SBI-0206965

製品コードS7885 バッチS788503

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

C21H21BrN4O5
分子量 489.32 CAS No. 1884220-36-3
Solubility (25°C)* 体外 DMSO 98 mg/mL (200.27 mM)
Ethanol 14 mg/mL warmed with 50ºC water bath (28.61 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 SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. SBI-0206965 inhibits autophagy and enhances apoptosis in human glioblastoma and lung cancer cells.
in vitro

In HEK293T transfected with WT or KI Myc-tagged ULK1 and WT Vps34, SBI-0206965 inhibits Ser249 phosphorylation of overexpressed Vps34 and Beclin1 Ser15 phosphorylation. SBI-0206965 suppresses autophagy induced by mTOR inhibition in A549 cells, and prevents ULK1-dependent cell survival in WT MEFs. In addition, SBI-0206965 also synergizes with mTOR inhibition to induce cancer cell death. [1]

プロトコル(参考用のみ)

キナーゼアッセイ ULK1 kinase assays
γ-32P-ATP assays to measure ULK1 kinase activity are performed. Briefly, Flag-ULK1 is transfected into HEK-293T cells and 20 hours later treated as indicated. The immmunoprecipitate is washed in IP buffer 3 times, and washed in kinase buffer (25 mM MOPS, pH 7.5, 1 mM EGTA, 0.1 mM Na3VO4, 15 mM MgCl2,). Hot and cold ATP are added at a 100 μM final concentration. As substrates, GST or the recombinant protein GST-Atg101 purified from E. coli were used at 1 μg for each reaction. Reactions are boiled and run out on SDS-PAGE gels. Gels are dried and imaged using PhosphoImager software.
細胞アッセイ 細胞株 A498 cells
濃度 10 μM
反応時間 24 h
実験の流れ

Cells were treated with indicated concentration of drug for 24 h.
動物実験 動物モデル Male BALB/c nude mice
投薬量 50 mg/kg
投与方法 i.p.

カスタマーフィードバック

, , Biochim Biophys Acta, 2017, 1863(11):2796-2807

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：

A multiplexed siRNA screen identifies key kinase signaling networks of brain glia [ Life Sci Alliance, 2023, 6(5)e202201605] PubMed: 36878638
MEK inhibition overcomes chemoimmunotherapy resistance by inducing CXCL10 in cancer cells [ Cancer Cell, 2022, S1535-6108(21)00662-0] PubMed: 35051357
Spatially resolved phosphoproteomics reveals fibroblast growth factor receptor recycling-driven regulation of autophagy and survival [ Nat Commun, 2022, 13(1):6589] PubMed: 36329028
Autophagy Enhances Longevity of Induced Pluripotent Stem Cell-Derived Endothelium via mTOR-Independent ULK1 Kinase [ Stem Cells Transl Med, 2022, 11(11):1151-1164] PubMed: 36173887
TP53 loss-of-function causes vulnerability to autophagy inhibition in aggressive prostate cancer [ Int J Urol, 2022, 29(9):1085-1094] PubMed: 35975690
PKCλ/ι inhibition activates an ULK2-mediated interferon response to repress tumorigenesis [ Mol Cell, 2021, S1097-2765(21)00729-2] PubMed: 34560002
Plasmalogens regulate the AKT-ULK1 signaling pathway to control the position of the axon initial segment [ Prog Neurobiol, 2021, S0301-0082(21)00137-4] PubMed: 34302896
Excessive ROS production and enhanced autophagy contribute to myocardial injury induced by branched-chain amino acids: Roles for the AMPK-ULK1 signaling pathway and α7nAChR [ Biochim Biophys Acta Mol Basis Dis, 2021, 1867(1):165980] PubMed: 32980459
Dysregulated Provision of Oxidisable Substrates to the Mitochondria in ME/CFS Lymphoblasts [ Int J Mol Sci, 2021, 22(4)2046] PubMed: 33669532
Nonclassical autophagy activation pathways are essential for production of infectious Influenza A virus in vitro [ Mol Microbiol, 2021, 10.1111/mmi.14865] PubMed: 34931347

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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