503555-55-3
Chemical Structure
PHA 408
- CAS No.: 503555-55-3
- Formula:C29H27ClFN7O2
- Molecular Weight:560.02
IUPAC Name: 8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide
InChIKey: ZLEZHGHFWIHCGU-UHFFFAOYSA-N
SMILES: O=C(C1=NN(C2=CC=C(F)C=C2)C3=C1CCC4=CC=C(NC(C5=C(Cl)C=NC(N6CCN(C)CC6)=C5)=O)C=C43)N
Biological Activity: PHA-408 is a highly selective, orally active and ATP-competitive IKK-2 inhibitor with an IC50 of 40 nM. PHA-408 blocks NF-κB signaling by suppressing IκBα phosphorylation and degradation, p65 phosphorylation, and pro-inflammatory cytokine production, and prevents TNF-α-induced premature senescence in HUVECs. PHA-408 alleviates LPS-and cigarette smoke-triggered pulmonary inflammation, reduces LPS-stimulated serum TNF-α release, and ameliorates joint damage in SCW-induced arthritis in rats. PHA-408 is applicable for the research of rheumatoid arthritis, chronic obstructive pulmonary disease (COPD), and Duchenne muscular dystrophy[1][2][3][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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PHA 408 | 99.40% | PHA-408 is a highly selective, orally active and ATP-competitive IKK-2 inhibitor with an IC50 of 40 nM. PHA-408 blocks NF-κB signaling by suppressing IκBα phosphorylation and degradation, p65 phosphorylation, and pro-inflammatory cytokine production, and prevents TNF-α-induced premature senescence in HUVECs. PHA-408 alleviates LPS-and cigarette smoke-triggered pulmonary inflammation, reduces LPS-stimulated serum TNF-α release, and ameliorates joint damage in SCW-induced arthritis in rats. PHA-408 is applicable for the research of rheumatoid arthritis, chronic obstructive pulmonary disease (COPD), and Duchenne muscular dystrophy. | ||||||||||||||||||||
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References
- [1]. Khan SY, et al. Premature senescence of endothelial cells upon chronic exposure to TNFα can be prevented by N-acetyl cysteine and plumericin. Sci Rep. 2017 Jan 3;7:39501. [Content Brief]
- [2]. Rajendrasozhan S, et al. Anti-inflammatory effect of a selective IkappaB kinase-beta inhibitor in rat lung in response to LPS and cigarette smoke. Pulm Pharmacol Ther. 2010 Jun;23(3):172-81. [Content Brief]
- [3]. Mbalaviele G, et al. A novel, highly selective, tight binding IkappaB kinase-2 (IKK-2) inhibitor: a tool to correlate IKK-2 activity to the fate and functions of the components of the nuclear factor-kappaB pathway in arthritis-relevant cells and animal models. J Pharmacol Exp Ther. 2009 Apr;329(1):14-25. [Content Brief]
- [4]. Carlson CG, et al. The effect of specific IKKβ inhibitors on the cytosolic expression of IκB-α and the nuclear expression of p65 in dystrophic (MDX) muscle. Am J Transl Res. 2015 Apr 15;7(4):670-82.
