BIRB 796

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Cat.No. 5989 - BIRB 796 | C31H37N5O3 | CAS No. 285983-48-4
Description: High affinity and selective p38 kinase inhibitor
Alternative Names: Doramapimod
Chemical Name: N-[3-(1,1-Dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl]-N'-[4-[2-(4-morpholinyl)ethoxy]-1-naphthalenyl]urea
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature
Pathways

Biological Activity

High affinity and selective p38 kinase inhibitor (Kd = 50-100 pM). Exhibits no significant inhibition on a panel of related kinases. Inhibits LPS-induced TNFα production in human PBMCs and whole blood (IC50 values are 21 and 960 nM, respectively). Also inhibits JNK2α2 and c-Raf-1 (IC50 values are 98 nM and 1.4 μM, respectively). Cell permeable.

Technical Data

M. Wt 527.66
Formula C31H37N5O3
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 285983-48-4
PubChem ID 156422
InChI Key MVCOAUNKQVWQHZ-UHFFFAOYSA-N
Smiles CC1=CC=C(N2N=C(C(C)(C)C)C=C2NC(NC3=CC=C(C4=C3C=CC=C4)OCCN5CCOCC5)=O)C=C1

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 52.77 100
ethanol 26.38 50

Preparing Stock Solutions

The following data is based on the product molecular weight 527.66. 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 1.9 mL 9.48 mL 18.95 mL
5 mM 0.38 mL 1.9 mL 3.79 mL
10 mM 0.19 mL 0.95 mL 1.9 mL
50 mM 0.04 mL 0.19 mL 0.38 mL

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References

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

Laufer et al (2008) Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. J.Med.Chem. 51 4122 PMID: 18578517

Regan et al (2003) Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). J.Med.Chem. 46 4676 PMID: 14561087

Goldstein et al (2010) Selective p38α inhibitors clinically evaluated for the treatment of chronic inflammatory disorders. J.Med.Chem. 53 2345 PMID: 19950901

Kuma et al (2005) BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo. J.Biol.Chem. 280 19472 PMID: 15755732


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Citations for BIRB 796

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Literature in this Area

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Cancer

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Kinases Product Listing

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

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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 BIRB 796

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.