An ATP-competitive inhibitor of p38 MAPK isoform p38α (IC50s = 5 nM) and p38β (97% inhibition at 1 µM); has little effect on a range of other kinases

Skepinone-L – 1 mg

Brand:
Cayman
CAS:
1221485-83-1
Storage:
-20
UN-No:
Non-Hazardous - /

Skepinone-L is an ATP-competitive inhibitor of p38 MAPK isoform p38α (IC50s = 5 nM) and p38β (97% inhibition at 1 µM).{26162,26163} It has little effect on a range of other kinases, including p38γ and p38δ. Skepinone-L dose-dependently blocks the phosphorylation of heat shock protein 27 (HSP27), a p38 MAPK substrate, in response to stimulation with anisomycin (Item No. 11308) in HeLa cells (IC50 = 25 nM) or TNF-α in THP-1 cells.{26162,26163} At 1 µM, it prevents phosphorylation of cytosolic phospholipase A2 in platelets in response to collagen-related peptide or thrombin (Item No. 13188), blunting platelet secretion and aggregation.{26164}  

 

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Description

An ATP-competitive inhibitor of p38 MAPK isoform p38α (IC50s = 5 nM) and p38β (97% inhibition at 1 µM); has little effect on a range of other kinases, including p38γ and p38δ; blocks the phosphorylation of HSP27, a p38 MAPK substrate, in response to stimulation with anisomycin in HeLa cells (IC50 = 25 nM)

Formal name: 2-[(2,4-difluorophenyl)amino]-7-[(2R)-2,3-dihydroxypropoxy]-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-one

Synonyms: 

Molecular weight: 425.4

CAS: 1221485-83-1

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

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