SB239063

製品コードS7741 バッチS774101

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

C20H21FN4O2
分子量 368.4 CAS No. 193551-21-2
Solubility (25°C)* 体外 DMSO 60 mg/mL (162.86 mM)
Ethanol (warmed with 50ºC water bath) 7 mg/mL (19.0 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO Corn oil
3.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 60 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 SB239063 is a potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms.
in vitro SB 239063 potently inhibits IL-1 and TNF-α production in LPS-stimulated human peripheral blood monocytes with IC50 of 120 and 350 nM, respectively. [1] In oxygen-glucose-deprived hippocampal slice cultures, SB239063 strikingly reduces the levels of the pro-inflammatory cytokine IL-1beta, causes cell death after oxygen-glucose deprivation and significantly diminishes microglia activation. [2] In human corneal endothelial cell, SB 239063 inhibits TGF-β(2) and FGF-2-induced cell migration. [4]
in vivo In both guinea pigs and mice, SB 239063 (10 mg/kg, p.o.) reduces antigen-induced airway eosinophilia. [1] In air- and ozone-exposed C57/BL6 and MKP-1(-/-) mice, SB239063 inhibits bronchial contraction. [3]

プロトコル(参考用のみ)

キナーゼアッセイ In Vitro Studies Kinase Assays
Yeast-expressed, activated, and purified p38α (3.55 nM) is added to the reaction mixture (30 μL) containing 25 mM HEPES, pH 7.5; 10 mM MgCl2; 0.2 mM sodium orthovanadate; 1 mM dithiothreitol; 0.1% BSA; 10% (w/v) glycerol; 0.17 mM/2.5 μCi of [γ-32P]ATP; 0.67 mM the endothelial growth factor receptor-derived T669 peptide as the substrate in the presence or absence of SB 239063. Incubation is for 25 min at 37°C in 96-well plates, the reactions are stopped by adding 10 μL of 0.3 M phosphoric acid, and phosphorylated peptide is isolated from the reaction mixture on phosphocellulose (p81) filters. Filters are washed three times with 75 mM phosphoric acid, followed by three times with H2O, and counted for bound32P. The inhibitor is preincubated with the reaction mixture on ice for 30 min before starting the reactions with [γ-32P]ATP.
動物実験 動物モデル Guinea pigs
投薬量 ~30 mg/kg
投与方法 p.o.

カスタマーフィードバック

, , Oncogene, 2017, 36(23):3312-3321

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：

Inhibition of Macropinocytosis Enhances the Sensitivity of Osteosarcoma Cells to Benzethonium Chloride [ Cancers (Basel), 2023, 15(3)961] PubMed: 36765917
Microglial P2Y12 Signaling Contributes to Cisplatin-induced Pain Hypersensitivity via IL-18-mediated Central Sensitization in the Spinal Cord [ J Pain, 2023, S1526-5900(23)00013-5] PubMed: 36646400
Conjugated secondary 12α-hydroxylated bile acids promote liver fibrogenesis [ EBioMedicine, 2021, 66:103290] PubMed: 33752128
Cardamonin inhibits the growth of human osteosarcoma cells through activating P38 and JNK signaling pathway [ Biomed Pharmacother, 2021, 134:111155] PubMed: 33370628
Polysaccharides from Ulva prolifera O.F. Müller inhibit cell proliferation via activating MAPK signaling in A549 and H1650 cells [ Food Funct, 2021, 12(15):6915-6924] PubMed: 34132294
Reparative Effects of Ethanol-Induced Intestinal Barrier Injury by Flavonoid Luteolin via MAPK/NF-κB/MLCK and Nrf2 Signaling Pathways [ J Agric Food Chem, 2021, 10.1021/acs.jafc.1c00199] PubMed: 33749262
A phospho-regulated ensemble signal motif of α-TAT1 drives dynamic microtubule 1 acetylation 2 [ HAL open science, 2021, 10.1101/2020.09.23.310235] PubMed: None
A stress response p38 MAP kinase inhibitor SB202190 promoted TFEB/TFE3-dependent autophagy and lysosomal biogenesis independent of p38. [ Redox Biol, 2020, 28:101445] PubMed: 32037305
Chronic-plus-binge Alcohol Intake Induces Production of Proinflammatory mtDNA-enriched Extracellular Vesicles and Steatohepatitis via ASK1-p38MAPKα-dependent Mechanisms [ JCI Insight, 2020, 136496] PubMed: 32544093
p38α Regulates Expression of DUX4 in a Model of Facioscapulohumeral Muscular Dystrophy [ J Pharmacol Exp Ther, 2020, 374(3):489-498] PubMed: 32576599

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。