3-TYP is a selective SIRT3 inhibitor with an IC50 value of 16 nM, which is more potent over SIRT1 and SIRT2. 3-TYP significantly attenuates melatonin-induced increases in deacetylated-SOD2 expression and SOD2 activity in HepG2 cells exposed to Cd.
In vivo, 3-TYP significantly decreases SIRT3 activity and increases the acetylation of SOD2 compared with that in the control group, without influencing SIRT3 expression. 3-TYP attenuates the cardioprotective effects of melatonin by decreasing the LVEF and LVFS after 24 hour of reperfusion. 3-TYP also increases the infarct size, serum LDH levels, and apoptotic ratio compared with those in the IR+Mel group.
|Cell lines||HepG2 cells|
|Preparation method||Cells are randomly divided into the following treatment groups: 10 μM Cd; melatonin (1 μM)+10 μM Cd; 3-TYP (50 μM)+10 μM Cd; and 3-TYP (50 μM)+melatonin (1 μM)+10 μM Cd. cells are treated for 12 h. The role of the SIRT3-SOD2 pathway in hepatic cell protection after melatonin pretreatment is investigated.|
|Incubation time||12 h|
|Animal models||Sprague-Dawley rats|
|Formulation||ethanol (70%), propylene glycol (20%), NaHCO3 (10%)|
|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: ≥ 25 mg/mL|
Melatonin ameliorates myocardial ischemia reperfusion injury through SIRT3-dependent regulation of oxidative stress and apoptosis.
Zhai M, et al. J Pineal Res. 2017 Sep;63(2). PMID: 28500761.
Polydatin ameliorates injury to the small intestine induced by hemorrhagic shock via SIRT3 activation-mediated mitochondrial protection.
Zeng Z, et al. Expert Opin Ther Targets. 2016 Jun;20(6):645-52. PMID: 27067422.
SIRT3-SOD2-mROS-dependent autophagy in cadmium-induced hepatotoxicity and salvage by melatonin.
Pi H, et al. Autophagy. 2015;11(7):1037-51. PMID: 26120888.
|Related Sirtuin Products|
|Salvianolic acid B
Salvianolic acid B is a cell protective antioxidant and free radical scavenger being investigated for a variety of conditions from ischemic heart disorders to Alzheimer′s disease.
OSS_128167 is a specific SIRT6 inhibitor with IC50 values of 89, 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively.
|Tenovin 6 Hydrochloride
Tenovin-6 Hydrochloride is a water soluble inhibitor of SIRT1 and SIRT2, slightly inhibits HDAC8, and is also a potent activator of p53, with IC50s of 21 μM, 10 μM, 67 μM for SirT1, SirT2, and SirT3, respectively.
Thiomyristoyl is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM. It inhibits SIRT1 with an IC50 value of 98 μM and does not inhibit SIRT3 even at 200 μM.
Nicotinamide is an active component of coenzymes NAD and NADP, and also act as an inhibitor of sirtuins.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.