p38 MAP Kinase Inhibitor III

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Company Name: Sigma-Aldrich  
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p38 MAP Kinase Inhibitor III manufacturers

p38 MAP Kinase Inhibitor III Basic information
Product Name:p38 MAP Kinase Inhibitor III
Synonyms:p38 MAP Kinase Inhibitor III - CAS 581098-48-8 - Calbiochem;(S)-p38 MAPK Inhibitor III;2-Pyridinamine, 4-[5-(4-fluorophenyl)-2-(methylthio)-1H-imidazol-4-yl]-N-[(1S)-1-phenylethyl]-;(S)-p38 MAP Kinase Inhibitor III;(S)-p-38 MAPK Inhibitor III,(S) p38 MAPK Inhibitor III,(S)p38 MAPK Inhibitor III;4-[5-(4-fluorophenyl)-2-(methylthio)-1H-imidazol-4-yl]-N-[(1S)-1-phenylethyl]-2-pyridinamine
CAS:581098-48-8
MF:C23H21FN4S
MW:404.5
EINECS:
Product Categories:
Mol File:581098-48-8.mol
p38 MAP Kinase Inhibitor III Structure
p38 MAP Kinase Inhibitor III Chemical Properties
Melting point 117-119 °C
Boiling point 589.4±60.0 °C(Predicted)
density 1.30±0.1 g/cm3(Predicted)
storage temp. +2C to +8C
solubility DMF: 20 mg/mL; DMSO: 12 mg/mL; Ethanol: 30 mg/mL; Ethanol:PBS (pH 7.2)(1:2): 0.33 mg/mL
form Yellow solid
pka9.07±0.10(Predicted)
color White to off-white
InChI1S/C23H21FN4S/c1-15(16-6-4-3-5-7-16)26-20-14-18(12-13-25-20)22-21(27-23(28-22)29-2)17-8-10-19(24)11-9-17/h3-15H,1-2H3,(H,25,26)(H,27,28)
InChIKeyVXPWQNBKEIVYIS-UHFFFAOYSA-N
SMILESFc1ccc(cc1)c2[nH]c(nc2c3cc(ncc3)NC(C)c4ccccc4)SC
Safety Information
WGK Germany WGK 1
Storage Class11 - Combustible Solids
MSDS Information
p38 MAP Kinase Inhibitor III Usage And Synthesis
Description(S)-p38 MAPK inhibitor III is a methylsulfanylimidazole that inhibits p38 MAP kinase (IC50 = 0.90 μM in vitro). It is cell-permeable, potently blocking the release of TNF-α and IL-1β from human peripheral blood mononuclear cells (IC50s = 0.37 and 0.044 μM, respectively).
Usesp38 MAP Kinase Inhibitor III (compound 7h) is a p38 MAPK inhibitor with an 50 of 0.9 μM. p38 MAP Kinase Inhibitor III also inhibits IL-1β and TNF-α release with 50 values of 0.37 μM and 0.044 μM, respectively[1].
General DescriptionA cell-permeable methylsulfanylimidazole compound that acts as a potent, selective, reversible, and ATP-competitive p38 MAP kinase inhibitor (IC50 = 0.38 μM for p38α). Shown to effectively suppresses LPS-induced cytokine release both in vitro (IC50 = 0.16 and 0.039 μM for TNF-α and IL-1β release, respectively, in human PBMC) and in vivo (ED50 = 1.33 mg/kg for TNF-α release in mouse). When compared with SB 203580 (Cat. No. 559389 and 559398), it exhibits reduced inhibitory activity against cytochrome P450-2D6 isoform and, therefore, is better suited for in vivo use. A 10 mM (1 mg/247 μl) solution of p38 MAP Kinase Inhibitor III (Cat. No. 506148) in DMSO is also available.
Biochem/physiol ActionsCell permeable: yes
IC 50p38 MAP kinase: 0.9 μM (IC50)
References[1] Stefan A Laufer, et al. Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. J Med Chem. 2003 Jul 17;46(15):3230-44. DOI:10.1021/jm030766k
p38 MAP Kinase Inhibitor III Preparation Products And Raw materials
Tag:p38 MAP Kinase Inhibitor III(581098-48-8) Related Product Information
EO 1428 p38 MAPK Monoclonal Antibody (Clone 9F12) PHENOL,2,2'-SULFONYLBIS[3,4,6-TRICHLORO]- 2-(4-Chlorophenyl)-4-(4-fluorophenyl)-5-pyridin-4-yl-1,2-dihydropyrazol-3-one p38-α MAPK-IN-1 2-Propenoic acid, 3-[2,6-dichloro-4-[[[4-[3-(2,2-dimethyl-1-propoxypropyl)-2-methoxyphenyl]-2-thiazolyl]amino]carbonyl]phenyl]-2-methyl-, (2E)-