FRAX 486

Cat. No. 5190

FRAX 486 C25H23Cl2FN6O [1232030-35-1]

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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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Wang et al (2016) P21-activated kinase inhibitors FRAX486 and IPA3: inhibition of prostate stromal cell growth and effects on smooth muscle contraction in the human prostate. PLoS One 11 e0153312. PMID: 27071060.

Dolan et al (2013) Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by the small-molecule PAK inhibitor FRAX486. Proc.Natl.Acad.Sci.U.S.A. 110 5671. PMID: 23509247.

Hayashi-Takagi et al (2013) PAKs inhibitors ameliorate schizophrenia-associated dendritic spine deterioration in vitro and in vivo during late adolescence. Proc.Natl.Acad.Sci.U.S.A. 111 6461. PMID: 24706880.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for FRAX 486 include:

Wang et al (2016) P21-activated kinase inhibitors FRAX486 and IPA3: inhibition of prostate stromal cell growth and effects on smooth muscle contraction in the human prostate. PloS One 11 e0153312. PMID: 27071060.

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Keywords: FRAX 486, supplier, FRAX486, potent, p21, activated, kinase, PAK, inhibitors, inhibits, neuroprotective, brain, penetrant, orally, bioavailable, Tocris Bioscience, P21-activated Kinases Inhibitor products

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