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.
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- CAS No.: 3078541-89-3
- Formule: C32H32ClFN6O4
- Masse moléculaire:619.09
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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IKK-2 37 nM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rat airway model of neutrophilia[1]
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Dosage:0.3-2.5 mg/mL, 100 μL
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Administration:Intratracheal administration
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Result:Suppressed neutrophil infiltration with an EC50 value of 1 mg/mL.
Suppressed BAL fluid TNF-α and PGE2 levels, and inhibited p65 translocation.
Chemical Information
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CAS No. 3078541-89-3
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Masse moléculaire 619.09
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Formule C32H32ClFN6O4
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SMILES
O=C(C1=NN(C2=C1CCC3=C2C=C(NC(C4=CC(N5C[C@](CO)([C@](CO)(C5)C)C)=NC=C4Cl)=O)C=C3)C6=CC=C(C=C6)F)N
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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. J Pharmacol Exp Ther. 2009 Aug;330(2):377-88. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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