diABZI STING agonist-1 trihydrochloride (Synonyms: Diamidobenzimidazole STING Agonist-1, STING Agonist (Compound 3), STING Agonist diABZI) |
Catalog No.GC35855
One-Click Copy Product Info
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diABZI STING agonist-1 trihydrochloride is a potent non-nucleotide small molecule STING receptor agonist (EC50=130nM, 186nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2138299-34-8
Sample solution is provided at 25 µL, 10mM.
diABZI STING agonist-1 trihydrochloride is a potent non-nucleotide small molecule STING receptor agonist (EC50=130nM, 186nM). diABZI STING agonist-1 trihydrochloride binds and activates endoplasmic reticulum-localized STING protein, stabilizes its open conformation, recruits and activates TBK1, promotes IRF3 phosphorylation and nuclear translocation, and induces type I interferon and multiple pro-inflammatory cytokines and chemokines expression. diABZI STING agonist-1 trihydrochloride can be used in tumor immunotherapy, antiviral and infectious disease research, and cGAS-STING innate immune signaling pathway studies[1-4].
In vitro, treatment of bone marrow monocytes (BMMs) with 10-200nM diABZI STING agonist-1 trihydrochloride for 6 days reduced the number and area of TRAP-positive multinucleated cells and decreased bone resorption pit area[5]. Treatment of A549 and H1975 cells with 20nM diABZI STING agonist-1 trihydrochloride for 3-14 days upregulated p-STING, cGAS, p-TBK1 and p-IRF3 protein expression, increased IFNβ, CCL5 and CXCL10 mRNA expression and corresponding protein secretion in culture supernatant, with effects similar to ESYT3 overexpression[6]. Treatment of 1G4 HA-TCR engineered T cells with 0.5-10μg/mL diABZI STING agonist-1 trihydrochloride for 3 hours enhanced T cell killing activity against Mel526 and NY-ESO-1 knockout Mel526 cells and increased IFNγ expression[7].
In vivo, a single subcutaneous injection of 2.5mg/kg diABZI STING agonist-1 trihydrochloride into the shaved back region of female BALB/cJ mice induced erythema on day 3, desquamation on day 4, and induration on day 9, along with epidermal thickening, hyperkeratosis, dermal inflammation and fibrosis, ulceration, and neutrophil infiltration[8]. Intratracheal instillation of 0.01-1μg diABZI STING agonist-1 trihydrochloride (40μL) into C57BL/6Rj mice for 3 consecutive days triggered acute neutrophilic airway inflammation, disrupted respiratory barrier function, induced CXCL1 release, neutrophil recruitment, MPO elevation, and total protein exudation in BALF[9]. On days 9 and 13 after tumor implantation, intracranial administration of 0.25mg/kg diABZI STING agonist-1 trihydrochloride via an implanted catheter into C57BL/6 mice bearing CT-2A intracerebral tumors, combined with 3Gy×3 local radiotherapy on days 7, 8, and 9, suppressed tumor growth and prolonged mouse survival[10].
References:
[1] Ramanjulu JM, Pesiridis GS, Yang J, et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Dec;564(7736):439-443.
[2] Li Y, Chen W, Zhang X, et al. STING agonist diABZI confers protection against swine acute diarrhea syndrome coronavirus in neonatal mice by activating antiviral immunity. J Virol. 2026 Feb 17;100(2):e0170325.
[3] Xu Z, Ma Z, Ren H, et al. Exercise training ameliorates high-fat diet-induced skeletal muscle atrophy and ferroptosis via downregulation of STING. Free Radic Biol Med. 2025 Dec 1;240:373-383.
[4] Linder A, Nixdorf D, Kuhl N, et al. STING activation improves T-cell-engaging immunotherapy for acute myeloid leukemia. Blood. 2025 May 8;145(19):2149-2160.
[5] Huang Y, Zhang M, Zhang J, et al. diABZI and poly(l:C) inhibit osteoclastic bone resorption by inducing IRF7 and IFIT3. Journal of Bone and Mineral Research. 2024 Aug;39(8):1132-1146.
[6] Luo Z, Li Y, Xu B, et al. Overexpression of ESYT3 improves radioimmune responses through activating cGAS-STING pathway in lung adenocarcinoma. Experimental Hematology & Oncology. 2024 Aug 5;13:77.
[7] Wang L, Liang Z, Guo Y, et al. STING agonist diABZI enhances the cytotoxicity of T cell towards cancer cells. Cell Death and Disease. 2024 Apr 13;15:265.
[8] Pyclik M, Durslewicz J, Papinska JA, et al. STING Agonist-Induced Skin Inflammation Is Exacerbated with Prior Systemic Innate Immune Activation. International Journal of Molecular Sciences. 2023 Feb 18;24(4):4128.
[9] Messaoud-Nacer Y, Culerier E, Rose S, et al. STING agonist diABZI induces PANoptosis and DNA mediated acute respiratory distress syndrome(ARDS). Cell Death and Disease. 2022 Mar 25;13:269.
