An IKKβ inhibitor
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PHA-408

Item No. 41279

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-[[[5-chloro-2-(4-methyl-1-piperazinyl)-4-pyridinyl]carbonyl]amino]-1-(4-fluorophenyl)-4,5-dihydro-1H-benz[g]indazole-3-carboxamide
CAS Number
503555-55-3
Synonyms
  • PHA-767408
Molecular Formula
C29H27ClFN7O2
Formula Weight
560.0
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly Soluble: 0.1-1 mg/mlMethanol: Slightly Soluble: 0.1-1 mg/ml
SMILES
O=C(C1=NN(C2=C1CCC3=C2C=C(NC(C4=C(Cl)C=NC(N5CCN(CC5)C)=C4)=O)C=C3)C6=CC=C(C=C6)F)N
InChi Code
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)
InChi Key
ZLEZHGHFWIHCGU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    PHA-408 is an inhibitor of IκB kinase β (IKKβ; IC50 = 0.04 µM).1 It is selective for IKKβ over IKKα, Pim-1, Pim-2, Tie2, TrkA, and p70S6K (IC50s = 0.6-28.4 µM), as well as a panel of 26 kinases (IC50s = >30 µM for all). PHA-408 inhibits IL-1β-induced production of prostaglandin E2 (PGE2; Item No. 14010) in synovial fibroblasts isolated from patients with rheumatoid arthritis (IC50 = ~0.6 µM). In vivo, PHA-408 (50 mg/kg) reduces serum LPS-induced TNF-α production in rats. It inhibits joint swelling and bone destruction in a rat model of streptococcal cell wall-induced arthritis when administered at a dose of 10 mg/kg. PHA-408 (15 and 45 mg/kg) inhibits LPS- or cigarette smoke-induced bronchoalveolar lavage fluid (BALF) neutrophil influx and reduces BALF levels of IL-6, TNF-α, and IL-1β in rats.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mbalaviele, G., Sommers, C.D., Bonar, S.L., et al. A novel, highly selective, tight binding IκB kinase-2 (IKK-2) inhibitor: A tool to correlate IKK-2 activity to the fate and functions of the components of the nuclear factor-κB pathway in arthritis-relevant cells and animal models. J. Pharmacol. Exp. Ther. 329(1), 14-25 (2009).

    2. Rajendrasozhan, S., Hwang, J.-W., Yao, H., et al. Anti-inflammatory effect of a selective IκB kinase-beta inhibitor in rat lung in response to LPS and cigarette smoke. Pulm. Pharmacol. Ther. 23(3), 172-181 (2010).