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STING agonist-4

  Cat. No.:  DC12505   Featured
Chemical Structure
2138300-40-8
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Field of application
STING agonist 4 is an amidobenzimidazole (ABZI)-based compound that functions as a STING agonist with Kd of 1.6 nM (binding of endogenous full-length STING, THP-1 cell lysates); caused dose-dependent phosphorylation of IRF3 and STING that was inhibited by the TBK1 inhibitor BX795, induced dose-dependent secretion of IFN-β with EC50 of 3.1 uM in PBMCs (18-fold more potent than cGAMP); promotes production of IFN-γ-induced protein 10 (IP-10), IL-6 and TNFα by a mechanism that is dependent on STING-mediated activation of TBK1; unlike cGAMP and DMXAA, compound 2 efficiently activates STING function while maintaining an open STING confirmation.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2138300-40-8
Chemical Name: 1,1'-(butane-1,4-diyl)bis(2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-1H-benzo[d]imidazole-5-carboxamide)
SMILES: C(N1C2=CC=C(C(N)=O)C=C2N=C1NC(C1N(CC)N=C(C)C=1)=O)CCCN1C2=CC=C(C(N)=O)C=C2N=C1NC(C1N(CC)N=C(C)C=1)=O
Formula: C34H38N12O4
M.Wt: 678.758
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: 1. Ramanjulu JM, et al. Nature. 2018 Nov 7. doi: 10.1038/s41586-018-0705-y.
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].
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC22331 STING agonist compound 3 STING agonist-3, compound 3, is a selective and non-nucleotide small-molecule STING agonist, which has durable anti-tumor effect and tremendous potential to improve treatment of cancer.
DC12505 STING agonist-4 STING agonist 4 is an amidobenzimidazole (ABZI)-based compound that functions as a STING agonist with Kd of 1.6 nM (binding of endogenous full-length STING, THP-1 cell lysates); caused dose-dependent phosphorylation of IRF3 and STING that was inhibited by the TBK1 inhibitor BX795, induced dose-dependent secretion of IFN-β with EC50 of 3.1 uM in PBMCs (18-fold more potent than cGAMP); promotes production of IFN-γ-induced protein 10 (IP-10), IL-6 and TNFα by a mechanism that is dependent on STING-mediated activation of TBK1; unlike cGAMP and DMXAA, compound 2 efficiently activates STING function while maintaining an open STING confirmation.
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