| Identification | Back Directory | [Name]
1H-Benzimidazole-5-carboxamide, 1,1'-(1,4-butanediyl)bis[2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]- | [CAS]
2138300-40-8 | [Synonyms]
STING agonist-4
1H-Benzimidazole-5-carboxamide, 1,1'-(1,4-butanediyl)bis[2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]- | [Molecular Formula]
C34H38N12O4 | [MDL Number]
MFCD32197200 | [MOL File]
2138300-40-8.mol | [Molecular Weight]
678.74 |
| Chemical Properties | Back Directory | [density ]
1.48±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: slightly soluble | [form ]
A solid | [pka]
11.97±0.43(Predicted) | [color ]
White to gray | [InChIKey]
ICZSAXDKFXTSGL-UHFFFAOYSA-N | [SMILES]
C(N1C(NC(C2N(CC)N=C(C)C=2)=O)=NC2=CC(C(N)=O)=CC=C21)CCCN1C(NC(C2N(CC)N=C(C)C=2)=O)=NC2=CC(C(N)=O)=CC=C21 |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
STING agonist-4 is a stimulator of receptor agonists of the interferon gene (STING) with an apparent inhibition constant IC50 of 20 nM, It is a compound containing two symmetrically related aminobenzimidazoles (ABZI ) based compounds. | [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 EC 50 of 3.1 μM. 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 (K d < /sub> ) of approximately 1.6 nM. It (Compound 2) (0-100 μM) is 18-fold more potent than cGAMP (an endogenous STING ligand), with an EC 50 of 53.9 μM. 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. Cell Viability Assay | Cell Line: | Human peripheral blood mononucl ear cells (PBMCs) | | Concentration: | 0.3 μM, 1 μM, 3 μM, 10 μM and 30 μM | | Incubation Time: | 2 hours | < td class="col1"> Result: | Caused phosphorylation of IRF3 and STING and induced secretion of IFN-β. | | [target]
IC50: 20 nM (STING agonist-4) | [References]
[1] Ramanjulu JM et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Dec;564(7736):439-443. DOI:10.1038/s41586-018-0705-y |
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BOC Sciences
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http://www.bocsci.com |
| Company Name: |
InvivoChem
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13549236410 |
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http://www.invivochem.cn/ |
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