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PHA 408

CAS 503555-55-3  

C29H27ClFN7O2  MW 560.02

Purity: 99%

Soluble in DMSO to 100 mM

Ordering Information:

Cat. No. Axon 1651     2012 Promotion

Qty1: 5 mg (research sample) / €135  $176

Qty2: 25 mg (research sample) / €485  $631

Qty3: on request

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Biological Activity:   Potent, highly selective and ATP-competitive IKB kinase-2 (IKK-2) inhibitor (IC50: 40 nM), which binds IKK-2 tightly with a relatively slow off rate; highly recommended tool to investigate the mechanisms by which IKK-2 regulates NF-KB signaling.   References:   G Mbalaviele et al. A novel, highly selective, tight binding IkB kinase-2 (IKK-2) inhibitor: a tool to correlate IKK-2 activity to the fate and functions of the components of the nuclear factor-kB pathway in arthritis-relevant cells and animal models. J. Pharmacol. Exp. Ther. 2009, 329(1), 14-25. [online]   CD Sommers et al. Novel tight-binding inhibitory factor-kB 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, 330(2), 377-388. [online]   S Rajendrasozhan et al. Anti-inflammatory effect of a selective IkB kinase-beta inhibitor in rat lung in response to LPS and cigarette smoke. Pulm. Pharmacol. Ther. 2010, 23(3), 172-181. [online]   S Mathialagan et al. Expression, purification and functional characterization of IkB kinase-2 (IKK-2) mutants. Protein Expr. Purif. 2010, 72(2), 254-261. [online]     Chemical Name: 8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide

PHA 408 | IKK-2 inhibitor | Axon Medchem | Axon 1651 | PHA408

Axon Ligands ^TM - Research chemicals for biological study. Some high-profile samples could be provided under terms of contract research synthesis.

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