PF-184 

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].

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].

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

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 T_1⁄2 (i.v.) value of 1 h, low oral bioavailability (5%), and high i.v. clearance (59 mL/min/kg)^[1].

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

619.09

C₃₂H₃₂ClFN₆O₄

Room temperature in continental US; may vary elsewhere.

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

• [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.  [Content Brief]