Skepinone-L

Skepinone-L (CBS3830) 是一种选择性 p38 丝裂原活化蛋白激酶抑制剂。

产品编号 T6130Cas号 1221485-83-1

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Skepinone-L

产品编号 T6130别名 CBS3830Cas号 1221485-83-1

Skepinone-L (CBS3830) 是一种选择性 p38 丝裂原活化蛋白激酶抑制剂。

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规格	价格	库存
1 mg	¥ 282	现货
2 mg	¥ 416	现货
5 mg	¥ 747	现货
10 mg	¥ 1,230	现货
25 mg	¥ 1,980	现货
50 mg	¥ 2,970	现货
100 mg	¥ 4,350	现货
500 mg	¥ 9,380	现货
1 mL x 10 mM (in DMSO)	¥ 822	现货

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"Skepinone-L"的相关化合物库

产品介绍

生物活性

产品描述	Skepinone-L (CBS3830) is a selective p38 mitogen-activated protein kinase inhibitor.
靶点活性	p38α:5 nM
体外活性	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]
体内活性	在体内，skepinone-L 通过77%的比率抑制Gal/LPS诱导的TNF-α释放。[1]
激酶实验	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.
细胞实验	Concentrations: 1 nM - 10 μM, dissolved in DMSO
别名	CBS3830

化学信息

分子量	425.42
分子式	C₂₄H₂₁F₂NO₄
CAS No.	1221485-83-1

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 50 mg/mL (117.53 mM), Sonication is recommended.

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

Ethanol: 79 mg/mL (185.7 mM)

溶液配制表

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	2.3506 mL	11.7531 mL	23.5062 mL	117.5309 mL
5 mM	0.4701 mL	2.3506 mL	4.7012 mL	23.5062 mL
10 mM	0.2351 mL	1.1753 mL	2.3506 mL	11.7531 mL
20 mM	0.1175 mL	0.5877 mL	1.1753 mL	5.8765 mL
50 mM	0.0470 mL	0.2351 mL	0.4701 mL	2.3506 mL
100 mM	0.0235 mL	0.1175 mL	0.2351 mL	1.1753 mL