FRAX 486

Biological Activity

FRAX 486 is a potent p21-activated kinase (PAK) inhibitor (IC₅₀ values are 14, 33, 39 and 575 nM for PAK1, PAK2, PAK3 and PAK4 respectively). Blocks and reverses the DISC1 knockdown-induced reduction in dendritic spine size in cortical neurons. Attenuates dendritic spine elimination and enhances spine generation in DISC1 knockdown mice. Ameliorates autism-like behavioral symptoms in fragile X mental retardation 1 (Fmr1) knockout mice. Brain penetrant and orally bioavailable.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. P21-Activated Kinase Inhibitors FRAX486 and IPA3: Inhibition of Prostate Stromal Cell Growth and Effects on Smooth Muscle Contraction in the Human Prostate.
   Wang Y, Gratzke C, Tamalunas A et al.
   PLoS One
2. P21-Activated Kinase Inhibitors FRAX486 and IPA3: Inhibition of Prostate Stromal Cell Growth and Effects on Smooth Muscle Contraction in the Human Prostate
   Y Wang, C Gratzke, A Tamalunas, N Wiemer, A Ciotkowska, B Rutz, R Waidelich, F Strittmatt, C Liu, CG Stief, M Hennenberg
   PLoS ONE, 2016;11(4):e0153312.
3. PAKs inhibitors ameliorate schizophrenia-associated dendritic spine deterioration in vitro and in vivo during late adolescence.
   Hayashi-Takagi et al.
   Proc.Natl.Acad.Sci.U.S.A., 2013;111:6461
4. Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by the small-molecule PAK inhibitor FRAX486.
   Dolan et al.
   Proc.Natl.Acad.Sci.U.S.A., 2013;110:5671

Product Datasheets