thiomyristoyl Thiomyristoyl is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM. It inhibits SIRT1 with an IC50 value of 98 μM and does not inhibit SIRT3 even at 200 μM.	J Cell Physiol, 2020, 10.1002
S8460	Salermide Salermide is a reverse amide with a strong in vitro inhibitory effect on Sirt1 and Sirt2. Compared with Sirt1, Salermide is even more efficient at inhibiting Sirt2.	Am J Transl Res, 2019, 11(8):4789-4799 J Proteome Res, 2018, 17(4):1436-1451
S8627	OSS_128167 OSS_128167 is a specific SIRT6 inhibitor with IC50 values of 89, 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively.	J Neuroinflammation, 2019, 16(1):47 Arthritis Res Ther, 2019, 21(1):220
S5914	AK 7 AK 7 is a brain-permeable selective SIRT2 inhibitor with an IC50 of 15.5 μM.
S8628	3-TYP 3-TYP is a selective SIRT3 inhibitor which is selective for Sirt3 over Sirt1 and Sirt2. The IC50 values for SITR1, SIRT2, SIRT3 are 88 nM, 92 nM, 16 nM respectively.	Oxid Med Cell Longev, 2020, 2020:6797154 Br J Pharmacol, 2019, 176(22):4388-4401 Br J Haematol, 2019, 187(1):49-64	Effects of HNK or 3‐TYP on surgery/anesthesia‐induced an increased expression of pro‐inflammatory cytokines in hippocampus. (A, E) Representative blots at postoperative 1 and 3 d, respectively. (B, F) MCP‐1 relative expression. (C, G) TNF‐α relative expression. (D, H) IL‐1β relative expression. The data are presented as the mean ±standard error of the mean for each group (n = 6 per group). *P < 0.05 vs the control group; #P < 0.05 vs the surgery+vehicle group; $P < 0.05 vs the honokiol group

Catalog No.	Information	Product Use Citations	Product Validations
S1129	SRT1720 HCl SRT1720 HCl 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. SRT1720 induces autophagy.	Redox Biol, 2020, 28:101356 Antioxid Redox Signal, 2020, 7 J Med Chem, 2020, 31	PAI-1 expression in HUVECs treated with drugs as indicated.(D) senescent HUVECs were treated with SRT1720, culturing for 24, 48 hours. PAI-1 mRNA and protein (E) levels were analyzed using real-time RT–PCR and Western blotting, respectively. The RNA and protein levels were normalized to the internal control β-actin. Data are presented as the mean±SEM of three independent experiments. P < 0.05 vs. corresponding control. P < 0.01 vs. corresponding control **P < 0.001 vs. corresponding control.
S8909^New	UBCS039 UBCS039 is the first synthetic SIRT6 activator with EC50 of 38 μM,induces a time-dependent activation of autophagy in several human tumor cell lines.
S2935^New	Nicotinamide Riboside Chloride (NIAGEN) Nicotinamide Riboside Chloride (NIAGEN) is the chloride salt form of nicotinamide riboside(NR).NR is a new form pyridine-nucleoside of vitamin B3 that functions as a precursor to nicotinamide adenine dinucleotide(NAD) or NAD⁺ .NIAGEN is generally recognized as safe (GRAS) in the United States for use in food products. Nicotinamide riboside chloride is a crystal form of Nicotinamide riboside (NR) chloride. Nicotinamide riboside chloride increases NAD[+] levels and activates SIRT1 and SIRT3, culminating in enhanced oxidative metabolism and protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside chloride is used in dietary supplements.
S4735	Salvianolic acid B Salvianolic acid B (Sal B), an antioxidant and free radical scavenging compound, is the most abundant bioactive compound extracted from the root of Salvia miltiorrhiza Bunge.	J Cell Mol Med, 2020, 29
S8270	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.	Hepatology, 2020, 10.1002/hep.31222 Cancer Res, 2020, 4 pii: canres Aging Cell, 2020, 19(6):e13163
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.	Cell Res, 2020, 27;1-16 Stem Cell Res Ther, 2020, 11(1):270 Front Oncol, 2020, 10;10:331	After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of Quercetin for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
S2298	Fisetin Fisetin (Fustel) is a potent sirtuin activating compound (STAC) and an agent that modulates sirtuins.	Cell Res, 2020, 27;1-16 BMC Cancer, 2020, 20(1):4 Drug Des Devel Ther, 2020, 14:773-782	Liver pathology and serum markers of liver injury in mice fed control (Ctrl), or ethanol (EtOH), or ethanol combined with fisetin (E/Fisetin) diet for 4 weeks. (A) Light microscopy with hematoxylin and eosin staining shows lipid accumulation (arrows) in the liver of mice after alcohol exposure, which was alleviated by fisetin administration. (B) Plasma alanine aminotransferase (ALT) and (C) aspartate aminotransferase (AST) activities. Infinity ALT and AST reagents were used formeasuring ALT and AST activities. Scale bar: 50 lm. Results are mean±SD (n = 3 to 6). Results for bars that do not share a letter differed significantly among groups (p < 0.05). Significant differences among groups are determined by analysis of variance followed by Tukey’s test.
S5918	CAY10602 CAY10602 is a potent SIRT1 activator.	J Med Chem, 2020, 31
S8481	SRT3025 HCl SRT3025 is an orally available small molecule activator of the SIRT1 enzyme.	Aging Cell, 2020, e13164 Acta Haematol, 2019, 142(3):142-148

Catalog No.	Information	Product Use Citations	Product Validations
S2347	Quercetin Dihydrate Quercetin, a polyphenolic flavonoid found in a wide variety of plant-based foods, such as apples, onions, berries, and red wine, is utilized in many different cultures for their nervous system and anticancer effects. Quercetin (dihydrate), a natural flavonoid, is a stimulator of recombinant SIRT1 and a PI3K inhibitor with IC50s of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.	Biomed Pharmacother, 2020, 127:110205	After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of Quercetin for 3h,followed by 20-minute stimolation of 100ng/ml EGF.

Catalog No.

Information

Product Use Citations

Product Validations

S2347

Quercetin Dihydrate

Quercetin, a polyphenolic flavonoid found in a wide variety of plant-based foods, such as apples, onions, berries, and red wine, is utilized in many different cultures for their nervous system and anticancer effects. Quercetin (dihydrate), a natural flavonoid, is a stimulator of recombinant SIRT1 and a PI3K inhibitor with IC50s of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.

Biomed Pharmacother, 2020, 127:110205