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The following MAPmates™ should not be plexed together:
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48-602MAG
Buffer Detection Kit for Magnetic Beads
1 Kit
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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).
More>>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). Less<<
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Description
Overview
A 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 Number
506172
Brand Family
Calbiochem®
Synonyms
1-(5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naphthalen-1-yl]urea, Doramapimod, BIRB796, JNK Inhibitor XVII
References
References
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.
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).
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 Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
p38 MAP Kinase Inhibitor X, BIRB 796 - CAS 285983-48-4 - Calbiochem Certificates of Analysis
Title
Lot 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.
Revision
10-May-2024 JSW
Synonyms
1-(5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naphthalen-1-yl]urea, Doramapimod, BIRB796, JNK Inhibitor XVII
Description
A 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).
Form
White solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
285983-48-4
Chemical formula
C₃₁H₃₇N₅O₃
Structure formula
Purity
≥97% by HPLC
Solubility
DMSO (50 mg/ml; clear, colorless solution)
Storage
Protect from light +2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity
Regulatory Review
References
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.