1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEThiomyristoylCat. No.: HY-101278CAS No.: 1429749-41-6分式: CHNOS分量: 581.85作靶點(diǎn): Sirtuin作通路: Cell Cycle/DNA Damage; Epigenetics儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 32 mg/mL (55.00 mM

2、)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.7187 mL 8.5933 mL 17.1866 mL5 mM 0.3437 mL 1.7187 mL 3.4373 mL10 mM 0.1719 mL 0.8593 mL 1.7187 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)

3、驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.30 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.30 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIO

4、LOGICAL ACTIVITY物活性 Thiomyristoyl效特異性的SIRT2抑制劑，IC50值為28 nM。IC50 & Target SIRT2 SIRT128 nM (IC50) 98 M (IC50)體外研究 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 degrada

5、tion, suggesting the therapeuticpotential of TM to target certain c-Myc-driven cancers. TM could inhibit SIRT2 with an IC50 of 28 nM, butinhibits SIRT1 with an IC50 value of 98 M and does not inhibit SIRT3 even at 200 M. TM inhibits threehuman breast cancer cell lines, MCF-7, MDA-MB-468, and MDA-MB-

6、231 1.體內(nèi)研究 TM inhibits tumor growth in mouse models of breast cancer. TM does not cause significant toxicity in miceand no significant weight loss is observed in TM-treated mice. S5H, the acetyl-a-tubulin level is moderatelybut statistically significantly increased in tumors from TM-treated mice com

7、pared with those from vehicle-treated mice, suggesting that TM indeed inhibits SIRT2 in vivo 1.PROTOCOLCell Assay 1 Cells are seeded into 96-well plates at 3,0004,000 cells per well. After 24 hr, test compounds(Thiomyristoyl) are added to cells to final concentrations ranging from 1 to 50 M. Cells a

8、re then incubatedfor 72 hr and cell viability is measured using the CellTiter-Blue viability assay. Relative cell viability in thepresence of test compounds is normalized to the vehicle-treated controls after background subtraction.GraphPad Prism software is used to determine the IC50 values. Knockd

9、own of SIRT1-7 in various cell linesis achieved by lentiviral infection 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Neoplasia. 2019 Mar 29;21(5):429-441.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. 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.McePdfHeightCaution: Product has not been fully validated f