PF 184

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Cat.No. 4238 - PF 184 | C32H32ClFN6O4 | CAS No. 1187460-81-6
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)
Datasheet
Citations (1)
Reviews
Literature

Biological Activity

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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 619.09. Batch specific molecular weights may vary from batch to batch due to solvent 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

Certificate of Analysis / Product Datasheet
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References

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


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View all IκB Kinase Inhibitors

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1 Citation for PF 184

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

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


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