Sirtuins

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  1. SIRT1 inhibitor

    EX 527 is a potent and selective SIRT1 class III histone deacetylase enzyme inhibitor with IC50 of 38 nM in a cell-free assay.
  2. Fisetin is a flavonol, a structurally distinct chemical substance that belongs to the flavonoid group of polyphenols. It can be found in many plants, where it serves as a colouring agent. Possible anti-aging, anti-inflammatory, anti-cancer, and anti-viral properties of fisetin are under active scientific investigation.
  3. SIRT1 Activator

    SRT1720 is an inhibitor developed intended as a small-molecule activator of the sirtuin subtype SIRT1.
  4. SIRT1 activator

    SRT3190 is a potent CXCR2 ligand.
  5. 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.
  6. 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.
  7. Sirt1/Sirt2 inhibitor

    Salermide is an inhibitor of Sirt1 and Sirt2; can cause strong cancer-specific apoptotic cell death.
  8. p53 activator

    Tenovin-6 is a analog of tenovin-1. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 in vitro with IC50 values of 21, 10, and 67 uM, respectively.
  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

    SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.
  13. SIRT2 inhibitor

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

    AK-1 inhibits SIRT2 selectively over SIRT1 and SIRT3.
  15. SIRT1 Activator

    SRT 1720 is a selective activator of human SIRT1 (EC1.5 = 0.16 μM) versus the closest sirtuin homologues, SIRT2 and SIRT3 (SIRT2: EC1.5 = 37 uM; SIRT3: EC1.5 > 300 uM).
  16. Selective SIRT2 inhibitor

    SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.
  17. 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.
  18. SIRT3 inhibitor

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

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

    MDL-800 is a first-in-class cellularly active SIRT6 allosteric activator.
  21. SIRT6 activator

    UBCS039 is the first synthetic, specific Sirtuin 6 (SIRT6) activator, inducing autophagy in human tumor cells, with an EC50 of 38 μM.
  22. 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.
  23. Sirt2 inhibitor

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

    CAY10602 is a SIRT1 activator.
  25. SIRT2 inhibitor

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

    SIRT5 inhibitor 1 is a potent Human Sirtuin 5 deacylase inhibitor, with an IC50 of 0.11 μM.
  27. 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.
  28. Sirt2 inhibitor

    SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC50 of 2.4 μM.
  29. SIRT1/2/3 inhibitor

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

    SIRT-IN-1 is a potent inhibitor of SIRT1/2/3, with IC50s of 15, 10, 33 μM, respectively.
  31. 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.
  32. Nicotinamide riboside chloride is a crystal form of Nicotinamide riboside (NR) chloride. Nicotinamide riboside chloride is used in dietary supplements.
  33. antidepressant agent

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

    4'-bromo-Resveratrol is a potent inhibitor of the deacetylases sirtuin 1 (SIRT1) and 3 (SIRT3).

  35. SIRT2 Inhibitor

    SIRT2-IN-8 is a selective inhibitor of SIRT2 (Sirtuin 2), a member of the sirtuin family of proteins implicated in various cellular processes. This compound exhibits strong inhibition of SIRT2 activity, making it a valuable tool for investigating the role of SIRT2 in neurodegenerative diseases, particularly Huntington's and Parkinson's diseases. Its use in research can contribute to a better understanding of the molecular mechanisms underlying these conditions and aid in the development of therapeutic strategies.
  36. SIRT Inhibitor

    Nicotinamide is a form of vitamin B3 or niacin. Nicotinamide Hydrochloride inhibits SIRT2 activity (IC50: 2 μM). Nicotinamide also inhibits SIRT1. Nicotinamide increases cellular NAD+, ATP, ROS levels. Nicotinamide inhibits tumor growth and improves survival. Nicotinamide also has anti-HBV activity.
  37. SIRT6 Inhibitor

    SIRT6-IN-3 is a selective inhibitor of SIRT6, exhibiting an IC50 of 7.49 μM. This compound effectively inhibits the proliferation of pancreatic ductal adenocarcinoma (PDAC) cells and promotes apoptosis. Additionally, SIRT6-IN-3 enhances the sensitivity of cancer cells to gemcitabine by obstructing the DNA damage repair pathway, making it a valuable tool in pancreatic cancer research.
  38. HDAC/Sirt2 Inhibitor

