Biological Activity
Dual-kinase inhibitor; inhibits both casein kinase 2 (CK2) and extracellular-signal-regulated kinase 8 (ERK8) (IC50 = 0.50 μM for both CK2 and ERK8). Displays selectivity for CK2 over protein kinases normally susceptible to CK2 inhibitors (Ki values are 0.25, 8.65, 11.90 and 15.25 μM for CK2, PIM1, DYRK1a and HIPK2 respectively).
Technical Data
| M. Wt | 534.82 |
| Formula | C11H9Br4N3O2 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 905105-89-7 |
| PubChem ID | 46943415 |
| InChI Key | PHAOTASRLQMKBE-UHFFFAOYSA-N |
| Smiles | BrC1=C2C(N(CC(O)=O)C(N(C)C)=N2)=C(Br)C(Br)=C1Br |
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 | 13.37 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 534.82. 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 | 1.87 mL | 9.35 mL | 18.7 mL |
| 5 mM | 0.37 mL | 1.87 mL | 3.74 mL |
| 10 mM | 0.19 mL | 0.93 mL | 1.87 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.37 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Pagano et al (2008) The selectivity of inhibitors of protein kinase CK2: an update. Biochem.J. 415 353 PMID: 18588507
Keywords: TMCB, supplier, casein, kinase, 2, ck2, extracellular-signal-regulated, kinase, 8, ERK8, dual, kinase, inhibitors, inhibits, Casein, Kinase, 2, ERK, Casein, Kinase, 2, Tocris Bioscience
