Sirtuins

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  1. SIRT2 Inhibitor

    A1B11 is a selective inhibitor of Sirtuin 2 (SIRT2) with an IC50 value of 5.3 μM. This compound is primarily utilized in research focused on neurodegenerative diseases, where SIRT2 modulation plays a critical role in the underlying mechanisms of pathology. A1B11 provides a valuable tool for investigating the therapeutic potential of SIRT2 inhibition in various neurodegenerative conditions.
  2. SIRT1/3 Activator

    Nicotinamide riboside (triflate) is a potent activator of the SIRT1 and SIRT3 pathways, functioning as an orally active precursor to NAD+. This compound significantly elevates NAD+ levels, thereby enhancing oxidative metabolism and providing protective effects against metabolic disturbances triggered by high-fat diets. Additionally, it has demonstrated neuroprotective properties, as evidenced by its ability to mitigate cognitive decline in transgenic mouse models of Alzheimer’s disease, making it valuable for research in metabolic health and neurodegenerative disorders.
  3. SIRT1 Inhibitor

    SIRT1-IN-1 is a selective inhibitor of SIRT1, exhibiting an IC50 of 0.205 μM. In addition to its primary target, it also inhibits SIRT2 with an IC50 of 11.5 μM. This indole compound demonstrates antiviral activity, particularly against cytomegalovirus (CMV), making it a valuable tool for research into SIRT1-related pathways and antiviral applications.
  4. SIRT Inhibitor

    Nicotinamide hydrochloride is an inhibitor of SIRT1 and SIRT2, targeting the sirtuin family of proteins critical for cellular regulation. This reagent has been shown to enhance cellular levels of NAD+ and ATP while increasing reactive oxygen species (ROS) levels. Research applications include investigation into tumor growth inhibition and potential improvements in survival, as well as exploring its anti-hepatitis B virus (HBV) activity.
  5. SIRT2 Inhibitor

    RK-9123016 is a selective inhibitor of SIRT2, effectively inhibiting its enzymatic activity with an IC50 of 0.18 µM, while showing no significant effect on SIRT1 or SIRT3 at concentrations up to 100 µM. This compound enhances the acetylation of eukaryotic translation initiation factor 5A (eIF5A), a known substrate of SIRT2, and is shown to decrease cell viability in human breast cancer cells, correlating with reduced expression of c-Myc. RK-9123016 is valuable for research into cancer biology and the role of sirtuins in cellular processes.
  6. SIRT1 Activator

    Altissimacoumarin F is a terpenylated coumarin that acts as an activator of SIRT1, a protein implicated in cellular stress response and longevity. This compound, isolated from the stem bark of Ailanthus altissima, enhances SIRT1 activity while simultaneously decreasing p53 transcriptional activity. Altissimacoumarin F is valuable for research into age-related disorders and related pathways, providing insights into potential therapeutic strategies.
  7. SIRT1 Inhibitor

    SIRT1-IN-6 is a selective SIRT1 inhibitor with an IC50 value of 9.7 μM. This compound effectively increases p53 acetylation, which is significant in regulating cell cycle and apoptosis. SIRT1-IN-6 is ideal for research applications related to neurodegenerative diseases and cancer, offering insights into potential therapeutic strategies for these conditions.
  8. SIRT1/2 Inhibitor

    Sirt1/2-IN-1 is a selective inhibitor of SIRT1 and SIRT2, exhibiting IC50 values of 1.81 and 2.10 µg/mL, respectively, while also inhibiting SIRT3 with an IC50 of 20.5 µg/mL. This compound induces hyperacetylation of α-tubulin, with an IC50 of 32.05 µg/mL, demonstrating its potential for modulating protein acetylation. Sirt1/2-IN-1 is particularly relevant in cancer research, showcasing significant anticancer activity that supports its use in investigating therapeutic strategies targeting sirtuin pathways.
  9. SIRT1/SIRT2 inhibitor

    Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 and 59 μM, respectively.
  10. SIRT1 inhibitor

    Inauhzin is a potent SIRT inhibitor, which effectively reactivates p53 by inhibiting SIRT1 activity, promotes p53-dependent apoptosis of human cancer cells without causing apparently genotoxic stress.
  11. SIRT2 inhibitor

    AK-7 is a cell- and brain-permeable inhibitor of SIRT2 (IC50 = 15.5 μM).
  12. SIRT1 activator

    SRT3190 is a potent CXCR2 ligand.
  13. Sirtuin-1 (SIRT1) activator

    SRT 2183 is a selective Sirtuin-1 (SIRT1) activator with an EC1.5 value of 0.36 μM. SRT 2183 induces growth arrest and apoptosis, concomitant with deacetylation of STAT3 and NF-κB, and reduction of c-Myc protein levels.
  14. sirtuin inhibitor

    Sirtinol is a cell-permeable, specific inhibitor of sirtuin NAD-dependant histone deacetylases. It is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively.
  15. Sirt1/Sirt2 inhibitor

    Salermide is an inhibitor of Sirt1 and Sirt2; can cause strong cancer-specific apoptotic cell death.
  16. SIRT2 inhibitor

    AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM.
  17. SIRT2 inhibitor

    AK-1 inhibits SIRT2 selectively over SIRT1 and SIRT3.
  18. SIRT 6 inhibitor

    OSS-128167, also known as SIRT6-IN-1, is a potent and selective SIRT 6 inhibitor with IC50 value of 89 μM.
  19. SIRT3 inhibitor

    3-TYP is a SIRT3 inhibitor.
  20. SIRT2 inhibitor

    Thiomyristoyl is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM.
  21. SIRT6 allosteric activator

    MDL-800 is a first-in-class cellularly active SIRT6 allosteric activator.
  22. antidepressant agent

    Gardenia yellow is an active member of crocin, increases mRNA expression of SIRT3, and acts as an orally active antidepressant agent.
  23. SIRT1/2/3 inhibitor

    SIRT-IN-2 is a potent inhibitor of SIRT1/2/3, with IC50s of 4, 4, 7 μM, respectively.
  24. SIRT1/2/3 inhibitor

    SIRT-IN-1 is a potent inhibitor of SIRT1/2/3, with IC50s of 15, 10, 33 μM, respectively.
  25. SIRT1 activator

    SRT 1720 Hydrochloride is a selective activator of SIRT1 with an EC50 of 0.10 μM, and shows less potent activities on SIRT2 and SIRT3.
  26. SIRT2 inhibitor

    JFD00244 is a sirtuin 2 (SIRT2) inhibitor. Anti-tumor effect.
  27. SIRT5 inhibitor

    SIRT5 inhibitor 1 is a potent Human Sirtuin 5 deacylase inhibitor, with an IC50 of 0.11 μM.
  28. Sirt2 degrader

    PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide cereblon ligand for E3 ubiquitin ligase.
  29. Sirt2 inhibitor

    SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC50 of 2.4 μM.
  30. SIRT6 activator

    UBCS039 is the first synthetic, specific Sirtuin 6 (SIRT6) activator, inducing autophagy in human tumor cells, with an EC50 of 38 μM.
  31. SIRT1 activator

    SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5>300 μM), and is more potent than Resveratrol and the closest sirtuin homologues.
  32. Sirt2 inhibitor

    Sirt2-IN-1 (Compound 9) is a sirtuin 2 (Sirt2) inhibitor with an IC50 of 163 nM.
  33. SIRT1 activator

    CAY10602 is a SIRT1 activator.
  34. SIRT6 Activator

    SIRT6 activator 12q is a potent and selective small molecule that acts as an activator of SIRT6, exhibiting an IC50 of 0.58 μM, while demonstrating much lower activity against other sirtuins such as SIRT1-3 and SIRT5. This compound has been shown to inhibit cell growth and migration, induce apoptosis, and cause cell cycle arrest at the G2 phase. With its potential anticancer properties, SIRT6 activator 12q is a valuable tool for research in cancer biology and therapeutic development targeting SIRT6 pathways.
  35. Nampt/SIRT1/PRDX5 Activator

    Myricanol is a diarylheptanoid that acts as a Nampt activator, enhancing SIRT1 and PRDX5 activities. This compound exhibits notable anti-inflammatory properties and mitigates glucocorticoid-induced muscle atrophy while regulating inflammatory mediators. Additionally, it demonstrates growth inhibition and promotes apoptosis in human lung adenocarcinoma A549 cells. Myricanol is also implicated in neuroprotection via autophagy-mediated clearance of microtubule-associated protein tau and contributes to cardiovascular health by inhibiting key signaling pathways such as PDGFRβ and NF-κB. Its activation of mitochondrial transcription factor A (TFAM) further supports anti-renal fibrosis effects and improves insulin sensitivity through AMPK activation.
  36. SIRT6/SIRT2 Inhibitor

    SIRT2/6-IN-1 is a dual inhibitor of SIRT6 and SIRT2 with IC50 values of 106 μM and 114 μM, respectively. This compound enhances histone H3K9 acetylation, promotes glucose uptake, and decreases TNF-α secretion in cellular models. SIRT2/6-IN-1 provides valuable insights for research into metabolic regulation and inflammatory responses, making it a useful tool for studying the roles of sirtuins in cellular processes.
  37. SIRT1/3 Inhibitor

    SPC-180002 is a dual inhibitor of SIRT1 and SIRT3, exhibiting IC50 values of 1.13 μM and 5.41 μM, respectively. This compound disrupts redox homeostasis through reactive oxygen species (ROS) generation, resulting in enhanced stability of the p21 protein and consequential mitochondrial dysfunction. SPC-180002 effectively inhibits cell cycle progression and reduces cancer cell proliferation, while also activating the Nrf2 signaling pathway, making it a valuable tool for cancer research and studies on metabolic dysregulation.
  38. SIRT2/Hsp70 Inhibitor

    YM-08 is a selective inhibitor of SIRT2 and Hsp70, exhibiting an IC50 of 19.9 μM for SIRT2. This compound effectively penetrates the blood-brain barrier, making it a valuable tool for studying neurodegenerative diseases and cellular stress responses. Its dual inhibitory activity allows for investigation into SIRT2 and Hsp70's roles in various biological processes and potential therapeutic applications.
  39. HSP70/SIRT2 Inhibitor

