Cat. No.: HY-112921A

diABZI STING agonist-1

Name: diABZI STING agonist-1
Brand: MedChemExpress
SKU: HY-112921A
Price: 450.00 USD
Availability: InStock
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52 Cited Publications

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Based on 52 publication(s) in Google Scholar

diABZI STING agonist-1 is a tautomerism of diABZI STING agonist-1 tautomerism (HY-112921). diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with EC₅₀s of 130, 186 nM for human and mouse, respectively.

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Pureté : 99.58%
CAS No.: 2138299-33-7
Formule: C₄₂H₅₁N₁₃O₇
Masse moléculaire:849.94

Stockage:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

diABZI STING agonist-1 Chemical Structure

CAS No.: 2138299-33-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (52)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

STING^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
H69AR	EC₅₀	0.035 μM Compound: 5; GSK	Agonist activity at STING in human THP1 Dual cells assessed as IRF reporter activation incubated for 20 hrs by quanti-blue SEAP reporter gene assay Agonist activity at STING in human THP1 Dual cells assessed as IRF reporter activation incubated for 20 hrs by quanti-blue SEAP reporter gene assay	[PMID: 35108011]
H69AR	EC₅₀	0.055 μM Compound: 5; GSK	Agonist activity at STING in human THP1-Dual cells assessed as NF-kappaB reporter activation incubated for 20 hrs by quanti-blue SEAP reporter gene assay Agonist activity at STING in human THP1-Dual cells assessed as NF-kappaB reporter activation incubated for 20 hrs by quanti-blue SEAP reporter gene assay	[PMID: 35108011]

In Vitro

diABZI STING agonist-1 (compound 3) is a selective stimulator of interferon genes (STING) receptor agonist, with EC₅₀s of 130, 186 nM for human and mouse, respectively. At a concentration of 1 μM, diABZI STING agonist-1 (compound 3) demonstrates high selectivity against more than 350 kinases tested^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .

In Vivo

diABZI STING agonist-1 (subcutaneous injection; 2.5 mg/kg) induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo^[1].
diABZI STING agonist-1 (intravenous injection; 3 mg/kg) exhibits systemic exposure with a half-life of 1.4 h and achieves systemic concentrations greater than the half-maximal effective concentration (EC₅₀) for mouse STING (200 ng/ml)^[1].
diABZI STING agonist-1 (intravenous injection; 1.5 mg/kg; days 1, 4 and 8; 43 days) results in significant tumour growth inhibition and significantly improves survival (P < 0.001) with 8 out of 10 mice remaining tumor free at the end of the study on day 43^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Wild and Sting^−/− C57Blk6 mice^[1]
Dosage:

2.5 mg/kg
Administration:

Subcutaneous injection; 2.5 mg/kg
Result:

Activated secretion of IFNβ, IL-6, TNF, and CXCL1 in wild-type but not Sting^−/− mice.

Animal Model:

Syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice^[1]
Dosage:

3 mg/kg
Administration:

Intravenous injection; 3 mg/kg
Result:

Exhibited a half-life of 1.4 hours and achieved systemic concentrations greater than EC₅₀ for mouse STING (200 ng/ml).

Animal Model:

Syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice^[1]
Dosage:

1.5 mg/kg
Administration:

Intravenous injection; 1.5 mg/kg; 43 days
Result:

Resulted in significant tumour growth inhibition and improved survival.

Chemical Information

CAS No. 2138299-33-7
Appearance Solid
Masse moléculaire 849.94
Formule C₄₂H₅₁N₁₃O₇
Color White to off-white
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Publications (52)

All In Vivo Efficacy StudyWBHistological Imaging/StainingRT-PCRIF

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Journal Impact Factor

Nat Nanotechnol

Amplifying STING activation by cyclic dinucleotide-manganese particles for local and systemic cancer metalloimmunotherapy. [Abstract]

2021 Nov;16(11):1260-1270. PMID: 34594005
Protein Cell

Drug target inference by mining transcriptional data using a novel graph convolutional network framework. [Abstract]

2022 Apr;13(4):281-301. PMID: 34677780
Exp Hematol Oncol

Overexpression of ESYT3 improves radioimmune responses through activating cGAS-STING pathway in lung adenocarcinoma. [Abstract]

