OSS-128167-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEOSS_128167Cat. No.: HY-107454CAS No.: 887686-02-4分式: CHNO分量: 366.32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 : 103.3 mg/mL (281.99 mM;

2、 Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.7299 mL 13.6493 mL 27.2985 mL5 mM 0.5460 mL 2.7299 mL 5.4597 mL10 mM 0.2730 mL 1.3649 mL 2.7299 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)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配

3、，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 (6.82 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.82 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.Med

4、ChemE物活性 OSS_128167個(gè)選擇性 SIRT6 抑制劑，對(duì)于 SIRT6，SIRT1 和 SIRT2 的 IC50 值分別為 89，1578 和 751 M。IC50 & Target SIRT6 SIRT2 SIRT189 M (IC50) 751 M (IC50) 1578 M (IC50)體外研究 OSS_128167 is a selective SIRT6 inhibitor with IC50s of 89, 1578 and 751 M for SIRT6, SIRT1 and SIRT2,respectively. OSS_128167 inhibits SIRT6

5、 in the micromolar range, but shows promising selectivity, since itsIC50 value for SIRT6 is approximately 17 times lower compare to the IC50 for SIRT1 and 9 times lowercompare to SIRT2 1. OSS_128167 (200 M) induces chemosensitization in primary multiple myeloma (MM)cells (NCI-H929), as well as in me

6、lphalan-resistant (LR-5) and doxorubicin-resistant (Dox40) MM cell lines2.PROTOCOLKinase Assay 1 TNF-a levels in supernatants from cells incubated for 18 h in the presence or absence of OSS_128167 (100M, final concentration) are measured by a commercially available ELISA kit according to the manufac

7、turersinstructions 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 Glucose uptake is evaluated using a fluorescent D-glucose analog, 2-NBDG, in L6 cells incubated for 18 h inthe presence or absence of OSS_128167 (100 M, final concentratio

8、n) 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Parenti MD, et al. Discovery of novel and selective SIRT6 inhibitors. J Med Chem. 2014 Jun 12;57(11):4796-804.2. Cea M, et al. Evidence for a role of the histone deacetylase SIRT6 in DNA damage response of multiple myeloma cells. Blood. 2016 Mar3;127(9):1138-50.McePdfHeightCaution: Product has not been fully validated for medical applicat