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Cat. No.: HY-112921

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diABZI STING agonist-1 (tautomerism)

2 Cited Publications

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diABZI STING agonist-1 tautomerism is a tautomerism of diABZI STING agonist-1 (HY-112921A). diABZI STING agonist-1 tautomerism 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: 99.91%
CAS No.: 2138498-18-5
Formule: C₄₂H₅₁N₁₃O₇
Masse moléculaire:849.94

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

diABZI STING agonist-1 (tautomerism) Chemical Structure

CAS No.: 2138498-18-5

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Activité biologique
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- IC₅₀ & Target
- Cellular Effect
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- In Vivo
Chemical Information
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Description

IC₅₀ & Target

EC50: 130 nM (human STNG in PBMCs) ^[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 tautomerism 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) tautomerism induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo^[1].
diABZI STING agonist-1 (intravenous injection; 3 mg/kg) tautomerism 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; 43 days) tautomerism results in significant tumour growth inhibition and significantly improves survival 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.

Chemical Information

CAS No. 2138498-18-5
Appearance Solid
Masse moléculaire 849.94
Formule C₄₂H₅₁N₁₃O₇
Color White to light yellow
SMILES

O=C(N)C1=CC(N/C(N2C/C=C/CN3/C(NC4=C3C(OCCCN5CCOCC5)=CC(C(N)=O)=C4)=N/C(C6=CC(C)=NN6CC)=O)=N\C(C7=CC(C)=NN7CC)=O)=C2C(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 (2)

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Cell Res

Intercellular transfer of activated STING triggered by RAB22A-mediated non-canonical autophagy promotes antitumor immunity. [Abstract]

2022 Dec;32(12):1086-1104. PMID: 36280710

diABZI STING agonist-1 (tautomerism) purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Dec;32(12):1086-1104. [Abstract]

Western blot analysis of EVPs isolated from HeLa, HCT116, and B16F10 cells treated with or without 10 µM STING agonist-1 (diABZI), 1 µM cGAMP, or 50 µg/mL DMXAA for 48 h.

diABZI STING agonist-1 (tautomerism) purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Dec;32(12):1086-1104. [Abstract]

Immunofluorescence analysis of STING (green) and Flag-RAB22AQ64L (red) in stable Flag-RAB22AQ64L NCI-H1975 cells treated with or without 1 µM STING agonist-1 (diABZI) for 1 h.

diABZI STING agonist-1 (tautomerism) purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Dec;32(12):1086-1104. [Abstract]

Western blot analysis of the WCL of the indicated stable 4T1 cells at the indicated time points after treatment with 10 µM STING agonist-1 (diABZI).
Data Brief

Data supporting the roles of BAP1, STING, and IFN-β in ISGF3 activation in ccRCC. [Abstract]

2022 Nov 11:45:108743. PMID: 36426057

Pureté et documentation

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Pureté: 99.98%

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Fiche technique (280 KB)
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- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

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Keywords

diABZI STING agonist-1 (tautomerism)

2 Cited Publications

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Pureté et documentation
Références

1/16
1/16

diABZI STING agonist-1 (tautomerism) purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Dec;32(12):1086-1104. [Abstract]

Customer Validation
Western blot analysis of EVPs isolated from HeLa, HCT116, and B16F10 cells treated with or without 10 µM STING agonist-1 (diABZI), 1 µM cGAMP, or 50 µg/mL DMXAA for 48 h.
1/16

diABZI STING agonist-1 (tautomerism) purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Dec;32(12):1086-1104. [Abstract]

Customer Validation
Immunofluorescence analysis of STING (green) and Flag-RAB22AQ64L (red) in stable Flag-RAB22AQ64L NCI-H1975 cells treated with or without 1 µM STING agonist-1 (diABZI) for 1 h.
1/16

diABZI STING agonist-1 (tautomerism) purchased from MedChemExpress. Usage Cited in: Cell Res. 2022 Dec;32(12):1086-1104. [Abstract]

Customer Validation
Western blot analysis of the WCL of the indicated stable 4T1 cells at the indicated time points after treatment with 10 µM STING agonist-1 (diABZI).

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diABZI STING agonist-1 (tautomerism)

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

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Publications (2)

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diABZI STING agonist-1 (tautomerism)

Immunology/Inflammation Compound Library

Small Molecule Immuno-Oncology Compound Library

Neurodegenerative Disease-related Compound Library

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

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Publications (2)

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Help & FAQs

diABZI STING agonist-1 (tautomerism) Related Classifications

HY-112921 Related Classifications