| 中文名称 | HJB-97 |
|---|---|
| 中文同义词 | |
| 英文名称 | HJB-97 |
| 英文同义词 | HJB-97;9H-Pyrimido[4,5-b]indole-2-carboxamide, 4-[(3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-4-isoxazolyl)-6-methoxy-N-methyl- |
| CAS号 | 2093391-24-1 |
| 分子式 | C26H28N8O3 |
| 分子量 | 500.55 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 2093391-24-1.mol |
| 结构式 |  |
HJB-97 性质
| 密度 | 1.52±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO：30 mg/mL (59.93 mM)；水：< 0.1 mg/mL（不溶） |
| 形态 | 固体 |
| 酸度系数(pKa) | 11.03±0.50(Predicted) |
| 颜色 | 浅黄至黄色 |
|
BRD2 BD1 0.9±0.2 nM (Ki) |
BRD2 BD2 0.27±0.09 nM (Ki) |
BRD3 BD1 0.18±0.01 nM (Ki) |
BRD3 BD2 0.21±0.03 nM (Ki) |
BRD4 BD1 0.5±0.2 nM (Ki) |
BRD4 BD2 1.0±0.1 nM (Ki) |
BRD2 BD1 3.1±0.7 nM (IC 50 ) |
BRD2 BD2 3.9±0.5 nM (IC 50 ) |
BRD3 BD1 6.6±0.2 nM (IC 50 ) |
BRD3 BD2 1.9±0.4 nM (IC 50 ) |
BRD4 BD1 7.0±0.6 nM (IC 50 ) |
BRD4 BD2 7.0±0.1 nM (IC 50 ) |
HJB97 is a highly potent and efficacious bomodomain and extra terminal (BET) inhibitor with IC
50
s of 3.1 nM (BRD2 BD1), 3.9 nM (BRD2 BD2), 6.6 nM (BRD3 BD1), 1.9 nM (BRD3 BD2), 7.0 nM (BRD4 BD1), 7.0 nM (BRD4 BD2).
HJB97 (10-1000 nM, 4 days) potently inhibits cell growth in RS4;11 and MOLM-13 acute leukemia cell lines with IC
50
s of 24.1 nM and 25.6 nM.
HJB97 can effectively down-regulate the level of c-Myc at concentrations of 300-1000 nM in the RS4;11 cell line (treated for 24 h).
Cell Viability Assay
| Cell Line: | The human acute leukemia RS4;11 cell line; The human acute leukemia MOLM-13 cell line |
| Concentration: | 10-1000 nM |
| Incubation Time: | 4 days |
| Result: | Achieved IC 50 s value of 24.1±5.3 nM and 25.6±1.9 nM in inhibition of the RS4;11 cell and MOLM-13 cell growth. |
Western Blot Analysis
| Cell Line: | RS4;11 cells |
| Concentration: | 30, 100, 300, 1000 nM |
| Incubation Time: | 24 h |
| Result: | Down-regulated the level of c-Myc but at concentrations of 300-1000 nM in the RS4;11 cell line. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-112429 | HJB97 | 1 mg | 1363元 | |
| 2024/08/19 | HY-112429 | HJB97 | 2093391-24-1 | 5mg | 3000元 |