| CAS NO: | 1221485-83-1 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 200mg | 电议 |
| Cas No. | 1221485-83-1 |
| 别名 | Skepinone L |
| 化学名 | 3-(2,4-difluoroanilino)-9-[(2R)-2,3-dihydroxypropoxy]-5,6-dihydrodibenzo[3,1-[7]annulen-11-one |
| Canonical SMILES | C1CC2=C(C=CC(=C2)NC3=C(C=C(C=C3)F)F)C(=O)C4=C1C=CC(=C4)OCC(CO)O |
| 分子式 | C24H21F2NO4 |
| 分子量 | 425.42 |
| 溶解度 | ≥ 21.25 mg/mL in DMSO, ≥ 46.5 mg/mL in EtOH with ultrasonic |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Skepinone-L is a selective inhibitor of p38 mitogen-activated protein kinase (MAPK) with IC50 value of 5 nM[1]. P38 MAPKs are a class of MAPK which are responsive for stress stimuli, such as heat shock and osmotic shock. They are involved in cell differentiation and apoptosis [1]. Skepinone-L is a ATP-competitive inhibitor of p38 MAPK [1]. For in vitro test, the phosphory!lation of heat shock protein 27 (HSP27) of the p38 MAPK pathway can be used as a marker to assess the activity of p38 MAPK. When HeLa cells were treated with anisomycin, skepinone-L showed dose-dependent inhibition of HSP27 phosphorylation with a cellular IC50 ~25 nM, which confirmed the inhibition of p38 MAPK. Additionally, in peripheral blood mononuclear cells (hPBMCs), treatment of skepinone-L resulted in the reduction of p38 MAPK downstream effectors including TNF-α, IL-1β and IL-10 [1]. In mouse model, oral administration of skepinone-L resulted in very high level of skepinone-L which was 240 nM and higher than the human whole-blood IC50 value of skepinone. Therefore, it resulted in the inhibition of TNF-α by 77% via the inhibition of upstream p38 MAPK. Thus, it demonstrated the pre!eminent pharmacodynamic properties of skepinone-L [1]. Reference: |
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