Sirtuin

亜型選択性的な製品

シグナル伝達経路

Sirtuinシグナル伝達経路

Sirtuin製品

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  • Sirtuin阻害剤 (18)
  • Sirtuin活性剤(15)
  • Sirtuinモジュレータ(1)
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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.
Nature, 2024, 10.1038/s41586-023-07009-0
Mol Med, 2024, 30(1):15
J Virol, 2024, 98(2):e0188823
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.
bioRxiv, 2024, 10.1101/2024.01.21.576539
Chinese Journal of Tissue Engineering Research, 2024, (28): 4447-4454.
Small, 2023, e2300584.
S1396 Resveratrol 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.
J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
Cell Death Dis, 2023, 14(6):367
Antiviral Res, 2023, 216:105674
S2804 Sirtinol Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively.
Drug Des Devel Ther, 2023, 17:563-577
Surg Open Sci, 2023, 12:35-42
Sci Total Environ, 2022, 838(Pt 1):155713
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. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4.
MedComm (2020), 2023, 4(5):e346
MedComm -2020), 2023, 4(5):e346
Aging Cell, 2023, e13771.
S1899 Nicotinamide Nicotinamide, a water-soluble vitamin, is an active component of coenzymes NAD and NADP, and also act as an inhibitor of sirtuins.
Clin Transl Med, 2024, 14(2):e1583
J Transl Med, 2023, 10.1186/s12967-023-04623-4
iScience, 2023, 26(12):108532
S2298 Fisetin Fisetin (Fustel) is a potent sirtuin activating compound (STAC) and an agent that modulates sirtuins.
Nat Commun, 2023, 14(1):4033
Acta Pharmacol Sin, 2023, 10.1038/s41401-023-01156-w
JCI Insight, 2023, 8(8)e166643
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.
bioRxiv, 2024, 10.1101/2023.01.18.524628
Preprint, 2024 , 2024011891
Autophagy, 2023, 1-15.
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.
Redox Biol, 2024, 69:102994
Elife, 2023, 12e85571
Elife, 2023, 12e85571
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.
Antioxidants (Basel), 2023, 12(3)714
Oxid Med Cell Longev, 2022, 2022:9035547
Cell Biol Toxicol, 2022, 10.1007/s10565-022-09735-z
S7792 SRT2104 (GSK2245840) SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.
Aging (Albany NY), 2024, 16(2):1352-1373
Invest Ophthalmol Vis Sci, 2023, 64(4):31
Neuro Oncol, 2021, 23(1):53-62
S7845 SirReal2 SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.
Biochemistry, 2023, 10.1021/acs.biochem.3c00381
Front Cell Infect Microbiol, 2022, 12:1031814
Pharmaceutics, 2022, 14-102168
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
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
Int J Mol Med, 2019, 44(3):1091-1105
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.
Int J Mol Sci, 2023, 24(5)4912
Biochemistry, 2023, 10.1021/acs.biochem.3c00381
Sci Adv, 2022, 8(31):eabo0412
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.
Front Physiol, 2023, 14:1164287
Cell Discov, 2022, 8(1):106
Cell Death Differ, 2022, 10.1038/s41418-022-00992-3
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.
Cell Transplant, 2023, 32:9636897231198167
Cell Transplant, 2023, 32:9636897231198167
Stem Cell Res Ther, 2021, 12(1):507
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.
Cell Death Dis, 2023, 14(10):667
Front Immunol, 2021, 12:685523
Biomed Pharmacother, 2020, 125:109948
S8270 SRT2183 SRT2183 is a small-molecule activator of the sirtuin subtype SIRT1, currently being developed by Sirtris Pharmaceuticals.
Cell Death Dis, 2023, 14(10):667
J Bone Res, 2023, 11(4)1000235
Neuro Oncol, 2021, 23(1):53-62
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
Aging (Albany NY), 2022, 14(23):9730-9757
Aging (Albany NY), 2022, 14(23):9730-9757
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
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
S5914 AK 7 AK 7 is a brain-permeable selective SIRT2 inhibitor with an IC50 of 15.5 μM.
Int J Mol Sci, 2023, 24(5)4912
Cell Rep, 2022, 40(2):111062
