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^[1].

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.

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.

554.66

C₃₁H₃₀N₄O₄S

2410423-31-1

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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Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]