2024 Aug 5;13(1):77. PMID: 39103908
Mol Cell

The mechanism of STING autoinhibition and activation. [Abstract]

2023 May 4;83(9):1502-1518.e10. PMID: 37086726
Genes Dis

Mitophagy deficiency activates stimulator of interferon genes activation and aggravates pathogenetic cardiac remodeling. [Abstract]

2023 Sep 2;11(6):101074. PMID: 39281830
MedComm (2020)

2026 Jun 13;7(6):e70828. PMID: 42292856
Adv Sci (Weinh)

Carnosic Acid Directly Targets STING C-Terminal Tail to Improve STING-Mediated Inflammatory Diseases. [Abstract]

2025 Apr;12(14):e2417686. PMID: 39965124

diABZI STING agonist-1 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Apr;12(14):e2417686. [Abstract]

Immunoblot assays of p-IRF3 and p-STING from hPBMCs administrated with CA (10 µM) for 1 h followed by treatment with HT-DNA, cGAMP, or diABZI (10 μg/mL) for 2 h.

diABZI STING agonist-1 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Apr;12(14):e2417686. [Abstract]

qPCR analysis of IFNB, ISG15, IL-6, and TNF-α mRNA levels from hPBMCs pretreated with CA (10 µM) for 1 h followed by treatment with HT-DNA, cGAMP, or diABZI (10 μg/mL) for 4 h.

diABZI STING agonist-1 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Apr;12(14):e2417686. [Abstract]

Immunofluorescence analysis of nuclear translocation of IRF3 from THP-1 cells pretreated with vehicle control (DMSO, 1000x) or CA (10 µM) for 1 h followed by administration with diABZI (10 µg mL−1) for 2 h.
Adv Sci (Weinh)

Ginkgetin Alleviates Inflammation and Senescence by Targeting STING. [Abstract]

2025 Jan;12(2):e2407222. PMID: 39558862
Cell Death Differ

STING directly interacts with PAR to promote apoptosis upon acute ionizing radiation-mediated DNA damage. [Abstract]

2025 Jun;32(6):1167-1179. PMID: 39939798
Cell Death Differ

Activating STING/TBK1 suppresses tumor growth via degrading HPV16/18 E7 oncoproteins in cervical cancer. [Abstract]

2024 Jan;31(1):78-89. PMID: 38007552
Cell Death Dis

The interaction between STING and NCOA4 exacerbates lethal sepsis by orchestrating ferroptosis and inflammatory responses in macrophages. [Abstract]

2022 Jul 28;13(7):653. PMID: 35902564
Cancer Lett

Activated STING-containing R-EVs from iPSC-derived MSCs promote antitumor immunity. [Abstract]

2024 Aug 10:597:217081. PMID: 38909776
Cancer Lett

Deubiquitinase USP4 suppresses antitumor immunity by inhibiting IRF3 activation and tumor cell-intrinsic interferon response in colorectal cancer. [Abstract]

2024 May 1:589:216836. PMID: 38556105
Cancer Lett

BAP1 maintains HIF-dependent interferon beta induction to suppress tumor growth in clear cell renal cell carcinoma. [Abstract]

2022 Oct 28:547:215885. PMID: 35995140

diABZI STING agonist-1 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2022 Oct 28:547:215885. [Abstract]

Treatment with diABZI (3 mg/kg, i.p.) significantly hindered BAP1 knockdown tumor growth over the course of treatment.

diABZI STING agonist-1 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2022 Oct 28:547:215885. [Abstract]

IHC revealed no differences in CD31 staining, but an increase in CD45 staining was observed in the diABZI (3 mg/kg, i.p.)-treated tumors.
J Exp Med

Type I interferon signaling mediates Mycobacterium tuberculosis-induced macrophage death. [Abstract]

2021 Feb 1;218(2):e20200887. PMID: 33125053
Chin Herb Med

Salvia miltiorrhiza water extract ameliorated cGAS-STING-mediated acute liver injury by blocking interaction between STING and TBK1. [Abstract]

2025 Jan 7;17(4):768-778. PMID: 41399788
Chin Herb Med

Amplifying protection against acute lung injury: Targeting both inflammasome and cGAS-STING pathway by Lonicerae Japonicae Flos-Forsythiae Fructus drug pair. [Abstract]

