Biological Activity
Potent and selective ASK1 inhibitor (IC50 = 93 nM). Selective for ASK1 over a panel of 210 kinases. Blocks LPS-induced ASK1 and p38 phosphorylation in cultured mouse astrocytes. Suppresses neuroinflammation in a mouse EAE model. Orally bioavailable and brain penetrant.
Technical Data
| M. Wt | 362.31 |
| Formula | C16H13F3N6O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1124381-43-6 |
| PubChem ID | 25214468 |
| InChI Key | XUKGFHHTSUKORV-UHFFFAOYSA-N |
| Smiles | O=C(C1=CC=CN=C1)NC2=NN3C(C=C(C(F)(F)F)C=C3NC4CC4)=N2 |
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 | 7.25 | 20 | |
| ethanol | 3.62 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 362.31. 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 | 2.76 mL | 13.8 mL | 27.6 mL |
| 5 mM | 0.55 mL | 2.76 mL | 5.52 mL |
| 10 mM | 0.28 mL | 1.38 mL | 2.76 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.55 mL |
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References
References are publications that support the products' biological activity.
Guo et al (2010) Regulation of the severity of neuroinflammation and demyelination by TLR-ASK1-p38 pathway. EMBO Mol.Med. 2 504 PMID: 21064192
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