KSI-028
KSI-028 is a STING inhibitor. KSI-028 disrupts STING-mediated signal transduction, reduces IFN-β and pro-inflammatory cytokine (IL-6, IL-1β and TNF-α) production. KSI-028 inhibits the phosphorylation of STING, TBK1, IRF3, and STAT1. KSI-028 attenuates renal and hepatic injury in a Cisplatin (HY-17394)-induced acute kidney injury mouse model.
For research use only. We do not sell to patients.
- Formula: C18H14N4O5S
- Molecular Weight:398.39
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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IL-1β |
IL-6 |
TBK1 |
STAT1 |
KSI-028 (0.3-20 μM; 1 h pretreatment) potently inhibits STING-dependent ISRE reporter activity in RAW264.7 cells with an IC50 of 0.652 μM for cGAMP (HY-12512) (10 μg/mL)-induced activity and 2.261 μM for MSA-2 (HY-136927) (100 μM)-induced activity, while maintaining high cell viability[1].
KSI-028 (0.3-20 μM; 1 h pretreatment) dose-dependently inhibits STING-dependent ISRE reporter activity in human THP-1 cells without inducing cytotoxicity[1].
KSI-028 (1.25-20 μM; 2 h pretreatment) potently suppresses STING-dependent IFN-β cytokine and IL-6, TNF-α pro-inflammatory factor production in RAW264.7 cells following stimulation with cGAMP or MSA-2[1].
KSI-028 (5-10 μM; 2 h pretreatment) disrupts STING-mediated signal transduction in RAW264.7 cells by inhibiting the phosphorylation of STING, TBK1, IRF3, and STAT1[1].
KSI-028 (20 μM) directly engages STING in intact RAW264.7 and THP-1 cells, increasing the protein's thermal stability[1].
KSI-028 (5-10 μM; 2 h pretreatment) broadly suppresses STING-dependent interferon-stimulated gene expression in RAW264.7 cells activated by cGAMP or MSA-2[1].
KSI-028 (10 μM; 5 min) exhibits modest, partial inhibition of human CYP450 isoforms 1A2, 2C9, 2D6, and 3A4[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:murine RAW264.7 cells
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Concentration:5, 10 μM
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Incubation Time:2 h pretreatment
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Result:Markedly reduced the phosphorylation of STING, TBK1, IRF3, and STAT1 following stimulation with either cGAMP or MSA-2.
Left total protein levels of STING, TBK1, IRF3, and STAT1 unchanged.
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Cell Line:murine RAW264.7 cells
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Concentration:5, 10 μM
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Incubation Time:2 h pretreatment
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Result:Significantly suppressed the transcription of multiple ISGs including ifnb, cxcl10, isg15, irf7, oas1a, ifit1, ifit2, ifit3, pkr, and rsad2 in cells activated by either cGAMP or MSA-2.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Acute kidney injury C57BL/6J mice (male, 8 weeks old, Cisplatin-induced acute kidney injury)[1]
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Dosage:30 mg/kg
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Administration:i.p.; twice daily; 3 days
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Result:Significantly reduced blood urea nitrogen and serum creatinine levels compared to the Cisplatin-only group.
Significantly lowered serum aspartate aminotransferase and alanine aminotransferase levels.
Substantially attenuated Cisplatin-induced elevations in mRNA levels of interferon-stimulated genes including ifnb, cxcl10, isg15, and irf7, as well as pro-inflammatory cytokine genes including IL-6, TNF-α, and IL-1β.
Reduced Cisplatin-induced increases in STING protein levels, phosphorylated TBK1, and phosphorylated p65.
Showed no significant systemic toxicity based on survival and body weight monitoring.
Chemical Information
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Molecular Weight 398.39
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Formula C18H14N4O5S
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SMILES
O=C(C1=CC=C(O1)[N+]([O-])=O)NC2=CC3=C(CCCN3C(C4=CC=NS4)=O)C=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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