STING-IN-8
STING-IN-8 (Compound 15b) emerges as a potent stimulator of interferon gene (STING) inhibitor with an IC50 value of 0.121 μM in human and an IC50 value of 0.033 μM in mouse. STING-IN-8 inhibits MSA-2 (HY-136927) or 2’, 3’ -cGAMP (HY-100564)-stimulated STING signaling and suppresses immune-inflammatory cytokine levels in both human and murine cells. STING-IN-8 is promising for research in the field of STING-associated inflammatory and autoimmune diseases.
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- Formule: C18H14F3N3O5S2
- Masse moléculaire:473.45
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
In Vitro
STING-IN-8 (0.1, 0.3, 1, 3 μM, 5 h) restrains the MSA-2 (10 μM) or 2’, 3’-cGAMP (10 μM) -induced p-TBK1 and p-IRF3 upregulation expression in both human and murine cells[1]. STING-IN-8 shows negligible cytotoxicity with CC50 of 30 μM in THP1-Dual and RAW-Lucia cells[1]. STING-IN-8 (0.3, 1, 3 μM and 0.1, 1, 3 μM, 9 h) effectively inhibits STING downstream immune-inflammatory cytokines in both human and mouse immune cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human monocyte derived THP1-Dual cell line, murine macrophage cells and mouse embryonic fibroblasts
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Concentration:0.1, 0.3, 1, 3 μM
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Incubation Time:5 h
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Result:Significantly down-regulate the the levels of phosphorylated TBK1 and IRF3 induced by MSA-2 (10 μM) and 2’, 3’ -cGAMP (10 μM) in all cell lines with better potency than SN-011 (HY-145010).
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Cell Line:THP1-Dual cell line and RAW-Lucia cells
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Concentration:0.3, 1, 3 μM and 0.1, 1, 3 μM
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Incubation Time:9 h
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Result:Significantly inhibited the MSA-2 (10 μM) or 2’, 3’-cGAMP (10 μM)-induced upregulation of STING signals expression in THP1-Dual cell line and RAW-Lucia cells.
In Vivo
STING-IN-8 (10 mg/kg, i.p., daily for two weeks) attenuates sustainably high levels of immune-inflammatory cytokines in the mice with Trex1 loss-of-function [1].
Pharmacokinetic parameters of STING-IN-8 in mice[1]
| Administration | T1/2 (h) | Tmax(h) | Cmax(ng/mL) | AUC0-∞ (ng·h/mL) | MRT(h) |
| p.o. 10 mg/ kg b | 1.75 | 0.25 | 77.6 | 109 | 2.53 |
| i.p. 5 mg/kgc | 4.86 | 0.18 | 137 | 100 | 4.73 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice[1]
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Dosage:10 MG/KG
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Administration:i.p., a single dose
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Result:Effectively reduced MSA-2 (10 MG/KG) -stimulated serum IL-6, CXCL10 levels and inhibited the expression of IFNβ, TNFα, ISG15, ISG56, Cxcl10, IL6 in kidney tissues.
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Animal Model:Kidney tissues of Trex1-D18N mice[1]
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Dosage:10 MG/KG
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Administration:i.p. daily for two weeks
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Result:Significantly reduced the ISG 15, ISG 56, CXCL10 levels in kidney and demonstrated anti-inflammatory effects in tongue and other muscle tissues of Trex1-D18N mice.
Chemical Information
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Masse moléculaire 473.45
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Formule C18H14F3N3O5S2
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SMILES
CS(=O)(NC1=C(C=CC(NC(C2=NC(C3=CC=C(C=C3)OC(F)(F)F)=CS2)=O)=C1)O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
STING-IN-8 Related Classifications
HY-163749 Related Classifications
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