Biological Activity
Potent PKCβ inhibitor (IC50 values are 6, 39, 83 and 110 nM for PKCβ, PKCα, PKCγ and PKCε, respectively). Suppresses proliferation and induces apoptosis in HCT116 colon carcinoma and U87MG glioblastoma cells in vitro. Reduces tumor growth and exhibits antiangiogenic activity in HT-29 colon carcinoma xenografts in mice. Also suppresses growth of HCT116 and U87MG xenografts in mice. Orally active.
Technical Data
| M. Wt | 515.6 |
| Formula | C32H29N5O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 170364-57-5 |
| PubChem ID | 176167 |
| InChI Key | AXRCEOKUDYDWLF-UHFFFAOYSA-N |
| Smiles | CN1C=C(C2=C(C3=CN(C4=C3C=CC=C4)C5CCN(CC5)CC6=CC=CC=N6)C(NC2=O)=O)C7=C1C=CC=C7 |
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 | 10.31 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 515.6. 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 | 1.94 mL | 9.7 mL | 19.39 mL |
| 5 mM | 0.39 mL | 1.94 mL | 3.88 mL |
| 10 mM | 0.19 mL | 0.97 mL | 1.94 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
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References
References are publications that support the products' biological activity.
Teicher et al (2001) Antiangiogenic and antitumor effects of a protein kinase Cβ inhibitor in human HT-29 colon carcinoma and human CaKi1 renal cell carcinoma xenografts. Anticancer Res. 21 3175 PMID: 11848470
Graff et al (2005) The protein kinase Cβ-selective inhibitor, Enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts. Cancer Res. 65 7462 PMID: 16103100
Keywords: Enzastaurin, supplier, Potent, PKCbeta, PKCb, PKCβ, inhibitors, inhibits, antitumor, orally, active, protein, kinases-C, LY317615, Protein, Kinase, C, Protein, Kinase, C, Tocris Bioscience
