HJB-97
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- CAS号:
- 2093391-24-1
- 英文名:
- HJB-97
- 英文别名:
- 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-
- 中文名:
- 中文别名:
- CBNumber:
- CB44668011
- 分子式:
- C26H28N8O3
- 分子量:
- 500.55
- MOL File:
- 2093391-24-1.mol
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HJB-97化学性质
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密度:
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1.52±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO : 30 mg/mL (59.93 mM);Water : < 0.1 mg/mL (insoluble)
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形态:
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Solid
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酸度系数(pKa):
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11.03±0.50(Predicted)
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颜色:
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Light yellow to yellow
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HJB-97性质、用途与生产工艺
HJB97 是一种高亲和力 BET 抑制剂，Ki 值分别为 0.9 nM (BRD2 BD1)，0.27 nM (BRD2 BD2)，0.18 nM (BRD3 BD1)，0.21 nM (BRD3 BD2)，0.5 nM (BRD4 BD1)，1.0 nM (BRD4 BD2)。HJB97 可用于开发设计 PROTAC BET 的降解剂，具有抗肿瘤活性。
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BRD2 BD1
0.9±0.2 nM (Ki)
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BRD2 BD2
0.27±0.09 nM (Ki)
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BRD3 BD1
0.18±0.01 nM (Ki)
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BRD3 BD2
0.21±0.03 nM (Ki)
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BRD4 BD1
0.5±0.2 nM (Ki)
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BRD4 BD2
1.0±0.1 nM (Ki)
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BRD2 BD1
3.1±0.7 nM (IC
50
)
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BRD2 BD2
3.9±0.5 nM (IC
50
)
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BRD3 BD1
6.6±0.2 nM (IC
50
)
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BRD3 BD2
1.9±0.4 nM (IC
50
)
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BRD4 BD1
7.0±0.6 nM (IC
50
)
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BRD4 BD2
7.0±0.1 nM (IC
50
)
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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
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Cell Line:
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The human acute leukemia RS4;11 cell line; The human acute leukemia MOLM-13 cell line
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Concentration:
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10-1000 nM
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Incubation Time:
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4 days
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Result:
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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.
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Western Blot Analysis
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Cell Line:
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RS4;11 cells
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Concentration:
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30, 100, 300, 1000 nM
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Incubation Time:
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24 h
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Result:
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Down-regulated the level of c-Myc but at concentrations of 300-1000 nM in the RS4;11 cell line.
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HJB-97
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
2093391-24-1, HJB-97 相关搜索:
- C26H28N8O3
- 2093391-24-1
- 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-
- HJB-97