SIRT1
SIRT1 is a NAD\\+-dependent deacetylase that functions as a central regulator of cellular metabolism, stress responses, genomic stability, and aging through deacetylation of histones and multiple transcriptional regulators[1][2]. Mechanistically, SIRT1 integrates nutrient and energy signals with transcriptional programs that control mitochondrial biogenesis, fatty acid oxidation, glucose metabolism, autophagy, and cellular adaptation to metabolic stress[1][3]. Through coordinated interactions with metabolic signaling networks, SIRT1 contributes to maintenance of metabolic health across liver, skeletal muscle, adipose tissue, heart, and other organs[1]. In disease-related contexts, altered SIRT1 activity has been associated with aging, chronic inflammatory conditions, obesity, metabolic dysfunction, cardiovascular disorders, neurodegenerative diseases, and cancer-related processes, making it a widely used experimental target in translational research[2][4][5]. Compared with related sirtuin isoforms, SIRT1 is the most extensively characterized mammalian sirtuin and primarily mediates transcriptional regulation through deacetylation of nuclear histone and non-histone substrates, whereas other family members display distinct cellular localization and substrate preferences[1][2][4]. For experimental applications, SIRT1 activity can be modulated by small-molecule activators and inhibitors, and naturally occurring polyphenols such as resveratrol have been reported to activate SIRT1 in multiple model systems, providing useful tools for mechanistic studies of metabolism, inflammation, oxidative stress, and aging biology[3][4].
References:
- [1]. Dijk W, et al. Regulation of lipoprotein lipase by Angptl4. Trends Endocrinol Metab. 2014 Mar;25(3):146-55. [Content Brief]
- [2]. Zhao L, et al. Sirtuins and their Biological Relevance in Aging and Age-Related Diseases. Aging Dis. 2020 Jul 23;11(4):927-945. [Content Brief]
- [3]. Chung S, et al. Regulation of SIRT1 in cellular functions: role of polyphenols. Arch Biochem Biophys. 2010 Sep 1;501(1):79-90. [Content Brief]
- [4]. Carafa V, et al. Sirtuins and disease: the road ahead. Front Pharmacol. 2012 Jan 31;3:4. [Content Brief]
- [5]. Herskovits AZ, et al. Sirtuin deacetylases in neurodegenerative diseases of aging. Cell Res. 2013 Jun;23(6):746-58. [Content Brief]
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SIRT1 Related Products (99)
Related Products (99)
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Antibodies (1)
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Nicotinamide riboside malate
0 ImagesNicotinamide riboside malate, an orally active NAD+ precursor, increases NAD+ levels and activates SIRT1 and SIRT3. Nicotinamide riboside malate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside malate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease.
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4'-Bromo-resveratrol
0 ImagesSynonyms: 4′‐BR4'-Bromo-resveratrol (4′‐BR) is a dual SIRT1/SIRT3 inhibitor with an IC50 of 0.2 mM for both targets. 4'-Bromo-resveratrol induces caspase-dependent apoptosis, induces G0/G1 cell cycle arrest, and inhiibits proliferation. 4'-Bromo-resveratrol reduces lactate production, glucose uptake, and NAD+/NADH ratio, and downregulates lactate dehydrogenase A and glucose transporter 1 (GLUT1). 4'-Bromo-resveratrol can be used for the research of melanoma.
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E1231
0 ImagesSynonyms: 1-{4-[2-(5-Methylfuran-2-yl)quinoline-4-carbonyl]piperazin-1-yl}ethan-1-oneE1231 is an orally active activator of Sirtuin 1 (SIRT1) (EC50=0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (KD=9.61 μM) and deacetylated liver X receptor-alpha (LXRα), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE-/- mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases.
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SIRT-IN-1
0 ImagesSIRT-IN-1 is a potent inhibitor of SIRT1/2/3, with IC50s of 15, 10, 33 nM, respectively.
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SIRT6-IN-3
0 ImagesSIRT6-IN-3 (compound 8a) is a selective inhibitor of SIRT6 (IC50=7.49 μM). SIRT6-IN-3 inhibits pancreatic ductal adenocarcinoma (PDAC) cells proliferation and induces apoptosis. SIRT6-IN-3 increases the sensitivity of cancer cells to gemcitabine (HY-17026) via blocking the DNA damage repair pathway. SIRT6-IN-3 is used in pancreatic cancer research.
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Myricanol
0 ImagesMyricanol is a diarylheptanoid and a Nampt activator. Myricanol exerts anti-inflammatory effects and alleviates glucocorticoid-induced muscle atrophy by increasing Sirtuin 1 (SIRT1) and PRDX5 activities while regulating inflammatory factors. Myricanol exhibits growth inhibition and induces apoptosis in human lung adenocarcinoma A549 cells. Myricanol promotes autophagy-mediated clearance of microtubule-associated protein tau to exert neuroprotective effects. Myricanol protects cardiovascular function by inhibiting PDGFRβ and NF-κB signaling pathways. Myricanol activates mitochondrial transcription factor A (TFAM) expression to exert anti-renal fibrosis effects. Myricanol improves insulin resistance through AMPK activation.
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JGB1741
0 ImagesSynonyms: ILS-JGB-1741JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC50 of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC50>100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediated apoptosis with modulation of Bax/Bcl2 ratio, cytochrome c release and PARP cleavage. JGB1741 has the potential for breast cancer research.
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Suramin
0 ImagesSuramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor.Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
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Tanshindiol C
0 ImagesTanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research.
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SIRT5 inhibitor 4
0 ImagesSIRT5 inhibitor 4 (compound 11) is a potent, selective SIRT5 inhibitor with IC50 values of 26.4 and >400μM for SIRT5 and other SIRT subtype, respectively.
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Nicotinamide riboside tartrate
0 ImagesNicotinamide riboside tartrate, an orally active NAD+ precursor, increases NAD+ levels and activates SIRT1 and SIRT3. Nicotinamide riboside tartrate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside tartrate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease.
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Palmitoyl tetrapeptide-20 TFA
0 ImagesCat. No.: HY-P5247ASynonyms: PTP20 TFAPalmitoyl tetrapeptide-20 (PTP20) TFA is a biomimetic peptide agonist of α-MSH. Palmitoyl tetrapeptide-20 TFA promotes hair pigmentation and delays hair graying by activating the MC1-R pathway (AC50: 0.16 nM), enhancing catalase activity to reduce H2O2 accumulation, and upregulating SIRT1 activity. Palmitoyl tetrapeptide-20 TFA can be used in research on preventing hair loss and improving hair graying.
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YK-3-237
0 ImagesYK-3-237, a SIRT1 activator, targets mutant p53. YK-3-237 inhibits the proliferation of triple-negative breast cancer cells.
