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Thiomyristoyl (Synonyms: TM)

Catalog No.GC17724

A potent and selective SIRT2 inhibitor

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Thiomyristoyl Chemical Structure

Cas No.: 1429749-41-6

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5mg
$114.00
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25mg
$387.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

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].

References:

[1]. Jing H, et al. A SIRT2-Selective Inhibitor Promotes c-Myc Oncoprotein Degradation and Exhibits Broad Anticancer Activity. Cancer Cell. 2016 Mar 14;29(3):297-310.

Background

Thiomyristoyl is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM.

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].

TM inhibits tumor growth in mouse models of breast cancer. TM does not cause significant toxicity in mice and no significant weight loss is observed in TM-treated mice. S5H, the acetyl-a-tubulin level is moderately but statistically significantly increased in tumors from TM-treated mice compared with those from vehicle-treated mice, suggesting that TM indeed inhibits SIRT2 in vivo[1].

References:
[1]. Jing H, et al. A SIRT2-Selective Inhibitor Promotes c-Myc Oncoprotein Degradation and Exhibits Broad Anticancer Activity. Cancer Cell. 2016 Mar 14;29(3):297-310.

Chemical Properties

Cas No. 1429749-41-6 SDF
Synonyms TM
Chemical Name (S)-benzyl (1-oxo-1-(phenylamino)-6-tetradecanethioamidohexan-2-yl)carbamate
Canonical SMILES O=C(N[C@H](C(NC1=CC=CC=C1)=O)CCCCNC(CCCCCCCCCCCCC)=S)OCC2=CC=CC=C2
Formula C34H51N3O3S M.Wt 581.37
Solubility ≥ 163mg/mL in DMSO Storage Room temperature
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.7201 mL 8.6004 mL 17.2007 mL
5 mM 0.344 mL 1.7201 mL 3.4401 mL
10 mM 0.172 mL 0.86 mL 1.7201 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 38 reference(s) in Google Scholar.)

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