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IKK-2 protein kinase inhibitor PHA 408, 5 mg  

IKK-2 protein kinase inhibitor PHA 408, 5 mg

8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide

PHA 408 is a potent, highly selective and ATP-competitive IKB kinase-2 (IKK-2) inhibitor.

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PKI-PHA408-005

Availability: within 3 days

156,00 €

Background: PHA 408 is a 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.

Chemical formula: C29H27ClFN7O2
Molecular weight: 560.02 g/mol
Purity: 99 %
Appearance: Off-white solid
Solubility: Soluble in DMSO
CAS Number: 503555-55-3

Manufacturer:  Axon Medchem BV

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.  

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 (...). J. Ph. Exp. Ther. 2009, 329(1), 14-25.

CD Sommers et al. Novel tight-binding inhibitory factor-kB kinase (IKK-2) inhibitors demonstrate target-specific anti-inflammatory activities in cellular assays (...). J. Pharmacol. Exp. Ther. 2009, 330(2), 377-388.

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.

S Mathialagan et al. Expression, purification and functional characterization of IkB kinase-2 (IKK-2) mutants. Protein Expr. Purif. 2010, 72(2), 254-261.