| Bioactivity | PF-184 is a potent and selective IKK-2 inhibitor (IC50: 37 nM) over rhIKK-1, IKKi, and more than 30 tyrosine and serine/threonine kinases. PF-184 can be used in the research of inflammation, such as asthma and chronic obstructive pulmonary disease[1]. |
| Invitro | PF-184 (0.7 nM-10 μM, 1 h) displays inhibitory activity after successive washes of LPS-stimulated PBMC kinase activation[1].PF-184 (1 h) broadly inhibits IKK-2-dependent inflammatory products in human disease-relevant cells (such as PBMC, neutrophils, airway epithelial cells, and airway endothelial cells), with IC50 values ranging from 8 nM to 343 nM[1].PF-184 (2 nM-10 μM, 1 h) inhibits IL-1β-induced TNF-α in a concentration-dependent manner in PBMCs[1]. |
| In Vivo | PF-184 (Intratracheal administration, 0.3-2.5 mg/mL, 100 μL) dose-dependently inhibits neutrophil infiltration and BAL cell cytokine production in rat airway inflammation model[1].PF-184 (i.v. 2 mg/kg or p.o. 5 mg/kg, rats) shows a T1⁄2 (i.v.) value of 1 h, low oral bioavailability (5%), and high i.v. clearance (59 mL/min/kg)[1]. Animal Model: |
| Name | PF-184 |
| Formula | C32H32ClFN6O4 |
| Molar Mass | 619.09 |
| 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]. Cynthia D Sommers, et al. Novel tight-binding inhibitory factor-kappaB kinase (IKK-2) inhibitors demonstrate target-specific anti-inflammatory activities in cellular assays and following oral and local delivery in an in vivo model of airway inflammation. |