首页 Cytoskeletal Signaling PAK FRAX486
FRAX486
编号 T6840    
CAS 1232030-35-1     分子式 C25H23Cl2FN6O     分子量 513.39
靶点: PAK1; PAK2; PAK3; PAK4;
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.
选择批次  
规格 库存 单价 数量
2 mg 上海现货 369.00
5 mg 上海现货 665.00
10 mg 上海现货 1197.00
25 mg 上海现货 1976.00
50 mg 上海现货 2964.00
100 mg 上海现货 5120.00
1 mL * 10 mM (in DMSO) 上海现货 1197.00
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生物活性

产品描述

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.

靶点活性

PAK1,14nM

PAK2,33nM

PAK3,39nM

PAK4,575nM

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].

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)

细胞系: WPMY-1 cells(an immortalized cell line obtained from nonmalignant human prostate stroma)

动物实验

动物模型:C57BL/6 mice

化学信息

分子量

513.39

分子式

C25H23Cl2FN6O

CAS

1232030-35-1

溶解度

DMSO: 10.3 mg/mL (20 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 1.948 ml 9.739 ml 19.478 ml
5 mM 0.39 ml 1.948 ml 3.896 ml
10 mM 0.195 ml 0.974 ml 1.948 ml
50 mM 0.039 ml 0.195 ml 0.39 ml
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