PF 184

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Description: Potent and selective IKKβ inhibitor
Chemical Name: 8-[[[5-Chloro-2-[3,4-dimethyl-3,4-bis(hydroxymethyl)-1-pyrrolidinyl]-4-pyridinyl]carbonyl]amino]-1-(4-fluorophenyl)-4,5-dihydro-1H-benz[g]indazole-3-carboxamide
Purity: ≥98% (HPLC)
Citations (3)
Reviews (1)

Biological Activity for PF 184

PF 184 is a potent and selective IKKβ inhibitor (IC50 = 37 nM). Displays selectivity over 85 other kinases. Inhibits IL-1β-induced TNF-α production in a steroid-insensitive in vitro model of oxidative stress.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data for PF 184

M. Wt 619.09
Formula C32H32ClFN6O4
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1187460-81-6
PubChem ID 57519531
Smiles FC(C=C4)=CC=C4N(N=C3C(N)=O)C2=C3CCC1=CC=C(NC(C5=CC(N(C6)C[C@@](C)(CO)[C@]6(CO)C)=NC=C5Cl)=O)C=C12

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for PF 184

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 61.91 100

Preparing Stock Solutions for PF 184

The following data is based on the product molecular weight 619.09. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.62 mL 8.08 mL 16.15 mL
5 mM 0.32 mL 1.62 mL 3.23 mL
10 mM 0.16 mL 0.81 mL 1.62 mL
50 mM 0.03 mL 0.16 mL 0.32 mL

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Product Datasheets for PF 184

Certificate of Analysis / Product Datasheet
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References for PF 184

References are publications that support the biological activity of the product.

Sommers et al (2009) Novel tight-binding inhibitory factor-κB kinase (IKK-2) inhibitors demostrate 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. 330 377 PMID: 19478133

If you know of a relevant reference for PF 184, please let us know.

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Keywords: PF 184, PF 184 supplier, PF184, pfizer, ikk-2, NF-kappaB, NF-kB, NF-κ, IκB, IkappaB, Kinases, Nuclear, Factor, Kappa, B, potent, selective, inhibitors, inhibits, inhibitory, factor-kappab, αb, kinases, IkB, Kinase, NF-kB/IkB, 4238, Tocris Bioscience

3 Citations for PF 184

Citations are publications that use Tocris products. Selected citations for PF 184 include:

Michael et al (2019) Interleukin-1β Induces mtDNA Release to Activate Innate Immune Signaling via cGAS-STING. Mol Cell 74 801-815.e6 PMID: 30952515

Charles et al (2020) In vitro benchmarking of NF-κB inhibitors. Eur J Pharmacol 873 172981 PMID: 32014486

Mora et al (2012) Bindarit: an anti-inflammatory small molecule that modulates the NFκB pathway. Cell Cycle 11 159 PMID: 22189654

Do you know of a great paper that uses PF 184 from Tocris? Please let us know.

Reviews for PF 184

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PF 184 blocks LPS-induced TNFa production.
By Anonymous on 12/11/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Macrophages

RAW macrophages were incubated with 1 μM PF 184 for 30 min prior to addition of 200 ng/ml LPS for 8 h to follow TNFa mRNA expression. LPS elevated TNFa mRNA levels that was significantly inhibited by pretreatment of cells with PF 184.

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