Bromosporine

Bromosporine is a potent BET inhibitor with an IC₅₀ value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-FU (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS^[1][2][3][4]. IC50 & Target: IC₅₀: 2.1 μM (PCAF)^[2]
Apoptosis, BET, CDK9, HIV-1^[1][3][4] In Vitro: Bromosporine (0-1000 nM; 72 h) synergistically inhibits cell growth in CRC cells with 5-FU (HY-90006)^[1].
Bromosporine (various concentration; 48 h) causes a distinct increase in the cells arrested at G1 phase when combined with 5-FU^[1].
Bromosporine (various concentration; 48 h) decreases the expressions of PARP, caspase 3, and 9^[1].
Bromosporine (0.1, 0.5 and 1 μM; 6-10 days) inhibits AML cells in a dose-dependent manner^[3].
Bromosporine (2.5 μM; 72 h) activates HIV-1 replication in vitro in latent HIV-1 J-Lat clone C11 cells^[4].
Bromosporine (1-50 μM; 48 h) does not induce marked toxicity in primary CD4+ T cells^[4]. In Vivo: Bromosporine (100 mg/kg; i.p.; daily for 10 days) shows better antitumor activity than individual when co-treated with 5-FU (HY-90006)^[1].