S9903 NRD167 NRD167 is a potent and selective SIRT5 inhibitor.
bioRxiv, 2024, 10.1101/2023.01.18.524628
Microbiome, 2023, 11(1):31
EMBO J, 2022, e110324
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.
Front Cell Infect Microbiol, 2022, 12:1031814
Cancer Lett, 2020, 501:20-30
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.
J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
S5918 CAY10602 CAY10602 is a potent SIRT1 activator.
J Med Chem, 2020, 31
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.
E1150 SIRT7 inhibitor 97491 In SIRT7-related cancers, SIRT7 inhibitor 97491 reduces deacetylase activity of SIRT7 in a dose-dependent manner, and induces apoptosis which is activated by p53 modification and affecting the caspase pathway.
S8942 Suramin sodium salt Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatase (PTPases) inhibitor, also is the potent inhibitor of sirtuins, purified topoisomerase II and SARS-CoV-2 RNA-dependent RNA polymerase (RdRp).
J Biol Chem, 2024, S0021-9258(24)00128-5
S2176 Tenovin-3 Tenovin-3 is an inhibitor of SIRT2. Tenovin-3 is able to increase p53 levels in MCF-7 cells.
E0394 YK 3-237 YK-3-237, a SIRT1 activator, reduces acetylation of mutant p53 and inhibits the proliferation of triple-negative breast cancer cells.
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.
E1267New MDL-800 MDL 800 is an allosteric activator of sirtuin 6 (SIRT6). It selectively activates SIRT6 deacetylase activity over SIRT1-5 and -7 and histone deacetylase 1 (HDAC1) and HDAC2-11 deacetylase activity in cell-free assays at 100 µM. It induces histone deacetylation, and reduces proliferation of BEL-7405 hepatocellular carcinoma (HCC) cells with EC50 of 90.4 µM.
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.
Nature, 2024, 10.1038/s41586-023-07009-0
Mol Med, 2024, 30(1):15
J Virol, 2024, 98(2):e0188823
S1396 Resveratrol 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.
J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
Cell Death Dis, 2023, 14(6):367
Antiviral Res, 2023, 216:105674
S2804 Sirtinol Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively.
Drug Des Devel Ther, 2023, 17:563-577
Surg Open Sci, 2023, 12:35-42
Sci Total Environ, 2022, 838(Pt 1):155713
S1899 Nicotinamide Nicotinamide, a water-soluble vitamin, is an active component of coenzymes NAD and NADP, and also act as an inhibitor of sirtuins.
Clin Transl Med, 2024, 14(2):e1583
J Transl Med, 2023, 10.1186/s12967-023-04623-4
iScience, 2023, 26(12):108532
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.
bioRxiv, 2024, 10.1101/2023.01.18.524628
Preprint, 2024 , 2024011891
Autophagy, 2023, 1-15.
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.
Redox Biol, 2024, 69:102994
Elife, 2023, 12e85571
Elife, 2023, 12e85571
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.
Antioxidants (Basel), 2023, 12(3)714
Oxid Med Cell Longev, 2022, 2022:9035547
Cell Biol Toxicol, 2022, 10.1007/s10565-022-09735-z
S7845 SirReal2 SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.
Biochemistry, 2023, 10.1021/acs.biochem.3c00381
Front Cell Infect Microbiol, 2022, 12:1031814
Pharmaceutics, 2022, 14-102168
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
Int J Mol Med, 2019, 44(3):1091-1105
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.
Int J Mol Sci, 2023, 24(5)4912
Biochemistry, 2023, 10.1021/acs.biochem.3c00381
Sci Adv, 2022, 8(31):eabo0412
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.
Cell Death Dis, 2023, 14(10):667
Front Immunol, 2021, 12:685523
Biomed Pharmacother, 2020, 125:109948
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
S5914 AK 7 AK 7 is a brain-permeable selective SIRT2 inhibitor with an IC50 of 15.5 μM.
Int J Mol Sci, 2023, 24(5)4912
Cell Rep, 2022, 40(2):111062
S9903 NRD167 NRD167 is a potent and selective SIRT5 inhibitor.
bioRxiv, 2024, 10.1101/2023.01.18.524628
Microbiome, 2023, 11(1):31
EMBO J, 2022, e110324
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.
Front Cell Infect Microbiol, 2022, 12:1031814
Cancer Lett, 2020, 501:20-30
E1150 SIRT7 inhibitor 97491 In SIRT7-related cancers, SIRT7 inhibitor 97491 reduces deacetylase activity of SIRT7 in a dose-dependent manner, and induces apoptosis which is activated by p53 modification and affecting the caspase pathway.
S8942 Suramin sodium salt Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatase (PTPases) inhibitor, also is the potent inhibitor of sirtuins, purified topoisomerase II and SARS-CoV-2 RNA-dependent RNA polymerase (RdRp).
J Biol Chem, 2024, S0021-9258(24)00128-5
S2176 Tenovin-3 Tenovin-3 is an inhibitor of SIRT2. Tenovin-3 is able to increase p53 levels in MCF-7 cells.
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.
bioRxiv, 2024, 10.1101/2024.01.21.576539
Chinese Journal of Tissue Engineering Research, 2024, (28): 4447-4454.
Small, 2023, e2300584.
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. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4.
MedComm (2020), 2023, 4(5):e346
MedComm -2020), 2023, 4(5):e346
Aging Cell, 2023, e13771.
S2298 Fisetin Fisetin (Fustel) is a potent sirtuin activating compound (STAC) and an agent that modulates sirtuins.
Nat Commun, 2023, 14(1):4033
Acta Pharmacol Sin, 2023, 10.1038/s41401-023-01156-w
JCI Insight, 2023, 8(8)e166643
S7792 SRT2104 (GSK2245840) SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.
Aging (Albany NY), 2024, 16(2):1352-1373
Invest Ophthalmol Vis Sci, 2023, 64(4):31
Neuro Oncol, 2021, 23(1):53-62
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.
Front Physiol, 2023, 14:1164287
Cell Discov, 2022, 8(1):106
Cell Death Differ, 2022, 10.1038/s41418-022-00992-3
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.
Cell Transplant, 2023, 32:9636897231198167
Cell Transplant, 2023, 32:9636897231198167
Stem Cell Res Ther, 2021, 12(1):507
S8270 SRT2183 SRT2183 is a small-molecule activator of the sirtuin subtype SIRT1, currently being developed by Sirtris Pharmaceuticals.
Cell Death Dis, 2023, 14(10):667
J Bone Res, 2023, 11(4)1000235
Neuro Oncol, 2021, 23(1):53-62
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
Aging (Albany NY), 2022, 14(23):9730-9757
Aging (Albany NY), 2022, 14(23):9730-9757
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
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.
J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
S5918 CAY10602 CAY10602 is a potent SIRT1 activator.
J Med Chem, 2020, 31
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.
E0394 YK 3-237 YK-3-237, a SIRT1 activator, reduces acetylation of mutant p53 and inhibits the proliferation of triple-negative breast cancer cells.
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.
E1267New MDL-800 MDL 800 is an allosteric activator of sirtuin 6 (SIRT6). It selectively activates SIRT6 deacetylase activity over SIRT1-5 and -7 and histone deacetylase 1 (HDAC1) and HDAC2-11 deacetylase activity in cell-free assays at 100 µM. It induces histone deacetylation, and reduces proliferation of BEL-7405 hepatocellular carcinoma (HCC) cells with EC50 of 90.4 µM.
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
E1267New MDL-800 MDL 800 is an allosteric activator of sirtuin 6 (SIRT6). It selectively activates SIRT6 deacetylase activity over SIRT1-5 and -7 and histone deacetylase 1 (HDAC1) and HDAC2-11 deacetylase activity in cell-free assays at 100 µM. It induces histone deacetylation, and reduces proliferation of BEL-7405 hepatocellular carcinoma (HCC) cells with EC50 of 90.4 µM.

Sirtuin阻害剤の選択性比較

Tags: Sirtuin activation | SIRT1 inhibition | SIRT1 activation | SIRT1 protein | SIRT1 cancer | SIRT1 activity | SIRT1 pathway | SIRT1 assay | Sirtuin protein | Sirtuin activity | SIRT activation | SIRT assay | Sirtuin cancer | Sirtuin pathway | SIRT1 phosphorylation | Sirtuin assay | SIRT2 cancer | SIRT pathway | SIRT2 protein | SIRT2 assay | SIRT1 inhibitor review