Skepinone-L
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Skepinone-L是一种选择性的p38丝裂原活化蛋白激酶(MAPK)抑制剂,IC50值为5 nM[1].
P38 MAPKs是一类丝裂原活化蛋白激酶,负责应力刺激,例如,热休克和渗透休克.它们参与细胞分化与细胞凋亡[1].
Skepinone-L是p38 MAPK的ATP竞争性抑制剂[1].体外实验中,p38 MAPK信号通路的热休克蛋白27(HSP27)的磷酸化作用可以作为评价p38 MAPK活性的标记.当HeLa细胞经茴香霉素处理后,skepinone-L剂量依赖性地抑制HSP27磷酸化, IC50值约为25 nM,这证实了p38 MAPK的抑制作用.此外,在外周血单核细胞(hPBMCs)中,skepinone-L可减少p38 MAPK的下游效应子(包括TNF-α\IL-1β及IL-10)[1].
在小鼠模型中,skepinone-L口服给药可导致skepinone-L水平高达240 nM,且比skepinone的人全血IC50值还要高.因此,它通过抑制上游p38 MAPK,导致77%的肿瘤坏死因子α(TNF-α)抑制.从而证明了skepinone-L的卓越药效学特性[1].
参考文献：
[1]. Koeberle, S C et al., Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor. Nature Chemical Biology, 2012, 8(2), 141-143.
2. Lv, Dan, et al. "Neuronal MHC Class I Expression Is Regulated by Activity Driven Calcium Signaling." PloS one 10.8 (2015): e0135223. PMID:26263390
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 425.42 |
| Cas No. | 1221485-83-1 |
| Formula | C24H21F2NO4 |
| Synonyms | Skepinone L |
| Solubility | ≥21.25 mg/mL in DMSO; insoluble in H2O; ≥46.5 mg/mL in EtOH with ultrasonic |
| Chemical Name | 3-(2,4-difluoroanilino)-9-[(2R)-2,3-dihydroxypropoxy]-5,6-dihydrodibenzo[3,1-[7]annulen-11-one |
| SDF | Download SDF |
| Canonical SMILES | C1CC2=C(C=CC(=C2)NC3=C(C=C(C=C3)F)F)C(=O)C4=C1C=CC(=C4)OCC(CO)O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | Skepinone-L是一种选择性的p38丝裂原活化蛋白激酶(MAPK)和TNF-α的抑制剂,IC50值分别为5 nM和40 nM. | |||||
| 靶点 | p38-MAPK | TNF-α | ||||
| IC50 | 5 nM | 40 nM | ||||
质量控制和MSDS
- 批次:
化学结构
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