ERK5-IN-1

製品コードS7334 バッチS733401

印刷

化学情報

Chemical Structure Synonyms XMD17-109 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C36H46N8O3
分子量 638.81 CAS No. 1435488-37-1
Solubility (25°C)* 体外 DMSO 100 mg/mL (156.54 mM)
Ethanol 100 mg/mL (156.54 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.

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生物活性

製品説明 ERK5-IN-1 (XMD17-109) is a potent, and selective ERK5 inhibitor with IC50 of 162 nM.
in vitro ERK5-IN-1 potently inhibits ERK5 biochemically with an IC50 of 162 nM and in cells with a cellular EC50 for inhibiting epidermal growth factor induced ERK5 autophosphorylation of 0.09 μM.[1]

プロトコル(参考用のみ)

キナーゼアッセイ ERK5 kinase activity in vitro assay
Kinase activity is determined in an assay volume of 40 μL in kinase buffer (50 mM Tris-HCl, pH 7.5, 0.1 mM EGTA, 1 mM 2-mercaptoethanol) containing 200 ng of pure active ERK5 and the indicated amount of inhibitor. Reaction starts by adding 10 mM magnesium acetate, and 50 μM [γ-32P]-ATP (500 cpm/pmol) and 250 μM PIMtide (ARKKRRHPSGPPTA) as substrates. Assays are carried out for 20 min at 30℃ and terminated by applying the reaction mixture onto p81 paper and the incorporated radioactivity is measured.

カスタマーフィードバック

Data from [Data independently produced by , , J Thromb Haemost, 2017, 15(8):1679-1688]

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：

Transcriptional control of pancreatic cancer immunosuppression by metabolic enzyme CD73 in a tumor-autonomous and -autocrine manner [ Nat Commun, 2023, 14(1):3364] PubMed: 37291128
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors [ J Med Chem, 2021, 10.1021/acs.jmedchem.1c01096] PubMed: 34710325
Reversal of ABCB1-related multidrug resistance by ERK5-IN-1. [ J Exp Clin Cancer Res, 2020, 12;39(1):50] PubMed: 32164732
Aurora kinase inhibition sensitizes melanoma cells to T-cell-mediated cytotoxicity [ Cancer Immunol Immunother, 2020, 10.1007/s00262-020-02748-9] PubMed: 33123754
Increased Expression of EGR1 and KLF4 by Polysulfide via Activation of the ERK1/2 and ERK5 Pathways in Cultured Intestinal Epithelial Cells [ Biomed Res, 2020, 41(3):119-129] PubMed: 32522929
Extracellular signal-regulated kinase 5 associates with casein kinase II to regulate GPIb-IX-mediated platelet activation via the PTEN/PI3K/Akt pathway [ J Thromb Haemost, 2017, 15(8):1679-1688] PubMed: 28603902

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。