中文名：dBET6
英文名：dBET6
纯度：Moligand™，≥98%
货号：D414163
Cas号：1950634-92-0
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
dBET6 is a highly cell-permeable PROTAC degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding. dBET6 also induces c-MYC downregulation and apoptosis .
Targets
BRD4 14 nM
In vitro
dBET6 is a highly cell-permeable degrader of BET bromodomains. It is potent in most cancer cell lines. dBET6 features highly increased cellular potency with evident degradation in the sub-nanomolar range. Treatment with 100 nM dBET6 leads to degradation of BRD4 after 1 hr, prompting subsequent downregulation of c-MYC and induction of apoptosis. dBET6 disrupts global productive transcription elongation. dBET6 treatment leads to a widespread decrease in steady-state mRNA levels, but observed an incommensurate impact on expression of members of the core regulatory circuitry of leukemogenic transcription factors. The collapse of the core transcriptional machinery prompted by BET degradation precedes a robust apoptotic response, of apparent translational significance.
In vivo
dBET6 is well tolerated. Upon dBET6 treatment, a significant reduction of leukemic burden is observed in a disseminated mouse model of T-ALL. Moreover, mice treated with dBET6 (7.5 mg/kg BID) exhibits a significant survival benefit compared to mice treated with vehicle control or JQ1 (20 mg/kg QD).
Cell Research(from reference)
Cell lines：MOLT4 cells deficient in CRBN expression
Concentrations：0.05, 0.1, 0.5, 1 μM
Incubation Time：3 hr
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关键字： CHEBI:189651 ; VALRUBICIN [ORANGE BOOK] ; A935629 ; EN300-23308290
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