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| Product | Description | |
|---|---|---|
| Skepinone-L | Skepinone-L is a selective p38α-MAPK inhibitor with IC50 of 5 nM. Grades: >98%. CAS No. 1221485-83-1. Molecular formula: C24H21F2NO4. Mole weight: 425.42. |  |
| p38 MAP Kinase Inhibitor XIX, Skepinone-L ((2-(2,4-Difluorophenylamino)-7-[2R-,3-dihydroxypropoxy]-10,11-dihydro-dibenzo[a,d]-cyclohepten-5-one)) | 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. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. US Biological Life Sciences. |  Worldwide |
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