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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C18H14N4O5S
- Molecular Weight:398.39
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
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. Further protocols information, click here.
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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.
Parmacokinetics
In Vivo
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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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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Nephrotoxicity Study
This protocol assesses nephrotoxicity by combining functional kidney injury readouts, urinary/tissue injury biomarkers, and renal histopathology. Serum creatinine and BUN reflect impaired kidney function, while KIM-1, NGAL, clusterin, osteopontin, IL-18, cystatin C, nephrin, Oat5, urinary protein, glucose, and alkaline phosphatase have been used to detect tubular injury in cisplatin-, gentamicin-, and acetaminophen-induced nephrotoxicity models.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
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Hepatotoxicity Study
This protocol evaluates hepatotoxicity using complementary in vivo mouse APAP acute liver injury and in vitro hepatocyte-based cytotoxicity readouts. In vivo APAP injury is assessed by serum ALT/AST, liver histology, hepatic glutathione, protein adducts, necrosis, inflammation, and regeneration-related endpoints. In vitro hepatotoxicity is assessed by loss of viability, leakage of ALT/AST/LDH, oxidative-stress markers, mitochondrial function, nuclear morphology, intracellular calcium, and high-content imaging endpoints.
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Pyroptosis Solutions
Pyroptosis is a lytic inflammatory cell-death pathway executed by gasdermin pores, most classically through inflammasome-mediated activation of caspase-1, cleavage of gasdermin D, membrane pore formation, LDH release, and secretion of IL-1β and IL-18. The canonical pathway is commonly modeled by priming cells with an inflammatory signal such as LPS to induce pro-IL-1β and inflammasome components, followed by an activation signal such as ATP or nigericin to activate NLRP3, ASC speck formation, caspase-1 cleavage, GSDMD cleavage, cytokine release, and pyroptotic membrane rupture. The non-canonical pathway is triggered when cytosolic LPS activates mouse caspase-11 or human caspase-4/5, leading to GSDMD cleavage and pyroptosis, and this can secondarily activate NLRP3-dependent IL-1β release. Pyroptosis is linked to inflammatory injury, infection, cancer, liver disease, ocular disease, placental inflammation, and other disease phenotypes, but unresolved questions include which gasdermin fam
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Liver Histomorphometry
Liver histomorphometry is a quantitative histological approach used to measure structural alterations in hepatic tissue, including parenchymal loss, steatosis, fibrosis, and vascular remodeling, by combining stained tissue section analysis with stereological or computerized image-based measurements. Classical morphometric frameworks quantify volume fractions of liver compartments and fibrotic regions using systematic sampling and image analysis, enabling objective comparison of pathological changes across experimental groups. These approaches are widely applied in liver cirrhosis and fibrosis studies to reduce subjectivity in histological scoring and improve reproducibility of tissue evaluation. Recent methodological advances integrate automated image analysis and radiomics-based extraction of histological features from standard liver stains (e. g. , H&E and fibrotic stains), enabling quantitative correlation between morphometric features and fibrosis stages in non-alcoholic fatty live
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How to Choose the Right Model Animal
Choosing the right model animal is a validity-driven decision in which the species, strain, sex, age, genetic background, disease-induction method, outcome measures, and welfare burden must match the scientific question rather than laboratory tradition or convenience. A model should be selected by judging face validity, construct validity, and predictive validity: whether it resembles the human phenotype, whether it reproduces relevant mechanisms, and whether results are likely to predict human biology or treatment response. Animal studies often fail to translate because of species differences, weak disease resemblance, poor experimental design, inadequate reporting, publication bias, and underuse of randomization, blinding, and sample-size justification. Unresolved questions include how to rank competing models objectively, how much human-disease complexity must be reproduced for a given objective, and when non-animal systems such as organoids, ex vivo tissue, or computational models
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)