STING agonist-4 (Synonyms: CS-0087594, Diamidobenzimidazole STING Agonist-2, diABZI-4, HY-123943, STING Agonist-4, STING Agonist diABZI Compound 2) |
カタログ番号GC37693 |
STING アゴニスト-4 は、20 nM の見かけの阻害定数 (IC50) を持つインターフェロン遺伝子 (STING) 受容体アゴニストの刺激因子です。 STING アゴニスト-4 は、STING と細胞機能への結合が強化された結合 ABZI (diABZI) を作成する、2 つの対称性に関連するアミドベンズイミダゾール (ABZI) ベースの化合物です。
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Cas No.: 2138300-40-8
Sample solution is provided at 25 µL, 10mM.
STING agonist-4 is an stimulator of Interferon Genes (STING) receptor agonist with an apparent inhibitory constant (IC50) of 20 nM. STING agonist-4 is a two symmetry-related amidobenzimidazole (ABZI)-based compound to create linked ABZIs (diABZIs) with enhanced binding to STING and cellular function[1]. IC50: 20 nM (STING agonist-4)[1]
STING agonist-4 (Compound 2) (0.3-30 μM; 2 hours) causes phosphorylation of IRF3 and STING that is inhibited by the TBK1 inhibitor BX795 and induces dose-dependent secretion of IFN-β with an EC50 of 3.1 μM[1]. STING agonist-4 (Compound 2) (0.001 nM-1 μM) inhibits binding of full-length STING to the solid support with an apparent dissociation constant (Kd) of approximately 1.6 nM[1].STING agonist-4 (Compound 2) (0-100 μM) is 18-fold more potent than cGAMP (an endogenous STING ligand), with an EC50 of 53.9 μM[1]. STING agonist-4 (Compound 2) (3 μM; 4 hours) promotes production of interferon γ-induced protein 10 (IP-10), IL-6 and TNF-α by a mechanism that is dependent on STING-mediated activation of TBK1[1]. Cell Viability Assay[1] Cell Line: Human peripheral blood mononuclear cells (PBMCs)
[1]. Ramanjulu JM et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Dec;564(7736):439-443.
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