GSK'872

製品コードS8465 バッチS846502

印刷

化学情報

Chemical Structure Synonyms GSK2399872A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H17N3O2S2
分子量 383.49 CAS No. 1346546-69-7
Solubility (25°C)* 体外 DMSO 76 mg/mL (198.17 mM)
Ethanol 76 mg/mL (198.17 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 GSK'872 is a potent and selective RIP3 kinase inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity.
in vitro When assayed at 1 μM, GSK'872 fails to inhibit most of 300 human protein kinases tested. It fails to inhibit RIP1 kinase when tested directly. GSK'872 blocks TNF-induced necroptosis in a concentration-dependent manner in HT-29 cells. In cell-based assays, there is a 100- to 1000-fold shift in the IC50 compared to the cell-free biochemical assays. GSK'872 also blocks necroptosis in primary human neutrophils isolated from whole blood. GSK'872 inhibits TLR3- or DAI-induced death, two RIP1-independent pathways of necroptosis. It induces caspase activation followed by apoptotic cell death[1].
in vivo GSK'872 treatment significantly decreases HIF-1α expression compared with no treatment after ischemia injury in vivo[3].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 3T3-SA cells
濃度 0.3, 1, 3 μM
反応時間 18 h
実験の流れ

Viability of 3T3-SA cells at 18 h after treatment with TNF in the presence of Z-VAD-fmk in vehicle control (DMSO) or treated with the indicated concentrations of RIP3 kinase inhibitors, GSK'843 or GSK'872 are assayed.
動物実験 動物モデル C57BL/6 mice
投薬量 1.9 mmol/kg
投与方法 i.p.

カスタマーフィードバック

Data from [Data independently produced by , , Cell Physiol Biochem, 2018, 46(2):699-712]

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：

EFHD2 suppresses intestinal inflammation by blocking intestinal epithelial cell TNFR1 internalization and cell death [ Nat Commun, 2024, 15(1):1282] PubMed: 38346956
Heterogeneous ferroptosis susceptibility of macrophages caused by focal iron overload exacerbates rheumatoid arthritis [ Redox Biol, 2024, 69:103008] PubMed: 38142586
NR4A1 depletion inhibits colorectal cancer progression by promoting necroptosis via the RIG-I-like receptor pathway [ Cancer Lett, 2024, 585:216693] PubMed: 38301909
Bacillus cereus cereolysin O induces pyroptosis in an undecapeptide-dependent manner [ Cell Death Discov, 2024, 10(1):122] PubMed: 38458999
Role of the RIP3-PGAM5-Drp1 pathway in aluminum-induced PC12 cells necroptosis [ Ecotoxicol Environ Saf, 2024, 270:115860] PubMed: 38142589
Cooperative sensing of mitochondrial DNA by ZBP1 and cGAS promotes cardiotoxicity [ Cell, 2023, 186(14):3013-3032.e22] PubMed: 37352855
The transcription factor ATF3 switches cell death from apoptosis to necroptosis in hepatic steatosis in male mice [ Nat Commun, 2023, 14(1):167] PubMed: 36690638
Dimethyl fumarate inhibits necroptosis and alleviates systemic inflammatory response syndrome by blocking the RIPK1-RIPK3-MLKL axis [ Pharmacol Res, 2023, 189:106697] PubMed: 36796462
Fighting cancer by triggering non-canonical mitochondrial permeability transition-driven necrosis through reactive oxygen species induction [ Free Radic Biol Med, 2023, 202:35-45] PubMed: 36963639
Celastrol inhibits necroptosis by attenuating the RIPK1/RIPK3/MLKL pathway and confers protection against acute pancreatitis in mice [ Int Immunopharmacol, 2023, 117:109974] PubMed: 37012867

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。