    HSP70/SIRT2-IN-2 is a dual inhibitor targeting SIRT2 and HSP70, demonstrating an IC50 of 45.1±5.0 μM for SIRT2. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research. Its ability to simultaneously inhibit these two proteins positions HSP70/SIRT2-IN-2 as a useful candidate for studies focused on tumor progression and potential therapeutic strategies.
  40. SIRT3 Agonist

    SKLB-11A is a selective, orally active allosteric agonist of SIRT3 (sirtuin 3), exhibiting a Kd value of 4.7 μM and demonstrating high selectivity for SIRT family members. This compound activates autophagy-related signaling pathways and plays a critical role in preventing mitochondrial dysfunction. SKLB-11A has shown efficacy in improving cardiac function in models of Doxorubicin-induced cardiotoxicity and myocardial ischemia/reperfusion, making it a valuable tool for research in cardiovascular protection and mitochondrial biology.
  41. SIRT6 Inhibitor

    SIRT6-IN-4 is a selective inhibitor of SIRT6, demonstrating an IC50 of 5.68 μM. This compound effectively inhibits the proliferation of MCF-7 cells with an IC50 of 8.30 μM, leading to cell cycle arrest at the G2/M phase. Additionally, SIRT6-IN-4 reduces cell migration and invasion while inducing apoptosis. Its antitumor efficacy has been confirmed in mouse models, making it a valuable tool for cancer research and therapeutic development.
  42. SIRT1 Agonist

    BF-175 is a selective agonist of SIRT1, a protein involved in cellular regulation and energy metabolism. It enhances the activation of PGC1-α, promoting autophagy and apoptosis, while also inhibiting the activity of SREBP. BF-175 demonstrates protective effects against high glucose-induced mitochondrial damage and shows potential in attenuating the progression of diabetic kidney disease. Additionally, this compound has been investigated for its inhibitory effects on endometrial carcinoma, making it a valuable tool for research in metabolic and cancer studies.
  43. SIRT2 Inhibitor

    SIRT2-IN-18 is a selective SIRT2 inhibitor, exhibiting IC50 values of 5.3 μM for SmSIRT2 and 12.3 μM for hSIRT2. This compound demonstrates significant antischistosomal effects against both Liberian and Puerto Rican strains of Schistosoma mansoni, effectively reducing schistosomula viability, adult worm pairing, and egg production while maintaining low cytotoxicity in mammalian cells. SIRT2-IN-18 also promotes histone H3 hyperacetylation and triggers cytochrome c-mediated apoptosis, making it a valuable tool for research into both parasitic infections and the modulation of acetylation pathways.
  44. Sirtuin Inhibitor

    Sirt1/2-IN-4 is a potent triple inhibitor of the sirtuin family, specifically targeting SIRT1 and SIRT2 with IC50 values of 1.2 μM and 1.9 μM, respectively, and showing moderate inhibition of SIRT3 at 18.6 μM. This compound effectively prevents the deacetylation of p53, highlighting its potential role in cancer research. Its ability to modulate sirtuin activity makes it a valuable tool for investigating the biological implications of sirtuin inhibition in various cancer models.
  45. SIRT1 Activator

    SRT 1720 dihydrochloride is a selective activator of SIRT1, exhibiting an EC50 of 0.10 μM. This compound demonstrates lower activity toward SIRT2 and SIRT3, making it an important tool for investigating SIRT1-related biological pathways. Its ability to modulate SIRT1 activity is particularly relevant in studies of metabolism, aging, and neuroprotection.
  46. SIRT6 Activator

    MDL-811 is a selective allosteric activator of SIRT6, exhibiting an EC50 of 5.7 μM. This compound demonstrates significant anti-inflammatory, antitumor, and neuroprotective properties, making it a valuable tool for research. MDL-811 is particularly relevant for studies related to colorectal cancer and ischemic stroke, providing insights into potential therapeutic strategies targeting SIRT6 modulation.
  47. Sirtuin-modulating Compound

    Sirtuin Modulator 9 is a sirtuin-modulating compound that enhances cellular lifespan and promotes mitochondrial activity. This compound has potential applications in research related to aging, inflammation, and cancer. Investigators may utilize Sirtuin Modulator 9 to explore its therapeutic effects in age-related disorders and diseases associated with compromised mitochondrial function.
  48. AMPK/SIRT3/PGC-1α Modulator

    MitoPBN is an AMPK/SIRT3/PGC-1α modulator that enhances mitochondrial function by acting as a reactive oxygen species scavenger. This compound promotes mitochondrial biogenesis through increased AMPK phosphorylation, restoration of SIRT3 expression, and upregulation of PGC-1α. MitoPBN is effective in regulating glucose metabolism, as it decreases blood glucose levels by inhibiting hepatic gluconeogenesis and enhancing glucose uptake, while also improving ATP production and maintaining mitochondrial membrane potential. Additionally, it can reduce apoptosis and enhance sperm motility and membrane integrity, making it a valuable reagent for research related to diabetes and metabolic disorders.

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