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) 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
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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