Skepinone-L

製品コードS7214 バッチS721401

化学情報

	Synonyms	CBS3830	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₄H₂₁F₂NO₄
	分子量	425.42	CAS No.	1221485-83-1
Solubility (25°C)*	体外	DMSO	85 mg/mL (199.8 mM)
		Ethanol	85 mg/mL (199.8 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Skepinone-L (CBS3830) is a selective p38α-MAPK inhibitor with IC50 of 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]

プロトコル(参考用のみ)

キナーゼアッセイ	Cell-free p38α-MAPK activity assay
キナーゼアッセイ	Microtiter plates are coated with 50 μl of ATF-2 (10 μ/mL in TBS) for 1.5 h at 37 °C, washed with bidistilled water, blocked with blocking buffer (BB; 0.05% Tween 20, 0.25% BSA, 0,02% NaN3 in TBS) for 30 min at room temperature, and washed again. 50 μL of the respective test solution is incubated for 1 h at 37 °C. Test solutions contained 12 ng/well p38-MAPK diluted in kinase buffer (50 mM Tris, pH 7.5, 10 mM MgCl₂, 10 mM β-glycerophosphate, 100 μg/mL BSA, 1 mM dithiothretiol, 0.1 mM Na₃VO₄, 100 μM rATP) with or without test substance (10 nM-100 μM). Test substances are dissolved in dimethyl sulfoxide to form stock solutions of 10 mM, all further dilution steps are carried out in kinase buffer. After subsequent washing, plates are blocked again with BB for 15 min followed by a washing step. 1. AB (50 μL, 1:500 in BB) was incubated for 1 h at 37 °C followed by washing and incubation with 50 μL of the 2. AB (alkaline phosphatase conjugated) (1:4000 in BB). After a final washing step, 100 μL of 4-nitrophenyl phosphate (NPP) is pipetted in each well and colour development was measured 1.5–2 h later with an enzyme-linked immunosorbent assay reader equipped with the SOFTmax PRO software at 405 nm.
動物実験	動物モデル	Mice
	投薬量	~3 mg/kg
	投与方法	Oral administration

参考

カスタマーフィードバック

: Data from [Data independently produced by , , Cell Physiol Biochem,2015, 36(2):631-641.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Cellular stress induces non-canonical activation of the receptor tyrosine kinase EphA2 through the p38-MK2-RSK signaling pathway [ J Biol Chem, 2023, S0021-9258(23)00341-1]	PubMed: 37059179
A CRISPRi/a platform in human iPSC-derived microglia uncovers regulators of disease states [ Nat Neurosci, 2022, 25(9):1149-1162]	PubMed: 35953545
Alternative splicing of apoptosis genes promotes human T cell survival [ Elife, 2022, 11e80953]	PubMed: 36264057
DUSP4 protects BRAF- and NRAS-mutant melanoma from oncogene overdose through modulation of MITF [ Life Sci Alliance, 2022, 5(9)e202101235]	PubMed: 35580987
Elucidation of cGMP-dependent induction of mitochondrial biogenesis through PKG and p38 MAPK in the kidney. [ Am J Physiol Renal Physiol, 2020, 318(2):F322-F328]	PubMed: 31841384
Phenotype-Based Screens with Conformation-Specific Inhibitors Reveal p38 Gamma and Delta as Targets for HCC Polypharmacology. [ Mol Cancer Ther, 2019, 18(9):1506-1519]	PubMed: 31213506
GADD45β loss ablates innate immunosuppression in cancer [Verzella D Cancer Res, 2018, 78(5):1275-1292]	PubMed: 29279355
Lab-Attenuated Rabies Virus Causes Abortive Infection and Induces Cytokine Expression in Astrocytes by Activating Mitochondrial Antiviral-Signaling Protein Signaling Pathway [ Front Immunol, 2017, 8:2011]	PubMed: 29403485
Curcumin Modulates Macrophage Polarization Through the Inhibition of the Toll-Like Receptor 4 Expression and its Signaling Pathways [Zhou Y, et al. Cell Physiol Biochem, 2015, 36(2):631-641]	PubMed: 25998190

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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