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Skepinone-L

Catalog No. T6130 CAS 1221485-83-1

Synonyms: CBS3830

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

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Skepinone-L, CAS 1221485-83-1

Pack Size	Availability	Price/USD
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

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Purity: 100%

Purity: 99.76%

Biological Description

Chemical Properties

Storage & Solubility Information

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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 79 mg/mL (185.7 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 79 mg/mL (185.7 mM)

References and Literature

1. Koeberle SC, et al. Nat Chem Biol. 2011, 8(2), 141-143. 2. Borst O, et al. Cell Physiol Biochem. 2013, 31(6), 914-924.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Human Metabolite Library Anti-Cancer Compound Library NO PAINS Compound Library Anti-Colorectal Cancer Compound Library Osteogenesis Compound Library Anti-COVID-19 Compound Library Neural Regeneration Compound Library Anti-Liver Cancer Compound Library

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Keywords

Skepinone-L 1221485-83-1 Autophagy MAPK p38 MAPK inhibit SkepinoneL Skepinone L CBS3830 CBS 3830 CBS-3830 Inhibitor inhibitor

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