ERK5-IN-1

製品コードS7334 バッチS733401

印刷

化学情報

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5mg/ml (7.83mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.25mg/ml (0.39mM)	Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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	ERK5-IN-1 (XMD17-109) は、162 nM の IC50 を持つ強力で選択的な ERK5 阻害剤です。
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.

プロトコル(参考用のみ)

キナーゼアッセイ	ERK5 kinase activity in vitro assay
キナーゼアッセイ	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.

参考

https://pubmed.ncbi.nlm.nih.gov/24239623/

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：

NKX2-5 regulates vessel remodeling in scleroderma-associated pulmonary arterial hypertension [ JCI Insight, 2024, 9(10)e164191]	PubMed: 38652537
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。

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