FRAX 486

Key Product Details

Product Description

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.

Product Specifications for FRAX 486

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for FRAX 486

The following data is based on the product molecular weight 513.39.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	9.74 mL	48.70 mL	97.39 mL
1 mM	1.95 mL	9.74 mL	19.48 mL
2 mM	0.97 mL	4.87 mL	9.74 mL
10 mM	0.19 mL	0.97 mL	1.95 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 15 publications citing the usage of this product.

• Dolan Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by the small-molecule PAK inhibitor FRAX486. Proc.Natl.Acad.Sci.U.S.A. 2013 PMID: 23509247
• Wang 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 2016 PMID: 27071060
• Hayashi-Takagi PAKs inhibitors ameliorate schizophrenia-associated dendritic spine deterioration in vitro and in vivo during late adolescence. Proc.Natl.Acad.Sci.U.S.A. 2013 PMID: 24706880

Product Documents for FRAX 486