2024 Apr 30;16(3):422-434. PMID: 39072201
Mater Today Bio

2025 Dec 24.
Sci China Life Sci

Targeting STING oligomerization with licochalcone D ameliorates STING-driven inflammatory diseases. [Abstract]

2024 Dec;67(12):2664-2677. PMID: 39190126
Proc Natl Acad Sci U S A

Activation of the NLRP1 inflammasome in human keratinocytes by the dsDNA mimetic poly(dA:dT). [Abstract]

2023 Jan 31;120(5):e2213777120. PMID: 36693106
Chin Med J (Engl)

Transcranial photobiomodulation mitigates neuroinflammation by suppressing the activation of neurotoxic microglia through inhibition of the cGAS-STING pathway following intracerebral hemorrhage in mice. [Abstract]

2026 Apr 27. PMID: 42045151
Cell Chem Biol

Identification of an STING inhibitor targeting the allosteric transmembrane domains. [Abstract]

2026 Apr 27:S2451-9456(26)00110-8. PMID: 42049033
EMBO J

STING induces HOIP-mediated synthesis of M1 ubiquitin chains to stimulate NF-κB signaling. [Abstract]

2025 Jan;44(1):141-165. PMID: 39578541
Cell Rep

2026 Jun 1;45(6).
Cell Rep

Herpes simplex virus type 1 disseminates from the cornea to the CNS in mice by thwarting type III interferon immune defenses. [Abstract]

2025 Nov 18;44(12):116581. PMID: 41259200
Chin Med

Total tanshinones ameliorates cGAS-STING-mediated inflammatory and autoimmune diseases by affecting STING-IRF3 binding. [Abstract]

2024 Aug 15;19(1):107. PMID: 39148120
J Invest Dermatol

EZH2 Inhibitor Enhances the STING Agonist‒Induced Antitumor Immunity in Melanoma. [Abstract]

2022 Apr;142(4):1158-1170.e8. PMID: 34571002
Front Immunol

Characterization of a Novel Compound That Stimulates STING-Mediated Innate Immune Activity in an Allele-Specific Manner. [Abstract]

2020 Jul 8:11:1430. PMID: 32733475
J Ethnopharmacol

Shuangdan Jiedu Decoction improved LPS-induced acute lung injury by regulating both cGAS-STING pathway and inflammasome. [Abstract]

2025 Jan 10:336:118661. PMID: 39159837
J Agric Food Chem

Butachlor-Induced BAZ2B Activation Promotes Cardiomyocyte Senescence through cGAS-STING pathway. [Abstract]

2026 Mar 25;74(11):9761-9773. PMID: 41823793
J Bone Miner Res

diABZI and poly(I:C) inhibit osteoclastic bone resorption by inducing IRF7 and IFIT3. [Abstract]

2024 Aug 21;39(8):1132-1146. PMID: 38874138
OncoImmunology

Stimulatory and inhibitory activity of STING ligands on tumor-reactive human gamma/delta T cells. [Abstract]

2022 Feb 1;11(1):2030021. PMID: 35127253
Int Immunopharmacol

Minimolide F alleviates inflammatory diseases by specifically targeting STING and blocking IRF3 recruitment. [Abstract]

2026 May 1:176:116468. PMID: 41819671
Int Immunopharmacol

Tubular STING drives renal fibrosis via extracellular vesicle-mediated activation of the SMO/GLI-1 pathway. [Abstract]

2026 Apr 1:174:116350. PMID: 41679184
Cell Oncol (Dordr)

Optimized patient-derived lung cancer organoids recapitulating the immune landscape for precision therapy evaluation. [Abstract]

2026 Jan 6;49(1):15. PMID: 41493730
Invest Ophthalmol Vis Sci

Involvement of cGAS/STING Signaling in the Pathogenesis of Candida albicans Keratitis: Insights From Genetic and Pharmacological Approaches. [Abstract]

2024 Jun 3;65(6):13. PMID: 38848078
Front Pharmacol

Licorice extract inhibits the cGAS-STING pathway and protects against non-alcoholic steatohepatitis. [Abstract]

2023 Apr 4:14:1160445. PMID: 37081966
Sci Rep

Signal strength of STING activation determines cytokine plasticity and cell death in human monocytes. [Abstract]

