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SL327 is a selective inhibitor for MEK1/2 with IC50 of 0.18 μM/0.22 μM; able to transport through the blood-brain barrier.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $31 | In Stock | |
10 mg | $40 | In Stock | |
25 mg | $64 | In Stock | |
50 mg | $98 | In Stock | |
100 mg | $163 | In Stock | |
1 mL x 10 mM (in DMSO) | $35 | In Stock |
Description | SL327 is a selective inhibitor for MEK1/2 with IC50 of 0.18 μM/0.22 μM; able to transport through the blood-brain barrier. |
Targets&IC50 | MEK1:0.18 μM, MEK2:0.22 μM |
In vitro | Administration of 30 mg/kg of SL327 significantly impairs spatial learning and memory in mice. At a higher dose of 50 mg/kg, SL327 can cross the blood-brain barrier and inhibit conditioned fear by suppressing the phosphorylation of MAPK/ERK. |
In vivo | SL327 does not inhibit a variety of other kinases, including PKA, PKC, or CamKII. |
Kinase Assay | The ligand binding competition assays are performed. Cytosolic cell extracts from Hepa-1 cells are generated by the resuspension of the cell pellets in HEDG buffer [25 mM Hepes, 1 mM EDTA, 1 mM dithiothreitol, and 10% (v/v) glycerol, pH 7.5] containing 0.4 mM leupeptin, 4 mg/mL aprotinin, and 0.3 mM phenylmethylsulfonyl fluoride, homogenization, and centrifugation at 100,000 g for 45 min. Aliquots of the supernatant (120 μg) are incubated at room temperature for 2 h with the indicated concentrations of Pifithrin-α in the presence of 3 nM [3H]TCDD in HEDG buffer. After incubation on ice with hydroxyapatite for 30 min, HEDG buffer with 0.5% Tween 80 is added. The samples are centrifuged, washed twice, resuspended in 0.2 mL of scintillation fluid, and subjected to scintillation counting. Nonspecific binding is determined using a 150-fold molar excess of TCDF and subtracted from the total binding to obtain the specific binding. The specific binding is reported relative to [3H]TCDD alone[2]. |
Alias | SL-327, SL 327 |
Molecular Weight | 335.35 |
Formula | C16H12F3N3S |
Cas No. | 305350-87-2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (149.1 mM), Sonication is recommended. Ethanol: 16.8 mg/mL (50 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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