FRAX486

FRAX486

Biochem/physiol Actions

FRAX486 is a potent, group I-selective p21-activated kinase (PAK) inhibitor (PAK1/2/3 IC50 = 8.25/39.5/55.3 nM; group II PAK4 IC50 = 779 nM). FRAX486 effectively inhibits PAK-mediated PKD1 Ser203 phosphorylation and PAK1/2 Ser144/141 autophosphorylation upon angiotensin II (ANGII) stimulation of rat IEC-18 cells (IC50 ~0.5 µM) and exhibits in vivo efficacy in rescuing the autism-like phenotypes among Fmr1 knockout fragile syndrome (FXS) mice (20 mg/kg s.c.) as well as in ameliorating schizophrenia-associated dendritic spine deterioration among Disc1 knockdown mice (10 µg/g or 10 mg/kg i.p.) with good pharmacokinetic properties and blood–brain barrier (BBB) permeability.

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3576063 FRAX486 white to beige SIGMA-ALDRICH −20°C DMSO: 2 mg/mL, clear powder ≥98% (HPLC)
£565.50 (exc VAT) per 25MG
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3576064 FRAX486 white to beige SIGMA-ALDRICH −20°C DMSO: 2 mg/mL, clear powder ≥98% (HPLC)
£139.29 (exc VAT) per 5MG
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