货号：J3058

储存条件：粉末-20°C可保存3年；液体-80°C可保存12月。

 产品描述 

BRDs (bromodomains) of human proteome can recognize the relaxed chromatin segments and bind to the acetylated nucleosomes, transcription factors and co-activators. (+)-JQ1 is a potent and selective bromodomain inhibitor with IC50 values of 77nM, 33nM and >10uM for BRD4(1), BRD4(2) and CREBBP, respectively. The (+)-JQ-1-specific inhibition of BRDs can affect the production of the targeted transcription factor-dependent protein, including NRF2-dependent HO-1, NADPH:quinone oxidoreductase-1 as well as GCLC, SOCS3, STAT5-mediated regulation of target genes, RUNX3, SIRT1, MYC and its downstream target genes, etc. JQ1 can induce the differentiation and growth arrest in NUT midline carcinoma. Treatment with (+)-JQ-1, 250nM for 48h, potently decreased the expression of both BRD4 target genes, RAD21 and RAN, in NMC cells. Treatment with JQ1, i.p., 50mg/kg for 18 days, can regress the tumor growth and prolong overall survival of NMC797 xenografted mice. In addition, (-)-JQ-1 is the negative control compound of (+)-JQ-1.

作用机制

JQ1 can bind lysine acetylation binding site of BET bromodomains competitively with chromatin in a cellular environment.

产品信息