货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T96707-1ml促销	10mM in DMSO	￥720.00 ￥648.00 T96707-1ml ￥648.00 现货	6 6	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T96707-1ml促销

10mM in DMSO

￥720.00 ￥648.00

产品描述：

普罗塔克;PROTAC;;InformationdBET6 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 .TargetsBRD4 14 nMIn vitrodBET6 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 vivodBET6 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

靶点：

IC50: 14 nM (BET)

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.189 ml	5.943 ml	11.885 ml
5 mM	0.238 ml	1.189 ml	2.377 ml
10 mM	0.119 ml	0.594 ml	1.189 ml
50 mM	0.024 ml	0.119 ml	0.238 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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