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Submit ReviewEnzastaurin 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.
分子量 | 515.6 |
公式 | C32H29N5O2 |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
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
关键词: Enzastaurin, Enzastaurin supplier, Potent, PKCbeta, PKCb, PKCβ, inhibitors, inhibits, antitumor, orally, active, protein, kinases-C, LY317615, Protein, Kinase, C, 5994, Tocris Bioscience
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