RWJ 67657

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Cat.No. 2999 - RWJ 67657 | C27H24FN3O | CAS No. 215303-72-3
Description: Potent, selective p38α and p38β inhibitor
Chemical Name: 4-[4-(4-Fluorophenyl)-1-(3-phenylpropyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]-3-butyn-1-ol
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature
Pathways

Biological Activity

Selective p38α and p38β inhibitor (IC50 values are 1 and 11 μM respectively) that displays no activity at p38γ, p38δ and a range of other kinases. Potently inhibits TNF-α and IL-1β release (IC50 values are 3 and 11 nM respectively) and suppresses HIV-1 replication in T cells in vitro. Displays cardioprotective and anti-inflammatory activity in vivo. Orally active.

Compound Libraries

RWJ 67657 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 425.5
Formula C27H24FN3O
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 215303-72-3
PubChem ID 3008319
InChI Key QSUSKMBNZQHHPA-UHFFFAOYSA-N
Smiles FC(C=C4)=CC=C4C(N=C(C#CCCO)N2CCCC3=CC=CC=C3)=C2C1=CC=NC=C1

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 42.55 100
ethanol 42.55 100

Preparing Stock Solutions

The following data is based on the product molecular weight 425.5. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.35 mL 11.75 mL 23.5 mL
5 mM 0.47 mL 2.35 mL 4.7 mL
10 mM 0.24 mL 1.18 mL 2.35 mL
50 mM 0.05 mL 0.24 mL 0.47 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Muthumani et al (2004) Suppresssion of HIV-1 viral replication and cellular pathogenesis by a novel p38/JNK kinase inhibitor. AIDS 18 739 PMID: 15075508

See et al (2004) p38 mitogen activated protein kinase inhibition improves cardiac function and attenuates left ventricular remodeling fowllowing myocardial infarction in the rat. J.Am.Coll.Cardiol. 44 1679 PMID: 15489104

Wadsworth et al (1999) RWJ 67657, a potent, orally active inhibitor of p38 mitogen-activated protein kinase. J.Pharm.Exp.Ther. 291 680 PMID:


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Keywords: Potent selective p38α p38alpha p38β p38beta inhibitors inhibits MAPK Signaling Signalling Mitogen-Activated Protein Kinases RWJ67657 p38

Citations for RWJ 67657

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Immunology

Immunology Product Listing

A collection of over 190 products for immunology research, the guide includes research tools for the study of:

  • Chemokine and Cytokine Signaling
  • Chemotaxis
  • Complement System
  • Immune Cell Signaling
  • Inflammation
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
MAPK Signaling

MAPK Signaling Scientific Review

MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.

Pathways for RWJ 67657

MAPK

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.

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