HJB97

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

HJB97  纯度: 98.24%

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。

HJB97

HJB97 Chemical Structure

CAS No. : 2093391-24-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3300 In-stock
5 mg ¥3000 In-stock
10 mg ¥5500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

HJB97 相关产品

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  • Targeted Diversity Library

生物活性

HJB97 is a high-affinity BET inhibitor with Kis of 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), respectively. HJB97 is employed for the design of potential PROTAC BET degrader and has antitumor activity[1].

IC50 & Target

BRD4 BD1

0.5±0.2 nM (Ki)

BRD4 BD1

7.0±0.6 nM (IC50)

BRD4 BD2

1.0±0.1 nM (Ki)

BRD4 BD2

7.0±0.1 nM (IC50)

BRD2 BD1

0.9±0.2 nM (Ki)

BRD2 BD2

0.27±0.09 nM (Ki)

BRD2 BD1

3.1±0.7 nM (IC50)

BRD2 BD2

3.9±0.5 nM (IC50)

BRD3 BD1

0.18±0.01 nM (Ki)

BRD3 BD2

0.21±0.03 nM (Ki)

BRD3 BD1

6.6±0.2 nM (IC50)

BRD3 BD2

1.9±0.4 nM (IC50)

体外研究
(In Vitro)

HJB97 is a highly potent and efficacious bomodomain and extra terminal (BET) inhibitor with IC50s 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)[1].
HJB97 (10-1000 nM, 4 days) potently inhibits cell growth in RS4;11 and MOLM-13 acute leukemia cell lines with IC50s of 24.1 nM and 25.6 nM[1].
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)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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 IC50s 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[1]

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.

分子量

500.55

Formula

C26H28N8O3

CAS 号

2093391-24-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 30 mg/mL (59.93 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9978 mL 9.9890 mL 19.9780 mL
5 mM 0.3996 mL 1.9978 mL 3.9956 mL
10 mM 0.1998 mL 0.9989 mL 1.9978 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.99 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.99 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.

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