Biological Activity
Inhibitor of protein kinase C (IC50 = 2.45 μM) that displays ~ 10-fold selectivity over protein kinase A (IC50 = 25.7 μM). Also inhibits β-lactamase, malate dehydrogenase and chymotrypsin (IC50 values are 8, 8 and 10 μM respectively). Exhibits antiviral activity against GCV-sensitive and -resistant strains of human cytomegalovirus (HCMV) (IC50 values range from 0.13 - 0.32 μM). Shows no activity against herpes simplex virus (HSV).
Technical Data
| M. Wt | 311.34 |
| Formula | C20H13N3O |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 85753-43-1 |
| PubChem ID | 3815 |
| InChI Key | MEXUTNIFSHFQRG-UHFFFAOYSA-N |
| Smiles | O=C(NC3)C1=C3C(C4=CC=CC=C4N5)=C5C2=C1C6=C(C=CC=C6)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 | 7.78 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 311.34. 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 | 3.21 mL | 16.06 mL | 32.12 mL |
| 5 mM | 0.64 mL | 3.21 mL | 6.42 mL |
| 10 mM | 0.32 mL | 1.61 mL | 3.21 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.64 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Fabre et al (1993) Protein kinase C inhibitors; structure-activity relationships in K252c-related compounds. Bioorg.Med.Chem. 1 193 PMID: 8081852
Zimmermann et al (2000) Indolocarbazoles exhibit strong antiviral activity against human cytomegalovirus and are potent inhibitors of the pUL97 protein kinase. Antiviral Res. 48 49 PMID: 11080540
McGovern and Shoichet (2003) Kinase inhibitors: not just for kinases anymore. J.Med.Chem. 46 1478 PMID: 12672248
Keywords: K-252c, supplier, Protein, kinases, C, inhibitors, inhibits, PKC, Staurosporinone, Protein, Kinase, C, Antivirals, Protein, Kinase, C, Tocris Bioscience
