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506174 p38 MAP Kinase Inhibitor XIX, Skepinone-L - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: (2-(2,4-Difluorophenylamino)-7-[2R-,3-dihydroxypropoxy]-10,11-dihydro-dibenzo[a,d]-cyclohepten-5-one)

506174
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Overview

Products

Catalogue NumberPackaging Qty/Pack
506174-5MG Glass bottle 5 mg
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Description
OverviewA 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 Number506174
Brand Family Calbiochem®
Synonyms(2-(2,4-Difluorophenylamino)-7-[2R-,3-dihydroxypropoxy]-10,11-dihydro-dibenzo[a,d]-cyclohepten-5-one)
References
ReferencesKoeberle, S.C., et al. 2012. J. Med. Chem. 55, 5868.
Koeberle, S.C., et al. 2011. Nat. Chem. Biol. 8, 141.
Product Information
FormLight yellow powder
Hill FormulaC₂₄H₂₁F₂NO₄
Chemical formulaC₂₄H₂₁F₂NO₄
Structure formula ImageStructure formula Image
Quality LevelMQ100
Biological Information
Purity≥99% by HPLC
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Global Trade Item Number
Catalogue Number GTIN
506174-5MG 04055977272406