FLI-06

製品コードS7399 バッチS739901

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H30N2O5
分子量 438.52 CAS No. 313967-18-9
Solubility (25°C)* 体外 DMSO 88 mg/mL (200.67 mM)
Ethanol 8 mg/mL (18.24 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 FLI-06 is a novel inhibitor of Notch signaling with EC50 of 2.3 μM.
in vitro In HeLa NotchΔE-eGFP cells, FLI-06 blocks Notch trafficking and processing. FLI-06 changes the maturation pattern of APP and abolishes the shedding of APPs in HEK293 cells stably expressing a mutated APP that yields robust amounts of amyloid β. FLI-06 disrupt the Golgi apparatus, and inhibits general secretion at a step before exit from the endoplasmic reticulum (ER), which is accompanied by a tubule-to-sheet morphological transition of the ER. [1]
in vivo FLI-06 (50 μM) inhibits endogenous Notch signaling in zebrafish embryos. [1]

プロトコル(参考用のみ)

キナーゼアッセイ EC50 determinations
EC50 values of FLI-06 is calculated from serial dilution series ranging from 200 to 0.1 μM. Cells are seeded in 96-well plates at a density of 5,000 cells per well in 100 μL medium. The next day, 100 μL medium containing FLI-06 is added. Cells are incubated for 16 h, fixed and processed for automated microscopy. For the putative GSIs, the enuc intensity is divided by the DAPT control, and for the trafficking inhibitors, the normalized percentage inhibition against DAPT or DMSO controls of log2-transformed nuc-to-enuc ratios are calculated. Relative activity values are read into R, and EC50 estimates are calculated using four-parameter log-logistic fit with the package drc46.
動物実験 動物モデル Zebrafish embryos.
投薬量 50 μM
投与方法 --

カスタマーフィードバック

Data from [Data independently produced by , , Am J Cancer Res, 2017, 7(9):1804-1819]

Data from [Data independently produced by , , Biochem Biophys Res Commun, 2016]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Regulation of reverse electron transfer at mitochondrial complex I by unconventional Notch action in cancer stem cells [ Dev Cell, 2022, 57(2):260-276.e9] PubMed: 35077680
Autophagy-based-unconventional-secretion-of-HMGB1-by-keratinocytes-plays-a-pivotal-role-in-psoriatic-skin-inflammation. [ Autophagy, 2020, 16:1-24] PubMed: 32019420
NCSTN promotes hepatocellular carcinoma cell growth and metastasis via β-catenin activation in a Notch1/AKT dependent manner [ J Exp Clin Cancer Res, 2020, 39(1):128] PubMed: 32631394
HDAC Inhibitor LBH589 Suppresses the Proliferation but Enhances the Antileukemic Effect of Human γδT Cells [ Mol Ther Oncolytics, 2020, 18:623-630] PubMed: 33005729
MYCN-mediated regulation of the HES1 promoter enhances the chemoresistance of small-cell lung cancer by modulating apoptosis. [ Am J Cancer Res, 2019, 9(9):1938-1956] PubMed: 31598396
FLI-06 Intercepts Notch Signaling And Suppresses The Proliferation And Self-renewal Of Tongue Cancer Cells. [ Onco Targets Ther, 2019, 12:7663-7674] PubMed: 31571917
Astrocyte Elevated Gene 1 (AEG-1) Acts as a Promoter Gene in Clear Cell Renal Cell Carcinoma Cell Growth and Metastasis [Yu DP Med Sci Monit, 2018, 24:8213-8223] PubMed: 30431025
NFκB mediated elevation of KCNJ11 promotes tumor progression of hepatocellular carcinoma through interaction of lactate dehydrogenase A [Zhang K Biochem Biophys Res Commun, 2018, 495(1):246-253] PubMed: 29108994
Zinc finger RNA-binding protein promotes non-small-cell carcinoma growth and tumor metastasis by targeting the Notch signaling pathway [Zhang H Am J Cancer Res, 2017, 7(9):1804-1819] PubMed: 28979805
Dysregulation of the ADAM17/Notch signalling pathways in endometriosis: from oxidative stress to fibrosis [ Mol Hum Reprod, 2017, 23(7):488-499] PubMed: 28486700

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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