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产品价格:电议      采购度:1595      原产地:美洲
发布时间:2021/8/2 16:58:17 所属地区:上海 上海市
简要描述:
Senexin A是CDK8的抑制剂,IC50值为280 nM。
标签:senexin
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CAS No. : 1366002-50-7
MCE 站:Senexin A
产品活性:Senexin A是CDK8的抑制剂,IC50值为280 nM。
作用靶点:CDK
In Vitro: Senexin A inhibits CDK8 and CDK19 ATP site binding with Kd50 of 0.83 μM and 0.31 μM, respectively and CDK8 kinase activity with IC50 of 0.28 μM. Senexin A inhibits β-catenin–dependent transcription in HCT116 colon carcinoma cells. The induction of transcription factor EGR1 upon serum starvation, followed by readdition of serum, is strongly inhibited by Senexin A in HT1080 cells. Senexin A inhibits only p21-induced transcription but not other biological effects of p21. Senexin A also decreases the expression of many secreted tumor-promoting factors in doxorubicin-treated wild-type HCT116 cells.
In Vivo: Five daily treatment of Senexin A fully reverses tumor-promoting effect of chemotherapy. Senexin A shows no detectable toxicity and no significant effects on body weight, organ weights, or blood cell counts in C57BL/6 mice during the treatment. This effect of doxorubicin treatment is completely abolished, however, when doxorubicin injection is followed by administration of Senexin A. Senexin A treatment strongly improves the response of A549/MEF tumors to doxorubicin.
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更新时间:2024/1/2 10:17:29
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