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。
| 生物活性 | HJB97 is a high-affinityBETinhibitor withKis of 0.9 nM (BRD2BD1), 0.27 nM (BRD2BD2), 0.18 nM (BRD3BD1), 0.21 nM (BRD3BD2), 0.5 nM (BRD4BD1), 1.0 nM (BRD4BD2), respectively. HJB97 is employed for the design of potentialPROTACBETdegrader 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) |
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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].
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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 30 mg/mL(59.93 mM;Need ultrasonic) 配制储备液 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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。 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本网站选购。
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