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Thiomyristoyl

Cat. No. M5265
Thiomyristoyl Structure
Size Price Availability Quantity
10mM/1mL In DMSO USD 330 In stock
1mg USD 105 In stock
5mg USD 245 In stock
10mg USD 435 In stock
25mg USD 790 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Customer Product Validations & Biological Datas
Source Mol Med Rep (2015). Figure 2. Thiomyristoyl
Method Weatern Blot
Cell Lines HEK293T cells
Concentrations 200 μM
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.
Protocol
Cell Experiment
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 Experiment
Animal models Mouse xenograft model
Formulation DMSO
Dosages 1.5 mg/50 μL (IP); 0.75 mg/50 μL (IT)
Administration intraperitoneal (IP) or intra-tumor (IT) injections
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 581.85
Formula C34H51N3O3S
CAS Number 1429749-41-6
Purity >98%
Solubility 100 mg/mL in DMSO
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Thiomyristoyl supplier, Sirtuin, inhibitors

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