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2138300-40-8

2138300-40-8 structure
2138300-40-8 structure
  • Name: STING agonist diABZI compound 2
  • Chemical Name: STING agonist-4
  • CAS Number: 2138300-40-8
  • Molecular Formula: C34H38N12O4
  • Molecular Weight: 678.74
  • Catalog: Signaling Pathways Immunology/Inflammation STING
  • Create Date: 2019-08-03 17:33:58
  • Modify Date: 2024-01-03 06:32:12
  • 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].

Name STING agonist-4
Description 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].
Related Catalog
Target

IC50: 20 nM (STING agonist-4)[1]

In Vitro 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) Concentration: 0.3 μM, 1 μM, 3 μM, 10 μM and 30 μM Incubation Time: 2 hours Result: Caused phosphorylation of IRF3 and STING and induced secretion of IFN-β.
References

[1]. Ramanjulu JM et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Dec;564(7736):439-443.

Molecular Formula C34H38N12O4
Molecular Weight 678.74