Biological Activity
Selective inhibitor of MEK1 and MEK2 (IC50 values are 0.18 and 0.22 μM respectively); blocks hippocampal LTP in vitro. Brain penetrant in vivo, blocking fear conditioning and learning in rats, and producing neuroprotection in mice, following systemic administration.
Compound Libraries
SL 327 is also offered as part of the Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 335.35 |
| Formula | C16H12F3N3S |
| Storage | Desiccate at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 305350-87-2 |
| PubChem ID | 9549284 |
| InChI Key | JLOXTZFYJNCPIS-FYWRMAATSA-N |
| Smiles | NC(SC1=CC=C(N)C=C1)=C(C#N)C1=CC=CC=C1C(F)(F)F |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 33.53 | 100 | |
| ethanol | 16.77 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 335.35. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.98 mL | 14.91 mL | 29.82 mL |
| 5 mM | 0.6 mL | 2.98 mL | 5.96 mL |
| 10 mM | 0.3 mL | 1.49 mL | 2.98 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.6 mL |
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References
References are publications that support the products' biological activity.
Davis et al (2000) The MAPK/ERK cascade targets both Elk-1 and cAMP response element-binding protein to control long-term potentiation-dependent gene expression in the dentate gyrus in vivo. J.Neurosci. 20 4563 PMID: 10844026
Scherle et al (2000) Regulation of cyclooxygenase-2 induction in the mouse uterus during decidualization. An event of early pregnancy. J.Biol.Chem. 275 37086 PMID: 10969080
Wang et al (2003) Significant neuroprotection against ischemic brain injury by inhibition of the MEK1 protein kinase in mice: exploration of potential mechanism associated with apoptosis. J.Pharmacol.Exp.Ther. 304 172 PMID: 12490588
Atkins et al (1998) The MAPK cascade is required for mammalian associative learning. Nature Neurosci. 1 602 PMID:
Keywords: SL 327, supplier, Selective, inhibitors, inhibits, MEK1, MEK2, brain, penetrant, Mitogen-Activated, Protein, Kinase, MEK, Kinases, SL327, MEK, MEK, Tocris Bioscience
