摘要：dBET1是一种有效的BRD4蛋白质降解物，其EC50值为430 nM。dBET1 是一种由 BRD4 抑制剂 JQ1 与 NSC 527179 衍生物通过 linker 产生的 PROTAC，能够在低纳摩尔浓度下诱导 BRD4 降解。

dBET1是一种有效的BRD4蛋白质降解物，其EC50值为430 nM。dBET1 是一种由 BRD4 抑制剂 JQ1 与 NSC 527179 衍生物通过 linker 产生的 PROTAC，能够在低纳摩尔浓度下诱导 BRD4 降解。

生物活性

dBET1 treatment down regulates MYC and PIM1 transcription. dBET1 also induces a potent and superior inhibitory effect on MV4;11 cell proliferation at 24 hours (measured by ATP content, IC50= 0.14 μM, compare to IC50= 1.1 μM with JQ1).

In vivo, administration of dBET1 attenuates tumor progression as determined by serial volumetric measurement, and decreases tumor weight assessed post-mortem. Acute pharmacodynamic degradation of BRD4 is observed four hours after a first or second daily treatment with dBET1 (50 mg/kg IP). A statistically significant destabilization of BRD4, down regulation of MYC and inhibition of proliferation is observed with dBET1 compare to vehicle control in excised tumors.

化学性质

分子量 785.27

溶解性（25°C） DMSO 40 mg/mL

储存条件 粉末型式 -20°C 3年；4°C 2年

溶于溶剂 -80°C 6个月；-20°C 1个月

运输方式 冰袋运输，根据产品的不同，可能会有相应调整。

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg

1 mM 1.2734 mL 6.3672 mL 12.7345 mL

5 mM 0.2547 mL 1.2734 mL 2.5469 mL

10 mM 0.1273 mL 0.6367 mL 1.2734 mL

参考文献

[1] Winter GE, et al. Science. Phthalimide conjugation as a strategy for in vivo target protein degradation.

来源：AbMole