Catalog Number: 5190
Chemical Name: 6-(2,4-Dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one
Biological Activity
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
  • M.Wt:
    513.39
  • Formula:
    C25H23Cl2FN6O
  • Solubility:
    Soluble to 20 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    1232030-35-1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. 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
  2. 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
  3. P21-activated kinase inhibitors FRAX486 and IPA3: inhibition of prostate stromal cell growth and effects on smooth muscle contraction in the human prostate.
    Wang et al.
    PLoS One, 2016;11:e0153312
Citations:

The citations listed below are publications that use Tocris products. Selected citations for FRAX 486 include:

1 Citations: Showing 1 - 1

  1. P21-activated kinase inhibitors FRAX486 and IPA3: inhibition of prostate stromal cell growth and effects on smooth muscle contraction in the human prostate.
    Authors: Wang Et al.
    PloS One 2016;11:e0153312

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