E1150New |
SIRT7 inhibitor 97491
|
SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway. |
|
|
S1396 |
Resveratrol (SRT501)
|
Resveratrol (SRT501, trans-Resveratrol) has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis. |
-
Int Immunopharmacol, 2022, 103:108489
-
Eur J Neurosci, 2022, 10.1111/ejn.15596
-
Adv Sci (Weinh), 2021, e2103360
|
|
S1541 |
Selisistat (EX 527)
|
Selisistat (EX 527, SEN0014196) 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. |
-
Dev Cell, 2022, 57(2):260-276.e9
-
Front Pharmacol, 2022, 13:797469
-
J Transl Med, 2022, 20(1):44
|
|
S1899 |
Nicotinamide (NSC 13128)
|
Nicotinamide (NSC 13128, Niacinamide, Vitamin PP, Nicotinic acid amide, Vitamin B3, NSC 27452), a water-soluble vitamin, is an active component of coenzymes NAD and NADP, and also act as an inhibitor of sirtuins. |
-
Cell Rep, 2022, 38(3):110250
-
Cell Death Dis, 2022, 13(1):43
-
Cell Metab, 2021, 33(1):110-127.e5
|
|
S2176 |
Tenovin-3
|
Tenovin-3 is an inhibitor of SIRT2. Tenovin-3 is able to increase p53 levels in MCF-7 cells. |
|
|
S2804 |
Sirtinol
|
Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively. |
-
J Cell Sci, 2022, jcs.259207
-
Front Pharmacol, 2022, 13:797469
-
Hepatology, 2021, 10.1002/hep.32245
|
|
S4900 |
Tenovin-6
|
Tenovin-6 is a small molecule activator of p53 transcriptional activity and inhibits dihydroorotate dehydrogenase (DHODH). Tenovin-6 is also an inhibitor of SirT1 and SirT2. |
-
Front Immunol, 2021, 12:685523
-
Biomed Pharmacother, 2020, 125:109948
-
J Cell Sci, 2019, 132(6)
|
|
S5914 |
AK 7
|
AK 7 is a brain-permeable selective SIRT2 inhibitor with an IC50 of 15.5 μM. |
|
|
S6744 |
Inauhzin
|
Inauhzin is a cell-permeable SIRT1 inhibitor with an IC50 of 0.7-2 μM and reactivates p53 by inhibiting SIRT1 deacetylation activity. |
-
Cancer Lett, 2020, 501:20-30
|
|
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. |
-
Dev Cell, 2022, 57(2):260-276.e9
-
Front Pharmacol, 2022, 13:797469
-
Cell Rep, 2021, 34(13):108921
|
|
S7845 |
SirReal2
|
SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.
|
-
Basic Res Cardiol, 2021, 116(1):48
-
Cancer Lett, 2020, 501:20-30
-
J Cell Physiol, 2020, 10.1002
|
|
S8000 |
Tenovin-1
|
Tenovin-1 protects against MDM2-mediated p53 degradation, which involves ubiquitination, and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also an inhibitor of dihydroorotate dehydrogenase (DHODH). |
-
J Pharm Biomed Anal, 2021, 201:114121
-
J Transl Med, 2019, 17(1):76
-
Sci Rep, 2019, 9(1):1897
|
|
S8245 |
Thiomyristoyl
|
Thiomyristoyl (TM) 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. |
-
Cell Metab, 2020, 32(3):420-436.e12
-
Cancer Lett, 2020, 501:20-30
-
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. |
-
Cancer Lett, 2020, 501:20-30
-
Am J Transl Res, 2019, 11(8):4789-4799
-
J Proteome Res, 2018, 17(4):1436-1451
|
|
S8627 |
OSS_128167
|
OSS_128167 (SIRT6-IN-1) is a specific SIRT6 inhibitor with IC50 values of 89, 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively. OSS_128167 has anti-viral effect in HBV transcription and replication. |
-
Biochem Pharmacol, 2022, 199:115022
-
Front Cell Dev Biol, 2021, 9:625540
-
Front Cell Dev Biol, 2021, 9:648627
|
|
S8628 |
3-TYP
|
3-TYP (3-(1H-1,2,3-triazol-4-yl) pyridine) 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.
