2093391-24-1
2093391-24-1 结构式
基本信息
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-
物理化学性质
常见问题列表
|
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. |