BJE6-106
| 中文名称 | BJE6-106 |
|---|---|
| 中文同义词 | 化合物 T10555 |
| 英文名称 | BJE6-106 (B106) |
| 英文同义词 | BJE6-106 (B106);B106;BJE6106,BJE-6-106,BJE6 106;2H-1-Benzopyran-8-carboxaldehyde, 6-[2-(9H-carbazol-9-yl)ethyl]-2,2-dimethyl- |
| CAS号 | 1564249-38-2 |
| 分子式 | C26H23NO2 |
| 分子量 | 381.47 |
| EINECS号 | |
| 相关类别 | 对照品 |
| Mol文件 | 1564249-38-2.mol |
| 结构式 |  |
BJE6-106 性质
| 沸点 | 548.1±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.16±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO:50.0(最大浓度 mg/mL);131.07(最大浓度 mM) |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
BJE6-106 (B106) 是一种有效的选择性 PKCδ 抑制剂，IC50 值为 0.05 μM，BJE6-106 (B106) 靶向 PKCδ 的选择性是 PKC 同工酶 PKCα 的 1000倍 (IC50=50 μM)。
BJE6-106 (B106) 可以诱导 caspase 依耐性细胞凋亡 (apoptosis)。BJE6-106 (B106) 具有肿瘤特异性作用。
|
PKCδ 0.05 μM (IC 50 ) |
PKCα 50 μM (IC 50 ) |
BJE6-106 (B106) (0.2 μM, 0.5 μM; 24-72 hours) suppresses cell survival in melanoma cell lines with NRAS mutations. BJE6-106 (B106) (0.2 μM, 0.5 μM; 6-24 hours) triggers caspase-dependent apoptosis, increases the activity of caspase 3/7, the effect of B106 is greater than rottlerin (10-fold) in SBcl2 cells. BJE6-106 (B106) (0.5 μM; 2-10 hours) activates the MKK4-JNK-H2AX Pathway by inducing MKK4, JNK and H2AX activation at different times in SBcl2 cells.
Cell Viability Assay
| Cell Line: | Melanoma cell lines with NRAS mutations: SBcl2, FM6, SKMEL2, WM1366, WM1361A, and WM852 cells |
| Concentration: | 0.2 μM, 0.5 μM |
| Incubation Time: | 24 hours, 48 hours, or 72 hours |
| Result: | Inhibited cell survival in melanoma cell lines. |
Apoptosis Analysis
| Cell Line: | SBcl2 cells |
| Concentration: | 0.2 μM, 0.5 μM |
| Incubation Time: | 6 hours, 12 hours, or 24 hours |
| Result: | Induced caspase 3/7 activation. |
Western Blot Analysis
| Cell Line: | SBcl2 cells |
| Concentration: | 0.2 μM, 0.5 μM |
| Incubation Time: | 2 hours, 5 hours, 10 hours |
| Result: | Increased phosphorylation of MKK4, JNK and H2AX. |