化合物FRAX486 T6840

Product Introduction
Bioactivity


英文名: FRAX486

描述: FRAX486 是一种有效的 p21 活化激酶 (PAK) 抑制剂，对 PAK1、PAK2、PAK3 和 PAK4 的 IC50 值分别为 14、33、39 和 575 nM。

细胞实验: 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.(Only for Reference)

体外活性: 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].

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 10.3 mg/mL (20 mM)


关键字: PAK | FRAX486 | p21 activated kinases | FRAX 486 | FRAX-486 | Inhibitor | inhibit

相关产品: PF-3758309 hydrochloride | PAK4-IN-3 | LCH-7749944 | ZMF-23 | FRAX1036 | GNE 2861 | G-5555 | Fingolimod | G-5555 hydrochloride (1648863-90-4 free base) | FRAX597

相关库: Anti-Aging Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Cytoskeletal Signaling Pathway Compound Library | Bioactive Compound Library

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