FRAX486

Description	in vitro: FRAX486 is an inhibitor of PAK, with excellent selectivity for group I over group II PAKs [1]. Different from W-7 and KN-62, FRAX355 and FRAX486 did not completely block the NMDA-R activation-mediated spine enlargement in the presence of control RNAi, suggesting that these FRAX compounds act less aversely to the synaptic plasticity. in vivo: Mice were administered FRAX486 at a concentration of 20 mg/kg, and brain tissue was collected 8 h after drug treatment. Indeed, the phenotype was rescued by treatment with FRAX486 8 h after a single treatment because spine density was decreased to levels similar to WT mice but significantly lower than untreated Fmr1 KO mice. FRAX486 also decreased spine density in Fmr1 KO mice in the neighboring segment. FRAX486 does not have an effect in segments 1–2 and 5–10, in which there is no phenotype in the mutant mice .
Pathways	Cell Cycle/DNA Damage
Targets	PAK

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