IKKβ-IN-1

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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.

For research use only. We do not sell to patients.

IKKβ-IN-1 Chemical Structure

CAS No. : 2410423-31-1

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IKK-α IKK-β IKK IKKε TBK1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

IKK-β

0.2 (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
RAW264.7	IC₅₀	> 10 μM Compound: 7a	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	[PMID: 31893550]
RAW264.7	IC₅₀	> 10 μM Compound: 7a	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	[PMID: 31893550]
RAW264.7	IC₅₀	> 10 μM Compound: 7a	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	[PMID: 31893550]
RAW264.7	IC₅₀	6.27 μM Compound: 7a	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	[PMID: 31893550]
RAW264.7	IC₅₀	9.83 μM Compound: 7a	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	[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.

Cell Viability Assay

Cell Line:	RAW 264.7 macrophage cells^[1]
Concentration:	0.1, 1 and 10 μM
Incubation Time:	24 hours
Result:	Did not show significant cytotoxicity at the tested three concentrations.

In Vivo

IKKβ-IN-1 (5 or 50 mg/kg; PO, single) exhibits an efficient protection of LPS-induced production of the inflammatory mediators at both of the two administered doses^[1].

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

Animal Model:	C57BL/6 male mice (6 or 10 weeks; LPS-induced production of the inflammatory mediators)^[1]
Dosage:	5 or 50 mg/kg
Administration:	PO, single (1 hour before LPS injection; survival was monitored for 36 hours)
Result:	Exhibited an efficient protection of LPS-induced production of the inflammatory mediators at both of the two administered doses.

Molecular Weight

554.66

Formula

C₃₁H₃₀N₄O₄S

CAS No.

2410423-31-1

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

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

Handling Instructions (2659 KB)

References

[1]. Elkamhawy A, Kim NY, Hassan AHE, et al. Thiazolidine-2,4-dione-based irreversible allosteric IKK-β kinase inhibitors: Optimization into in vivo active anti-inflammatory agents. Eur J Med Chem. 2020;188:111955. [Content Brief]

IKKβ-IN-1 Related Classifications

Inflammation/Immunology

NF-κB
IKK

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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:

IKKβ-IN-12410423-31-1IKKIκB kinaseI kappa B kinaseIKKβPGE2TNF-αBSeptic shockInflammatoryRAW 264.7C57BL/6 miceOralInhibitorinhibitorinhibit

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