| Bioactivity | 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]. |
| Invitro | 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]. Cell Viability Assay Cell Line: |
| 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]. Animal Model: |
| Name | IKKβ-IN-1 |
| CAS | 2410423-31-1 |
| Formula | C31H30N4O4S |
| Molar Mass | 554.66 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |