受注:045-509-1970 |
技術サポート:[email protected] 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
||||
化学式 | C14H18N2O |
||||||
分子量 | 230.31 | CAS No. | 2049868-46-2 | ||||
Solubility (25°C)* | 体外 | DMSO (warmed with 50ºC water bath) | 200 mg/mL (868.39 mM) | ||||
Ethanol | 46 mg/mL (199.73 mM) | ||||||
Water | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
|
||||||
* <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. |
製品説明 | GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases. |
---|---|
in vitro | GSK'963 inhibits RIP1-dependent cell death with an IC50 of between 1 and 4 nM in human and murine cells[1]. |
in vivo | GSK'963 is a potent inhibitor of a TNF+zVAD-mediated lethal shock. At 2 mg/kg, GSK'963 would maintain blood concentrations above the concentration required for 90% inhibition of RIP1 activity for an extended period of time compared with Nec-1[1]. |
細胞アッセイ | 細胞株 | BMDM |
---|---|---|
濃度 | 100 nM | |
反応時間 | 30 min | |
実験の流れ | For immunoblot analysis, BMDM pretreated with GSK'963 (100 nM), GSK'962 (100 nM) or Nec-1 (10 μM) for 30 min, are stimulated with 50 ng/ml TNF for 5 and 15 min. Lysates prepared in 1× Cell Lysis Buffer containing protease and phosphatase inhibitors are separated on 4-12% SDS-PAGE and blotted onto nitrocellulose membrane. Blots are probed for IκB, phospho-IκB, and tubulin as a loading control. |
|
動物実験 | 動物モデル | C57BL/6 mice |
投薬量 | 0.2, 2 and 10 mg/kg | |
投与方法 | i.p. |
Bacillus cereus cereolysin O induces pyroptosis in an undecapeptide-dependent manner [ Cell Death Discov, 2024, 10(1):122] | PubMed: 38458999 |
Polyunsaturated fatty acids-induced ferroptosis suppresses pancreatic cancer growth [ Sci Rep, 2024, 14(1):4409] | PubMed: 38388563 |
Toxoplasma gondii secreted effectors co-opt host repressor complexes to inhibit necroptosis [ Cell Host Microbe, 2021, S1931-3128(21)00192-X] | PubMed: 34043960 |
The MK2/Hsp27 axis is a major survival mechanism for pancreatic ductal adenocarcinoma under genotoxic stress [ Sci Transl Med, 2021, 13(622):eabb5445] | PubMed: 34851698 |
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。