Skepinone-L is an ATP-competitive, dibenzosuberone-based inhibitor of p38-MAPK and TNF-a, with IC50 values of 5 and 40 nM, respectively. [1] At 1000 nM, Skepinone-L (Kd = 1.5 nM) did not inhibit any other member of an Ambit panel of 402 kinases. [2]
In vitro HeLa cell assays determined that Skepinone-L showed a concentration-dependent inhibition of HSP27 (Ser82) phosphorylation at an IC50 of 25 nM. [2]. Furthermore, Skepinone-L reduced concentrations of well known p38 MAPK substrates, such as IL-1b and IL10 (IC50 = 30-50 nM). [2]
Technical information:
| Chemical Formula: | C24H21F2NO4 | |
| CAS #: | 1221485-83-1 | |
| Molecular Weight: | 425.42 | |
| Purity: | >99% | |
| Appearance: | Yellow | |
| Chemical Name: | (R)-2-((2,4-difluorophenyl)amino)-7-(2,3-dihydroxypropoxy)-10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-one | |
| Solubility: | Up to 22 mM in DMSO | |
| Synonyms: | Skepinone-L |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Koeberle et al., Design, synthesis, and biological evaluation of novel disubstituted dibenzosuberones as highly potent and selective inhibitors of p38 mitogen activated protein kinase. J. Med. Chem. 2012, 55, 5868-5877. Pubmed ID: 22676210 |
| 2. | Koeberle et al., Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor. Nat. Chem. Biol. 2012, 8, 141-143. Pubmed ID: 22198732 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
