506174 Sigma-Aldrichp38 MAP Kinase Inhibitor XIX, Skepinone-L - Calbiochem
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Overview
Pricing & Availability
| Catalogue Number | Availability | Packaging | Qty/Pack | Price | Quantity | |
|---|---|---|---|---|---|---|
| 506174-5MG |
|
Glass bottle | 5 mg |
|
— |
| Description | |
|---|---|
| Overview | A cell-permeable phenylamino-dibenzosuberone-diol with a rigid molecular structure specifically designed to target hydrophobic region I in p38α & p38β, but not in other kinases with bulky entrance-blocking gatekeeper residues. Shown to selectively inhibit p38α (IC50 = 5 nM; [ATP] = 100 µM) and p38β (97% inhibition at1 µM), while exhibiting little affinity toward 400 other kinase constructs, including p38δ, p38γ, 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 (Cat. No. 176880) in HeLa (IC50 = 25 nM) or by TNF-α in THP-1 cultures. Unlike the ATP-binding site-targeting BIRB 796 (Cat. No. 506172) and SB 203580 (Cat. Nos. 559389, 559395, and 559398), Skepinone-L does not inhibit JNK-mediated c-Jun or ERK-dependent CREB phosphorylation in THP-1 cultures. Oral administration to D-Gal- (Cat. No. 34539) sensitized mice is reported to greatly reduce plasma TNF-α production upon LPS (Cat. No. 437625) challenge (by 77%; 3 mg/kg p.o.) in vivo. |
| Catalogue Number | 506174 |
| Brand Family | Calbiochem® |
| Synonyms | (2-(2,4-Difluorophenylamino)-7-[2R-,3-dihydroxypropoxy]-10,11-dihydro-dibenzo[a,d]-cyclohepten-5-one) |
| References | |
|---|---|
| References | Koeberle, S.C., et al. 2012. J. Med. Chem. 55, 5868. Koeberle, S.C., et al. 2011. Nat. Chem. Biol. 8, 141. |
| Product Information | |
|---|---|
| Form | Light yellow powder |
| Hill Formula | C₂₄H₂₁F₂NO₄ |
| Chemical formula | C₂₄H₂₁F₂NO₄ |
| Structure formula Image | |
| Quality Level | MQ100 |
| Biological Information | |
|---|---|
| Purity | ≥99% by HPLC |
| Packaging Information | |
|---|---|
| Packaged under inert gas | Packaged under inert gas |
| Global Trade Item Number | |
|---|---|
| Catalogue Number | GTIN |
| 506174-5MG | 04055977272406 |