Skepinone-L (CBS3830) is a selective p38 mitogen-activated protein kinase inhibitor.

p38α:5 nM

Skepinone-L 在细胞内通过p38 MAPK途径对HSP27 (Ser82) 的磷酸化表现出浓度依赖性的抑制作用，其IC50约为25 nM，并且还能降低TNF-α、IL-1β和IL-10的浓度，这些均由p38 MAPK调控，其IC50范围在30至50 nM之间。[1] 当细胞受到CRP、凝血酶或血栓素A2类似物U-46619的刺激时，Skepinone-L (1 μM) 能够抑制血小板p38 MAPK底物Hsp27的磷酸化，并且阻碍了血小板的分泌和聚集。[2]

在体内，skepinone-L 通过77%的比率抑制Gal/LPS诱导的TNF-α释放。[1]

CDK1 kinase activity is tested by the CDK1/cyclin B complex purified from baculovirus to phosphorylate a biotinylated peptide substrate containing the consensus phosphorylation site for histone H1, which is phosphorylated in vivo by CDK1. Inhibition of CDK1 activity is measured by observing a decreased amount of 33P-γ-ATP incorporation into the immobilized substrate in streptavidin-coated 96-well scintillating microplates. CDK1 enzyme is diluted in 50 mM Tris-HCl (pH 8), 10 mM MgCl2, 0.1 mM Na3VO4, 1 mM DTT, 1% DMSO, 0.25 μM peptide, 0.1 μCi per well 33P-γ-ATP, and 5 μM ATP in the presence or absence of various concentrations of JNJ-7706621 and incubated at 30 °C for 1 hour. The reaction is terminated by washing with PBS containing 100 mM EDTA and plates are counted in a scintillation counter. IC50 is determined by Linear regression analysis of the percent inhibition by JNJ-7706621.

Concentrations: 1 nM - 10 μM, dissolved in DMSO