| 产品描述: | PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε) |
| 靶点: |
human PKCβ1:21 nM (IC50);human PKCβ2:5 nM (IC50);PKCα:331 nM (IC50);Apoptosis; PKC |
| 体外研究: |
PKCβ inhibitor 1 (0-30 μM; 48 hours) suppresses tumor cell proliferation in a time- and dose-dependent manner. PKCβ inhibitor 1 (14 μM; 2-48 hours) induces apoptosis in 2F7 cells. PKCβ inhibitor 1 (15 μM; 2-48 hours) inhibits cell cycle progression in 2F7 and BCBL-1 cells. PKCβ (15 or 14 μM, respectively; 2-48 hours) inhibitor 1 reduces the expression of phospho-PKCβ in BCBL-1 and 2F7 cells. PKCβ inhibitor 1(0-48 hours) suppresses GSK3β, mTOR, and S6 phosphorylation. Cell Proliferation Assay Cell Line: 2F7, BCBL-1 cells Concentration: 0, 5, 10, 20, and 30 μM Incubation Time: 48 hours Result: A dose-dependent reduction in viability of the 2F7 and BCBL-1 cells starting at 5 μM and increasing with elevated inhibitor concentration. Apoptosis Analysis Cell Line: 2F7 cells Concentration: 14 μM Incubation Time: 2-48 hours Result: Apoptotic induction in 2.1% of the 2F7 cells above background after 2 hours of treatment, increasing through 48 hours of treatment. Cell Cycle Analysis Cell Line: BCBL-1 Cells Concentration: 15 μM (the IC50) Incubation Time: 2-48 hours Result: Inhibits cell cycle progression in 2F7 and BCBL-1 cells. Western Blot Analysis Cell Line: BCBL-1 and 2F7 cell lines Concentration: 15 or 14 μM (at the IC50 respectively) Incubation Time: 2-48 hours Result: The expression of phospho-PKCβ in BCBL-1 and 2F7 cells reduced. |
| 参考文献: |
1. Tanaka M, et al. Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5171-4. 2. Saba NS, et al. Protein kinase C-beta inhibition induces apoptosis and inhibits cell cycle progression in acquired immunodeficiency syndrome-related non-hodgkin lymphoma cells. J Investig Med. 2012 Jan;60(1):29-38 |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.43 ml |
12.152 ml |
24.304 ml |
| 5 mM |
0.486 ml |
2.43 ml |
4.861 ml |
| 10 mM |
0.243 ml |
1.215 ml |
2.43 ml |
| 50 mM |
0.049 ml |
0.243 ml |
0.486 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |