Abnormal gene transcription and constitutive activation of signaling pathways are major contributors to cancer development. Recent developments in cancer research have focused on targeting epigenetic regulators, such as the bromodomain and extra-terminal (BET) family, to effectively modulate gene expression and inhibit tumor growth.
Bromosporine is a potent BET inhibitor with a nanomolar affinity for several bromodomains
Bromosporine, a potent BET inhibitor, has shown promising results in preclinical and clinical studies. It is a potent BET inhibitor with an IC50 value of 2.1 μM for PCAF. Studies have demonstrated that bromosporine effectively modulates cell proliferation, clonogenic growth, and gene expression in leukemic cell lines.
In Vitro ：Firstly, Bromosporine (0-1000 nM; 72 h) synergistically inhibits cell growth in CRC cells with 5-FU (HY-90006).It (various concentration; 48 h) causes a distinct increase in the cells arrested at G1 phase when combined with 5-FU.Secondly, Bromosporine (various concentration; 48 h) decreases the expressions of PARP, caspase 3, and 9. Meanwhile, it (0.1, 0.5 and 1 μM; 6-10 days) inhibits AML cells in a dose-dependent manner. And Bromosporine (2.5 μM; 72 h) activates HIV-1 replication in vitro in latent HIV-1 J-Lat clone C11 cells.Furthermore, (1-50 μM; 48 h) does not induce marked toxicity in primary CD4+ T cells. In Vivo：Bromosporin (100 mg/kg; i.p. When combined with 5-FU, the antitumor activity was better than that of single use.
In a word, Bromosporine is a potent BET inhibitor and can be used for the research of hematologic neoplasms research.
References:
[1] Reyes-Garau D, et al. Cancers (Basel). 2019 Oct 2;11(10):1483.
[2] Cheng X, et al. Biochem Biophys Res Commun. 2020 Jan 22;521(4):840-845.
[3] Picaud S, et al. Sci Adv. 2016 Oct 12;2(10):e1600760.