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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥ 150 mg/mL|
SIRT1 activation enhances HDAC inhibition-mediated upregulation of GADD45G by repressing the binding of NF-κB/STAT3 complex to its promoter in malignant lymphoid cells
A Scuto, et al. Cell Death Dis. 2013 May 16;4(5):e635. PMID: 23681230.
Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes
Jill C Milne, et al. Nature. 2007 Nov 29;450(7170):712-6. PMID: 18046409.
|Related Sirtuin Products|
UBCS039 is an synthetic SIRT6 activator, with EC50 of 38 μM.
|Nicotinamide Riboside Chloride
Nicotinamide Riboside Chloride is a pyridine-nucleoside form of vitamin B3 that functions as a precursor to nicotinamide adenine dinucleotide or NAD+.
SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.
SRT2104 is a selective brain-permeable activator of SIRT1.
3-TYP is a selective SIRT3 inhibitor, more potent over SIRT1 and SIRT2, with IC50 values of 88 nM, 92 nM, 16 nM for SITR1, SIRT2, SIRT3, respectively.
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