Biological Activity
Protein kinase C inhibitor, with activity at other protein kinases (IC50 values are 33, 3, 8, 15 and 38 nM for PKCα, MAPKAP-K1b, MSK1, GSK3β and S6K1 respectively). Activates JNK and glycogen synthase, and inhibits MAPK and ERK2, in rat adipocytes and L6 myotubes. Also inhibits voltage-dependent Na+ channels in the micromolar range.
Compound Libraries
Ro 31-8220 mesylate is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 553.65 |
| Formula | C25H23N5O2S.CH3SO3H |
| Storage | Desiccate at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 138489-18-6 |
| PubChem ID | 11628205 |
| InChI Key | SAWVGDJBSPLRRB-UHFFFAOYSA-N |
| Smiles | CS(O)(=O)=O.CN1C=C(C2=CC=CC=C12)C1=C(C(=O)NC1=O)C1=CN(CCCSC(N)=N)C2=CC=CC=C12 |
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 | 55.37 | 100 | |
| ethanol | 2.77 | 5 |
Preparing Stock Solutions
The following data is based on the product molecular weight 553.65. 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 | 1.81 mL | 9.03 mL | 18.06 mL |
| 5 mM | 0.36 mL | 1.81 mL | 3.61 mL |
| 10 mM | 0.18 mL | 0.9 mL | 1.81 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Davis et al (1989) Potent, selective inhibitors of protein kinase C. FEBS Lett. 259 61 PMID: 2532156
Lingameneni et al (2000) Inhibition of voltage-dependent sodium channels by Ro 31-8220, a 'specific' protein kinase C inhibitor. FEBS Lett. 473 265 PMID: 10812087
Davies et al (2000) Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem.J. 351 95 PMID: 10998351
Standaert et al (1999) RO 31-8220 activates c-Jun N-terminal kinase and glycogen synthase in rat adipocytes and L6 myotubes. Comparison to actions of insulin. Endocrinology 150 2145 PMID:
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