2. Immunology/Inflammation
  3. STING
  4. 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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STING-IN-8 Chemical Structure

STING-IN-8 Chemical Structure

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STING-IN-8 Related Antibodies

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Pharmacokinetic parameters of STING-IN-8 in mice[1]

药代动力学分析[1]
Description

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[1].
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.

STING-IN-8 Related Antibodies

Western Blot Analysis[1]

Cell Line: Human monocyte derived THP1-Dual cell line, murine macrophage cells and mouse embryonic fibroblasts
Concentration: 0.1, 0.3, 1, 3 μM
Incubation Time: 5 h
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).

Real Time qPCR[1]

Cell Line: THP1-Dual cell line and RAW-Lucia cells
Concentration: 0.3, 1, 3 μM and 0.1, 1, 3 μM
Incubation Time: 9 h
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.) effectively inhibits STING downstream cytokines in MSA‑2 (10 MG/KG) ‑stimulated mice[1].
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].
1.19 合并列 符号

： 代表后面的三列被合并 是列
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.

Animal Model: C57BL/6 mice
Dosage: 10 MG/KG
Administration: i.p., a single dose
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[1]
Animal Model: Kidney tissues of Trex1-D18N mice
Dosage: 10 MG/KG
Administration: i.p. daily for two weeks
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[1]
Molecular Weight

473.45

Formula

C18H14F3N3O5S2

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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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
Handling Instructions (2659 KB)
References
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STING-IN-8 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

STING-IN-8STINGStimulator of Interferon GenesTMEM173MITAERISMPYSSTING-associated inflammatory and autoimmune diseasesTrex1-D18N miceTHP1-Dual cellRAW-Lucia cellInhibitorinhibitorinhibit

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