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|
|Source||Mol Med Rep (2015). Figure 2. Thiomyristoyl|
|Cell Lines||HEK293T cells|
|Incubation Time||24 h|
|Results||TNFα from the cells treated with the four Sirt6 inhibitors had increased fluorescent labelling (and thus increased fatty acylation levels) compared to TNFα from the control cells, suggesting that these thiomyristoyl peptides could inhibit SIRT6 in cells.|
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.
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