RU.521

製品コードS6841 バッチS684102

印刷

化学情報

Chemical Structure Synonyms RU320521 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C19H12Cl2N4O3
分子量 415.23 CAS No. 2262452-06-0
Solubility (25°C)* 体外 DMSO 83 mg/mL (199.88 mM)
Ethanol 2 mg/mL (4.81 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
2%DMSO 98%Corn oil
0.5mg/ml Taking the 1 mL working solution as an example, add 20 μL of 25 mg/ml clear DMSO stock solution to 980 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
2% DMSO 40% PEG 300 5%Tween80 53%ddH2O
1.0mg/ml Taking the 1 mL working solution as an example, add 20 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 530 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 RU.521 (RU320521) is an active, potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS) that inhibits the cGAS-mediated signaling with IC50 of 700 nM. RU.521 binds to the cGAS/dsDNA complex with Kd of 36.2 nM.
in vitro

RU.521, a cGAS inhibitor, impares the overexpression of interferon-stimulated genes (ISGs) in response to cytolethal distending toxin (CDT), confirming the crucial role of cGAS-STING axis in CDT-induced type I IFN signaling.[2]
in vivo

RU.521 alleviated the inflammatory response and alleviated the damage induced by oxidative stress, leading to cardiac protection via increased Sirt3 expression in the hearts of mice with sepsis.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Mouse Embryonic Fibroblasts (MEFs)
濃度 1 μM
反応時間 3, 7, 40 days
実験の流れ

MEFs are exposed with or without STINGi or cGASi to CDT 7.5 ng/ml for the indicated times or to the H153A CDT mutant for 40 days. The mRNA level of the indicated genes is analyzed by RT-qPCR and the IL-6 or TNFα production in the culture supernatant are determined by ELISA. For ELISA assays, a 2 days exposure to LPS 100 ng/ml is used as positive control.
動物実験 動物モデル Mice
投薬量 5 mg/kg
投与方法 i.p.

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：

Inhibiting autophagy enhanced mitotic catastrophe-mediated anticancer immune responses by regulating the cGAS-STING pathway [ Cancer Lett, 2024, 586:216695] PubMed: 38325769
Luteolin inhibits herpes simplex virus 1 infection by activating cyclic guanosine monophosphate-adenosine monophosphate synthase-mediated antiviral innate immunity [ Phytomedicine, 2023, 120:155020] PubMed: 37632997
Spinal TAOK2 contributes to neuropathic pain via cGAS-STING activation in rats [ iScience, 2023, 26(10):107792] PubMed: 37720090
Spinal TAOK2 contributes to neuropathic pain via cGAS-STING activation in rats [ iScience, 2023, 26(10):107792] PubMed: 37720090
FLASH X-ray spares intestinal crypts from pyroptosis initiated by cGAS-STING activation upon radioimmunotherapy [ Proc Natl Acad Sci U S A, 2022, 119(43):e2208506119] PubMed: 36256824
AKT1 Is Required for a Complete Palbociclib-Induced Senescence Phenotype in BRAF-V600E-Driven Human Melanoma [ Cancers (Basel), 2022, 14(3)572] PubMed: 35158840
Inhibition of cGAS in Paraventricular Nucleus Attenuates Hypertensive Heart Injury Via Regulating Microglial Autophagy [ Mol Neurobiol, 2022, 59(11):7006-7024] PubMed: 36070120
Inhibition of the cGAS-STING Pathway Attenuates Lung Ischemia/Reperfusion Injury via Regulating Endoplasmic Reticulum Stress in Alveolar Epithelial Type II Cells of Rats [ J Inflamm Res, 2022, 15:5103-5119] PubMed: 36091334
Chronic exposure to Cytolethal Distending Toxin (CDT) promotes a cGAS-dependent type I interferon response [ Cell Mol Life Sci, 2021, 10.1007/s00018-021-03902-x] PubMed: 34308492
The cGAS-STING signaling pathway contributes to the inflammatory response and autophagy in Aspergillus fumigatus keratitis [ Exp Eye Res, 2020, S0014-4835(20)30624-2] PubMed: 33227296

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。