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PHA 408
- Soluble in DMSO
- MF: C29H27ClFN7O2
- MW: 560.02
Description
PHA 408 is a potent, highly selective and ATP-competitive IκB kinase-2 (IKK-2/IKKβ) inhibitor with an IC50 value of 40 nM.
IKK-2 controls canonical NF-κB activation through phosphorylation of IκB proteins. PHA 408 is a useful pharmacological tool for dissecting inflammatory signaling, cytokine responses and IKKβ-dependent transcriptional programs.
Key Features
- Potent ATP-competitive IKK-2/IKKβ inhibitor
- IC50: 40 nM for IKK-2
- Tight binding with relatively slow dissociation
- Blocks canonical NF-κB pathway activation
Applications
- NF-κB signaling studies
- Inflammation and cytokine pathway research
- IKK kinase assay development
- Mechanistic studies of immune transcriptional regulation
More Information
| Parent CAS No. | 503555-55-3 |
|---|---|
| Chemical Name | 8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide |
| SMILES | C(C1=NN(C2C=CC(F)=CC=2)C2C3=CC(NC(C4=C(C=NC(N5CCN(C)CC5)=C4)Cl)=O)=CC=C3CCC1=2)(=O)N |
| MFCD | N.A. |
| InChi | InChI=1S/C29H27ClFN7O2/c1-36-10-12-37(13-11-36)25-15-23(24(30)16-33-25)29(40)34-19-6-2-17-3-9-21-26(28(32)39)35-38(27(21)22(17)14-19)20-7-4-18(31)5-8-20/h2,4-8,14-16H,3,9-13H2,1H3,(H2,32,39)(H,34,40) |
| InChiKey | ZLEZHGHFWIHCGU-UHFFFAOYSA-N |
| CID | 22291652 |
| Short Description | IKK-2 inhibitor |
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.
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