Home Cytoskeletal Signaling PAK inhibitor FRAX486 For research use only.

FRAX486

FRAX486 is a potent p21-activated kinase (PAK) inhibitor with IC50 values of 14, 33, 39 and 575 nM for PAK1, PAK2, PAK3 and PAK4 respectively.

FRAX486 Chemical Structure

FRAX486 Chemical Structure

CAS No. 1232030-35-1

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FRAX486 Related Products

Signaling Pathway

PAK Signaling Pathways

PAK Signaling Pathway

Biological Activity

Description FRAX486 is a potent p21-activated kinase (PAK) inhibitor with IC50 values of 14, 33, 39 and 575 nM for PAK1, PAK2, PAK3 and PAK4 respectively.
Targets
PAK1 [1]
(Cell-free assay)		 PAK2 [1]
(Cell-free assay)		 PAK3 [1]
(Cell-free assay)		 PAK4 [1]
(Cell-free assay)
14 nM 33 nM 39 nM 575 nM
In vitro
In vitro In WPMY-1 cells, FRAX486 induces concentration-dependent (1-10 μM) degeneration of actin filaments. This was paralleled by attenuation of proliferation rate, being observed from 1 to 10 μM FRAX486. Cytotoxicity of FRAX486 in WPMY-1 cells is time- and concentration-dependent. In WPMY-1 cells, effects of FRAX486 on actin organization, survival, and proliferation occurred already at concentrations of 1-5 μM. In these concentrations, full inhibition of PAK1-3 may be expected, while PAK4 may be inhibited only partially[2].
Cell Research Cell lines WPMY-1 cells(an immortalized cell line obtained from nonmalignant human prostate stroma)
Concentrations 1, 5, 10 μM
Incubation Time 24, 48, 72 h
Method Cells are grown in 96-well plates (20,000 cells/well) for 24 h, before FRAX486, IPA3, or DMSO are added in indicated concentrations (1, 5, 10 μM). Subsequently, cells are grown for different periods (24, 48, 72 h). Separate controls are performed for each period. At the end of this period, 10 μl of [2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium monosodium salt (WST-8) from CCK-8 is added, and absorbance in each well is measured at 450 nm after incubation for 2 h at 37°C.
In Vivo
In vivo FRAX486 crosses the blood-brain barrier and that therapeutically useful concentrations of FRAX486 are in the brain as early as 1 h and remain as long as 24 h after administration, with the maximum concentration in the target tissue at 8 h. Daily dosing results in steady-state levels of FRAX486 in the brain. FRAX486 specifically rescues the Fmr1 KO abnormality in which the spine phenotype is present in apical neurons and not simply decreasing spine density irrespective of genotype or existence of a phenotype. Also, FRAX486 reduces hyperactivity and stereotypical movements, both of which are phenotypes that characterize the mouse model of Fragile X syndrome[3].
Animal Research Animal Models Male C57BL/6 mice
Dosages 3 mg/kg(i.v.) or 30 mg/kg(p.o.)
Administration i.v. or p.o.

Chemical Information & Solubility

Molecular Weight 513.39 Formula

C25H23Cl2FN6O
CAS No. 1232030-35-1 SDF Download FRAX486 SDF
Smiles CCN1C2=NC(=NC=C2C=C(C1=O)C3=C(C=C(C=C3)Cl)Cl)NC4=CC(=C(C=C4)N5CCNCC5)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 15 mg/mL ( (29.21 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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