DYRK1B抑制剂(AZ191)
| 中文名称 | DYRK1B抑制剂(AZ191) |
|---|---|
| 中文同义词 | DYRK1B抑制剂(AZ191);化合物AZ191;N-(2-甲氧基-4-(4-甲基哌嗪-1-基)苯基)-4-(1-甲基-1H-吡咯并[2,3-C]吡啶-3-基)嘧啶-2-胺;AZ 191,DYRK1B抑制剂 |
| 英文名称 | AZ191 |
| 英文同义词 | N-[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]-4-(1-methyl-1h-pyrrolo[2,3-c]pyridin-3-yl)-2-pyrimidinamine, AZ191;[2-Methoxy-4-(4-methyl-piperazin-1-yl)-phenyl]-[4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)-pyrimidin-2-yl]-amine;AZ191;AZ-191;AZ 191;CS-1824;N-[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]-4-(1-methyl-1h-pyrrolo[2,3-c]pyridin-3-yl)-2-pyrimidinamine;2-Pyrimidinamine, N-[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]-4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)-;Inhibitor,AZ-191,Dual specificity tyrosine regulated kinase,AZ191,Dual specificity tyrosine phosphorylation regulated kinase,inhibit,AZ 191,DYRK |
| CAS号 | 1594092-37-1 |
| 分子式 | C24H27N7O |
| 分子量 | 429.52 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂，天然产物;细胞生物学试剂;Inhibitors |
| Mol文件 | 1594092-37-1.mol |
| 结构式 |  |
DYRK1B抑制剂(AZ191) 性质
| 沸点 | 705.3±70.0 °C(Predicted) |
|---|---|
| 密度 | 1.29±0.1 g/cm3(Predicted) |
| 储存条件 | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
| 溶解度 | DMSO：可溶10mg/mL，澄清 |
| 形态 | 粉末 |
| 酸度系数(pKa) | 7.76±0.42(Predicted) |
| 颜色 | 白色至黄色至浅棕色 |
AZ191 是 DYRK1B 高效选择性抑制剂，IC50 值 17 nM。
IC50: 17 nM (DYRK1B)
AZ191 (0.01-60μM; 5 days) inhibits SW872 and SW982 cell lines in dose-dependent manner with IC
50
s of 3.183 μM and 1.279 μM, respectively.
AZ191 (1-5 μM; 48 hours) down-regulates three anti-apoptotic proteins (Bcl-2, p21, and survivin) at higher concentrations.
Cell Proliferation Assay
| Cell Line: | SW872, SW982 liposarcoma cells |
| Concentration: | 0.01, 0.03, 0.1, 0.3, 0.6, 1, 3, 6, 10, 20, 60 μM |
| Incubation Time: | 5 days |
| Result: | Dose-dependent growth inhibition with IC 50 s of 3.183 μM and 1.279 μM for SW872 and SW982 cell lines, respectively. |
Western Blot Analysis
| Cell Line: | SW872, SW982 liposarcoma cells |
| Concentration: | 1, 2, 3, 4, 5 μM |
| Incubation Time: | 48 hours |
| Result: | Down-regulated three anti-apoptotic proteins (Bcl-2, p21, and survivin) at higher concentrations. |
安全信息
| WGK Germany | 3 |
|---|
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-12277 | AZ191 | 1 mg | 340元 | |
| 2024/01/25 | HY-12277 | DYRK1B抑制剂(AZ191) AZ191 | 1594092-37-1 | 5mg | 750元 |