Sirtuin (Sir2 proteins) are a class of proteins that possess either mono-ADP-ribosyltransferase, or deacylase activity, including deacetylase, desuccinylase, demalonylase, demyristoylase and depalmitoylase activity. Sirtuins regulate important biological pathways in bacteria, archaeaand eukaryotes. Sirtuins have been implicated in influencing a wide range of cellular processes like aging, transcription, apoptosis, inflammation and stress resistance, as well as energy efficiency and alertness during low-calorie situations. Sirtuins can also control circadian clocks and mitochondrial biogenesis.
Cat. No. | Product Name | CAS No. | Information |
---|---|---|---|
H9480 |
Inaxaplin |
2446816-88-0 | Inaxaplin is a potent apolipoprotein L1 (APOL1) function inhibitor with IC50 of < 0.25μM toward thallium assay and trypanosoma assay. |
H9142 |
Nicotinamide riboside Chloride |
23111-00-4 | Nicotinamide riboside Chloride is an orally active NAD+ precursor, increases NAD+ levels and activates SIRT1 and SIRT3. Nicotinamide riboside is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease. |
H9141 |
Nicotinamide riboside |
1341-23-7 | Nicotinamide riboside is an orally active NAD+ precursor, increases NAD+ levels and activates SIRT1 and SIRT3. Nicotinamide riboside is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease. |
H8812 |
Dalosirvat |
1360540-81-3 | Dalosirvat a potent small molecule sirtuin (SIRT) activator. |
H2843 |
YK-3-237 |
1215281-19-8 | A novel small molecule sirtuin-1 (SIRT1) activator that reduces acetylation of mutant 53 and exhibits anti-proliferative effects against TNBC cells carrying mutant p53; demonstrates proliferation inhibition in breast cancer cell panel with EC50 of 0.1-5 uM, also induces PARP-dependent apoptotic cell death and arrests the cell cycle at G2/M phase; enhances expression of α-SMA and fibronectin in cultured rat renal interstitial fibroblasts (NRK-49F). |
H2842 |
UBCS039 |
358721-70-7 | UBCS039 (UBCS-039) is the first synthetic activator of the NAD+-dependent protein lysine deacetylase SIRT6 with EC50 of 38 uM; shows robust activating effects on Sirt6-dependent H3K18ac deacetylation of full-length histone proteins and complete HeLa nucleosomes, with no statistically significant effects on basal Sirt1, 2, and 3 deacetylation activities; induces autophagosome accumulation and promotes autophagic flux in human cancer cells, triggers ROS accumulation and activates the AMPK/ULK1 signaling pathway. |
H2841 |
Thiomyristoyl |
1429749-41-6 | Thiomyristoyl is a highly selective and potent SIRT2 inhibitor with IC50 of 28 nM, displays no significant activity against SIRT1/3/5/6/7 (Ic50>100 uM); promotes c-Myc ubiquitination and degradation, exhibits broad anticancer effect in various human cancer cells while having limited effects on non-cancerous cells; demonstrates in vivo effect in mouse models of breast cancer. |
H2840 |
Tenovin-D3 |
1258283-70-3 | A novel selective, small-molecule inhibitor of sirtuin SITR2 with IC50 of 21.8 uM; shows much weaker actvity for SIRT1 (IC50>90 uM), SIRT3 and HDAC8; promotes expression of the cell-cycle regulator and p53 target p21(WAF1/CIP1) (CDKN1A) in a p53-independent manner, fails to increase p53 levels or transcription factor activity. |
H2839 |
Tenovin-1 |
380315-80-0 | Tenovin-1 (Tenovin1) is a small molecules that activate p53 and decreases tumor growth through inhibition of the protein-deacetylating activities of SirT1 and SirT2; causes significantly greater growth inhibition, cell death via apoptosis, as well as superior p53 promoter upregulation in wtp53 MyLa cells when combined with vorinostat; elicits caspase-mediated cell death in p53 wild-type cells, but caspase-independent cell death in p53 null cells. |
H2838 |
SRTCX1003 |
1203480-93-6 | SRTCX1003 (SRTCX-1003) is a small molecule activator of SIRT1 (STAC) with EC1.5 of 0.61 uM, enhances deacetylation of cellular p65 protein with IC50 of 1.42 uM in cellular p65 acetylation assay; suppresses TNFα-induced NF-κB transcriptional activation and reduction of LPS-stimulated TNFα secretion in a SIRT1-dependent manner, decreases the production of the proinflammatory cytokines TNFα and IL-12 in acute mouse model of LPS-induced inflammation. |
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