GSK8612

製品コードS8872 バッチS887201

印刷

化学情報

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

C17H17BrF3N7O2S
分子量 520.33 CAS No. 2361659-62-1
Solubility (25°C)* 体外 DMSO 100 mg/mL (192.18 mM)
Ethanol 6 mg/mL (11.53 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 GSK8612 is a highly potent and selective inhibitor for TBK1 (Tank-binding Kinase-1) with pKd of 8.0. Within 10-fold affinity with respect to TBK1, no off-targets of GSK8612 could be identified.
in vitro

In cellular assays, this small molecule inhibits toll-like receptor (TLR)3-induced interferon regulatory factor (IRF)3 phosphorylation in Ramos cells and type I interferon (IFN) secretion in primary human mononuclear cells. In THP1 cells, GSK8612 is able to inhibit secretion of interferon beta (IFNβ) in response to dsDNA and cGAMP, the natural ligand for STING. GSK8612 has lower affinity for phosphorylated TBK1. GSK8612 inhibits recombinant TBK1 with an average pIC50 of 6.8 in a biochemical functional assay. The actual selectivity of GSK8612 for TBK1 in the cells will depend on the activation state of TBK1[1].
in vivo

GSK8612 is highly protein bound in mouse, rat and human blood[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Ramos cells
濃度 6.8 (pKd)
反応時間 1 h
実験の流れ

Ramos cells were exposed to GSK8612 for 60 min in cell culture media (RPMI1640, Gibco) containing 2% fetal bovine serum (FBS, Gibco) and then stimulated with poly(I:C) (30 µg/mL, Invivogen) for 120 min at 37°C, 5% CO2.
動物実験 動物モデル Male BALB/c nude and C57BL/6 mice
投薬量 5 mg/kg
投与方法 p.o.

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：

A TLR4/TRAF6-dependent signaling pathway mediates NCoR coactivator complex formation for inflammatory gene activation [ Proc Natl Acad Sci U S A, 2024, 121(2):e2316104121] PubMed: 38165941
Galectin-9 blockade synergizes with ATM inhibition to induce potent anti-tumor immunity [ Int J Biol Sci, 2023, 19(3):981-993] PubMed: 36778120
Galectin-9 blockade synergizes with ATM inhibition to induce potent anti-tumor immunity [ Int J Biol Sci, 2023, 19(3):981-993] PubMed: 36778120
Serine/threonine kinase TBK1 promotes cholangiocarcinoma progression via direct regulation of β-catenin [ Oncogene, 2023, 42(18):1492-1507] PubMed: 36928362
Regulation of Synovial γδ T Cell Ligand Expression by Mitochondrial Reactive Oxygen Species and Gasdermin-D [ J Immunol, 2023, 210(1):61-71] PubMed: 36445376
FACT subunit SUPT16H associates with BRD4 and contributes to silencing of interferon signaling [ Nucleic Acids Res, 2022, 50(15):8700-8718] PubMed: 35904816
MD2 deficiency prevents high-fat diet-induced AMPK suppression and lipid accumulation through regulating TBK1 in non-alcoholic fatty liver disease [ Clin Transl Med, 2022, 12(3):e777] PubMed: 35343085
Molecular mechanism of RIPK1 and caspase-8 in homeostatic type I interferon production and regulation [ Cell Rep, 2022, 41-1:111434] PubMed: 36198273
cGAS-STING activation contributes to podocyte injury in diabetic kidney disease [ iScience, 2022, 25(10):105145] PubMed: 36176590
Pharmacological Inhibition of IKK to Tackle Latency and Hyperinflammation in Chronic HIV-1 Infection [ Int J Mol Sci, 2022, 23(23)15000] PubMed: 36499329

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。

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