FRAX486
FRAX486
CAS: 1232030-35-1
Molecular Formula: C25H23Cl2FN6O
FRAX486 - Names and Identifiers
FRAX486 - Physico-chemical Properties
| Molecular Formula | C25H23Cl2FN6O |
| Molar Mass | 513.39 |
| Solubility | DMSO : 21.2 mg/mL (41.29 mM; Need ultrasonic and warming) |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | -20°C |
| Use | FRAX486 is a PAK inhibitor with IC50 values of 14,33 and 39 nM for PAK1,PAK2 and PAK3, respectively. |
| In vitro study | In vitro kinase assays using pure enzymes reveal IC 50 s for FRAX486 between 10-100 nM for PAK1-3, while the IC 50 of 779 nM for PAK4 is just below the micromolar range. For FRAX486, an EC 50 value of 500 nM has been reported from cells (5-50 fold higher than IC 50 ). FRAX486 (30 μM) inhibits endothelin-1 and -2 induced contractions. In WPMY-1 cells, FRAX486 (24 h) induces concentration-dependent (1-10 μM) degeneration of actin filaments. This is 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. FRAX486 significantly reduces the relative proliferation rate in the remaining populations of WPMY-1 cells. While 68% of solvent-treated (24 h) cells shows proliferation, proliferation rate after application of FRAX486 (1-10 μM, 24 h) ranges around 45%. 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. |
| In vivo study | FRAX486 displays the highest penetrance of blood–brain barrier in DISC1-knockdown C57BL/6 mice. Daily administration of FRAX486, but not that of vehicle, between P35 and P60 blocks the exacerbated spine loss during adolescence. In addition to the significant blockade of spine elimination, a trend of enhanced spine generation is observed by treatment with FRAX486. FRAX486 treatment ameliorates a deficit in prepulse inhibition in adulthood. |
FRAX486 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 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 |
| 5 mM | 0.039 ml | 0.195 ml | 0.39 ml |
Last Update：2024-01-02 23:10:35
FRAX486 - Reference Information
| biological activity | FRAX486 is a PAK inhibitor with an IC50 of 14 for PAK1,PAK2 and PAK3, respectively, 33 and 39 nM. |
| Target | PAK1 14 nM (IC 50 ) PAK2 33 nM (IC 50 ) PAK3 39 nM (IC 50 ) |
| In vitro study | In vitro kinase using, while the IC 50 of 779 nM for PAK4 is just below the micromolecular range. For FRAX486, an EC 50 value of 500 nM has been reported from cells (5-50 fold higher than IC 50). FRAX486 (30 μM) inhibits endothelin-1 and -2 induced contractions. In WPMY-1 cells, FRAX486 (24 h) induces concentration-dependent (1-10 μM) degeneration of actin filaments. This is 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. FRAX486 significantly reduces the relative proliferation rate in the remaining populations of WPMY-1 cells. While 68% of solvent-treated (24 h) cells shows proliferation, proliferation rate after application of FRAX486 (1-10 μM, 24 h) ranges around 45%. 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.|
| in vivo studies | FRAX486 displays the high cost of blood-brain Barrett in DISC1-knockdown C57BL/6 mice. Daily administration of FRAX486, but not that of vehicle, between P35 and P60 blocks during adolescence. In addition to the significant blockade of spine elimination, a trend of enhanced spine generation is observed by treatment with FRAX486. FRAX486 treatment ameliorates a deficit in prepulse inhibition in adulthood. |
Last Update：2024-04-09 02:00:02
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Tel: 609-228-6898
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Mobile: 609-228-6898
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Tel: 18301782025
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