IKKβ-IN-1
IKKβ-IN-1 is a potent and orally active IkappaB (IKK-β) inhibitor with IC50 of 0.20 μM. IKKβ-IN-1 can reduce PGE2 and TNF-α production in mouse macrophage cells. IKKβ-IN-1 has the ability to protect mice against septic shock induced mortality.
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- CAS No.: 2410423-31-1
- Formule: C31H30N4O4S
- Masse moléculaire:554.66
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[1]|
IKK-β 0.2 (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | IC50 |
>10 μM
Compound: 7a
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Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction in LPS-induced IL-6 level incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction in LPS-induced IL-6 level incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
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[PMID: 31893550] |
| RAW264.7 | IC50 |
>10 μM
Compound: 7a
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Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction in LPS-induced NO level incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by Griess reagent based assay
Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction in LPS-induced NO level incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by Griess reagent based assay
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[PMID: 31893550] |
| RAW264.7 | IC50 |
>10 μM
Compound: 7a
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Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 24 hrs in presence of LPS by MTT assay
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 24 hrs in presence of LPS by MTT assay
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[PMID: 31893550] |
| RAW264.7 | IC50 |
6.27 μM
Compound: 7a
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Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction in LPS-induced TNF-alpha level incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction in LPS-induced TNF-alpha level incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
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[PMID: 31893550] |
| RAW264.7 | IC50 |
9.83 μM
Compound: 7a
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Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction in LPS-induced PGE2 level incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction in LPS-induced PGE2 level incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
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[PMID: 31893550] |
In Vitro
IKKβ-IN-1 (compound 7a) (0.1, 1 and 10 μM; 24 hours) does not show significant cytotoxicity at the tested three concentrations[1].
IKKβ-IN-1 (0.1, 1 and 10 μM; 1 hours) significantly reduces PGE2 production even at the low 0.1 μM concentration, and IC50 is 9.83 μM[1].
IKKβ-IN-1 (0.1, 1 and 10 μM; 1 hours) elicits 44% reduction of TNF-α production at 10 μM concentration, and IC50 is 6.27 μM[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 macrophage cells[1]
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Concentration:0.1, 1 and 10 μM
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Incubation Time:24 hours
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Result:Did not show significant cytotoxicity at the tested three concentrations.
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/6 male mice (6 or 10 weeks; LPS-induced production of the inflammatory mediators)[1]
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Dosage:5 or 50 mg/kg
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Administration:PO, single (1 hour before LPS injection; survival was monitored for 36 hours)
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Result:Exhibited an efficient protection of LPS-induced production of the inflammatory mediators at both of the two administered doses.
Chemical Information
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CAS No. 2410423-31-1
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Masse moléculaire 554.66
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Formule C31H30N4O4S
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SMILES
N#CC1=CC=C(OC2=CC=C(/C=C(SC(N3C4=CC=C(OCCCN5CCN(C)CC5)C=C4)=O)/C3=O)C=C2)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IKKβ-IN-1 Related Classifications
HY-146723 Related Classifications
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