Skepinone-L

Skepinone-L is an ATP-competitive inhibitor of p38 MAPK isoform p38alpha (IC50s = 5 nM) and p38beta (97% inhibition at 1 µM). It has little effect on a range of other kinases, including p38gamma and p38delta. Skepinone-L dose-dependently blocks the phosphorylation of heat shock protein 27 (HSP27), a p38 MAPK substrate, in response to stimulation with anisomycin (Cay-11308) in HeLa cells (IC50 = 25 nM) or TNF-alpha in THP-1 cells. At 1 µM, it prevents phosphorylation of cytosolic phospholipase A2 in platelets in response to collagen-related peptide or thrombin (Cay-13188), blunting platelet secretion and aggregation.Formal Name: 2-[(2,4-difluorophenyl)amino]-7-[(2R)-2,3-dihydroxypropoxy]-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-one. CAS Number: 1221485-83-1. Molecular Formula: C24H21F2NO4. Formula Weight: 425.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 15 mg/ml, Ethanol: 20 mg/ml, Ethanol:PBS (pH 7.2) (1:4): 0.2 mg/ml. lambdamax: 246, 358, 362 nm. SMILES: FC1=CC=C(NC2=CC(CCC(C=CC(OC[C@H](O)CO)=C3)=C3C4=O)=C4C=C2)C(F)=C1. InChi Code: InChI=1S/C24H21F2NO4/c25-16-4-8-23(22(26)10-16)27-17-5-7-20-15(9-17)2-1-14-3-6-19(11-21(14)24(20)30)31-13-18(29)12-28/h3-11,18,27-29H,1-2,12-13H2/t18-/m1/s1. InChi Key: HXMGCTFLLWPVFM-GOSISDBHSA-N.