|
-
Dev Cell, 2022, 57(2):260-276.e9
-
Exp Mol Med, 2022, 10.1038/s12276-022-00745-9
-
Toxicol Lett, 2022, 354:14-23
|
|
S9903New |
NRD167
|
NRD167 is a potent and selective SIRT5 inhibitor.
|
|
|
A5039 |
SIRT6 Rabbit Recombinant mAb
|
SIRT6 Antibody detects endogenous levels of SIRT6.
|
|
|
A5049 |
SIRT1 Rabbit Recombinant mAb
|
SIRT1 Antibody detects endogenous levels of total SIRT1.
|
|
|
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. |
-
FEBS J, 2022, 10.1111/febs.16353
-
J Diabetes Res, 2022, 2022:1755563
-
bioRxiv, 2022, 2022.01.04.474979
|
|
S2298 |
Fisetin
|
Fisetin (Fustel) is a potent sirtuin activating compound (STAC) and an agent that modulates sirtuins. |
-
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
-
Cancer Lett, 2022, S0304-3835(22)00021-0
-
Front Immunol, 2021, 12:692321
|
|
S2391 |
Quercetin (NSC 9221)
|
Quercetin (NSC 9221, Sophoretin, C.I. 75720), 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. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4. |
-
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
-
Mol Neurobiol, 2022, 10.1007/s12035-021-02712-3
-
Nucleic Acids Res, 2021, gkab538
|
|
S2935 |
Nicotinamide Riboside Chloride
|
Nicotinamide Riboside Chloride 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+ . 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. |
-
PLoS One, 2021, 16(6):e0252554
-
Nat Metab, 2021, 3(8):1109-1124
|
|
S3168 |
cis-Resveratrol
|
cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively. |
|
|
S3262 |
Scopolin
|
Scopolin, a coumarin isolated from Arabidopsis thaliana (Arabidopsis), attenuates hepatic steatosis through activation of SIRT1-mediated signaling cascades, a potent regulator of lipid homeostasis. |
|
|
S4735 |
Salvianolic acid B
|
Salvianolic acid B (Sal B, Lithospermate B, Lithospermic acid B), an antioxidant and free radical scavenging compound, is the most abundant bioactive compound extracted from the root of Salvia miltiorrhiza Bunge. |
-
Stem Cell Res Ther, 2021, 12(1):507
-
Research Square, 2021, 10.21203/rs.3.rs-372611/v1
-
J Cell Mol Med, 2020, 29
|
|
S5918 |
CAY10602
|
CAY10602 is a potent SIRT1 activator. |
-
J Med Chem, 2020, 31
|
|
S6880 |
SRT-1460
|
SRT-1460 is a potent and selective activator of Sirtuin 1 (SIRT1) with EC1.5 of 2.9 μM. SRT-1460 reduces cell viability and growth of pancreatic cancer cells and induces apoptosis. |
|
|
S7792 |
SRT2104 (GSK2245840)
|
SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.
