Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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25mg |
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Other Sizes |
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Purity: ≥98%
STING agonist-4 (diABZI STING agonist-2) is a novel and potent agonist of stimulator of Interferon Genes (STING) receptor 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. It dose-dependentally induced phosphorylation of IRF3 and secretion of IFN-β, promoting production of IFN-γ-induced protein 10 (IP-10), IL-6 and TNFα.
ln Vitro |
STING agonist-4 (Compound 2) (0.3-30 μM; 2 hours) induces dose-dependent secretion of IFN-β with an EC50 of 3.1 μM and phosphorylates STING and IRF3, which is inhibited by the TBK1 inhibitor BX795 [1]. The binding of full-length STING to solid supports is inhibited by STING agonist-4 (Compound 2) (0.001 nM-1 μM), which has an apparent dissociation constant (Kd) of roughly 1.6 nM [1]. With an EC50 of 53.9 μM, STING agonist-4 (Compound 2) (0-100 μM) is 18 times more potent than cGAMP, an endogenous STING ligand [1]. Compound 2, also known as STING agonist-4, (3 μM; 4 hours) stimulates the production of TNF-α, IL-6, and interferon gamma-inducible protein 10 (IP-10), via a mechanism reliant on STING-mediated activation of TBK1 [1].
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Cell Assay |
Cell viability assay[1]
Cell Types: Human peripheral blood mononuclear cells (PBMC) Tested Concentrations: 0.3 μM, 1 μM, 3 μM, 10 μM and 30 μM Incubation Duration: 2 hrs (hours) Experimental Results: Causes phosphorylation of IRF3 and STING and induces secretion Interferon-beta. |
References |
[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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Molecular Formula |
C34H38N12O4
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Molecular Weight |
678.7435
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CAS # |
2138300-40-8
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SMILES |
O=C(C1=C([H])C(C([H])([H])[H])=NN1C([H])([H])C([H])([H])[H])N([H])C1=NC2C([H])=C(C(N([H])[H])=O)C([H])=C([H])C=2N1C([H])([H])C([H])([H])C([H])([H])C([H])([H])N1C(N([H])C(C2=C([H])C(C([H])([H])[H])=NN2C([H])([H])C([H])([H])[H])=O)=NC2C([H])=C(C(N([H])[H])=O)C([H])=C([H])C1=2
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~10 mg/mL (~14.73 mM)
H2O : < 0.1 mg/mL |
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Solubility (In Vivo) |
Solubility in Formulation 1: 1 mg/mL (1.47 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1 mg/mL (1.47 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.4733 mL | 7.3666 mL | 14.7332 mL | |
5 mM | 0.2947 mL | 1.4733 mL | 2.9466 mL | |
10 mM | 0.1473 mL | 0.7367 mL | 1.4733 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.