BRD4354是HDAC5和HDAC9适度抑制剂，其IC50值分别为0.85，1.88μM。
BRD 4354 is a moderately potent inhibitor of HDAC5 and HDAC9, with IC50s of 0.85 and 1.88 μM, respectively.
BRD 4354 is a moderately potent inhibitor of HDAC5 and HDAC9, with BRD4354 having half-maximum inhibitory concentrations (IC50) of 0.85 μM and 1.88 μM, respectively. BRD 4354 also inhibits HDACs 4, 6, 7, and 8 at higher concentrations (3.88-13.8 μM) but demonstrates less of an inhibitory effect on other class I HDACs 1, 2, and 3 (IC50>40 μM) [1].
[1]. Boskovic ZV, ET AL. Inhibition of Zinc-Dependent Histone Deacetylases with a Chemically Triggered Electrophile. ACS Chem Biol. 2016 Jul 15;11(7):1844-51.
Cell experiment: | A549 adenocarcinoma cells were treated with BRD 4354 for 24 h at 10 μM, and the top 50 upregulated and top 50 down regulated genes are compared to other compound treatments involving drugs, bioactive compounds with established MoA, and novel synthetic compounds[1]. |
参考文献: [1]. Boskovic ZV, ET AL. Inhibition of Zinc-Dependent Histone Deacetylases with a Chemically Triggered Electrophile. ACS Chem Biol. 2016 Jul 15;11(7):1844-51. | |
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