2022 Oct 24;12(1):17827. PMID: 36280676
ACS Infect Dis

STING Agonist-Mediated Cytokine Secretion Is Accompanied by Monocyte Apoptosis. [Abstract]

2022 Mar 11;8(3):463-471. PMID: 35132859
FASEB J

STING Facilitates Vascular Calcification via p-STAT1/NLRP3 Signal. [Abstract]

2025 Apr 15;39(7):e70530. PMID: 40193045
Infect Immun

STING agonists reduce genital chlamydial infection and attenuate inflammation and pathology. [Abstract]

2026 Apr 30;94(6):e0076125. PMID: 42059376
Cell Immunol

STING agonist and IDO inhibitor combination therapy inhibits tumor progression in murine models of colorectal cancer. [Abstract]

2021 Aug:366:104384. PMID: 34182334
Am J Cancer Res

Disulfiram combined with chemoimmunotherapy potentiates pancreatic cancer treatment efficacy through the activation of cGAS-STING signaling pathway via suppressing PARP1 expression. [Abstract]

2023 May 15;13(5):2055-2065. PMID: 37293156
PLoS One

UMP-CMP kinase 2 gene expression in macrophages is dependent on the IRF3-IFNAR signaling axis. [Abstract]

2021 Oct 27;16(10):e0258989. PMID: 34705862
World J Tradit Chin Med

2025 Oct 28.
World J Tradit Chin Med

2025 April 17.
Thorac Cancer

Increased activation of cGAS-STING pathway enhances radiosensitivity of non-small cell lung cancer cells. [Abstract]

2022 May; 13(9): 1361–1368. PMID: 35429143
bioRxiv

2025 Nov 18.
bioRxiv

Characterization of a Novel Transmembrane Activating STING Agonist using Genetically Humanized Mice. [Abstract]

2025 Jul 18:2025.07.14.664814. PMID: 40791406
bioRxiv

Comparative Molecular, Innate, and Adaptive Impacts of Chemically Diverse STING Agonists. [Abstract]

2025 Feb 27:2025.02.21.639458. PMID: 40060577
Biomed Pharmacother

Irisin improves diabetic cardiomyopathy-induced cardiac remodeling by regulating GSDMD-mediated pyroptosis through MITOL/STING signaling. [Abstract]

2024 Feb:171:116007. PMID: 38171238
University of California San Diego

2023

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (117.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.1766 mL

5.8828 mL

11.7655 mL

5 mM

0.2353 mL

1.1766 mL

2.3531 mL

10 mM

0.1177 mL

0.5883 mL

1.1766 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 3.5 mg/mL (4.12 mM); Clear solution

This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 3.5 mg/mL (4.12 mM); Clear solution

This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
Elemental Analysis Report (2659 KB)
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Instruction de manipulation (2659 KB)

Références

[1]. Ramanjulu JM, et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Nov 7. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.1766 mL	5.8828 mL	11.7655 mL	29.4138 mL
	5 mM	0.2353 mL	1.1766 mL	2.3531 mL	5.8828 mL
	10 mM	0.1177 mL	0.5883 mL	1.1766 mL	2.9414 mL
	15 mM	0.0784 mL	0.3922 mL	0.7844 mL	1.9609 mL
	20 mM	0.0588 mL	0.2941 mL	0.5883 mL	1.4707 mL
	25 mM	0.0471 mL	0.2353 mL	0.4706 mL	1.1766 mL
	30 mM	0.0392 mL	0.1961 mL	0.3922 mL	0.9805 mL
	40 mM	0.0294 mL	0.1471 mL	0.2941 mL	0.7353 mL
	50 mM	0.0235 mL	0.1177 mL	0.2353 mL	0.5883 mL
	60 mM	0.0196 mL	0.0980 mL	0.1961 mL	0.4902 mL
	80 mM	0.0147 mL	0.0735 mL	0.1471 mL	0.3677 mL
	100 mM	0.0118 mL	0.0588 mL	0.1177 mL	0.2941 mL

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Keywords

diABZI STING agonist-1

52 Cited Publications

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diABZI STING agonist-1

Publications Citing Use of MedChemExpress (MCE) diABZI STING agonist-1