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FRAX 486
- Soluble in DMSO
- MF: C25H23Cl2FN6O
- MW: 513.39
Description
FRAX 486 is a bioavailable and brain-penetrant group I p21-activated kinase (PAK) inhibitor with IC50 values of 8.25 nM, 39.5 nM and 55.3 nM for PAK1, PAK2 and PAK3, respectively. It shows selectivity over PAK4 and rescues dendritic spine and behavioral phenotypes in Fmr1 knockout models.
Group I PAKs link Rac/Cdc42 GTPase signaling to cytoskeletal remodeling, synaptic structure and neurodevelopmental phenotypes. FRAX 486 is useful for studying PAK-dependent neuronal morphology, Fragile X syndrome biology and neuropsychiatric disease mechanisms.
Key Features
- Brain-penetrant group I PAK inhibitor
- IC50: 8.25 nM at PAK1
- Inhibits PAK2 and PAK3 in the low-nanomolar range
- Rescues dendritic spine phenotypes in Fmr1 models
Applications
- PAK kinase pharmacology
- Fragile X syndrome model studies
- Dendritic spine morphology assays
- Neurodevelopmental and synaptic signaling research
More Information
| Parent CAS No. | 1232030-35-1 |
|---|---|
| Chemical Name | 6-(2,4-dichlorophenyl)-8-ethyl-2-(3-fluoro-4-(piperazin-1-yl)phenylamino)pyrido[2,3-d]pyrimidin-7(8H)-one |
| SMILES | C1(NC2=CC=C(N3CCNCC3)C(F)=C2)=NC=C2C=C(C3=CC=C(Cl)C=C3Cl)C(=O)N(CC)C2=N1 |
| MFCD | N.A. |
| InChi | InChI=1S/C25H23Cl2FN6O/c1-2-34-23-15(11-19(24(34)35)18-5-3-16(26)12-20(18)27)14-30-25(32-23)31-17-4-6-22(21(28)13-17)33-9-7-29-8-10-33/h3-6,11-14,29H,2,7-10H2,1H3,(H,30,31,32) |
| InChiKey | DHKFOIHIUYFSOF-UHFFFAOYSA-N |
| CID | 68060125 |
| Short Description | PAK inhibitor |
References
- B.M. Dolan et al. 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 Apr 2;110(14):5671-6.
- A. Hayashi-Takagi et al. PAKs inhibitors ameliorate schizophrenia-associated dendritic spine deterioration in vitro and in vivo during late adolescence. Proc Natl Acad Sci U S A. 2014 Apr 29;111(17):6461-6.
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