Biological Activity
Potent ASK1 inhibitor (IC50 = 14 nM); displays selectivity for ASK1 over other kinases including ASK2 (IC50 = 0.51 μM), MEKK1, TAK1, IKKβ, ERK1, JNK1, p38α, GSK-3β, PKCθ and B-raf (IC50 values are > 10 μM). Blocks downstream JNK1/p38 phosphorylation in cells. Orally bioavailable.
Compound Libraries
TC ASK 10 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 432.35 |
| Formula | C21H21N5O.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1005775-56-3 |
| PubChem ID | 68661090 |
| InChI Key | IKKLFEDUYFZNBO-UHFFFAOYSA-N |
| Smiles | O=C(C4=CC=C(C(C)(C)C)C=C4)NC1=CN2C(C=CC(N3C=NC=C3)=C2)=N1.Cl.Cl |
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 | 43.23 | 100 | |
| water | 43.23 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 432.35. 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 | 2.31 mL | 11.56 mL | 23.13 mL |
| 5 mM | 0.46 mL | 2.31 mL | 4.63 mL |
| 10 mM | 0.23 mL | 1.16 mL | 2.31 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Terao et al (2012) Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors. Bioorg.Med.Chem.Lett. 22 7326 PMID: 23147077
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