2. Immunology/Inflammation Apoptosis NF-κB JAK/STAT Signaling Stem Cell/Wnt
  3. STING IFNAR Interleukin Related TNF Receptor IKK STAT
  4. 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.

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KSI-028

KSI-028 Chemical Structure

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KSI-028 Related Antibodies

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Description

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[1].

IC50 & Target[1]

IL-1β

 

IL-6

 

TBK1

 

STAT1

 

In Vitro

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.

KSI-028 Related Antibodies

Western Blot Analysis[1]

Cell Line: murine RAW264.7 cells
Concentration: 5, 10 μM
Incubation Time: 2 h pretreatment
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.

Real Time qPCR[1]

Cell Line: murine RAW264.7 cells
Concentration: 5, 10 μM
Incubation Time: 2 h pretreatment
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.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-∞ F
Mice[1] 5 mg/kg i.v. 21.26 h / / 0.19 μg·h/mL /
Mice[1] 10 mg/kg i.p. 18 h 1.53 h 0.02 μg/mL 0.1 μg·h/mL 37.35 %
Mice[1] 10 mg/kg p.o. 72.43 h 0.92 h / 0.1 μg·h/mL 13.11 %
In Vivo

KSI-028 (30 mg/kg; i.p.; twice daily; 3 days) confers robust protection against Cisplatin (HY-17394)-induced renal and hepatic injury in mice by suppressing STING-mediated type I interferon and inflammatory responses[1].

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

Animal Model: Acute kidney injury C57BL/6J mice (male, 8 weeks old, Cisplatin-induced acute kidney injury)[1]
Dosage: 30 mg/kg
Administration: i.p.; twice daily; 3 days
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.
Molecular Weight

398.39

Formula

C18H14N4O5S
SMILES

O=C(C1=CC=C(O1)[N+]([O-])=O)NC2=CC3=C(CCCN3C(C4=CC=NS4)=O)C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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KSI-028 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:

KSI-028KSI028KSI 028STINGIFNARInterleukin RelatedTNF ReceptorIKKSTATStimulator of Interferon GenesTMEM173MITAERISMPYSInterferon-α/β receptorInterferon-alpha/beta receptor ILTumor Necrosis Factor ReceptorTNFRIκB kinaseI kappa B kinaseIRF3RAW264.7 cellsTBK1pro-inflammatory cytokinetype I interferonSTAT1CYP450 isoformsacute kidney injuryTHP-1 cellsInhibitorinhibitorinhibit

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