85-2075-17　［取扱停止］p38 MAP Kinase Inhibitor XIX, Skepinone-L ((2-(2,4-Difluorophenylamino)-7-[2R-,3-dihydroxypropoxy]-10,11-dihydro-dibenzo[a,d]-cyclohepten-5-one)) 5mg　217619

特徴

• A cell-permeable phenylamino-dibenzosuberone-diol with a rigid molecular structure specifically designed to target hydrophobic region I in p38alpha & p38beta, but not in other kinases with bulky entrance-blocking gatekeeper residues. Shown to selectively inhibit p38alpha (IC50 = 5nM; [ATP] = 100uM) and p38beta (97% inhibition at 1uM), while exhibiting little affinity toward 400 other kinase constructs, including p38delta, p38upsilon, Erk1/2/3/4/5/8, JNK1/2/3, and MEK1/2/3/4/6. Shown to prevent cellular HSP27 Ser82 phosphorylation upon p38 activation by Anisomycin in HeLa (IC50 = 25nM) or by TNF-alpha in THP-1 cultures. Unlike the ATP-binding site-targeting BIRB 796 and SB 203580, Skepinone-L does not inhibit JNK-mediated c-Jun or ERK-dependent CREB phosphorylation in THP-1 cultures. Oral administration to D-Gal-sensitized mice is reported to greatly reduce plasma TNF-alpha production upon LPS challenge (by 77%; 3mg/kg p.o.) in vivo.
• Formula:C24H21F2NO4
• Solubility:DMSO
• Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.