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Submit ReviewEnzastaurin
Discontinued Product
Enzastaurin (Cat. No. 5994) has been withdrawn from sale for commercial reasons.
Description: Potent PKCβ inhibitor
Alternative Names: LY317615
Chemical Name: 3-(1-Methyl-1H-indol-3-yl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Purity: ≥98% (HPLC)
Biological Activity for Enzastaurin
Enzastaurin is a 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 for Enzastaurin
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for Enzastaurin
References for Enzastaurin
References are publications that support the biological activity of the product.
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
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