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You are here:Home-Inhibitors & Agonists-Epigenetics-Sirtuin

Request The Product List ofSirtuin Sirtuin

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
GY04397

AK-1

330461-64-8

A potent, selective and brain-permeable SIRT2 inhibitor with IC50 of 12.5 uM; induces proteasomal degradation of the Snail transcription factor through inactivation of the NF-κB/CSN2 pathway; increases the ubiquitination of HIF-1α in a VHL-dependent manner, leading to the degradation of HIF-1α via a proteasomal pathway.

GY04395

SRT 1720

925434-55-5

A potent, selective SIRT1 activator with EC1.5 of 0.16 uM; displays good selectivity for activation of SIRT1 versus SIRT2 (EC1.5=37 uM) and SIRT3 (EC1.5>300 uM); 1,000-fold more potent than resveratrol; improve insulin sensitivity, lower plasma glucose, and increase mitochondrial capacity in obese mice model.

GY04361

AK-7

420831-40-9

A potent, selective and brain-permeable SIRT2 inhibitor with IC50 of 15.5 uM; reduces cholesterol in cultured naive neuronal cells and brain slices from wild-type mice; shows neuroprotective activity in Huntington's disease mouse models, and reduces cholesterol in neuronal models.

GY02546

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.

GY10176

MDL-800

2275619-53-7

MDL-800 (MDL800) is a first-in-class, selective, cellular active SIRT6 allosteric activator, increases SIRT6 deacetylation activity with EC50 of 10.3 uM in RHKK-ac-AMC and FDL assays; dramatically enhanced SIRT6 deacetylation activity by more than 22-fold, displays no activity toward SIRT1, SIRT3, SIRT4, and HDAC1-11 at 50-100 uM, as well as >10-fold selectivity toward SIRT2, SIRT5, and SIRT7; activates SIRT6 through a surface allosteric site induces H3K9ac and H3K56ac deacetylation and represses proliferation of HCC cells (IC50=23.3 uM); inhibits xenograft tumor growth of HCC cells in immunocompromised mice by activating the deacetylase activity of SIRT6.

GY10272

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.

GY10292

SirT1 enhancer A03

66171-75-3

SirT1 enhancer A03 is a specific, orally bioavailable, brain penetrant apolipoprotein E4 (ApoE4)-targeted sirtuin1 (SirT1) enhancer, increases the levels of the neuroprotective enzyme SirT1 while not affecting levels of neurotoxic SirT2 in vitro in ApoE4-transfected cells (EC50=2 uM); increases SirT1 levels in the hippocampus of Alzheimer's disease (AD) model mice and elicits cognitive improvement while inducing no observed toxicity

GY10486

JH-T4

JH-T4 is a potent small molecule SIRT2 inhibitor with IC50 of 0.3 uM (sirtuin deacylation activity), increase intracellular K-Ras4a lysine fatty acylation; inhibited both the deacetylation and defatty-acylation activity of SIRT2 in vitro with IC50 of 30-50 nM; JH-T4 is the first small molecule inhibitor that can modulate the lysine fatty acylation levels of K-Ras4a. JH-T4 also inhibits SIRT1 and SIRT3 in vitro.

GY05343

SRTCX1002

1203479-63-3

SRTCX1002 (SRTCX-1002) is a small molecule activator of SIRT1 (STAC) with EC1.5 of 0.4 uM, enhances deacetylation of cellular p65 protein with IC50 of 0.84 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.

GY05342

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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