FRAX1036 is a potent, group I-selective p21-activated kinase (PAK) inhibitor (PAK1/4 Ki = 23 nM/1.4 μM; PAK1/4 IC50 = 2 nM/>500 nM; >96% PAK1/2/3 inhibition vs. 5.1%/8.2%/22.2% PAK4/5/6 inhibition at 1 μM) with significant inhibitory activity toward only 11 other kinases at a high concentration of 1 μM (78.7-100% inhibition) among a panel of 240. FRAX1036 exhibits higher antiproliferation activity in PAK negative regulator NF2-deficient meningioma cultures (NF2-/- Ben-Men-1/KT21-MG1 IC50 = 1.888/1.991 μM vs.NF2+/+ MN328/MN525 IC50 = 4.239/3.296 μM) by inhibiting cellular PAK autophosphorylation and downstream signaling events. When administered orally in a murine orthotopic meningioma model, FRAX1036 effectively suppresses the growth of established KT21 and Ben-Men tumors in vivo (30 mg/kg/d p.o.).
Orally active, potent group I-selective p21-activated kinase (PAK1/2/3) inhibitor with in vivo efficacy in a murine orthotopic meningioma model.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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Molecular and cellular biology, 35(23), 3990-4005 (2015-09-24)
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p21-activated kinases (Paks) are Cdc42/Rac-activated serine-threonine protein kinases that regulate several key cancer-relevant signaling pathways, such as the Mek/Erk, PI3K/Akt and Wnt/b-catenin signaling pathways. Pak1 is frequently overexpressed and/or hyperactivated in different human cancers, including human breast, ovary, prostate and
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