BMS-582949

製品コードS8124 バッチS812401

印刷

化学情報

Chemical Structure Synonyms PS540446 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C22H26N6O2
分子量 406.48 CAS No. 623152-17-0
Solubility (25°C)* 体外 DMSO 81 mg/mL (199.27 mM)
Water Insoluble
Ethanol 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 BMS-582949 (PS540446) is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM,inhibiting both p38 kinase activity and activation of p38.
in vitro BMS-582949 is found to inhibit p38 activation in cells, as measured by phosphorylation of p38. BMS-582949 treatment of cells in which p38 has been activated by LPS rapidly reversed p38 activation as shown by loss of phosphorylation of p38. BMS-582949 is therefore a dual action p38 kinase inhibitor, inhibiting both p38 kinase activity and p38 activation in cells. BMS-582949 binding to p38a results in a conformational change of the activation loop which is phosphorylated by upstream kinases, therefore it inhibits phosphorylation of p38 by upstream MKK by inducing a less accessible conformation of the activation loop[2].
in vivo The mouse clearance rate for BMS-582949 is 4.4 mL/min/kg. And at an oral dose of 10 mg/kg, the mouse AUC0-8 h for BMS-582949 is 75.5 μM•h. BMS-582949 exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively[1].

プロトコル(参考用のみ)

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：

ASK1 inhibitor NQDI‑1 decreases oxidative stress and neuroapoptosis via the ASK1/p38 and JNK signaling pathway in early brain injury after subarachnoid hemorrhage in rats [ Mol Med Rep, 2023, 27(2)47] PubMed: 36633130
Reciprocal priming between receptor tyrosine kinases at recycling endosomes orchestrates cellular signalling outputs [ EMBO J, 2021, e107182] PubMed: 34086370
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] PubMed: 32645325
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] PubMed: 32645325
Melatonin protects mouse testes from palmitic acid-induced lipotoxicity by attenuating oxidative stress and DNA damage in a SIRT1-dependent manner [ J Pineal Res, 2020, 69(4):e12690] PubMed: 32761924
Melatonin Protects Mouse Testes from Palmitic Acid-Induced Lipotoxicity by Attenuating Oxidative Stress and DNA Damage in a SIRT1-Dependent Manner [ J Pineal Res, 2020, e12690] PubMed: 32761924
5-HT7 Receptor Contributes to Proliferation, Migration and Invasion in NSCLC Cells. [ Onco Targets Ther, 2020, 13:2139-2151] PubMed: 32210580
Corticosteroids inhibit Mycobacterium tuberculosis-induced necrotic host cell death by abrogating mitochondrial membrane permeability transition. [ Nat Commun, 2019, 10(1):688] PubMed: 30737374
Curcuminoid WZ35 synergize with cisplatin by inducing ROS production and inhibiting TrxR1 activity in gastric cancer cells. [ J Exp Clin Cancer Res, 2019, 38(1):207] PubMed: 31113439
Piperlongumine potentiates the antitumor efficacy of oxaliplatin through ROS induction in gastric cancer cells. [ Cell Oncol (Dordr), 2019, 10.1007/s13402-019-00471-x] PubMed: 31493144

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。