In vitro: Thiomyristoyl(TM) is a highly selective SIRT2 inhibitor. It cannot efficiently inhibit SIRT3, SIRT5, SIRT6, or SIRT7. In vitro, it shows great inhibition of cell viability and its cytotoxicity is relatively selective toward cancer cells. TM decreases c-Myc oncoprotein level in cancer cells, the ability of TM to decrease c-Myc abundance in different cell lines correlates with the sensitivity of the cell lines to TM. In vivo: The anticancer effect of TM correlates with its ability to decrease c-Myc level. TM has limited effects on non-cancerous cells and tumor-free mice.
|Cell lines||breast cancer cell lines MCF-7|
|Preparation method||Human MCF-7 cells are grown in DMEM media contained 10% (vol/vol) heat-inactivated fetal bovine serum and 1% penicillin-streptomycin and treated with in the presence of 200 nM TSA for 6 hr. The acetylation level of p53 protein is determined by western blot using anti-acetyl-p53 (K382) antibody. β-actin serves as a loading control.|
|Concentrations||1, 5, 10, 25, 50 μM|
|Incubation time||6 h|
|Animal models||Mouse xenograft model|
|Dosages||1.5 mg/50 μL (IP); 0.75 mg/50 μL (IT)|
|Administration||intraperitoneal (IP) or intra-tumor (IT) injections|
|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||100 mg/mL in DMSO|
Efficient demyristoylase activity of SIRT2 revealed by kinetic and structural studies.
Teng YB, et al. Sci Rep. 2015 Feb 23;5:8529. PMID: 25704306.
Thiomyristoyl peptides as cell-permeable Sirt6 inhibitors.
He B, et al. Org Biomol Chem. 2014 Oct 14;12(38):7498-502. PMID: 25163004.
|Related Sirtuin Products|
Nicotinamide is an active component of coenzymes NAD and NADP, and also act as an inhibitor of sirtuins.
Fisetin (Fustel) is a potent sirtuin activating compound (STAC) and an agent that modulates sirtuins.
Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM, respectively.
Resveratrol is a phytoestrogen with antitumor, antioxidant, antiplatelet, anti-inflammatory and antifungal effects.
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).
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.