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

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESalermideCat. No.: HY-101073CAS No.: 1105698-15-4分式: CHNO分量: 394.47作靶點: Sirtuin作通路: Cell Cycle/DNA Damage; Epigenetics儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL (126.75 mM)H2O

2、 : 90% corn oilSolubility: 2.5 mg/mL (6.34 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 Salermide是Sirt1 and Sirt2的抑制劑，可引起強效的癌癥特異性的凋亡性細胞死亡。IC50 & Target SIRT1 SIRT2體外研究 Salermide shows a dose-dependent inhibition that rises to 80% at 90 M and 25 M against

3、 Sirt1 and Sirt2,respectively. Salermide can prompt tumour-specific cell death in a wide range of human cancer cell linesderived from leukaemia (MOLT4, KG1A, K562), lymphoma (Raji), colon (SW480) and breast (MDA-MB-231).Incubation with 100 M Salermide alone resulted in an increase of cytosolicactiva

4、ted caspase 3 and adecrease of mitochondrialcytochrome. Salermide alone can induce apoptosis through both extrinsic andintrinsic pathways. Salermide had several antitumorigenic advantages over the earlier described class IIIHDAC inhibitors: firstly, it mimics the universal proapoptotic effect on can

5、cer samples exhibited by theclassical class I, II and IV HDAC inhibitors, and secondly, its proapoptotic effect is cancer-specific 1.體內(nèi)研究 Salermide is well tolerated by mice at concentrations up to 100 M. Salermides mechanism of action in vivois specifically mediated by Sirt1. Intraperitoneal feedin

6、g of Salermide has no apparent toxicity in nude mice1.PROTOCOLCell Assay 1 Cell lines (SW480, MDA-MB-231, MOLT4, KG1A, K562 and Raji) are used in the study. Cell viability isdetermined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. IC50 index iscalculated using four Sa

7、lermide concentrations (25, 50, 75 and 100 M) for 24 h. The percentage ofapoptotic cells is determined with the FACSCalibur apparatus 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: To assess possible adverse effects of Salermide in vivo.

8、 To do this, a group of 10 nude mice areAdministration 1 intraperitoneal injected 100 L of 100 M of Salermide to over 34 days. Diet consumption, body-weight gain,and postural and behavioural changes are monitored throughout the study 1.MCE has not independently confirmed the accuracy of these method

9、s. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Mol Cell Proteomics. 2019 Mar;18(3):520-533. bioRxiv. 2019 Mar.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Lara E, et al. Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect. Oncogene. 2009 Feb 12;28(6):781-91.McePdfHeight Caution: Product has not been fully validated for medi