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2093391-24-1

中文名稱 HJB97
英文名稱 HJB-97
CAS 2093391-24-1
分子式 C26H28N8O3
分子量 500.55
MOL 文件 2093391-24-1.mol
更新日期 2023/03/20 15:41:21
2093391-24-1 結(jié)構(gòu)式 2093391-24-1 結(jié)構(gòu)式

基本信息

英文別名
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-

物理化學性質(zhì)

密度1.52±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO : 30 mg/mL (59.93 mM);Water : < 0.1 mg/mL (insoluble)
酸度系數(shù)(pKa)11.03±0.50(Predicted)
形態(tài)Solid
顏色Light yellow to yellow
HJB97價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2026/06/05HY-112429HJB972093391-24-11 mg1363元
2026/06/05HY-112429HJB972093391-24-15mg3000元
2026/06/05HY-112429HJB972093391-24-110mM * 1mLin DMSO3304元

常見問題列表

生物活性
HJB97 是一種高親和力 BET 抑制劑,Ki 值分別為 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 可用于開發(fā)設(shè)計 PROTAC BET 的降解劑,具有抗腫瘤活性。
靶點

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 )

體外研究

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.
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