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Purity: =99.29%
Thiomyristoyl, a thiomyristoyl lysine compound, is a novel, potent and specific SIRT2 inhibitor with IC50 of 28 nM. In mouse models of breast cancer and a variety of human cancer cells, thiomyristoyl demonstrated broad-spectrum anticancer activity; however, it had minimal effect on non-cancerous cells. The lack of powerful and targeted inhibitors and inconsistent data have made targeting sirtuins for cancer treatment a contentious issue. The ability of thiomyristoyl to lower c-Myc levels is correlated with its anticancer effect. The limited effects of thiomyristoyl on tumor-free mice and non-cancerous cells indicate that cancer cells have a greater reliance on SIRT2, which may be used therapeutically. A potential general strategy to target some c-Myc driven cancers is thiomyristoyl, a promising anticancer agent.
| Targets |
SIRT2 ( IC50 = 28 nM ); SIRT1 ( IC50 = 98 μM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
Thiomyristoyl, a thiomyristoyl lysine compound, is a novel, potent and selective inhibitor of SIRT2 with IC50 of 28 nM. It is unable to effectively inhibit SIRT3, SIRT5, SIRT6, or SIRT7.
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| Cell Assay |
Three thousand to four thousand cells are seeded into each well of 96-well plates. The cells are treated with test compounds (Thiomyristoyl) at final concentrations ranging from 1 to 50 μM after a 24-hour period. Following a 72-hour incubation period, the CellTiter-Blue viability assay is used to determine the viability of the cells. Background subtraction is used to normalize relative cell viability in the presence of test compounds to the vehicle-treated controls. The IC50 values are found using GraphPad Prism software. Lentivral infection is used to knockdown SIRT1-7 in a variety of cell lines[1].
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| Animal Protocol |
Mouse xenograft model
1.5 mg/50 μL (IP); 0.75 mg/50 μL (IT) intraperitoneal (IP) or intra-tumor (IT) injections |
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| References |
| Molecular Formula |
C34H51N3O3S
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| Molecular Weight |
581.85
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| Exact Mass |
581.37
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| Elemental Analysis |
C, 70.18; H, 8.84; N, 7.22; O, 8.25; S, 5.51
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| CAS # |
1429749-41-6
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CCCCCCCCCCCCCC(=S)NCCCC[C@@H](C(=O)NC1=CC=CC=C1)NC(=O)OCC2=CC=CC=C2
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| InChi Key |
CJQGLLUJIVNREL-HKBQPEDESA-N
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| InChi Code |
InChI=1S/C34H51N3O3S/c1-2-3-4-5-6-7-8-9-10-11-18-26-32(41)35-27-20-19-25-31(33(38)36-30-23-16-13-17-24-30)37-34(39)40-28-29-21-14-12-15-22-29/h12-17,21-24,31H,2-11,18-20,25-28H2,1H3,(H,35,41)(H,36,38)(H,37,39)/t31-/m0/s1
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| Chemical Name |
benzyl N-[(2S)-1-anilino-1-oxo-6-(tetradecanethioylamino)hexan-2-yl]carbamate
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| Synonyms |
TM; Thiomyristoyl
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7187 mL | 8.5933 mL | 17.1866 mL | |
| 5 mM | 0.3437 mL | 1.7187 mL | 3.4373 mL | |
| 10 mM | 0.1719 mL | 0.8593 mL | 1.7187 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 TM inhibits human cancer cells.Cancer Cell.2016 Mar 14;29(3):297-310. |
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 TM specifically inhibits SIRT2 in cells.Cancer Cell.2016 Mar 14;29(3):297-310. |
 Analysis of tumor growth and histopathological findings of xenografted mice treated by intraperitoneal TM injection.Cancer Cell.2016 Mar 14;29(3):297-310. |
 Mammary tumorigenesis in MMTV-PyMT female mice following intraperitoneal TM injection.Cancer Cell.2016 Mar 14;29(3):297-310. |
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 TM inhibits various types of human cancer cell lines and decreases c-Myc protein level.Cancer Cell.2016 Mar 14;29(3):297-310. |
 Decreasing c-Myc protein abundance contributes to the anticancer effect of TM.Cancer Cell.2 |
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