Thiomyristoyl
Based on 5 publication(s) in Google Scholar
Thiomyristoyl is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM.
For research use only. We do not sell to patients.
- Purity: 98.23%
- CAS No.: 1429749-41-6
- Formula: C34H51N3O3S
- Molecular Weight:581.85
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Thiomyristoyl
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Biological Activity
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SIRT2 28 nM (IC50) |
SIRT1 98 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
17.3 μM
Compound: TM
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Growth inhibition of human A549 cells after 72 hrs by CellTiter-Blue assay
Growth inhibition of human A549 cells after 72 hrs by CellTiter-Blue assay
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[PMID: 30986062] |
| BXPC-3 | GI50 |
13.3 μM
Compound: TM
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Growth inhibition of human BxPC3 cells after 72 hrs by CellTiter-Blue assay
Growth inhibition of human BxPC3 cells after 72 hrs by CellTiter-Blue assay
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[PMID: 30986062] |
| HCT-116 | GI50 |
131.6 μM
Compound: TM
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Growth inhibition of human HCT116 cells after 72 hrs by CellTiter-Blue assay
Growth inhibition of human HCT116 cells after 72 hrs by CellTiter-Blue assay
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[PMID: 30986062] |
| HCT-116 | GI50 |
16.7 μM
Compound: TM
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Inhibition of anchorage-independent cell growth in human HCT116 cells assessed as reduction in colony formation incubated for 5 days followed by compound re-addition and measured after 9 to 11 days by nitro blue tetrazolium chloride-based soft agar colony
Inhibition of anchorage-independent cell growth in human HCT116 cells assessed as reduction in colony formation incubated for 5 days followed by compound re-addition and measured after 9 to 11 days by nitro blue tetrazolium chloride-based soft agar colony
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[PMID: 30986062] |
| MCF7 | GI50 |
37 μM
Compound: TM
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Growth inhibition of human MCF7 cells after 72 hrs by CellTiter-Blue assay
Growth inhibition of human MCF7 cells after 72 hrs by CellTiter-Blue assay
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[PMID: 30986062] |
| MDA-MB-231 | GI50 |
42.8 μM
Compound: TM
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Growth inhibition of human MDA-MB-231 cells after 72 hrs by CellTiter-Blue assay
Growth inhibition of human MDA-MB-231 cells after 72 hrs by CellTiter-Blue assay
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[PMID: 30986062] |
| MDA-MB-468 | GI50 |
15.7 μM
Compound: TM
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Growth inhibition of human MDA-MB-468 cells after 72 hrs by CellTiter-Blue assay
Growth inhibition of human MDA-MB-468 cells after 72 hrs by CellTiter-Blue assay
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[PMID: 30986062] |
| NCI-H23 | GI50 |
16.4 μM
Compound: TM
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Growth inhibition of human NCI-H23 cells after 72 hrs by CellTiter-Blue assay
Growth inhibition of human NCI-H23 cells after 72 hrs by CellTiter-Blue assay
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[PMID: 30986062] |
| SW948 | GI50 |
19.2 μM
Compound: TM
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Growth inhibition of human SW948 cells after 72 hrs by CellTiter-Blue assay
Growth inhibition of human SW948 cells after 72 hrs by CellTiter-Blue assay
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[PMID: 30986062] |
Thiomyristoyl (TM) is a potent SIRT2-specific inhibitor with broad anticancer activity but little effect on non-cancerous cells. SIRT2-inhibition promotes c-Myc ubiquitination and degradation, suggesting the therapeutic potential of TM to target certain c-Myc-driven cancers. TM could inhibit SIRT2 with an IC50 of 28 nM, but inhibits SIRT1 with an IC50 value of 98 μM and does not inhibit SIRT3 even at 200 μM. TM inhibits three human breast cancer cell lines, MCF-7, MDA-MB-468, and MDA-MB-231[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1429749-41-6
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Appearance Solid
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Molecular Weight 581.85
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Formula C34H51N3O3S
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Color White to off-white
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SMILES
O=C(OCC1=CC=CC=C1)N[C@H](C(NC2=CC=CC=C2)=O)CCCCNC(CCCCCCCCCCCCC)=S
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
Neoplasia
The SIRT2/cMYC Pathway Inhibits Peroxidation-Related Apoptosis In Cholangiocarcinoma Through Metabolic Reprogramming. [Abstract]2019 May;21(5):429-441. PMID: 30933885
Thiomyristoyl purchased from MedChemExpress. Usage Cited in: Neoplasia. 2019 May;21(5):429-441. [Abstract]
HuCCT1 and RBE cells are treated with 0, 25, or 50 μm Tm (Thiomyristoyl) and subjected to western blotting
Thiomyristoyl purchased from MedChemExpress. Usage Cited in: Neoplasia. 2019 May;21(5):429-441. [Abstract]
After treatment with Tm (Thiomyristoyl), NAC, or a combination of both, the levels of ROS and proteins are detected.
Thiomyristoyl purchased from MedChemExpress. Usage Cited in: Neoplasia. 2019 May;21(5):429-441. [Abstract]
cMYC, p-PDHA1, PHGDH, PSAT1 and PSPH protein levels in xenograft tissues from control and Tm (Thiomyristoyl) group are detected by staining and Western blotting.
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Phytother Res
Isobavachalcone, a natural sirtuin 2 inhibitor, exhibits anti-triple-negative breast cancer efficacy in vitro and in vivo. [Abstract]2024 Apr;38(4):1815-1829. PMID: 38349045 -
Int Immunopharmacol
Thiomyristoyl ameliorates colitis by blocking the differentiation of Th17 cells and inhibiting SIRT2-induced metabolic reprogramming. [Abstract]2021 Jan;90:107212. PMID: 33310666 -
Prostate
SIRT2 promotes cell proliferation and migration through mediating ERK1/2 activation and lactosylceramide accumulation in prostate cancer. [Abstract]2023 Jan;83(1):71-81. PMID: 36082450
Solvent & Solubility
DMSO : ≥ 32 mg/mL (55.00 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 15.29 mg/mL (26.28 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (270 KB)
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SDS (761 KB)
- English - EN (761 KB)
- Français - FR (761 KB)
- Deutsch - DE (761 KB)
- Norwegian - NO (761 KB)
- Español - ES (761 KB)
- Swedish - SV (761 KB)
- Italian - IT (761 KB)
- Portuguese - PT (761 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 1.7187 mL | 8.5933 mL | 17.1866 mL | 42.9664 mL |
| 5 mM | 0.3437 mL | 1.7187 mL | 3.4373 mL | 8.5933 mL | |
| 10 mM | 0.1719 mL | 0.8593 mL | 1.7187 mL | 4.2966 mL | |
| 15 mM | 0.1146 mL | 0.5729 mL | 1.1458 mL | 2.8644 mL | |
| 20 mM | 0.0859 mL | 0.4297 mL | 0.8593 mL | 2.1483 mL | |
| 25 mM | 0.0687 mL | 0.3437 mL | 0.6875 mL | 1.7187 mL | |
| DMSO | 30 mM | 0.0573 mL | 0.2864 mL | 0.5729 mL | 1.4322 mL |
| 40 mM | 0.0430 mL | 0.2148 mL | 0.4297 mL | 1.0742 mL | |
| 50 mM | 0.0344 mL | 0.1719 mL | 0.3437 mL | 0.8593 mL |