Activators & Inhibitors

GSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM and inactive against a panel of demethylases of the JMJ family.

I-BET151(GSK1210151A) is a BET bromodomain inhibitor. I-BET151 displays potent binding affinity to BRD2, BRD3 and BRD4 with Kd of 0.02-0.1 µM. I-BET151 (0.5 or 5 µM) inhibits the binding of BETs (BRD2, BRD3, BRD4, and BRD9) but not the binding of 23 other bromodomain proteins. I-BET151 also blocks recruitment of BET to chromatin.

I-BET151(GSK1210151A) is a BET bromodomain inhibitor. I-BET151 displays potent binding affinity to BRD2, BRD3 and BRD4 with Kd of 0.02-0.1 µM. I-BET151 (0.5 or 5 µM) inhibits the binding of BETs (BRD2, BRD3, BRD4, and BRD9) but not the binding of 23 other bromodomain proteins. I-BET151 also blocks recruitment of BET to chromatin.

I-BET151(GSK1210151A) is a BET bromodomain inhibitor. I-BET151 displays potent binding affinity to BRD2, BRD3 and BRD4 with Kd of 0.02-0.1 µM. I-BET151 (0.5 or 5 µM) inhibits the binding of BETs (BRD2, BRD3, BRD4, and BRD9) but not the binding of 23 other bromodomain proteins. I-BET151 also blocks recruitment of BET to chromatin.

I-BET-762 is a small molecule inhibitor of the BET family of bromodomaincontaining proteins. It has been shown to bind to the acetylated lysine recognition motifs on the bromodomain of BET proteins. This binding prevents the interaction of between BET proteins and acetylated histone peptides.

I-BET-762 is a small molecule inhibitor of the BET family of bromodomaincontaining proteins. It has been shown to bind to the acetylated lysine recognition motifs on the bromodomain of BET proteins. This binding prevents the interaction of between BET proteins and acetylated histone peptides.

JNJ-26481585, also known as Quisinostat, is a potent pan-HDAC inhibitor. JNJ-26481585 induces histone acetylationand inhibits cancer cell proliferation.

JNJ-26481585, also known as Quisinostat, is a potent pan-HDAC inhibitor. JNJ-26481585 induces histone acetylationand inhibits cancer cell proliferation.

JNJ-26481585, also known as Quisinostat, is a potent pan-HDAC inhibitor. JNJ-26481585 induces histone acetylationand inhibits cancer cell proliferation.