|
-
Neuro Oncol, 2021, 23(1):53-62
-
Front Pharmacol, 2021, 12:653233
-
Hepatology, 2020, 10.1002/hep.31222
|
|
S8270 |
SRT2183
|
SRT2183 is a small-molecule activator of the sirtuin subtype SIRT1, currently being developed by Sirtris Pharmaceuticals. |
-
Neuro Oncol, 2021, 23(1):53-62
-
Cell Death Differ, 2021, 10.1038/s41418-021-00841-9
-
Life Sci, 2020, S0024-3205(20)31542-3
|
|
S8481 |
SRT3025 HCl
|
SRT3025 is an orally available small molecule activator of the SIRT1 enzyme. |
-
Neuro Oncol, 2021, 23(1):53-62
-
Aging Cell, 2020, e13164
-
Acta Haematol, 2019, 142(3):142-148
|
|
S8909 |
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. |
-
Cell Death Discov, 2022, 8(1):96
|
|
S2347 |
Quercetin Dihydrate
|
Quercetin (Sophoretin), 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. |
-
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
-
Nucleic Acids Res, 2021, gkab538
-
Front Immunol, 2021, 12:649285
|
|
E1150New |
SIRT7 inhibitor 97491
|
SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway. |
|
|
S1396 |
Resveratrol (SRT501)
|
Resveratrol (SRT501, trans-Resveratrol) has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis. |
- Int Immunopharmacol, 2022, 103:108489
- Eur J Neurosci, 2022, 10.1111/ejn.15596
- Adv Sci (Weinh), 2021, e2103360
|
|
S1541 |
Selisistat (EX 527)
|
Selisistat (EX 527, SEN0014196) 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. |
- Dev Cell, 2022, 57(2):260-276.e9
- Front Pharmacol, 2022, 13:797469
- J Transl Med, 2022, 20(1):44
|
|
S1899 |
Nicotinamide (NSC 13128)
|
Nicotinamide (NSC 13128, Niacinamide, Vitamin PP, Nicotinic acid amide, Vitamin B3, NSC 27452), a water-soluble vitamin, is an active component of coenzymes NAD and NADP, and also act as an inhibitor of sirtuins. |
- Cell Rep, 2022, 38(3):110250
- Cell Death Dis, 2022, 13(1):43
- Cell Metab, 2021, 33(1):110-127.e5
|
|
S2176 |
Tenovin-3
|
Tenovin-3 is an inhibitor of SIRT2. Tenovin-3 is able to increase p53 levels in MCF-7 cells. |
|
|
S2804 |
Sirtinol
|
Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively. |
- J Cell Sci, 2022, jcs.259207
- Front Pharmacol, 2022, 13:797469
- Hepatology, 2021, 10.1002/hep.32245
|
|
S4900 |
Tenovin-6
|
Tenovin-6 is a small molecule activator of p53 transcriptional activity and inhibits dihydroorotate dehydrogenase (DHODH). Tenovin-6 is also an inhibitor of SirT1 and SirT2. |
- Front Immunol, 2021, 12:685523
- Biomed Pharmacother, 2020, 125:109948
- J Cell Sci, 2019, 132(6)
|
|
S5914 |
AK 7
|
AK 7 is a brain-permeable selective SIRT2 inhibitor with an IC50 of 15.5 μM. |
|
|
S6744 |
Inauhzin
|
Inauhzin is a cell-permeable SIRT1 inhibitor with an IC50 of 0.7-2 μM and reactivates p53 by inhibiting SIRT1 deacetylation activity. |
- Cancer Lett, 2020, 501:20-30
|
|
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. |
- Dev Cell, 2022, 57(2):260-276.e9
- Front Pharmacol, 2022, 13:797469
- Cell Rep, 2021, 34(13):108921
|
|
S7845 |
SirReal2
|
SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.
|
- Basic Res Cardiol, 2021, 116(1):48
- Cancer Lett, 2020, 501:20-30
- J Cell Physiol, 2020, 10.1002
|
|
S8000 |
Tenovin-1
|
Tenovin-1 protects against MDM2-mediated p53 degradation, which involves ubiquitination, and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also an inhibitor of dihydroorotate dehydrogenase (DHODH). |
- J Pharm Biomed Anal, 2021, 201:114121
- J Transl Med, 2019, 17(1):76
- Sci Rep, 2019, 9(1):1897
|
|
S8245 |
Thiomyristoyl
|
Thiomyristoyl (TM) 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. |
- Cell Metab, 2020, 32(3):420-436.e12
- Cancer Lett, 2020, 501:20-30
- 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. |
- Cancer Lett, 2020, 501:20-30
- Am J Transl Res, 2019, 11(8):4789-4799
- J Proteome Res, 2018, 17(4):1436-1451
|
|
S8627 |
OSS_128167
|
OSS_128167 (SIRT6-IN-1) is a specific SIRT6 inhibitor with IC50 values of 89, 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively. OSS_128167 has anti-viral effect in HBV transcription and replication. |
- Biochem Pharmacol, 2022, 199:115022
- Front Cell Dev Biol, 2021, 9:625540
- Front Cell Dev Biol, 2021, 9:648627
|
|
S8628 |
3-TYP
|
3-TYP (3-(1H-1,2,3-triazol-4-yl) pyridine) 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.
