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Thiomyristoyl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Thiomyristoyl图片
CAS NO:1429749-41-6
规格:≥98%
包装与价格:
包装价格(元)
1mg电议
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
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500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 581.85
Formula C34H51N3O3S
CAS No. 1429749-41-6
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (171.86 mM)
Water: N/A
Ethanol: 100 mg/mL warmed (171.86 mM)
SMILES CodeO=C(OCC1=CC=CC=C1)N[C@@H](CCCCNC(CCCCCCCCCCCCC)=S)C(NC2=CC=CC=C2)=O
Synonyms

TM; Thiomyristoyl;

Chemical Name: benzyl (S)-(1-oxo-1-(phenylamino)-6-tetradecanethioamidohexan-2-yl)carbamate

Exact Mass: 581.3651

实验参考方法
In Vitro

In vitro activity: Thiomyristoyl, a thiomyristoyl lysine compound, is a novel, potent and specific SIRT2 inhibitor with IC50 of 28 nM. Thiomyristoyl showed broad-spectrum of anticancer activity in various human cancer cells and mouse models of breast cancer but has little effect on non-cancerous cells. Targeting sirtuins for cancer treatment has been a topic of debate due to conflicting reports and lack of potent and specific inhibitors. The anticancer effect of Thiomyristoyl correlates with its ability to decrease c-Myc level. Thiomyristoyl had limited effects on non-cancerous cells and tumor-free mice, suggesting that cancer cells have an increased dependency on SIRT2 that can be exploited for therapeutic benefit. Thiomyristoyl is a promising anticancer agent and may represent a general strategy to target certain c-Myc-driven cancers. 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


Kinase Assay: Thiomyristoyl, a thiomyristoyl lysine compound, is a novel, potent and specific SIRT2 inhibitor with IC50 of 28 nM. It cannot efficiently inhibit SIRT3, SIRT5, SIRT6, or SIRT7.


Cell Assay: Cells are seeded into 96-well plates at 3,000–4,000 cells per well. After 24 hr, test compounds (Thiomyristoyl) are added to cells to final concentrations ranging from 1 to 50 μM. Cells are then incubated for 72 hr and cell viability is measured using the CellTiter-Blue viability assay. Relative cell viability in the presence of test compounds is normalized to the vehicle-treated controls after background subtraction. GraphPad Prism software is used to determine the IC50 values. Knockdown of SIRT1-7 in various cell lines is achieved by lentiviral infection.

In VivoThe 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
Animal model Kaplan-Meier tumor-free survival curve of MMTV-PyMT mice
Formulation & DosageIP injection with either the vehicle (DMSO) or TM (1.5 mg TM in 50 μL DMSO; n = 10) daily.
References Cancer Cell. 2016 Mar 14;29(3):297-310.