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A cell-permeable, potent, reversible, ATP-competitive, and specific inhibitor of human p38 MAP Kinase (IC50 = 60 nM). Binds to an extended pocket in the active site of the enzyme. Exhibits over 2000-fold greater selectivity for p38 MAPK over ERK (p42/p44 MAP kinase), 500-fold over PKA, 50-fold over PKC, and >1000-fold over EGFR. Also acts as a potent inhibitor of angiogenesis and as an inhibitor of LPS-induced TNF-α production.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number
559396
Brand Family
Calbiochem®
Synonyms
5-(2-Amino-4-pyrimidinyl)-4-(4-fluorophenyl)-1-(4-piperidinlyl)imidazole, p38 MAP Kinase Inhibitor XIV
References
References
Jackson, J.R., et al. 1998. J. Pharmacol. Exp. Ther.284, 687. Wang, Z., et al. 1998. Structure6, 1117.
Jackson, J.R., et al. 1998. J. Pharmacol. Exp. Ther.284, 687. Wang, Z., et al. 1998. Structure6, 1117.
数据表
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
21-November-2014 JSW
Synonyms
5-(2-Amino-4-pyrimidinyl)-4-(4-fluorophenyl)-1-(4-piperidinlyl)imidazole, p38 MAP Kinase Inhibitor XIV
Description
A potent and specific inhibitor of human p38 mitogen-activated protein (MAP) kinase (IC50 = 60 nM). Binds to an extended pocket in the active site of the enzyme. Exhibits >2500-fold greater selectivity for p38 MAPK over ERK (p42/p44 MAP kinase), 500-fold over PKA, 50-fold over PKC, and >1600-fold over EGFRK. Also acts as a potent inhibitor of angiogenesis and as an inhibitor of LPS-induced TNF-α production.
Form
White to pale yellow solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
165806-53-1
Chemical formula
C₁₈H₁₉FN₆
Structure formula
Purity
≥98% by HPLC
Solubility
DMSO (22 mg/ml)
Storage
Protect from light
-20°C
Hygroscopic
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Jackson, J.R., et al. 1998. J. Pharmacol. Exp. Ther.284, 687. Wang, Z., et al. 1998. Structure6, 1117.