GSK'872

製品コードS8465 バッチS846503

印刷

化学情報

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)

Water

Insoluble

Ethanol

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。	2.500mg/ml (6.52mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 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.

* <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. This compound 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. It also blocks necroptosis in primary human neutrophils isolated from whole blood. This chemical 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 this compound 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.

参考

https://pubmed.ncbi.nlm.nih.gov/25459880/
https://pubmed.ncbi.nlm.nih.gov/24019532/
https://pubmed.ncbi.nlm.nih.gov/28724891/

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：

Soluble tissue factor generated by necroptosis-triggered shedding is responsible for thrombosis [ Cell Res, 2025, 10.1038/s41422-025-01167-8]	PubMed: 40940518
Ferroptosis-activating metabolite acrolein antagonizes necroptosis and anti-cancer therapeutics [ Nat Commun, 2025, 16(1):4919]	PubMed: 40425585
ZBP1-sensed hypoxic stress triggers intrinsic necroptosis in hepatocytes, aggravating hepatic ischemia-reperfusion injury: an experimental study [ Int J Surg, 2025, 10.1097/JS9.0000000000003018]	PubMed: 40697084
The NSP5, ORF6 and NSP13 of SARS-CoV-2 Cooperate to Modulate Inflammatory Cell Death Activation [ Adv Sci (Weinh), 2025, 12(41):e03977]	PubMed: 40810650
A bacterial network of T3SS effectors counteracts host pro-inflammatory responses and cell death to promote infection [ EMBO J, 2025, 10.1038/s44318-025-00412-5]	PubMed: 40128366
Cholesterol 25-Hydroxylase Enhances Myeloid-Derived Suppressor Cell (MDSC) Immunosuppression via the Stimulator of Interferon Genes (STING)-Tank-Binding Kinase 1 (TBK1)-Receptor-Interacting Protein Kinase 3 (RIPK3) Pathway in Colorectal Cancer [ MedComm (2020), 2025, 6(10):e70411]	PubMed: 41020041
RIPK1 is required for ZBP1-driven necroptosis in human cells [ PLoS Biol, 2025, 23(2):e3002845]	PubMed: 39982916
Plasticity of cell death pathways ensures GSDMD activation during Yersinia pseudotuberculosis infection [ Cell Rep, 2025, 44(1):115216]	PubMed: 39823227
T3SS effector EseJ in Edwardsiella piscicida inhibits PANoptosis in macrophages [ Commun Biol, 2025, 8(1):1420]	PubMed: 41044169
Targeting alveolar epithelial cells with lipid micelle-encapsulated necroptosis inhibitors to alleviate acute lung injury [ Commun Biol, 2025, 8(1):573]	PubMed: 40188179

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。