(+)-JQ1是一种BET bromodomain抑制剂,与BET bromodomain结构域的Kac位点结合,作用于BRD4(1/2),IC50值分别为77 nM和33 nM。几乎所有癌症患者中MYC都会高表达,而(+)-JQ1可以抑制MYC表达,另外,(+)-JQ1抑制细胞生长,诱导细胞周期在G1期停滞,诱导细胞凋亡,通过下调WNT表达来干扰信号通路。
As a class, 'BET' inhibitors disrupt binding of bromodomain and extra-terminal motif (BET) proteins, BRD2, BRD3, BRD4 and BRDT, to acetylated histones preventing recruitment of RNA polymerase 2 to enhancers and promoters, especially super-enhancers, to inhibit gene transcription. As such, BET ...
As a class, ‘BET’ inhibitors disrupt binding of bromodomain and extra-terminal motif (BET) proteins, BRD2, BRD3, BRD4 and BRDT, to acetylated histones preventing recruitment of RNA polymerase 2 to enhancers and promoters, especially super-enhancers, to
(+)-JQ1是一种BET bromodomain抑制剂,与BET bromodomain结构域的Kac位点结合,作用于BRD4(1/2),IC50值分别为77 nM和33 nM。几乎所有癌症患者中MYC都会高表达,而(+)-JQ1可以抑制MYC表达,另外,(+)-JQ1抑制细胞生长,诱导细胞周期在G1期停滞,诱导细胞凋亡,通过下调WNT表达来干扰信号通路。
Bromodomain inhibitor JQ1 enhances adenovirus type 2 (Ad2) infection. (A) Effect of Bromodomain inhibitors on Ad infection. A549 cells were mock-treated (0.1% DMSO in culture medium) or treated with RVX-208 at 500 nM, PFI-1 at 500 nM, JQ1 at 300 nM, or with 300 nM (−)...
The bromodomain inhibitor JQ1 triggers growth arrest and apoptosis in testicular germ cell tumours in vitro and in vivo. J Cell Mol Med. 2016; in press.Jostes S, Nettersheim D, Fellermeyer M, Schneider S, Hafezi F, Honecker F, et al. The bromodomain inhibitor JQ1 triggers growth arrest...
溴域抑制剂,(+)-JQ1(1毫克)产品是Cell-permeable. A potent and highly specific inhibitor for the BET (bromodomain and extra-terminal) family of bromodomains. (+)-JQ1 binds to BRD4 bromodomains 1 and 2 with Kd values of ~ 50 and 90 nM, respectively. The binding is competitive with acetyl...
Structure: CAS Registry #: N/A Purity: ≥95% Chemical Formula: C23H25ClN4O2S Molecular Weight: 456.99 Description: (+)-JQ1 is a specific inhibitor of the BET family of acetyl-lysine recognition motifs,including the BRD2, BRD3, BRD4 and BRDT bromodomains. Appearance: A crystalline solid...
(+)-JQ1-OH is the major metabolite of (+)-JQ1. (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor with IC50s of 77 nM and 33 nM for the first and second bromodomains (BRD4(1/2)), respectively. (+)-JQ-1 can also activate autophagy. ...
英文名:JQ1;(+)-JQ1;BET bromodomain inhibitor;UNII-1MRH0IMX0W CAS号:1268524-70-4 结构式:Cc1c(sc-2c1C(=N[C@H](c3n2c(nn3)C)CC(=O)OC(C)(C)C)c4ccc(cc4)Cl)C 分子式:C23H25ClN4O2S 分子量:456.988 闪点:322.9±34.3 °C ...