Sirtuin
Signaling Pathway Map
Research Area
Inhibitory Selectivity
Isoform-specific Inhibitors
Sirtuin Products
| 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. |
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.
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| S2804 |
SirtinolSirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively. |
Effects of Cap pretreatment with or without coadministration of sirtinol on the activities of caspase-3 in the rat primary cardiomyocytes after A/R. A/R induced a significant increase in the activities of caspase-3. Cap significantly decreased the change in the activities of caspase-3 caused by A/R, and sirtinol significantly blocked the effects of Cap. Values were expressed as the mean ± SEM (n = 6). ∗∗P < 0.01 versus the control group; ▲▲P < 0.01 versus the A/R group; ##P < 0.01 versus the Cap + A/R group.
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| 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. |
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. |
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| S7845 |
SirReal2SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM. |
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| S5914New |
AK 7AK 7 is a brain-permeable selective SIRT2 inhibitor with an IC50 of 15.5 μM. |
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| S4900 |
Tenovin-6Tenovin-6 is a small molecule activator of p53 transcriptional activity. |
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| S7577 |
AGK2AGK2 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. |
Masson trichrome staining of tubulointerstitium areas from Sham, UUO, UUO+AGK2 mice (original magnification: × 400).
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| S8245 |
ThiomyristoylThiomyristoyl 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. |
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| S8460 |
SalermideSalermide 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. |
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| S8627 |
OSS_128167OSS_128167 is a specific SIRT6 inhibitor with IC50 values of 89, 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively. |
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| S8628 |
3-TYP3-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. |
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
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| S1129 |
SRT1720 HClSRT1720 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. |
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| S5918New |
CAY10602CAY10602 is a potent SIRT1 activator. |
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| S4735 |
Salvianolic acid BSalvianolic 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. |
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| S8270 |
SRT2183SRT2183 is a small-molecule activator of the sirtuin subtype SIRT1, currently being developed by Sirtris Pharmaceuticals. |
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| S7792 |
SRT2104 (GSK2245840)SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2. |
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| S2391 |
QuercetinQuercetin, 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. |
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. |
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| S2298 |
FisetinFisetin (Fustel) is a potent sirtuin activating compound (STAC) and an agent that modulates sirtuins. |
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.
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| S8481 |
SRT3025 HClSRT3025 is an orally available small molecule activator of the SIRT1 enzyme. |
| 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. |
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 |
SirtinolSirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively. |
Effects of Cap pretreatment with or without coadministration of sirtinol on the activities of caspase-3 in the rat primary cardiomyocytes after A/R. A/R induced a significant increase in the activities of caspase-3. Cap significantly decreased the change in the activities of caspase-3 caused by A/R, and sirtinol significantly blocked the effects of Cap. Values were expressed as the mean ± SEM (n = 6). ∗∗P < 0.01 versus the control group; ▲▲P < 0.01 versus the A/R group; ##P < 0.01 versus the Cap + A/R group.
|
|
| 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. |
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 |
SirReal2SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM. |
||
| S5914New |
AK 7AK 7 is a brain-permeable selective SIRT2 inhibitor with an IC50 of 15.5 μM. |
||
| S4900 |
Tenovin-6Tenovin-6 is a small molecule activator of p53 transcriptional activity. |
||
| S7577 |
AGK2AGK2 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. |
Masson trichrome staining of tubulointerstitium areas from Sham, UUO, UUO+AGK2 mice (original magnification: × 400).
|
|
| S8245 |
ThiomyristoylThiomyristoyl 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. |
||
| S8460 |
SalermideSalermide 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. |
||
| S8627 |
OSS_128167OSS_128167 is a specific SIRT6 inhibitor with IC50 values of 89, 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively. |
||
| S8628 |
3-TYP3-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. |
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 HClSRT1720 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. |
|
|
| S5918New |
CAY10602CAY10602 is a potent SIRT1 activator. |
||
| S4735 |
Salvianolic acid BSalvianolic 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. |
||
| S8270 |
SRT2183SRT2183 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 |
QuercetinQuercetin, 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. |
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 |
FisetinFisetin (Fustel) is a potent sirtuin activating compound (STAC) and an agent that modulates sirtuins. |
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.
|
|
| S8481 |
SRT3025 HClSRT3025 is an orally available small molecule activator of the SIRT1 enzyme. |
