FRAX 486

• Supplier: Tocris Bioscience
• Catalog: 3091
• Prices: $205.00, $845.00
• Sizes: 10 mg, 50 mg
• Function Type: Inhibitor
• Cas Number: 1232030-35-1
• Chemical Name: 6-(2,4-Dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one
• Formula: C25H23Cl2FN6O
• Molecular Weight: 513.39
• Purity: >98 %
• Description: Potent p21-activated kinase (PAK) inhibitor (IC 50 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 References

Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by the small-molecule PAK - Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by the small-molecule PAK

Dolan BM, Duron SG, Campbell DA, Vollrath B, Shankaranarayana Rao BS, Ko HY, Lin GG, Govindarajan A, Choi SY, Tonegawa S. Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5671-6. doi:

PAKs inhibitors ameliorate schizophrenia-associated dendritic spine deterioration - PAKs inhibitors ameliorate schizophrenia-associated dendritic spine deterioration

Hayashi-Takagi A, Araki Y, Nakamura M, Vollrath B, Duron SG, Yan Z, Kasai H, Huganir RL, Campbell DA, Sawa A. Proc Natl Acad Sci U S A. 2014 Apr 29;111(17):6461-6. doi: