Tenovin-1 - Sirtuin 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETenovin-1Cat. No.: HY-13423CAS No.: 380315-80-0分式: CHNOS分量: 369.48作靶點(diǎn): Sirtuin; MDM-2/p53; Autophagy作通路: Cell Cycle/DNA Damage; Epigenetics; Apoptosis; Autophagy儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 mo

2、nth溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 33.33 mg/mL (90.21 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.7065 mL 13.5325 mL 27.0651 mL5 mM 0.5413 mL 2.7065 mL 5.4130 mL10 mM 0.2707 mL 1.3533 mL 2.7065 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

3、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，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 90% corn oilSolubility: 2.5 mg/mL (6.77 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Tenovin-1sirtuin 1 和 sirtuin 2 的抑制劑，同時(shí)可激活 p53，在癌癥研究中可能具有潛在的治療作。1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEI

4、C50 & Target Sirtuin MDM-2/p53體外研究 Tenovin-1 (1-10 M) induces a bell-shaped concentration-dependent cell death in SK-N-MC cells. Tenovin-1alters the gene and protein expression of Bcl-2 family members. However, Tenovin-1 has a more powerfuleffect both on mRNA and protein expression levels at a lower

5、 concentration than does the higherconcentration. Furthermore, Tenovin-1-induced cytotoxic effects depend on caspases in p53 wild-type WE-68 cells, but not in p53 null SK-N-MC cells. AIF plays a major role in tenovin-1-induced cell death in p53 nullSK-N-MC cells, but not in p53 wild-type WE-68 cells

6、. Reactive oxygen species are also involved in tenovin-1-mediated cell death in SK-N-MC cells. In addition, Tenovin-1 causes DNA damage in SK-N-MC cells 1.Tenovin-1 (5 M) increases the nuclear size in glioblastoma cells and rat primary astrocytes. Tenovin-1induces cellular senescence, wich does not

7、appear to be related to cell death 2. Tenovin-1 protects p53from mdm2-mediated degradation with little effect on p53 synthesis. Tenovin-1 targets a factor(s) upstreamof p53 that not only modulates p53 function but also other cellular pathways. Tenovin-1 (10 M) inhibits SirT2deacetylase activity 3. T

8、enovin-1 (10 M) reduces proliferation and anchorage independent growth ofNSCLC cells. Tenovin-1 also inhibits cell growth of H358 lung cancer cells 4.體內(nèi)研究 Tenovin-1 (92 mg/kg, i.p.) reduces growth of tumors in SCID mice derived from BL2 cells or ARN8 cells 5.PROTOCOLCell Assay 4 Cell viability is me

9、asured by thiazolyl blue tetrazolium bromide (MTT) assay. Cells are seeded in 96-wellplates. When indicated they are treated with 10 M Tenovin-1 (tnv-1) or are transfected with siRNAs. Afterthe specified period of time, MTT solution (0.5 mg/mL) is added. The formazan crystals are dissolved in anextr

10、action buffer (50% dimethylformamide and 20% SDS, pH 4.7). The absorbance (540/690 nm) ismeasured in a SunRise plate reader 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal ARN8 melanoma or BL2 Burkitts lymphoma cells are injected into the flank

11、 of SCID mice and allowed toAdministration 5 develop until tumors become palpable. Tenovin-1 (in 70% cyclodextrin) is administered daily (14 days) byintraperitoneal injection at 92.5 mg/kg and tumor growth is measured over a period of 18 days. Controlanimals are treated with 70% cyclodextrin. In the

12、 BL2 experiment, n = 12 for each treatment. In the ARN8experiment, n = 14 for the control group and n = 16 for the tenovin-1 treated group. Growth measurementsare averaged between groups and plotted 5.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)

13、品發(fā)表的科研獻(xiàn) Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2966.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Marx C, et al. The sirtuin 1/2 inhibitor tenovin-1 induces a nonlinear apoptosis-inducing factor-dependent cell death

14、in a p53 null Ewingssarcoma cell line. Invest New Drugs. 2017 Nov 18.2. Yoon KB, et al. Induction of Nuclear Enlargement and Senescence by Sirtuin Inhibitors in Glioblastoma Cells. Immune Netw. 2016Jun;16(3):183-8.3. Lain S, et al. Discovery, in vivo activity, and mechanism of action of a small-mole

15、cule p53 activator. Cancer Cell. 2008 May;13(5):454-63.4. Grbesa I, et al. Expression of sirtuin 1 and 2 is associated with poor prognosis in non-small cell lung cancer patients. PLoS One. 2015Apr 27;10(4):e0124670.5. Lain S, et al. Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator. Cancer Ce