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SRT2183 is a selective activator of Sirtuin-1 (SIRT1) with EC1.5 value of 0.36 μM. SRT2183 induces growth arrest and apoptosis, concomitant with deacetylation of STAT3 and NF-κB, and reduction of c-Myc protein levels. SRT2183 leads to increased mRNA levels of pro-apoptosis and DNA-damage-response genes, accompanied by accumulation of phospho-H2A.X levels. SRT2183 reduces the DNA-binding activity of both NF-κB and STAT3 to the promoter of GADD45G, which is one of the most upregulated genes following SRT2183 treatment.
| Molecular Weight | 468.57 |
| Formula | C27H24N4O2S |
| CAS Number | 1001908-89-9 |
| Solubility (25°C) | DMSO ≥ 150 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Sirtuin Products |
|---|
| Selisistat
Selisistat (EX 527) is a potent and selective SIRT1 class III histone deacetylase enzyme inhibitor with an IC50 of 98 nM. |
| SRT1720 Hydrochloride
SRT1720 Hydrochloride is a selective small molecule activator of SIRT1 that is 1,000-fold more potent than resveratrol (EC1.5 = 0.16 versus 46.2 µM, respectively). SRT1720 increased the activity of SIRT1 and AMPKα phosphorylation at Ser485 via the cAMP-protein kinase A (PKA) pathway. |
| Resveratrol
Resveratrol is a phytoestrogen with antitumor, antioxidant, antiplatelet, anti-inflammatory and antifungal effects. |
| Sirtinol
Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM, respectively. |
| Ganoderic-acid-D
Ganoderic acid D is a highly oxidized tetracyclic triterpenoid that is the main active ingredient in Ganoderma lucidum. Ganoderic acid D upregulates protein expression for SIRT3 and induces deacetylated cyclophilic protein D (CypD) through SIRT3. Ganoderic acid D inhibits energy reprogramming in colon cancer cells, including glucose uptake, lactate production, pyruvate, and acetyl-Coenzyme production in colon cancer cells. |
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