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dBET1

CAS No. : 1799711-21-9

MCE 国际站：dBET1

产品活性：dBET1 是由Cereblon配体和BRD4配体相连的PROTAC，其 EC₅₀ 值为 430 nM。dBET1 是一种由 BRD4 抑制剂 JQ1 (HY-13030) 与 NSC 527179 (HY-14658) 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。

研究领域：PROTAC  |  Epigenetics

作用靶点：PROTACs  |  Epigenetic Reader Domain

In Vitro: Treatment with dBET1 down regulates MYC and PIM1 transcription. Degradation of BRD4 by dBET1 is associated with a more potent apoptotic consequence in MV4;11 cell line. Significantly increased apoptosis after only 4 h of dBET1 treatment is enhanced at 8 h. 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. Two weeks of dBET1 is well tolerated by mice without a meaningful effect on weight, white blood count, hematocrit or platelet count.

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