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外観
白色~わずかにうすい褐色、結晶~粉末
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溶解性
エタノール及びジメチルスルホキシドに溶ける。
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使用上の注意
アルゴン封入
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説明
The dual specific threonine/tyrosine kinase MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates a diverse array of cellular processes. SL 327 is an inhibitor of MEK1 and MEK2 (IC50s = 0.18 and 0.22 μM), the kinases upstream of ERK1/2. It inhibits ERK1, MKK/p38, MKK4, JNK, and PKC at much higher concentrations (IC50s = >50, 21, >100, >100, >10 μM, respectively). Since SL 327 rapidly passes the blood-brain barrier, it has been used to dissect the effect of RAS/RAF/MEK/ERK signaling pathway inhibition on behavior, including long-term memory, spatial learning, and fear/operant conditioning.
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使用
SL-327 is a selective inhibitor of MEK1 and MEK2, and ERK1, MEK-3/p38, MEK-4, JNK, and PKC at higher concentrations.
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定義
ChEBI: A nitrile that is acrylonitrile in which the hydrogen attached to the same carbon as the cyano group has been replaced by an o-(trifluoromethyl)phenyl group, while the remaining hydrogens of the ethenyl group have been replaced by amino and (4
aminophenyl)sulfanyl groups. The configuration of the double bond is not specified. It is an inhibitor of MEK1 and MEK2.
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生物活性
Selective inhibitor of MEK1 and MEK2 (IC 50 values are 0.18 and 0.22 μ M respectively); blocks hippocampal LTP in vitro . Brain penetrant in vivo , blocking fear conditioning and learning in rats, and producing neuroprotection in mice, following systemic administration.