    Mz325 is a dual inhibitor of histone deacetylases (HDAC) and Sirtuin 2 (Sirt2), with an IC50 of 9.7 μM for Sirt2. By modulating deacetylation processes, Mz325 exhibits bioactivity that can influence cellular pathways involved in cancer progression and neurodegenerative diseases. This compound is useful for research focused on the role of epigenetic regulation in these pathologies.
  39. SIRT1 Activator

    BML-278 is a potent SIRT1 activator with an effective concentration (EC150) of 1 μM. It enhances histone modifications by increasing H3K9 methylation and inhibiting H3K9 acetylation, which contributes to improved early embryonic development. Additionally, BML-278 induces G1/S phase cell cycle arrest and reduces senescence in primary human mesenchymal cells. In U937 cells, this compound reduces tubulin acetylation while promoting increased mitochondrial density in murine C2C12 myoblasts, highlighting its versatility in cellular and developmental research applications.
  40. SIRT6 PROTAC Degrader

    SZU-B6 is a SIRT6-protein-targeting chimeric degrader that achieves a DC50 of 45 nM and 154 nM in SK-HEP-1 and Huh-7 cell lines, respectively. It effectively inhibits the proliferation of SK-HEP-1 cells with an IC50 of 1.51 μM and suppresses colony formation in both SK-HEP-1 and Huh-7 cells. Additionally, SZU-B6 induces apoptosis and causes a cell cycle arrest in the G2/M phase in SK-HEP-1 cells, demonstrating notable antitumor efficacy in mouse models. This compound serves as a valuable tool for studying the functional roles of SIRT6 in cancer research.
  41. SIRT1 Inhibitor

    JGB1741 is a potent and selective inhibitor of SIRT1, exhibiting an IC50 of approximately 15 μM. It displays weak inhibitory effects on SIRT2 and SIRT3, with IC50 values greater than 100 μM. JGB1741 enhances the levels of acetylated p53, promoting p53-mediated apoptosis through modulation of the Bax/Bcl2 ratio, cytochrome c release, and PARP cleavage. This compound is valuable for research applications focusing on breast cancer.
  42. Sirtuin Inhibitor

    Sirt1/2-IN-2 is a dual inhibitor targeting SIRT1 and SIRT2, exhibiting IC50 values of 1.8 μM and 2.4 μM, respectively. This compound effectively prevents the deacetylation of p53 while promoting acetylation of p53 and α-tubulin. Sirt1/2-IN-2 demonstrates pro-apoptotic properties and exhibits anti-proliferative effects on human leukemia cell lines, making it a valuable tool in cancer research and therapeutic studies targeting the sirtuin family.
  43. Sirtuin Inhibitor

    Sirt1/2-IN-3 is a dual inhibitor of the sirtuin family, specifically targeting SIRT1 and SIRT2 with IC50 values of 1.4 μM and 2.0 μM, respectively. This compound effectively prevents the deacetylation of p53, leading to increased acetylation of both p53 and α-tubulin. Sirt1/2-IN-3 has been demonstrated to induce apoptosis and exhibit anti-proliferative effects on human leukemia cell lines, making it a valuable tool for cancer research and the study of cellular aging mechanisms.
  44. SIRT Inhibitor

    SIRT-IN-7 is a selective inhibitor targeting the SIRT family of proteins, specifically SIRT1, SIRT2, and SIRT3. This compound enhances the acetylation and activation of the tumor suppressor protein p53, leading to the inhibition of proliferation and the induction of apoptosis and autophagy in breast cancer cells. SIRT-IN-7 demonstrates significant anti-tumor activity, making it a valuable tool for research in cancer biology and therapeutic development.
  45. SIRT7 Inhibitor

    SIRT7 Inhibitor 97491 is a selective inhibitor of the SIRT7 enzyme, exhibiting an IC50 of 325 nM and effectively reducing its deacetylase activity in a dose-dependent manner. This compound enhances tumor suppression by stabilizing the p53 protein through acetylation at lysine residues K373 and K382. Additionally, SIRT7 Inhibitor 97491 promotes apoptosis via the caspase signaling pathway, making it a valuable tool for cancer research and studies focused on elucidating the role of SIRT7 in tumor progression.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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