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Submit ReviewPF 184
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)
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 |
| InChI Key | JUOWWGNRWRLBSV-MEKGRNQZSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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
Mora et al (2012) Bindarit: an anti-inflammatory small molecule that modulates the NFκB pathway. Cell Cycle 11 159 PMID: 22189654
Charles et al (2020) In vitro benchmarking of NF-κB inhibitors. Eur J Pharmacol 873 172981 PMID: 32014486
Do you know of a great paper that uses PF 184 from Tocris? Please let us know.
Reviews for PF 184
Average Rating: 5 (Based on 1 Review.)
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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.
