An inhibitor of p38α (IC50 = 39 nM) and p38β MAP kinases with 82 and 93% inhibition

p38 MAPK Inhibitor VIII – 5 mg

Brand:
Cayman
CAS:
321351-00-2
Storage:
-20
UN-No:
Non-Hazardous - /

p38 MAP kinase inhibitor VIII is an inhibitor of p38α (IC50 = 39 nM) and p38β MAP kinases with 82 and 93% inhibition, respectively, in a kinase assay when used at a concentration of 1 µM.{38865} It is selective for p38α and 38β, lacking activity at p38γ, p38δ, ERK1/2, and JNK1 at a concentration of 1 µM. p38 MAP kinase inhibitor VIII inhibits IL-1β, TNF-α, IL-6, IL-8, and IL-10, but not IFN-γ release from human peripheral blood mononuclear cells (PBMCs; IC50s = 30, 5, 17, 4, 10, and >1,000 nM, respectively). It also decreases ear swelling in mouse models of allergic and chronic irritative contact dermatitis when administered topically at a dose of 0.5 mg/ear.  

 

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Description

An inhibitor of p38α (IC50 = 39 nM) and p38β MAP kinases with 82 and 93% inhibition, respectively, in a kinase assay (1 µM); selective for p38α and 38β, lacking activity at p38γ, p38δ, ERK1/2, and JNK1 at 1 µM; inhibits IL-1β, TNF-α, IL-6, IL-8, and IL-10, but not IFN-γ release from human peripheral blood mononuclear cells (IC50s = 30, 5, 17, 4, 10, and >1,000 nM, respectively); decreases ear swelling in mouse models of allergic and chronic irritative contact dermatitis (0.5 mg/ear, topical)

Formal name: [4-[(2-amino-4-bromophenyl)amino]-2-chlorophenyl](2-methylphenyl)-methanone

Synonyms:  ​p38 MAP Kinase Inhibitor VIII|EO 1428|p38 Mitogen-activated Protein Kinase Inhibitor VIII

Molecular weight: 415.7

CAS: 321351-00-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|p38 MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling|p38 MAPK Signaling||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Innate Immunity

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