Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Skepinone-L (CBS3830) is a selective p38 mitogen-activated protein kinase inhibitor.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 32.00 | |
2 mg | In stock | $ 45.00 | |
5 mg | In stock | $ 72.00 | |
10 mg | In stock | $ 122.00 | |
25 mg | In stock | $ 219.00 | |
50 mg | In stock | $ 329.00 | |
100 mg | In stock | $ 489.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 79.00 |
Description | Skepinone-L (CBS3830) is a selective p38 mitogen-activated protein kinase inhibitor. |
Targets&IC50 | p38α:5 nM |
In vitro | Skepinone-L shows concentration-dependent inhibition of HSP27 (Ser82) phosphorylation through the p38 MAPK pathway with a cellular IC50 of approximately 25 nM, and also reduces concentrations of TNF-α, IL-1β and IL-10, regulated by p38 MAPK, with IC50 ranging from 30 to 50 nM . [1] Skepinone-L (1 μM) abrogates the phosphorylation of platelet p38 MAPK substrate Hsp27 activated by stimulation with CRP, thrombin or thromboxane A2 analogue U-46619, and impairs platelet secretion and aggregation. [2] |
In vivo | In vivo, skepinone-L inhibits Gal/ LPS-induced TNF-α release by 77%. [1] |
Kinase Assay | 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. |
Cell Research | Concentrations: 1 nM - 10 μM, dissolved in DMSO |
Synonyms | CBS3830 |
Molecular Weight | 425.42 |
Formula | C24H21F2NO4 |
CAS No. | 1221485-83-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 79 mg/mL (185.7 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 79 mg/mL (185.7 mM)
You can also refer to dose conversion for different animals. More
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Skepinone-L 1221485-83-1 Autophagy MAPK p38 MAPK inhibit SkepinoneL Skepinone L CBS3830 CBS 3830 CBS-3830 Inhibitor inhibitor