SL 327

Description

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.

The Uses of SL 327

SL-327 is a selective inhibitor of MEK1 and MEK2, and ERK1, MEK-3/p38, MEK-4, JNK, and PKC at higher concentrations.

What are the applications of Application

SL-327 is a selective inhibitor of MEK1 and MEK2, and ERK1, MEK-3/p38, MEK-4, JNK, and PKC at higher concentrations

Definition

ChEBI: A nitrile that is acrylonitrile in which the hydrogen attached to the same carbon as the cyano group has been replaced by an o-(trifluoromethyl)phenyl group, while the remaining hydrogens of the ethenyl group have been replaced by amino and (4 aminophenyl)sulfanyl groups.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.

Biological Activity

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.

Biochem/physiol Actions

SL327 is a selective MEK1/2inhibitor (IC50 values are 0.18 and 0.22 μM for MEK1 and MEK2 respectively), which blocks hippocampal LTP in vitro. SL327 is a brain penetrant in vivo blocking fear conditioning and learning in rats, and producing neuroprotection in mice following systemic administration.

Storage

+4°C (desiccate)