[10] Zhang P, Rashidi A, Zhao J, et al. STING agonist-loaded, CD47/PD-L1-targeting nanoparticles potentiate antitumor immunity and radiotherapy for glioblastoma. Nature Communications. 2023 Mar 23;14:1610.
| Cell experiment [1]: | |
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Cell lines |
A549 cells (human lung adenocarcinoma cell line), H1975 cells (human lung adenocarcinoma cell line) |
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Preparation Method |
A549 and H1975 cells were maintained in RPMI-1640 medium with 10% fetal bovine serum at 37°C, 5% CO2. Cells were treated with 20nM diABZI STING agonist-1 trihydrochloride for a duration matching downstream assays; after treatment, western blot for p-STING, cGAS, p-TBK1, p-IRF3 was performed, RT-qPCR and ELISA for IFNβ, CCL5, CXCL10 mRNA and secreted protein were conducted. |
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Reaction Conditions |
20nM; for 3-14 days |
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Applications |
diABZI STING agonist-1 trihydrochloride upregulated p-STING, cGAS, p-TBK1 and p-IRF3 protein levels, increased IFNβ, CCL5 and CXCL10 mRNA expression, and elevated secreted IFNβ, CCL5 and CXCL10 protein levels in culture supernatant of A549 and H1975 cells, with effects comparable to ESYT3 overexpression. |
| Animal experiment [2]: | |
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Animal models |
Female C57BL/6Rj mice, Tmem173-/- (STING-/-) mice, Mb21d1-/- (cGAS-/-) mice, Nlrp3-/- mice, AIM2-/- mice, IFNAR-/- mice, TLR9-/- mice |
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Preparation Method |
Mice were anesthetized with 2% isoflurane and challenged intratracheally with diABZI STING agonist-1 trihydrochloride at 0.01-1μg in 40μL saline daily for 3 consecutive days. In some groups, DNase I (50μg i.t.) was given on the 3 consecutive days of diABZI STING agonist-1 trihydrochloride administration, or Cl-amidine (200μg i.p.) was given on the 3 consecutive days. Bronchoalveolar lavage (BAL) was performed 24h after the last challenge; left lung lobe was taken for histology (PAS staining), post-caval lung for RT-qPCR, right lobes for western blot and cytokine measurement. BALF was used for neutrophil count, MPO, protein, dsDNA, mtDNA/nDNA, LDH, IFNα, IFNβ, CXCL10, IL-6, TNFα, CXCL1 ELISAs/Luminex; lung tissue for immunoblot of STING dimer, p-STING, cGAS, p-TBK1, IRF3, p-MLKL, cleaved Caspase3, cleaved GSDMD, ZBP1, pyH2AX, Cit-H3 and confocal of Caspase8/ASC/RIPK3 in BAL cells. |
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Dosage form |
0.01-1μg; i.t.; daily for 3 days |
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Applications |
diABZI STING agonist-1 trihydrochloride triggered acute neutrophilic airway inflammation with CXCL1 release, neutrophil recruitment, MPO elevation, protein extravasation, extracellular self-dsDNA and mtDNA release, NET formation, lung histopathology, PANoptosis (cleaved Caspase3, cleaved GSDMD, pMLKL, ZBP1, Caspase8/ASC/RIPK3 colocalization, pyH2AX), STING pathway activation. DNase I abrogated BALF dsDNA, reduced neutrophil recruitment and CXCL10, impaired NETs and ZBP1, and reduced cell death. Cl-amidine prevented neutrophil recruitment and NETs, reduced PANoptosis markers and STING protein, and alleviated LDH release. The response was absent in STING-/- and IFNAR-/- mice, retained in cGAS-/-, NLRP3-/-, AIM2-/- mice, and reduced in TLR9-/- mice. |
References: [1] Luo Z, Li Y, Xu B, et al. Overexpression of ESYT3 improves radioimmune responses through activating cGAS-STING pathway in lung adenocarcinoma. Experimental Hematology and Oncology. 2024 Aug 5;13:77. [2] Messaoud-Nacer Y, Culerier E, Rose S, et al. STING agonist diABZI induces PANoptosis and DNA mediated acute respiratory distress syndrome(ARDS). Cell Death and Disease. 2022 Mar 25;13:269. | |
| Cas No. | 2138299-34-8 | SDF | |
| Synonyms | Diamidobenzimidazole STING Agonist-1, STING Agonist (Compound 3), STING Agonist diABZI | ||
| Canonical SMILES | O=C(N)C1=CC(N=C(NC(C2=CC(C)=NN2CC)=O)N3C/C=C/CN4C(NC(C5=CC(C)=NN5CC)=O)=NC6=C4C(OCCCN7CCOCC7)=CC(C(N)=O)=C6)=C3C(OC)=C1.Cl.Cl.Cl | ||
| Formula | C42H54Cl3N13O7 | M.Wt | 959.32 |
| Solubility | DMSO: 125 mg/mL (130.30 mM) | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.0424 mL | 5.212 mL | 10.4241 mL |
| 5 mM | 208.5 μL | 1.0424 mL | 2.0848 mL |
| 10 mM | 104.2 μL | 521.2 μL | 1.0424 mL |
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)