|
- Dev Cell, 2022, 57(2):260-276.e9
- Exp Mol Med, 2022, 10.1038/s12276-022-00745-9
- Toxicol Lett, 2022, 354:14-23
|
|
S9903New |
NRD167
|
NRD167 is a potent and selective SIRT5 inhibitor.
|
|
|
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. |
- FEBS J, 2022, 10.1111/febs.16353
- J Diabetes Res, 2022, 2022:1755563
- bioRxiv, 2022, 2022.01.04.474979
|
|
S2298 |
Fisetin
|
Fisetin (Fustel) is a potent sirtuin activating compound (STAC) and an agent that modulates sirtuins. |
- ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
- Cancer Lett, 2022, S0304-3835(22)00021-0
- Front Immunol, 2021, 12:692321
|
|
S2391 |
Quercetin (NSC 9221)
|
Quercetin (NSC 9221, Sophoretin, C.I. 75720), 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. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4. |
- ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
- Mol Neurobiol, 2022, 10.1007/s12035-021-02712-3
- Nucleic Acids Res, 2021, gkab538
|
|
S2935 |
Nicotinamide Riboside Chloride
|
Nicotinamide Riboside Chloride 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+ . 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. |
- PLoS One, 2021, 16(6):e0252554
- Nat Metab, 2021, 3(8):1109-1124
|
|
S3168 |
cis-Resveratrol
|
cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively. |
|
|
S3262 |
Scopolin
|
Scopolin, a coumarin isolated from Arabidopsis thaliana (Arabidopsis), attenuates hepatic steatosis through activation of SIRT1-mediated signaling cascades, a potent regulator of lipid homeostasis. |
|
|
S4735 |
Salvianolic acid B
|
Salvianolic acid B (Sal B, Lithospermate B, Lithospermic acid B), an antioxidant and free radical scavenging compound, is the most abundant bioactive compound extracted from the root of Salvia miltiorrhiza Bunge. |
- Stem Cell Res Ther, 2021, 12(1):507
- Research Square, 2021, 10.21203/rs.3.rs-372611/v1
- J Cell Mol Med, 2020, 29
|
|
S5918 |
CAY10602
|
CAY10602 is a potent SIRT1 activator. |
- J Med Chem, 2020, 31
|
|
S6880 |
SRT-1460
|
SRT-1460 is a potent and selective activator of Sirtuin 1 (SIRT1) with EC1.5 of 2.9 μM. SRT-1460 reduces cell viability and growth of pancreatic cancer cells and induces apoptosis. |
|
|
S7792 |
SRT2104 (GSK2245840)
|
SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.
|
- Neuro Oncol, 2021, 23(1):53-62
- Front Pharmacol, 2021, 12:653233
- Hepatology, 2020, 10.1002/hep.31222
|
|
S8270 |
SRT2183
|
SRT2183 is a small-molecule activator of the sirtuin subtype SIRT1, currently being developed by Sirtris Pharmaceuticals. |
- Neuro Oncol, 2021, 23(1):53-62
- Cell Death Differ, 2021, 10.1038/s41418-021-00841-9
- Life Sci, 2020, S0024-3205(20)31542-3
|
|
S8481 |
SRT3025 HCl
|
SRT3025 is an orally available small molecule activator of the SIRT1 enzyme. |
- Neuro Oncol, 2021, 23(1):53-62
- Aging Cell, 2020, e13164
- Acta Haematol, 2019, 142(3):142-148
|
|
S8909 |
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. |
- Cell Death Discov, 2022, 8(1):96
|
|