SR12460
SR12460 is a NEMO-binding domain mimetic and an inhibitor of the IKKβ-NEMO complex with an IC50 of 11.34 μM. SR12460 disrupts the IKKβ-NEMO interaction, thereby inhibiting NF-κB activation, including TNF-α- and LPS-induced NF-κB activation. SR12460 inhibits LPS-induced acute lung inflammation in mice and alleviates inflammatory infiltration, necrosis, and muscle degeneration in a mouse model of Duchenne muscular dystrophy. SR12460 is used for research on acute lung inflammation and Duchenne muscular dystrophy.
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- CAS. Nr.: 2055101-66-9
- Formel: C15H14ClF2N3O
- Molecular Weight:325.74
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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
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
11.34 μM
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Inhibition of TNF-α-induced NF-κB activation in human HEK293 cells measured via NF-κB dual-luciferase reporter assay, with 30 minutes of pretreatment followed by 3 hours of TNF-α stimulation.
Inhibition of TNF-α-induced NF-κB activation in human HEK293 cells measured via NF-κB dual-luciferase reporter assay, with 30 minutes of pretreatment followed by 3 hours of TNF-α stimulation.
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29889904 |
In Vitro
SR12460 (50 μM; 30 min pretreatment, followed by 2 h LPS stimulation) suppresses the expression of multiple LPS-induced NF-κB target genes in Raw 264.7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Raw 264.7 mouse macrophage cells
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Concentration:50 μM
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Incubation Time:30 min pretreatment, followed by 2 h LPS stimulation
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Result:Significantly inhibited the LPS-induced transcription of the NF-κB target genes cyclooxygenase 2 (COX-2), interleukin-6 (IL-6), interleukin-1β (IL-1β), TNF-α, IκBα, and inducible nitric oxide synthase (iNOS).
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Cell Line:Raw 264.7 mouse macrophage cells
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Concentration:25, 50 μM
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Incubation Time:1 h pretreatment, followed by 24 h LPS stimulation
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Result:Significantly inhibited LPS-induced IL-6 secretion in a dose-dependent manner.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (female, 8-10 weeks old, 20-30 g, intraperitoneal LPS challenge)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Suppressed LPS-induced expression of NF-κB target genes iNOS, IκBα, COX-2, and IL-6 in lung tissue.
Suppressed only COX-2 expression in liver tissue.
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Animal Model:C57BL/10ScSn-Dmdmdx/J (mdx) (sex-matched, 3 weeks old at treatment initiation)[1]
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Dosage:30 mg/kg
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Administration:i.p.; 3 times per week; 4 weeks
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Result:Reduced the percentage of tibialis anterior muscle area with necrosis and inflammation.
Increased expression of muscle regeneration markers eMyHC and Pax7.
Improved forelimb grip strength normalized to body weight after 4 weeks of treatment.
Chemical Information
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CAS. Nr. 2055101-66-9
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Molecular Weight 325.74
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Formel C15H14ClF2N3O
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SMILES
O=C(CNCCC1=CC(F)=CC(F)=C1)NC2=NC=C(C=C2)Cl
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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.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
SR12460 Related Classifications
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