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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

Replacement Information

Key Spec Table

CAS #Empirical Formula
285983-48-4C₃₁H₃₇N₅O₃

Products

Catalogue NumberPackaging Qty/Pack
506172-10MG Glass bottle 10 mg
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
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
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
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
506172-10MG 04055977272383

Documentation

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

Title

Safety Data Sheet (SDS) 

p38 MAP Kinase Inhibitor X, BIRB 796 - CAS 285983-48-4 - Calbiochem Certificates of Analysis

TitleLot Number
506172

References

Reference overview
Liu. 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.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision10-May-2024 JSW
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
DescriptionA 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 in cultures in vitro (IC50 = 18 and 780 nM using THP-1 cells and in human whole blood, respectively) and in mice in vivo (by 84% and 63%, respectively, with oral dosage of 30 mg/kg and 10 mg/kg).
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number285983-48-4
Chemical formulaC₃₁H₃₇N₅O₃
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (50 mg/ml; clear, colorless solution)
Storage Protect from light
+2°C to +8°C
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.
Toxicity Regulatory Review
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.