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Spautin-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Spautin-1图片
CAS NO:1262888-28-7
规格:≥98%
包装与价格:
包装价格(元)
1mg电议
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产品介绍
理化性质和储存条件
Molecular Weight (MW)271.26
FormulaC15H11F2N3
CAS No.1262888-28-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 54 mg/mL (199.1mM)
Water: < 1 mg/mL
Ethanol: 7 mg/mL (25.8 mM)
SMILES CodeFC1=CC=C(CNC2=C3C=C(F)C=CC3=NC=N2)C=C1
SynonymsSpautin-1; Spautin 1; Spautin1
实验参考方法
In Vitro

In vitro activity: In Bcap-37 cells, Spautin-1 dramatically enhanced cell death in glucose-free media and induces apoptotic morphology. In Bax-Bak DKO cells, spautin-1 inhibits etoposide induced autophagic cell death. Spautin-1 promots the degradation of Vps34 complexes by regulating the deubiquitination activity of USP10 and USP13, and reduces the levels of PtdIns3P. In PDGF-treated cells, spautin-1 stabilizes α-smooth muscle cell actin and calponin, prevents actin filament disorganization, diminishes production of extracellular matrix, and abrogates VSMC hyperproliferation and migration. In CML cells, spautin-1 markedly inhibits IM-induced autophagy by downregulating Beclin-1, and enhances IM-induced apoptosis by inactivating PI3K/AKT and activating downstream GSK3β. Spautin-1 also specifically reduces infectious dengue virus titers in BHK-21 cells.


Kinase Assay: Apoptotic morphology was studied by staining the cells with Hoechst 33258 (KeyGen Biotech) fluorescent stain. Cells (1×105/ml) were seeded into a 12-well plate with indicated concentration of IM (500 nM) for 12 h. Then spautin-1 (10 μM) or DMSO was added to K562 medium for further 36 h. After incubation, cells were stained with 20 mg/ml of Hoechst 33258 for 10 min and observed under a fluorescence microscope (Olympus).


Cell Assay: Spautin-1 promotes the degradation of Vps34 PI3 kinase complexes via inhibiting two ubiquitinspecific peptidases, USP10 and USP13, that target the Beclin1 subunit of Vps34 complexes. Spautin-1 had no effect on the growth and survival of Bcap-37 cells under normal culture conditions but dramatically enhanced cell death in glucose-free media. Under glucose-free conditions, western blotting for LC3 further confirmed that autophagy was induced, which was inhibited by spautin-1. Similar results were obtained with MCF-7 and BT549 cells. Therefore, spautin-1 can sensitize tumor cells to apoptosis under nutritional deprived conditions.

In VivoSpautin-1 ameliorates the pathogenesis of acute pancreatitis induced by cerulein or L-arginine. Spautin-1 pretreatment significantly diminishes the elevation of serum amylase and lipase levels, which are indicative of trypsin activity. Increasing levels of serum TNFα caused by cerulein are inhibited in the presence of spautin-1. Spautin-1 treatment can ameliorate the inflammation damage induced by cerulein, such as edema, degeneration, coagulative necrosis and infiltration of inflammatory cells.
Animal model Mice models with acute pancreatitis, including cerulein- and L-arginine-induced models
Formulation & Dosage Four intraperitoneal injections of cerulein (50 μg/kg body weight) are given consecutively at hourly intervals; The L-arginine-induced model received hourly intraperitoneal injections of 1.4 g/kg (optimal dosage for this study) L-arginine three times
ReferencesCell. 2011 Sep 30;147(1):223-34; Biochem J. 2013 May 1;451(3):375-88; Int J Oncol. 2014 May;44(5):1661-8.