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FRAX486

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Chemical Structure| 1232030-35-1 同义名 : -
CAS号 : 1232030-35-1
货号 : A225881
分子式 : C25H23Cl2FN6O
纯度 : 99%+
分子量 : 513.394
MDL号 : MFCD26793866
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 20 mg/mL(38.96 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • PAK

    PAK4, IC50:39 nM

    PAK1, IC50:14 nM

  • PAK1

    PAK1, IC50:14 nM

  • PAK3

    PAK3, IC50:39 nM

  • PAK2

    PAK2, IC50:33 nM

  • PAK4

    PAK4, IC50:575 nM
描述 FRAX486 is a p21-activated kinase (PAK) inhibitor with IC50s of 14, 33 and 39 nM for PAK1, PAK2 and PAK3, respectively. in vitro kinase assays using pure enzymes reveal IC50s for FRAX486 between 10-100 nM for PAK1-3, while the IC50 of 779 nM for PAK4 is just below the micromolar range. In WPMY-1 cells, FRAX486 (24 h) induces concentration-dependent (1-10 μM) degeneration of actin filaments. FRAX486 (1-10 μM, 24 h) causes concentration-dependent degeneration of actin filaments. Actin filaments in solvent-treated control cells are arranged to bundles, forming long and thin protrusions, with elongations from adjacent cells overlapping each other. FRAX486 in concentrations of 1 μM causes partial loss of actin organization, including regressing degree of actin polymerization and degeneration of protrusions. FRAX486 in concentrations of 5 or 10 μM causes complete breakdown of filament organization, resulting in a rounded cell shape without protrusions[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.95mL

0.39mL

0.19mL

9.74mL

1.95mL

0.97mL

19.48mL

3.90mL

1.95mL
参考文献

[1]Wang Y, et al. P21-Activated Kinase Inhibitors FRAX486 and IPA3: Inhibition of Prostate Stromal Cell Growth and Effects on Smooth Muscle Contraction in the Human Prostate. PLoS One. 2016 Apr 12;11(4):e0153312.

[2]Hayashi-Takagi A, 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.