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506172 p38 MAP Kinase Inhibitor X, BIRB 796 - CAS 285983-48-4 - Calbiochem

p38 MAP Kinase Inhibitor X, BIRB 796, CAS 285983-48-4, is a cell-permeable, highly potent, slow binding, high affinity inhibitor of p38a (IC50 = 8 and 97 nM with or without 2 h preincubation).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 1-(5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naphthalen-1-yl]urea, JNK Inhibitor XVII, Doramapimod, BIRB796

506172
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Overview

Key Spec Table

CAS #Empirical Formula
285983-48-4C₃₁H₃₇N₅O₃

Products

Catalogue NumberPackaging Qty/Pack
506172-10MG Glass bottle 10 mg
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Description
OverviewA cell-permeable pyrazolo-napthalenyl urea compound that acts as a highly potent, slowly binding (IC50 = 8 and 97 nM, respectively, against human p38α, respectively, with or without 2 h preincubation), but high affinity (t1/2 of dissociation from human p38α = 23 h), p38-selective inhibitor by simultaneously targeting the ATP-binding site and an adjacent DFG-out conformation-specific allosteric cavity. It inhibits JNK2α2 and c-Raf-1 only at much higher concentrations (IC50 = 98 nM and 1.4 µM, respectively) and displays little or no activity toward 10 other kinases (IC50 >20 µM). Shown to inhibit LPS-induced TNF-α production both in vitro (IC50 = 18 and 780 nM using THP-1 cells and in human whole blood, respectively) and in mice in vivo (by 84%; 30 mg/kg p.o.).
Catalogue Number506172
Brand Family Calbiochem®
Synonyms1-(5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naphthalen-1-yl]urea, JNK Inhibitor XVII, Doramapimod, BIRB796
References
ReferencesLiu. Y. and Gray, N.S., 2006. Nat. Chem. Biol. 2, 358.
Regan, J., et al. 2003. J. Med. Chem. 46, 4676.
Pargellis, C., et al. 2002. Nat. Struct. Biol. 9, 268.
Regan, J., et al. 2002. J. Med. Chem. 45, 2994.
Product Information
CAS number285983-48-4
FormWhite solid
Hill FormulaC₃₁H₃₇N₅O₃
Chemical formulaC₃₁H₃₇N₅O₃
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Applicationp38 MAP Kinase Inhibitor X, BIRB 796, CAS 285983-48-4, is a cell-permeable, highly potent, slow binding, high affinity inhibitor of p38a (IC50 = 8 and 97 nM with or without 2 h preincubation).
Biological Information
Purity≥97% by HPLC
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Regulatory Review
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Global Trade Item Number
Catalogue Number GTIN
506172-10MG 04055977272383